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smiles
large_stringlengths
1
1.05k
oral_bioavailability_value
float64
0
942
canonical_endpoint_key
large_stringclasses
2 values
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1 value
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2 values
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1 value
species_exact
large_stringclasses
48 values
scalar_value
float64
0
942
unit_normalized
large_stringclasses
1 value
scalar_is_approximate
bool
1 class
molecule_name
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1
192
bioavailability_report_type
large_stringclasses
2 values
species_or_population
large_stringlengths
2
157
dose
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1
107
oral_exposure_mode
large_stringlengths
2
158
qualifying_conditions
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2
207
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2
85
species_or_population_normalized
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condition_key_repro
large_stringlengths
22
263
pmid
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5
8
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64
64
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int64
1
49.2k
input_sha256
large_stringclasses
1 value
parent_provenance_id
large_stringlengths
64
64
child_id
large_stringlengths
64
64
extra_details
large_stringlengths
3
318
support_text
large_stringlengths
29
481
O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1
88
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
88
percent
false
solifenacin
absolute
healthy volunteers
10mg
oral
null
5mg iv dose
human
healthy volunteers | oral | not specified | 5mg iv dose
15293866
starling
starling_oba
b17248363323cee8df278636d6c4bd423217358ffc4f3a25c5f96a8c7fd1009e
1
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
b17248363323cee8df278636d6c4bd423217358ffc4f3a25c5f96a8c7fd1009e
f0188a2c69159fe7ec04bb17674a1bc4cacf30dc96a49890b1eb77046badebca
The value was close to the value predicted from oral data alone (approximately 87%).
The absolute oral bioavailability of solifenacin was determined to be 88% in healthy volunteers following a single 10mg oral dose compared to a single 5mg IV dose, which was close to the value of approximately 87% predicted from oral data alone.
Cc1ccc([C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)cc1Cc1ccc(-c2ccc(F)cc2)s1
65
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
65
percent
false
canagliflozin
absolute
participants
300 mg
null
null
vs iv
human
participants | not specified | not specified | vs iv
27136910
starling
starling_oba
aa2749798c5223b5e585723a2df3094245ad440bd52e50ae046dbca181467cd9
2
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
aa2749798c5223b5e585723a2df3094245ad440bd52e50ae046dbca181467cd9
60c1573de053c6987347251c79068abd891b7695401491deb7b111dabfc904ea
Calculated using geometric mean ratio estimates of AUC∞.
Based on the comparison of geometric mean ratio estimates of AUC∞ of oral and dose-normalized intravenous infusion of canagliflozin, the mean absolute oral bioavailability of canagliflozin was 65% (90% CI: 55.41; 76.07).
CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C
27
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
dog
27
percent
false
Medroxyprogesterone acetate
absolute
dogs
2.5, 5, and 10 mg
tablets
null
vs iv
dog
dogs | tablets | not specified | vs iv
8499584
starling
starling_oba
ff92503280827f45969bf0d09345e9c7e9fdff4b33f27f3409e2a22d066952a4
3
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
ff92503280827f45969bf0d09345e9c7e9fdff4b33f27f3409e2a22d066952a4
a40c9f43d95b960a26d5866f0082589f2b70371fd66a4c111a3c6561e8d2fcb0
Oral absorption was reported to be dose-linear over the studied dosage range.
In dogs, the oral absorption of Medroxyprogesterone acetate (MPA) appeared to be dose-linear over the studied dosage range (2.5, 5, and 10 mg tablets), and the absolute bioavailability was estimated at 27 per cent compared to an intravenous dose.
CC(C)Nc1ccc(OC(C)C(=O)O)cc1
3
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
pig
3
percent
false
metoprolol
absolute
anaesthetised göttingen mini-pigs
null
oral administration
null
buccal dosing (58-107%)
pig
anaesthetised göttingen mini-pigs | oral administration | not specified | buccal dosing (58-107%)
23500040
starling
starling_oba
0afbea79b7c35c87a05f87421f9d7d76c86cea4cb4a7678c95836ffb4485177c
5
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
0afbea79b7c35c87a05f87421f9d7d76c86cea4cb4a7678c95836ffb4485177c
600b80501b6dc5f8ef414b1eeb1f461025d375ddd0b5a8bbb3c33dedb1fbfffd
null
In anaesthetised Göttingen mini-pigs, metoprolol showed an absolute bioavailability of 3% following oral administration, which was significantly lower than the 58–107% observed after buccal dosing.
O=C(O)c1ccc(CCN(CCc2ccccc2OCc2ccc(-c3ccc(C(F)(F)F)cc3)cc2Cl)[C@H]2CCCc3nc(C(=O)O)ccc32)cc1
23
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
23
percent
false
Mosliciguat
absolute
enrolled subjects
null
null
null
null
human
enrolled subjects | not specified | not specified | not specified
40402373
starling
starling_oba
284e6faae1db98471648403490c5aa9a3cad1cd6bb3f532c6d6b0255e9c7f560
6
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
284e6faae1db98471648403490c5aa9a3cad1cd6bb3f532c6d6b0255e9c7f560
442368269ee58d686e178c9a120208766d40f039a7c000fa2288770423f9ddd3
null
Absolute bioavailability for oral mosliciguat was reported to be 23%.
O=C(O)c1ccc(CCN(CCc2ccccc2OCc2ccc(-c3ccc(C(F)(F)F)cc3)cc2Cl)[C@H]2CCCc3nc(C(=O)O)ccc32)cc1
23.1
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
23.1
percent
false
Mosliciguat
absolute
healthy male volunteers
1000 μg
oral solution
null
vs iv
human
healthy male volunteers | oral solution | not specified | vs iv
40402373
starling
starling_oba
b4cafd84e01b773b0c20edd832082608b2dd4847956d54f7467552d1f8d7358f
7
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
b4cafd84e01b773b0c20edd832082608b2dd4847956d54f7467552d1f8d7358f
043ce6b3089fc5f5f6919f573bdc1ef13dbd5eb5e9e52186845549b01469ce69
Study 1 (Part 2); IV dose was 100 μg
In Study 1 (Part 2), the absolute bioavailability of oral mosliciguat was 23.1% in healthy male volunteers. This was based on a 1000 μg oral solution dose compared to a 100 μg intravenous dose.
O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1
90
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
90
percent
false
solifenacin
absolute
null
null
null
not decreased by multiple dosing and concomitant food intake
null
null
null
19566112
starling
starling_oba
74a2e592cfbe001467dc58f2b0ae6d985e488b0045405c473f64abec82f5f4b1
8
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
74a2e592cfbe001467dc58f2b0ae6d985e488b0045405c473f64abec82f5f4b1
ce2239bb1f3cbe1b9bb066376773d2ebacca4b1e70a6cd333082299c1bcfe298
null
Orally administered solifenacin has a high absolute bioavailability of 90%, which is not decreased by multiple dosing and concomitant food intake.
C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C
69.8
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
69.8
percent
false
osimertinib
absolute
healthy subjects
80-mg
null
null
vs iv microtracer dose of [14c]osimertinib
human
healthy subjects | not specified | not specified | vs iv microtracer dose of [¹⁴c]osimertinib
29683562
starling
starling_oba
46d5df4923e75e7dae943680c993e01f408577e671ac747dba7bb961f8cc5aeb
9
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
46d5df4923e75e7dae943680c993e01f408577e671ac747dba7bb961f8cc5aeb
d9a81e3595a0f7f8b4c6a0672c57defb635e865c294d8c607d537149c92f9957
Geometric mean absolute oral bioavailability.
In a phase I study, ten healthy subjects (21–61 years) received a single oral 80-mg dose of osimertinib concomitantly with a 100 µg IV microtracer dose of [¹⁴C]osimertinib. The geometric mean absolute oral bioavailability of osimertinib was 69.8% (90% confidence interval, 66.7, 72.9).
CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](O[C@@H]2O[C@H](C(=O)O)[C@@H](O)[C@H](O)[C@H]2O)C=C[C@H]3[C@H]1C5
11
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
11
percent
false
M6G
absolute
volunteers
20 mg
p.o.
null
vs i.v.
human
volunteers | p.o. | not specified | vs i.v.
11966664
starling
starling_oba
d371bee531dcfeeff0e723dfc03e48c6b517c49864519451fc5392d29517761b
11
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
d371bee531dcfeeff0e723dfc03e48c6b517c49864519451fc5392d29517761b
64da2b2c940c1441c8d65bb08b41b5e2ebab32a9a28931d74275dee79baf94ea
90% CI: 9–12%; bioavailability derived using AUC(0,t_n) values.
In a study of 10 volunteers, the oral (p.o.) administration of 20 mg of M6G resulted in a mean absolute bioavailability F(0, ∞) of 11 ± 3% (90% CI 9–12%), calculated using AUC(0,t_n) values.
COc1cc(Nc2ncc(F)c(Nc3ccc4c(n3)N(COP(=O)(O)O)C(=O)C(C)(C)O4)n2)cc(OC)c1OC
55
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
human
55
percent
false
fostamatinib
absolute
human
null
null
null
null
human
human | not specified | not specified | not specified
27858108
starling
starling_oba
88780609d698f9edae053eb0916d2b9b5763e3ebaccacbe6511acc0146872b6e
12
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
88780609d698f9edae053eb0916d2b9b5763e3ebaccacbe6511acc0146872b6e
5ff629201f443d2ed4fe8138e220d58c52e5e602470f96e8012688bb1b8bc91d
null
The absolute oral bioavailability of fostamatinib was ~55%.
COc1ccc(-c2nc3cc(C4=NNC(=O)CC4C)ccc3[nH]2)cc1
70
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
dog
70
percent
false
Pimobendan
absolute
healthy dogs
0.25 mg/kg
p.o.
null
vs iv
dog
healthy dogs | p.o. | not specified | vs iv
25989021
starling
starling_oba
f9faad2d0de34b83af4af3166d296a174813b79882bf4d10aebc80fab055108e
13
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
f9faad2d0de34b83af4af3166d296a174813b79882bf4d10aebc80fab055108e
2742f56633bf4e46e740b354adaa8830003eb5b6427cf8c8cd0dad10f1063e29
Intravenous dose was 0.125 mg/kg.
The bioavailability of pimobendan after oral dosing (0.25 mg/kg) in healthy dogs was 70%, with an intravenous dose of 0.125 mg/kg used as a comparator.
Cc1ccc([C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)cc1Cc1ccc(-c2ccc(F)cc2)s1
65
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
65
percent
false
canagliflozin
absolute
healthy men
300 mg
oral
null
intravenous [14c]-canagliflozin
human
healthy men | oral | not specified | intravenous [¹⁴c]-canagliflozin
27136910
starling
starling_oba
5ace889ef35b6892f7b7e95721a1c17df12ac8d840ea592bd8177c4e05e9cd75
14
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
5ace889ef35b6892f7b7e95721a1c17df12ac8d840ea592bd8177c4e05e9cd75
215eb90c0c5d5183c1204635577e96130ac538fe77a136276b04c1823acd994d
Assessed via simultaneous oral administration with intravenous [¹⁴C]-canagliflozin microdose infusion (10 µg) in nine healthy men.
The absolute oral bioavailability of canagliflozin was 65% (90% confidence interval: 55.41; 76.07) following a single-dose oral administration of 300 mg in nine healthy men, assessed using a simultaneous intravenous [¹⁴C]-canagliflozin microdose infusion.
O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1
88
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
88
percent
false
solifenacin
absolute
healthy male volunteers
10mg
null
null
vs iv
human
healthy male volunteers | not specified | not specified | vs iv
15293866
starling
starling_oba
b9cb04d2490b370df2efea34e318b0e89525f5d5a9b428b87e82f76944894031
15
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
b9cb04d2490b370df2efea34e318b0e89525f5d5a9b428b87e82f76944894031
c8051f4c74da9868b2815a1f629204b48292a8bf18a245bb7c74c6ff338073bd
Calculated as oral (AUC∞/dose) divided by IV (AUC∞/dose).
In a study with healthy male volunteers, the absolute bioavailability of solifenacin following a 10mg oral dose was 88.0% (95% CI 75.8, 102.1), calculated as the ratio of oral (AUC∞/dose) to IV (AUC∞/dose).
CN1CCCC1c1cccnc1.O=C(O)C(O)C(O)C(=O)O
41
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
human
41
percent
false
nicotine tartrate
absolute
healthy human subjects
3 mg
delayed-release oral capsules
ileocolonic delivery, eudragit s100 coated
vs intravenous nicotine tartrate
human
healthy human subjects | delayed-release oral capsules | ileocolonic delivery, eudragit s100 coated | vs intravenous nicotine tartrate
9354194
starling
starling_oba
846744f7fc87266a3082a0aec90c308ddc6770a64535cc309d50662c996f0492
16
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
846744f7fc87266a3082a0aec90c308ddc6770a64535cc309d50662c996f0492
f02921fa9e1c940c4c72a4bece287eb6c58a1262c5b12b7ae5d332220833c840
reported as mean bioavailability
The mean bioavailabilities of nicotine after ileocolonic nicotine tartrate administration via delayed-release oral capsules at a dose of 3 mg nicotine were 41%. This was determined in twenty healthy human subjects who also received intravenous nicotine tartrate.
CN1CCCC1c1cccnc1.O=C(O)C(O)C(O)C(=O)O
42
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
human
42
percent
false
nicotine tartrate
absolute
healthy human subjects
6 mg
delayed-release oral capsules
ileocolonic delivery, eudragit s100 coated
vs intravenous nicotine tartrate
human
healthy human subjects | delayed-release oral capsules | ileocolonic delivery, eudragit s100 coated | vs intravenous nicotine tartrate
9354194
starling
starling_oba
3483057c1a4242b117af8a6613838188dcb10e7ee494577ebbf9801a1cbd2487
17
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
3483057c1a4242b117af8a6613838188dcb10e7ee494577ebbf9801a1cbd2487
8a4d1fb17b768e51ad6373b2e57d3b8e4873d26f3ecf95c6b7e6b5281b627368
reported as mean bioavailability
The mean bioavailabilities of nicotine after ileocolonic nicotine tartrate administration via delayed-release oral capsules at a dose of 6 mg nicotine were 42%. This was determined in twenty healthy human subjects who also received intravenous nicotine tartrate.
Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O
100
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
100
percent
false
flavoxate
absolute
healthy male volunteers
2.55 ± 0.14 mg/kg
oral
null
vs iv
human
healthy male volunteers | oral | not specified | vs iv
14606931
starling
starling_oba
e3d3c3937691a92d76f01cf5f9ecdfe546af55e79055b738ee8043822a19d3e8
18
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
e3d3c3937691a92d76f01cf5f9ecdfe546af55e79055b738ee8043822a19d3e8
7320a5e13438ef5f4c2410d7f90733906202bb8e66b838e57c7e5c06bbae4d8f
Calculated based on a comparison of oral and intravenous data in different subjects.
Oral bioavailability of flavoxate, based on a comparison of oral and intravenous data in different healthy male volunteers receiving oral doses of 2.55 ± 0.14 mg/kg, appeared to be close to 100%.
CC(C)Cc1ccc(C(C)C(=O)O)cc1.NCCCC[C@H](N)C(=O)O
102.7
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
102.7
percent
false
ibuprofen lysine
absolute
healthy male volunteers
500 mg
coated tablets
lysine salt
intravenous injections of ibuprofen solutions
human
healthy male volunteers | coated tablets | lysine salt | intravenous injections of ibuprofen solutions
2109643
starling
starling_oba
63a7e6e9e2e19f2387c84b36270054bb7040359b8f2561e21e94ddb595d790c0
19
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
63a7e6e9e2e19f2387c84b36270054bb7040359b8f2561e21e94ddb595d790c0
fc482ae9600a81cc9f1952430c0c95c9900fe06ee824183ddd1a531b0ef9ebd4
indicating a complete absorption of ibuprofen; sample size of 8 volunteers
In a study involving 8 healthy male volunteers, the absolute bioavailability of ibuprofen administered as a single oral dose of 500 mg of ibuprofen lysine (via coated tablets) was determined to be 102·7 per cent, indicating complete absorption, using intravenous injections of ibuprofen solutions as a reference.
COc1cc(C(=O)O)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F
40
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
40
percent
false
idasanutlin
absolute
patients
300 mg
sdp formulation
sdp formulation
vs iv tracer dose (100 μg)
human
patients | sdp formulation | sdp formulation | vs iv tracer dose (100 µg)
31062077
starling
starling_oba
ae81834344aeef521d03806ef815a23e3bf7764a07fe05180944c2748871fab8
22
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
ae81834344aeef521d03806ef815a23e3bf7764a07fe05180944c2748871fab8
a6d91f594c6e3f2dae236a02e7cac12c0badaf05fb38b3292488bc3730806e8d
Co-administered with a single oral dose of 100 mg MBP.
In a study involving patients, co-administration of an IV tracer dose (100 µg) with a single oral dose of 100 mg MBP and 300 mg SDP idasanutlin resulted in the absolute bioavailability of idasanutlin SDP of ~40%.
O=c1c(-n2ccnn2)c[nH]n1-c1cc(N2CCOCC2)ncn1
59
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
59
percent
false
Molidustat
absolute
participants
50 mg
ir tablet formulation
null
vs iv
human
participants | ir tablet formulation | not specified | vs iv
32248614
starling
starling_oba
0c9ed16e5a0c545517b95b37c1c34bf8b41065c11d3ca7a309bfff2088ef2528
25
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
0c9ed16e5a0c545517b95b37c1c34bf8b41065c11d3ca7a309bfff2088ef2528
46fe26dedf3b916ba47bc5ae42eaa18c60d613b2d98e0de3dcf8a93cba5122eb
Sample size n = 16.
The absolute bioavailability of molidustat 50 mg administered orally as an IR tablet formulation was 59.0% (90% CI: 55.3%-63.0%) compared to intravenous administration.
O=c1c(-n2ccnn2)c[nH]n1-c1cc(N2CCOCC2)ncn1
59
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
59
percent
false
Molidustat
absolute
participants
50 mg
ir tablet formulation
null
null
human
participants | ir tablet formulation | not specified | not specified
32248614
starling
starling_oba
3933fff04e955cd50355661e7610b0dbeba7030225c7b6bef8caeed3aa7d7c01
26
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
3933fff04e955cd50355661e7610b0dbeba7030225c7b6bef8caeed3aa7d7c01
7680b1ec1434789d4ad1b71f144535acff4da822957785a389cc608996cfedfc
null
Molidustat has an absolute bioavailability of 59% when orally administered as an IR tablet formulation at a dose of 50 mg.
Cc1cccc2sc3nncn3c12
93.9
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
93.9
percent
false
tricyclazole
absolute
rat
2 mg/kg
gavage
null
vs iv
rodent
rat | gavage | not specified | vs iv
31461669
starling
starling_oba
02c4427ff200df327ada02a7a8ad9e626c264f5c85de9f1bd5e250e79979e2f4
27
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
02c4427ff200df327ada02a7a8ad9e626c264f5c85de9f1bd5e250e79979e2f4
c41ff85ab50abbbec895a721af5fdb2122a9d73472877b083e1e614794d5bbd4
AUC0-tlast values were 11.7 µg h/ml for the oral group and 12.5 µg h/ml for the IV group; study performed in Rat Fischer 344.
In the oral bioavailability study from Johnson et al. (2004), based on AUC values determined from ¹⁴C-tricyclazole equivalent concentration time curves, the absolute bioavailability for tricyclazole was 93.9% in rats following gavage administration compared to intravenous administration.
CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(F)c(F)c2)c2nnn([C@@H]3C[C@H](OCCO)[C@@H](O)[C@H]3O)c2n1
36
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
36
percent
false
Ticagrelor
absolute
healthy volunteers
null
null
null
iv
human
healthy volunteers | not specified | not specified | iv
27536453
starling
starling_oba
048abaeabc3408afbc7d2c7d0475a7514a633e1d33a6eecd0430b2d6c28a915b
28
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
048abaeabc3408afbc7d2c7d0475a7514a633e1d33a6eecd0430b2d6c28a915b
973057ce09b715abf1720c97fdc0713201558a1f975603ef44b7bb9c30f084b2
The study that determined this value was the first to determine the pharmacokinetics of ticagrelor following IV administration.
In a study of healthy volunteers, the mean absolute bioavailability of ticagrelor was found to be 36% (95% CI = 30–42).
COC(=O)[C@@H]1CC2=CC(=O)CC[C@]2(C)[C@@]23O[C@@H]2C[C@@]2(C)[C@@H](CC[C@@]24CCC(=O)O4)[C@H]13
94.5
starling.oral_bioavailability.systemic_availability.percent
oral_bioavailability
systemic_availability
percent
dog
94.5
percent
false
[¹⁴C]EP
systemic availability
dog
null
oral administration
null
null
dog
dog | oral administration | not specified | not specified
11205738
starling
starling_oba
049b5fd46a169e54b2fb6d05a47ee31b3bae4b2c2796d65479fa957a978e35be
29
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
049b5fd46a169e54b2fb6d05a47ee31b3bae4b2c2796d65479fa957a978e35be
9f53428fc1992ede893a7a905d1db8690d2cb1dd59312c9e59e7e75104e32d15
Reported as the systemic availability of total radioactivity.
After oral administration of [¹⁴C]EP in the dog, the systemic availability of total radioactivity was 94.5 ± 6.6%, indicating good absorption.
COC(=O)[C@@H]1CC2=CC(=O)CC[C@]2(C)[C@@]23O[C@@H]2C[C@@]2(C)[C@@H](CC[C@@]24CCC(=O)O4)[C@H]13
79.2
starling.oral_bioavailability.systemic_availability.percent
oral_bioavailability
systemic_availability
percent
dog
79.2
percent
false
EP
systemic availability
dog
null
oral administration
null
null
dog
dog | oral administration | not specified | not specified
11205738
starling
starling_oba
087e8219502c3641d3b714ea0ab437d2ccf5b5cac65be5b7f17491bbfc458b57
30
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
087e8219502c3641d3b714ea0ab437d2ccf5b5cac65be5b7f17491bbfc458b57
075dce6bca1f5845b312713a6a4da157ab898e2ec77b496cdfc3e3a14180224e
null
Following oral administration in dogs, the systemic availability of EP was 79.2%.
COC(=O)[C@@H]1CC2=CC(=O)CC[C@]2(C)[C@@]23O[C@@H]2C[C@@]2(C)[C@@H](CC[C@@]24CCC(=O)O4)[C@H]13
90
starling.oral_bioavailability.systemic_availability.percent
oral_bioavailability
systemic_availability
percent
dog
90
percent
false
total EP
systemic availability
dog
null
oral administration
null
null
dog
dog | oral administration | not specified | not specified
11205738
starling
starling_oba
b3de993148c672ba01b3c80984c24e01b8d935731422c32954b47bdea35ca5bf
31
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
b3de993148c672ba01b3c80984c24e01b8d935731422c32954b47bdea35ca5bf
37630ce937f6613a4210681ce11e6147e9818d2fce70dff782de553b099e808a
null
The mean systemic availability of total EP after oral administration in dogs was 90.0%, indicating good absorption of EP.
C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C
69.8
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
69.8
percent
false
osimertinib
absolute
healthy subjects
80-mg
single oral dose
null
vs [14c] radiolabeled iv microtracer dose
human
healthy subjects | single oral dose | not specified | vs [¹⁴c] radiolabeled iv microtracer dose
29683562
starling
starling_oba
0bb7838a7dea017592c5555e51bd3b10b73e8f204a2ede2bb31622525489d4e4
32
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
0bb7838a7dea017592c5555e51bd3b10b73e8f204a2ede2bb31622525489d4e4
e4740986cfd00c147d777b6755883b27416dd187ee3da633f4baa634fb62ee38
suggesting that osimertinib is well absorbed in humans
The oral absolute bioavailability of an 80-mg single oral dose of osimertinib in healthy subjects was 69.8%, suggesting that osimertinib is well absorbed in humans.
O=C1N(c2ccccc2)CCN1c1ccccc1
87.5
starling.oral_bioavailability.systemic_availability.percent
oral_bioavailability
systemic_availability
percent
null
87.5
percent
false
Phenytoin
systemic availability
null
null
oral administration
products with high quality
null
null
null
378503
starling
starling_oba
997d28e0b35e6e428ca94ad73b691378e735a6e739b0fbdeaad67c509527b900
34
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
997d28e0b35e6e428ca94ad73b691378e735a6e739b0fbdeaad67c509527b900
233e6edbdaf56b9a63c37184659f0a14a176a775e94476d23a8a13c3388cc0cb
The author notes that no significant first-pass metabolism occurs during gastrointestinal absorption.
The systemic bioavailability of phenytoin is of the order of 80 to 95% after the oral administration of products with high quality, which suggests that there is no significant first-pass metabolism during gastrointestinal absorption.
CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(F)c(F)c2)c2nnn([C@@H]3C[C@H](OCCO)[C@@H](O)[C@H]3O)c2n1
36
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
36
percent
false
Ticagrelor
absolute
individuals
90 mg
null
null
vs iv
human
individuals | not specified | not specified | vs iv
27536453
starling
starling_oba
cdbe98b9f6b3968c914143132239bcb1b22a7ac2d7a21cdaf64048e2f061e5cb
37
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
cdbe98b9f6b3968c914143132239bcb1b22a7ac2d7a21cdaf64048e2f061e5cb
c76ccab922783dcbf94f050ed211442346eb4f17f8658e009969b040f0b7f22c
Bioavailability in individuals ranged from 25.4–64.0%; the dose used for the oral administration was 90 mg as specified in the associated pharmacokinetic data.
The mean absolute bioavailability of ticagrelor was 36% (95% confidence interval [CI] = 30–42%), with bioavailability in individuals ranging from 25.4–64.0%.
C[C@H]1COc2c(N3CCN(C)CC3)c(F)cc3c(=O)c(C(=O)O)cn1c23
99
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
99
percent
false
Levofloxacin
absolute
null
500-1000mg once daily
oral administration
null
intravenous
null
null
14664657
starling
starling_oba
553096c07a1ef6eb023577adb76cd62acc103821ac7098777e654c3a8f044648
38
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
553096c07a1ef6eb023577adb76cd62acc103821ac7098777e654c3a8f044648
2d708ec8c72feb82c390385576bb85d10e311638890828f5c02a4db6eb672535
pharmacokinetics are linear over the dosage range 500–1000mg once daily for multiple-dose administration; oral and intravenous routes are considered interchangeable
Levofloxacin is rapidly absorbed after oral administration, with an absolute bioavailability of approximately 99%. Its pharmacokinetics are linear over the dosage range of 500–1000mg once daily for multiple-dose administration, and the oral and intravenous routes are considered interchangeable.
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2
11
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
11
percent
false
mycophenolate mofetil
absolute
null
null
oral administration
null
vs intravenous administration
null
null
8728345
starling
starling_oba
f17ef84ea437fe398cc92f88bc0477202466b78df8f0e58b5ef0ce30c6fd7b93
39
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
f17ef84ea437fe398cc92f88bc0477202466b78df8f0e58b5ef0ce30c6fd7b93
d04276d735964db5ca052c9088c3a72fc044c8e3a296192a170dbc2d064eca28
This value represents the upper limit based on the ratio of plasma Cmax values (0.4/3.5).
The upper limit of the absolute bioavailability of MMF after oral administration (based on the ratio of plasma Cmax values for MMF) was therefore 0.4/3.5, or 11%.
[O-][Cl+][O-]
23
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
mouse
23
percent
false
MnTE-2-PyP⁵⁺
absolute
mice
10 mg/kg
oral gavage
null
vs iv
rodent
mice | oral gavage | not specified | vs iv
23328731
starling
starling_oba
d86864b2d7a2b24a002d5a91ed79ea771104964dd22ed609ad12a1ce408878f1
41
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
d86864b2d7a2b24a002d5a91ed79ea771104964dd22ed609ad12a1ce408878f1
febe7900f0b30fbaacea0838d9ed19fe35c4e6b532a844ebfdb43fa43dc4a675
Calculated using AUC ratio; intravenous dose was also 10 mg/kg.
For MnTE-2-PyP⁵⁺ in mice, an oral availability of 23% was calculated using identical oral and intravenous doses of 10 mg/kg.
O=[N+]([O-])[O-]
21
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
mouse
21
percent
false
MnTnHex-2-PyP⁵⁺
absolute
mice
2 mg/kg
oral gavage
null
vs iv
rodent
mice | oral gavage | not specified | vs iv
23328731
starling
starling_oba
18ab0cb0e23d52f3d1c4350943407bb18debe05b30e8471ea0cbeeeba98fad3e
42
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
18ab0cb0e23d52f3d1c4350943407bb18debe05b30e8471ea0cbeeeba98fad3e
f129cc634a07cd825ccb386ba4aa1ff4f5a2ee82be9b7c56b04794d7241e94e0
Calculated using AUC ratio; intravenous dose was limited to 0.5 mg/kg due to toxicity (blood pressure drop).
The oral availability of MnTnHex-2-PyP⁵⁺ in mice was determined to be 21%, based on an oral dose of 2 mg/kg and an intravenous dose of 0.5 mg/kg.
C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(O)(c2ccccc2)CC1
22.8
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
22.8
percent
false
Traxoprodil
absolute
cyp2d6 extensive metabolisers
50mg
po
null
vs 100mg iv
null
cyp2d6 extensive metabolisers | po | not specified | vs 100mg iv
16984212
starling
starling_oba
68bf1c079ca2251ffd4d7f41a153258a43bdbf14f9f1ccec32bac2c938c890ad
43
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
68bf1c079ca2251ffd4d7f41a153258a43bdbf14f9f1ccec32bac2c938c890ad
9afd3e60b6f7f3f5066a8cb6d2252bd111277e0da28db36aad72c4eedf2be9d8
Sample size n = 3; bioavailability calculated based on the 100mg intravenous dose.
In CYP2D6 extensive metabolisers, the absolute oral bioavailability (F) of traxoprodil after a 50mg oral (PO) dose was 22.8%.
C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(O)(c2ccccc2)CC1
39.5
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
39.5
percent
false
Traxoprodil
absolute
cyp2d6 extensive metabolisers
100mg
po
null
vs 100mg iv
null
cyp2d6 extensive metabolisers | po | not specified | vs 100mg iv
16984212
starling
starling_oba
16fc9680ad187887c377e62c83fd1242bc01612d3d44a0c4b5a7f37462c273a0
44
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
16fc9680ad187887c377e62c83fd1242bc01612d3d44a0c4b5a7f37462c273a0
ac7ebaa8146da6536f3bafbfac67eea3aa66e3d9ad7602e1a8e83e269f7b2319
Sample size n = 10; bioavailability calculated based on the 100mg intravenous dose.
In CYP2D6 extensive metabolisers, the absolute oral bioavailability (F) of traxoprodil after a 100mg oral (PO) dose was 39.5 (20.1)%.
C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(O)(c2ccccc2)CC1
62.1
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
62.1
percent
false
Traxoprodil
absolute
cyp2d6 extensive metabolisers
300mg
po
null
vs 100mg iv
null
cyp2d6 extensive metabolisers | po | not specified | vs 100mg iv
16984212
starling
starling_oba
d880927ef644637769e2bef5223cbb907ffa96cfe405334dbf0f779af5f7de93
45
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
d880927ef644637769e2bef5223cbb907ffa96cfe405334dbf0f779af5f7de93
619754ad2f5a173479cc3331e66bbdecc3bdd296e738c04d357166b89e043bcb
Sample size n = 5; bioavailability calculated based on the 100mg intravenous dose.
In CYP2D6 extensive metabolisers, the absolute oral bioavailability (F) of traxoprodil after a 300mg oral (PO) dose was 62.1 (26.9)%.
O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1
88
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
88
percent
false
solifenacin
absolute
healthy men
10mg
null
null
vs iv
human
healthy men | not specified | not specified | vs iv
15293866
starling
starling_oba
b73c31d9ca23857465fb43fe47ccfb0fed9216b88e1123c2b07da55869454702
49
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
b73c31d9ca23857465fb43fe47ccfb0fed9216b88e1123c2b07da55869454702
900642dd2b6c9d16050a41c1d327f1b5f681f0ef5b0950bd2fb96a80a9be73a3
Bioavailability was calculated by comparing plasma concentrations after a 10mg oral dose and a 5mg IV dose.
Pharmacokinetic analyses of twelve healthy men (aged 20–45 years) demonstrated that solifenacin has a high absolute oral availability of 88%, determined by comparing a single 10mg oral dose with a single 5mg intravenous (IV) dose.
O=C([O-])c1ccc(/C=C/S(=O)(=O)Cc2ccc(Cl)cc2)cc1.[Na+]
30
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
30
percent
false
ON 01210.Na
absolute
monkeys
125 mg/kg
50% peg
null
i.v.
monkey
monkeys | 50% peg | not specified | i.v.
21341279
starling
starling_oba
73856f53478618dde7be96f8b0fd6b0ab7fb2364f30cb1cfe08da00a7acab209
55
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
73856f53478618dde7be96f8b0fd6b0ab7fb2364f30cb1cfe08da00a7acab209
d35faa5d35af8eb2973f7965fc999deb1a039c561ff161de05a90f1e4acb262a
Cmax: 28.6 (4.87) µg/ml, AUC: 154 (14.5) µg*h/ml; bioavailability estimated based on ratio of dose-normalized AUC.
Following p.o. administration of a 50% PEG formulation of ON 01210.Na to monkeys at a dose of 125 mg/kg, the bioavailability was 30%, calculated based on the ratio of dose-normalized AUC compared with i.v. dosing.
C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(O)(c2ccccc2)CC1
80
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
80
percent
false
Traxoprodil
absolute
healthy male volunteers
50, 100 and 300mg
solution
cyp2d6 poor metabolisers
iv
human
healthy male volunteers | solution | cyp2d6 poor metabolisers | iv
16984212
starling
starling_oba
2d13447a00009e7531906f68b176f7459518a3668b3be7027a7223219bc63640
56
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
2d13447a00009e7531906f68b176f7459518a3668b3be7027a7223219bc63640
ca5ee6e30b61ff98cd04dca41a808b0845f224115a9ea5e79e0ce56888a7a110
Sample size n = 6; consistent with a liver extraction ratio of ~20% (plasma clearance of ~4 mL/min/kg), indicating near complete absorption.
In poor metabolisers (n = 6), the oral bioavailability of traxoprodil was ~80%, which was consistent with a liver extraction ratio of ~20% and indicated near complete absorption.
C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(O)(c2ccccc2)CC1
39.5
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
39.5
percent
false
Traxoprodil
absolute
healthy male volunteers
100mg
solution
cyp2d6 extensive metabolisers
iv
human
healthy male volunteers | solution | cyp2d6 extensive metabolisers | iv
16984212
starling
starling_oba
cb39718cf325ca319e5e5ac9c1331cb1d7fba3bda62b021a3e1ba10a8761d1e8
57
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
cb39718cf325ca319e5e5ac9c1331cb1d7fba3bda62b021a3e1ba10a8761d1e8
a2fb20ae4f29b018da26ba572d156af4b3d7ad8410ca2c06c1b26a7166983b2c
Sample size n = 11; oral bioavailability was reported as dose-dependent and nonlinear in this population.
In extensive metabolisers (n = 11), traxoprodil oral bioavailability was dose-dependent and nonlinear; at the 100mg dose, the absolute oral bioavailability was ~39.5%.
C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(O)(c2ccccc2)CC1
22.8
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
22.8
percent
false
Traxoprodil
absolute
healthy male volunteers
null
solution
cyp2d6 extensive metabolisers
iv
human
healthy male volunteers | solution | cyp2d6 extensive metabolisers | iv
16984212
starling
starling_oba
cf95892ec79b8a5fcabfd4146c9ec8276e8cb70ffec728c148593f743c91819c
58
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
cf95892ec79b8a5fcabfd4146c9ec8276e8cb70ffec728c148593f743c91819c
2d1160c377ba0b0f82d855efd92bfa2803314088a421988a7d66c89869844e8f
Sample size n = 11; estimation was confounded by large differences in plasma concentrations at oral doses without equivalent intravenous doses.
Overall, the oral bioavailability of traxoprodil in extensive metabolisers ranged from 22.8% to 62.1%.
NC(=O)N/N=C/c1ccc([N+](=O)[O-])o1
114.97
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rabbit
114.97
percent
false
Nitrofurazone
absolute
rabbits
63.5 mg/kg
gavage
null
vs iv
rabbit
rabbits | gavage | not specified | vs iv
23957951
starling
starling_oba
d683b0e77d5ffac0b6ce2d21b203e379f20b5bd90a7f694ab17f800592c38fa7
59
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
d683b0e77d5ffac0b6ce2d21b203e379f20b5bd90a7f694ab17f800592c38fa7
40b0932b7d3c5f27cad66c77d03ebe02e73ae2c8757843352230a700d65a5023
n=5 subjects
For Nitrofurazone (NF) administered orally at 63.5 mg/kg via gavage, the absolute bioavailability (F absolute) was reported as 114.97% in a study with n=5 subjects, compared to intravenous administration.
O=C(O)/C=C/C(=O)O.O=C(c1ccc(F)c(F)c1Nc1ccc(I)cc1F)N1CC(O)([C@@H]2CCCCN2)C1.O=C(c1ccc(F)c(F)c1Nc1ccc(I)cc1F)N1CC(O)([C@@H]2CCCCN2)C1
46.2
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
46.2
percent
false
(S)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl][3-hydroxy-3-(piperidin-2-yl)-azetidin-1-yl]methanone hemifumarate
absolute
healthy subjects
20 mg
null
null
2 mg intravenous infusion
human
healthy subjects | not specified | not specified | 2 mg intravenous infusion
24010577
starling
starling_oba
7d6a65881cd0e0121e8562fb2a437b3d79c15f72630da3051e6e56bc04994063
60
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
7d6a65881cd0e0121e8562fb2a437b3d79c15f72630da3051e6e56bc04994063
5171a7c2d9fcce9ab6c7dca474bd20e46f74c453b0d1776e57f3642733b70933
CV 24.2%, n = 13
In a crossover trial involving 13 healthy subjects, the absolute bioavailability of (S)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl][3-hydroxy-3-(piperidin-2-yl)-azetidin-1-yl]methanone hemifumarate (cobimetinib) was 46.2% (CV 24.2%) following a 20 mg oral dose compared to a 2 mg intravenous infusion.
CC1C2OC3(C)CC(=O)C1CC3(O)O2
80
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
80
percent
false
Paeonimetabolin I
absolute
rats
0.2 mg/kg
null
null
vs iv
rodent
rats | not specified | not specified | vs iv
9178932
starling
starling_oba
f35eb5a34c328388ef54bf0bf020b1b8840df32c1d74687922ee130bee9eefa5
61
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
f35eb5a34c328388ef54bf0bf020b1b8840df32c1d74687922ee130bee9eefa5
d13ab24dcde0409c073886ef1cfd0a26a20714e2821779f1be0a3e3f388e2a4b
Calculated from the AUCs after intravenous and oral administration.
After oral administration of Paeonimetabolin I (PM-I, 2) to rats at a dose of 0.2 mg/kg, the bioavailability (F) was reported as 0.8 ± 0.15.
CC1C2OC3(C)CC(=O)C1CC3(O)O2
107
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
107
percent
false
Paeonimetabolin I
absolute
rats
2 mg/kg
null
null
vs iv
rodent
rats | not specified | not specified | vs iv
9178932
starling
starling_oba
9e8dc88a723e2e1a93b7f6d602cca82c1f3cedd27c46ddf3a1b307754dd7ec98
62
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
9e8dc88a723e2e1a93b7f6d602cca82c1f3cedd27c46ddf3a1b307754dd7ec98
eb975b2d618f134d97240ffc0cbe8416625e9ff19a0edd1b6c241a05e8644066
Calculated from the AUCs after intravenous and oral administration.
After oral administration of Paeonimetabolin I (PM-I, 2) to rats at a dose of 2 mg/kg, the bioavailability (F) was reported as 1.07 ± 0.07.
COc1cc(Nc2ncc(F)c(Nc3ccc4c(n3)N(COP(=O)(O)O)C(=O)C(C)(C)O4)n2)cc(OC)c1OC
54.6
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
human
54.6
percent
false
Fostamatinib
absolute
humans
null
oral
null
null
human
humans | oral | not specified | not specified
27858108
starling
starling_oba
4f0c6c4ebca2fed15fa2a4d1edb1b0ef0389fa42164dfa82f95af0757f9349cd
63
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
4f0c6c4ebca2fed15fa2a4d1edb1b0ef0389fa42164dfa82f95af0757f9349cd
b56ef855704863b737f3edef2adc87be65e5af925d315a09f0176e3a6facac74
null
Clinical studies were performed to determine the absolute oral bioavailability of fostamatinib, which was found to be 54.6 %.
CN1CCN(C2=Nc3ccccc3Oc3ccc(Cl)cc32)CC1
29
starling.oral_bioavailability.systemic_availability.percent
oral_bioavailability
systemic_availability
percent
human
29
percent
false
Loxapine
systemic availability
humans
null
null
null
null
human
humans | not specified | not specified | not specified
15359567
starling
starling_oba
3ba3faeed353e2bd23bbd25ef90eb30aa6593465b9564bb85c66950ae1f2391c
64
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
3ba3faeed353e2bd23bbd25ef90eb30aa6593465b9564bb85c66950ae1f2391c
5af0700b4d5ae48383a4bd117e26e50833e444dae0068fa3a28fab0027e477fa
The drug is described as highly extracted with a hepatic extraction ratio (EH) of 0.71.
For loxapine, the fraction of the parent drug absorbed into the systemic circulation (F) was estimated as 0.29, indicating that the drug is highly extracted with a hepatic extraction ratio (EH) of 0.71.
O=S(=O)(c1ccc(O)cc1)c1ccc(O)cc1
57.4
starling.oral_bioavailability.systemic_availability.percent
oral_bioavailability
systemic_availability
percent
pig
57.4
percent
false
BPS
systemic availability
male and female piglets (28-42 d)
40 μg/kg
oral
null
null
pig
male and female piglets (28-42 d) | oral | not specified | not specified
32853628
starling
starling_oba
b31c5a4ec0a0ff4e52f7fb27ad14550764fba17d89d85b95fabc6d4c990eea85
65
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
b31c5a4ec0a0ff4e52f7fb27ad14550764fba17d89d85b95fabc6d4c990eea85
10a861df6fb20cb0b7d78b490d14c116c15660273affa8fef372837134253b61
~ 99% of the administered dose was absorbed with the maximum concentration, Cmax, reached at 0.5 h.
In male and female piglets (28–42 d), following a 40 µg/kg oral dose of BPS, the estimated systemic bioavailability was 57.4%, with approximately 99% of the administered dose being absorbed.
O=S(=O)(c1ccc(O)cc1)c1ccc(O)cc1
62
starling.oral_bioavailability.systemic_availability.percent
oral_bioavailability
systemic_availability
percent
human
62
percent
false
deuterated BPS
systemic availability
human volunteers
0.1 mg/kg
oral
deuterated bps
null
human
human volunteers | oral | deuterated bps | not specified
32853628
starling
starling_oba
08c3430dcb5f4f8c7b12931c83f2be41045700f788582bc48e081c5bf6e351e8
66
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
08c3430dcb5f4f8c7b12931c83f2be41045700f788582bc48e081c5bf6e351e8
184ced7af578bbc2ffaf497213d0763be2bcff92f57e44b4ff76f659c56b98ec
Cmax was reached at 0.7 h and 1.1 h for BPS and its glucuronide, respectively, with plasma elimination half-lives of 7.9 h and 9.3 h, respectively.
In a study where six human volunteers were administered 0.1 mg/kg deuterated BPS orally, the estimated systemic bioavailability was 62%.
Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1
110
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
cockatiel
110
percent
false
celecoxib
absolute
cockatiels (nymphicus hollandicus)
10 mg/kg bw
oral (po)
standard solution (std)
vs iv
bird
cockatiels (nymphicus hollandicus) | oral (po) | standard solution (std) | vs iv
28947805
starling
starling_oba
a603cd83dfdbb2b90e72b653c612fc829891909a54eff582e811510c6aa1620a
67
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
a603cd83dfdbb2b90e72b653c612fc829891909a54eff582e811510c6aa1620a
404cf502231102d5612a33e86e6384f48fc5037793d871697ecbbcb91e4fa813
Dose specified in paragraph 10.
In cockatiels, the absolute oral bioavailability (F%) of celecoxib was 110% when administered as a standard solution (STD).
Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1
56
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
cockatiel
56
percent
false
celecoxib
absolute
cockatiels (nymphicus hollandicus)
10 mg/kg bw
oral (po)
commercial formulation (cf)
vs iv
bird
cockatiels (nymphicus hollandicus) | oral (po) | commercial formulation (cf) | vs iv
28947805
starling
starling_oba
0d4966e9c5499f6974222087a8b5f71d8a9f3a402ca506798c8154f152587acb
68
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
0d4966e9c5499f6974222087a8b5f71d8a9f3a402ca506798c8154f152587acb
b7d57bf5728be511f5116ce51734bed5f76312ed8c3e39306e45cab9b277d28b
Dose specified in paragraph 10.
In cockatiels, the absolute oral bioavailability (F%) of celecoxib was 56% when administered as a commercial formulation (CF).
NS(=O)(=O)c1ccc(-n2nc(C(F)(F)F)cc2-c2ccc(F)cc2)cc1
113
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
cockatiel
113
percent
false
mavacoxib
absolute
cockatiels (nymphicus hollandicus)
4 mg/kg bw
oral (po)
standard solution (std)
vs iv
bird
cockatiels (nymphicus hollandicus) | oral (po) | standard solution (std) | vs iv
28947805
starling
starling_oba
1ce7a12c71bd155da8638eda7478a0584fd7dfa3e9bd56558eed054809e3bee9
69
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
1ce7a12c71bd155da8638eda7478a0584fd7dfa3e9bd56558eed054809e3bee9
23b0f98dfb34219b00aaa32a88d5c371a05977750c2a654c06a88285aa8cf87c
Dose specified in paragraph 16.
For mavacoxib in cockatiels, the absolute oral bioavailability (F%) was 113% for the standard solution (STD).
NS(=O)(=O)c1ccc(-n2nc(C(F)(F)F)cc2-c2ccc(F)cc2)cc1
111
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
cockatiel
111
percent
false
mavacoxib
absolute
cockatiels (nymphicus hollandicus)
4 mg/kg bw
oral (po)
commercial formulation (cf)
vs iv
bird
cockatiels (nymphicus hollandicus) | oral (po) | commercial formulation (cf) | vs iv
28947805
starling
starling_oba
2dfaba166e74c63bbbdb67e8fcb01ba6855f714223bde96079e0d972c0ef921e
70
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
2dfaba166e74c63bbbdb67e8fcb01ba6855f714223bde96079e0d972c0ef921e
097d7bc644f9afec77d525aa892457b965ff77af7b846fc77c9e3172da5737ad
Dose specified in paragraph 16.
For mavacoxib in cockatiels, the absolute oral bioavailability (F%) was 111% for the commercial formulation (CF).
O=c1c(-n2ccnn2)c[nH]n1-c1cc(N2CCOCC2)ncn1
59
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
59
percent
false
molidustat
absolute
healthy male participants
null
immediate release tablets
null
intravenous administration
human
healthy male participants | immediate release tablets | not specified | intravenous administration
32248614
starling
starling_oba
e235def906deb6453e735fda3eef80db2a235505a195ae7ee5a73155015b6cf6
71
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
e235def906deb6453e735fda3eef80db2a235505a195ae7ee5a73155015b6cf6
29f9552a151cc042d2afc7c47a8c756b04b329138abeccec234854eb085b20a1
Reported in Study 2.
In Study 2, which investigated healthy male participants, orally administered molidustat immediate release tablets had an absolute bioavailability of 59%.
O=c1c(-n2ccnn2)c[nH]n1-c1cc(N2CCOCC2)ncn1
34
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
34
percent
false
molidustat
absolute
rat
null
null
null
null
rodent
rat | not specified | not specified | not specified
32248614
starling
starling_oba
bbe3edfe47a0fa288e27d1104de07082964ed12f0de45c9d7af83c482605e4f8
72
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
bbe3edfe47a0fa288e27d1104de07082964ed12f0de45c9d7af83c482605e4f8
23664f8cc11d6ef45ad3273d237b01a4205d1a5db1322009799a55a139c3956d
null
The absolute bioavailability (F) of molidustat varies among species, including 34% in rat.
O=c1c(-n2ccnn2)c[nH]n1-c1cc(N2CCOCC2)ncn1
61
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
61
percent
false
molidustat
absolute
monkey
null
null
null
null
monkey
monkey | not specified | not specified | not specified
32248614
starling
starling_oba
b6925b24bd4272be87c22ee73348eb5986189626049e9742c7c12b6d5f27c1ce
73
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
b6925b24bd4272be87c22ee73348eb5986189626049e9742c7c12b6d5f27c1ce
472aa928721505f927eb00cf11897271147ede02bcb734f6e8ddcc74716e8e49
null
The absolute bioavailability (F) of molidustat varies among species, including 61% in monkey.
O=c1c(-n2ccnn2)c[nH]n1-c1cc(N2CCOCC2)ncn1
71
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
dog
71
percent
false
molidustat
absolute
dog
null
null
null
null
dog
dog | not specified | not specified | not specified
32248614
starling
starling_oba
a64fcce1d44b4bfb8557fcf1edfc8f22c6328f19672d9900731714108adb8188
74
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
a64fcce1d44b4bfb8557fcf1edfc8f22c6328f19672d9900731714108adb8188
9ba19df34cd633400f767f0d8fabb34dcb4d323f64b903998fcc6043eb5df31c
null
The absolute bioavailability (F) of molidustat varies among species, including 71% in dog.
CC1=C[C@H]2O[C@@H]3[C@H](O)C[C@](C)([C@@]2(CO)[C@H](O)C1=O)[C@]31CO1
19.3
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
chicken
19.3
percent
false
deoxynivalenol
absolute
broilers
0.75 mg/kg bw
bolus
null
intravenously
bird
broilers | bolus | not specified | intravenously
23099502
starling
starling_oba
107ede91fdc74df4cb1b3adbefd87827f6b482041805c00bcf3e4bfaf6a0b391
75
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
107ede91fdc74df4cb1b3adbefd87827f6b482041805c00bcf3e4bfaf6a0b391
0677ebac0d5b5c338a11bb1996ad9fe90c142d1c2631049a7077909f635b6da4
The value was described as low.
In broilers, deoxynivalenol administered as a bolus of 0.75 mg/kg BW showed a low absolute oral bioavailability of 19.3%.
CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](O[C@@H]2O[C@H](C(=O)O)[C@@H](O)[C@H](O)[C@H]2O)C=C[C@H]3[C@H]1C5
11
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
11
percent
false
M6G
absolute
subjects
20 mg
oral
null
vs iv
human
subjects | oral | not specified | vs iv
11966664
starling
starling_oba
3f4d24257f38ec5eedd9b8e595a920a1e17d165d7ae0608bf72cf931361fbb42
76
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
3f4d24257f38ec5eedd9b8e595a920a1e17d165d7ae0608bf72cf931361fbb42
55d600b6fbcc2c8991f1ab35d12fc4f06358d7bd08c3a6eaa1d02adac9c90132
Range 6–15%, 90% CI 9, 12%; calculated using AUC(0,tn). Dose of 20 mg given in 50 ml water.
The overall bioavailability of oral M6G (using AUC(0,tn)) was 11 ± 3% (range 6–15%, 90% CI 9, 12%), with the highest value occurring in the subject with the highest i.v. M6G clearance.
CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](O[C@@H]2O[C@H](C(=O)O)[C@@H](O)[C@H](O)[C@H]2O)C=C[C@H]3[C@H]1C5
4
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
4
percent
false
M6G
absolute
subjects
20 mg
oral
directly absorbed oral m6g (contributing to the first plasma m6g peak)
vs iv
human
subjects | oral | directly absorbed oral m6g (contributing to the first plasma m6g peak) | vs iv
11966664
starling
starling_oba
1940ae45de645d6742845bfc95213343c844831d127d64375aebc07397236cf2
77
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
1940ae45de645d6742845bfc95213343c844831d127d64375aebc07397236cf2
b2271b0cf4e333a0a1e7ac575162d313fa4ede28feb5930899852a2b81558fe8
Range 1–12%. Dose of 20 mg given in 50 ml water.
The bioavailability of directly absorbed oral M6G, contributing to the first plasma M6G peak before the appearance of morphine or M3G, was 4 ± 4% (range 1–12%).
O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1
90
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
90
percent
false
Solifenacin succinate
absolute
healthy adults
null
null
null
null
human
healthy adults | not specified | not specified | not specified
19566112
starling
starling_oba
efd005a747cf3fc3cf36f1c2abd48f61cadc59c08cdfe5f59b3e45122a7f3371
79
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
efd005a747cf3fc3cf36f1c2abd48f61cadc59c08cdfe5f59b3e45122a7f3371
e3f6fb54f5e3e3e827e4f608069b61e263cd93740593198148e7a13b78e7cd30
Bioavailability does not decrease with concomitant food intake.
Studies in healthy adults have shown that solifenacin succinate has a high absolute bioavailability of about 90%, which does not decrease with concomitant food intake.
Cc1ccc(-c2ncc(Cl)cc2-c2ccc(S(C)(=O)=O)cc2)cn1
100
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
100
percent
false
Etoricoxib
absolute
healthy subjects
120-mg
tablet
fasted state
vs iv
human
healthy subjects | tablet | fasted state | vs iv
12638395
starling
starling_oba
714a73f8bc01712d29a683e78fabe93672c56305658d4081017d421dd5636977
80
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
714a73f8bc01712d29a683e78fabe93672c56305658d4081017d421dd5636977
a90020043bbcfe0a27e7e2a1da9f4f9584b91c83c30d3c33d5cf927fe1e132d8
Bioavailability was estimated to be 100% based on a comparison between a 120-mg tablet and a 25-mg IV dose in healthy subjects.
Etoricoxib administered as a 120-mg tablet was rapidly and completely absorbed and available, with the absolute bioavailability estimated to be 100%.
O=C1CCc2cc(OCCCCc3nnnn3C3CCCCC3)ccc2N1
4.2
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
4.2
percent
false
Cilostazol
absolute
male rats
0.5 mg/kg
oral administration
null
vs iv
rodent
male rats | oral administration | not specified | vs iv
21718207
starling
starling_oba
d2e8d0eef267c0a90e08dd5650557dab2c276a2bf8f8d269687dab47f88d89d1
81
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
d2e8d0eef267c0a90e08dd5650557dab2c276a2bf8f8d269687dab47f88d89d1
098cc8bd8cbef9e33daa93830db25747879b5f7d7b2520d4ffd2c3001f8ba360
calculated utilizing the results of in vivo intravenous administration study
The absolute bioavailability after oral dosing of 0.5 mg/kg of cilostazol was calculated to be 4.2 ± 1.2% in male rats.
O=C1CCc2cc(OCCCCc3nnnn3C3CCCCC3)ccc2N1
6.4
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
6.4
percent
false
Cilostazol
absolute
male rats
1 mg/kg
oral administration
null
vs iv
rodent
male rats | oral administration | not specified | vs iv
21718207
starling
starling_oba
34e9d2ff87e764f95b27a0b752e06947bcf2cd4303a2277a684675afd4bee893
82
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
34e9d2ff87e764f95b27a0b752e06947bcf2cd4303a2277a684675afd4bee893
82b5b24ae97e59efc45263b8fea668f2cbd582594026e4475013122dc2bd6ccf
calculated utilizing the results of in vivo intravenous administration study
The absolute bioavailability after oral dosing of 1 mg/kg of cilostazol was calculated to be 6.4 ± 0.7% in male rats.
O=C1CCc2cc(OCCCCc3nnnn3C3CCCCC3)ccc2N1
21.1
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
21.1
percent
false
Cilostazol
absolute
female rats
0.5 mg/kg
oral administration
null
vs iv
rodent
female rats | oral administration | not specified | vs iv
21718207
starling
starling_oba
bea5d2023871894e33645ff0b19bbbae2afb15097bad71af042c1bd1e4ecf59e
83
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
bea5d2023871894e33645ff0b19bbbae2afb15097bad71af042c1bd1e4ecf59e
ba655da8a045a9f40d034ab817663592de734067011daaf8a978b7b949429c15
calculated utilizing the results of in vivo intravenous administration study
The absolute bioavailability after oral dosing of 0.5 mg/kg of cilostazol was calculated to be 21.1 ± 6.1% in female rats.
O=C1CCc2cc(OCCCCc3nnnn3C3CCCCC3)ccc2N1
37.2
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
37.2
percent
false
Cilostazol
absolute
female rats
1 mg/kg
oral administration
null
vs iv
rodent
female rats | oral administration | not specified | vs iv
21718207
starling
starling_oba
15126758149825a7dec6502358b891c9429676175f37fd17c0e8501722905593
84
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
15126758149825a7dec6502358b891c9429676175f37fd17c0e8501722905593
dd93e9476d11ad7ee785a220eb5a2c2e4ee53bf9f84078da38cd02a664d82c08
calculated utilizing the results of in vivo intravenous administration study
The absolute bioavailability after oral dosing of 1 mg/kg of cilostazol was calculated to be 37.2 ± 2.8% in female rats.
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)O)C(=O)OC2
94.1
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
94.1
percent
false
mycophenolic acid
absolute
healthy volunteers
1.5 g
oral
administered as prodrug mycophenolate mofetil
vs intravenous route
human
healthy volunteers | oral | administered as prodrug mycophenolate mofetil | vs intravenous route
8728345
starling
starling_oba
0f7a0118e1a30b26436f171fbf0ad078700969b8a05b6dcda7d11d7d7d21ad53
85
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
0f7a0118e1a30b26436f171fbf0ad078700969b8a05b6dcda7d11d7d7d21ad53
2ba0c95ec60da843a8cd0a2bb956a63a3791f04e7e455c09b5404920985de90a
The bioavailability was estimated based on the total area under the concentration-time curve (AUC) and was found to be statistically equivalent (80-120 rule) between routes.
In a study of 12 healthy volunteers, the mean bioavailability of mycophenolic acid (MPA) following oral administration of a 1.5-g dose of the prodrug mycophenolate mofetil (MMF) was estimated as 94.1% relative to the intravenous route.
CC1=C[C@H]2O[C@@H]3[C@H](O)C[C@](C)([C@@]2(CO)[C@H](O)C1=O)[C@]31CO1
70.5
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
pig
70.5
percent
false
DON
absolute
pigs
100 μg/kg
gavage
null
vs iv
pig
pigs | gavage | not specified | vs iv
26633505
starling
starling_oba
6164ae60dc2462aa717d525af889b22fdbb18c7551fac320363e0f4a5c6534c7
89
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
6164ae60dc2462aa717d525af889b22fdbb18c7551fac320363e0f4a5c6534c7
6d0aa018115a4eed39bd24ffdda8326fbc05ae43926fb72590a2460ce7faa5d4
Estimated by deconvolution analysis.
Deconvolution analysis estimated the absolute bioavailability of DON in pigs at 70.5% ± 25.6% after oral administration of 100 µg/kg.
Cc1cccc2sc3nncn3c12
93.9
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
93.9
percent
false
tricyclazole
absolute
male fischer 344 rats
2 mg/kg
oral
null
vs iv
rodent
male fischer 344 rats | oral | not specified | vs iv
31461669
starling
starling_oba
9f3a37358c9201c65ac3a8985ae58ad6d35771cb702aaeeabd31934963412bf7
92
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
9f3a37358c9201c65ac3a8985ae58ad6d35771cb702aaeeabd31934963412bf7
ce8abbc68b583ab6aeb7c212eed8779ba98589e696fd446f2925c2ba82c2286a
AUC₀–96hr was 11.7 µg h/mL for oral dosing and 12.5 µg h/mL for I.V. injection.
In a study by Johnson et al. (2014), Male Fischer 344 rats were administered tricyclazole at a dose of 2 mg/kg either orally or intravenously. The absolute bioavailability value determined for tricyclazole in this study is 93.9%.
O=c1oc2ccccc2c(O)c1Cc1c(O)c2ccccc2oc1=O
61
starling.oral_bioavailability.systemic_availability.percent
oral_bioavailability
systemic_availability
percent
rat
61
percent
false
dicumarol
systemic availability
rat
50 mg/kg
po
intravenous phenobarbital treatment (75 mg/kg/day iv beginning 5 days before dicumarol administration)
vs iv
rodent
rat | po | intravenous phenobarbital treatment (75 mg/kg/day iv beginning 5 days before dicumarol administration) | vs iv
90143
starling
starling_oba
4fbebb12880d5ceb668bda7d0112c7ef4abaaaa3c7b102987d2f56d8c2cc4f9e
93
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
4fbebb12880d5ceb668bda7d0112c7ef4abaaaa3c7b102987d2f56d8c2cc4f9e
5b7e2e05ee19c78211045d3103bf6f21edb01a17eeab70fbbe22f40ad3ca4bc9
Determined by simultaneous administration of unlabeled dicumarol orally and 14C-dicumarol intravenously.
Intravenous phenobarbital reduced the extent of absorption of orally administered dicumarol (50 mg/kg po) to 61% of the dose in rats.
OC[C@@H]1CC[C@H](n2cnc3c(O)ncnc32)O1
43
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
43
percent
false
didanosine
absolute
patients with aids and advanced aids-related complex
0.8 to 10.2 mg/kg
solution with an antacid
null
iv
human
patients with aids and advanced aids-related complex | solution with an antacid | not specified | iv
1903100
starling
starling_oba
4b20e7f09978865dbec779cf1a740f0d4f96f0b064156163b89bd79cd7685d26
94
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
4b20e7f09978865dbec779cf1a740f0d4f96f0b064156163b89bd79cd7685d26
fc16f951637d0bf0ce22c3dee745008806815b856626b1333ad02dcac1f7b9e8
Oral bioavailability was determined by evaluating pharmacokinetics after both intravenous and oral administration.
Bioavailability of didanosine when administered as a solution with an antacid was approximately 43% for doses from 0.8 to 10.2 mg/kg in patients with AIDS and advanced AIDS-related complex.
C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(O)(c2ccccc2)CC1
79.6
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
79.6
percent
false
Traxoprodil
absolute
cyp2d6 poor metabolisers
50mg
null
null
vs iv
null
cyp2d6 poor metabolisers | not specified | not specified | vs iv
16984212
starling
starling_oba
7c3f04f68210629de1a4dc9330ff0a8383118457a63691fe537ebb63f53d58c0
97
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
7c3f04f68210629de1a4dc9330ff0a8383118457a63691fe537ebb63f53d58c0
f8f81efbf0b5f2e424df45734d71916eefe113e9ba03a69dce0ffbfe92319c65
Reported in Table IV; text in [p:62] describes bioavailability as similar (~80%) at the two oral doses.
In CYP2D6 poor metabolisers, the absolute oral bioavailability (F) of Traxoprodil was 79.6% following a 50mg oral dose.
C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(O)(c2ccccc2)CC1
84.7
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
84.7
percent
false
Traxoprodil
absolute
cyp2d6 poor metabolisers
100mg
null
null
vs iv
null
cyp2d6 poor metabolisers | not specified | not specified | vs iv
16984212
starling
starling_oba
06884e57fb517cd0c43ecdf43d02014fc1142db987c40402a31c3984518e0343
98
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
06884e57fb517cd0c43ecdf43d02014fc1142db987c40402a31c3984518e0343
b5ef8707ea2cc95e5d76b29260aa49c3c359cc5255cf17ddbb697ab531ca882c
Reported in Table IV; text in [p:62] describes bioavailability as similar (~80%) at the two oral doses.
In CYP2D6 poor metabolisers, the absolute oral bioavailability (F) of Traxoprodil was 84.7% following a 100mg oral dose.
Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Nc4nccc(-c5cccnc5)n4)c3)cc(C(F)(F)F)c2)cn1
31
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
31
percent
false
Nilotinib
absolute
null
null
oral
null
null
null
null
21827214
starling
starling_oba
3476626070ea60671ba2bffac8c381a80311934f44dff1828330c24353064eaa
99
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
3476626070ea60671ba2bffac8c381a80311934f44dff1828330c24353064eaa
e2960ff8888e2b2ca1f2a581616b2bfe315b93742217fcb1d42fb64283c50e6b
bioavailability is substantially increased with food
Following oral administration of nilotinib, a low absolute bioavailability of about 31% is assumed for the drug, although its bioavailability is substantially increased with food.
[O-][n+]1cccc(-c2nc3c(Cl)cccc3cc2[C@@H](Nc2ncnc3cccnc23)C(F)(F)F)c1
97
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
97
percent
false
seletalisib
absolute
healthy subjects
30 mg
reference formulation
null
vs iv
human
healthy subjects | reference formulation | not specified | vs iv
28650526
starling
starling_oba
68e28414d936543cfdd6f40fa96ea5a8a0c9a81bb58e1607afa40e6b9303a8ec
102
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
68e28414d936543cfdd6f40fa96ea5a8a0c9a81bb58e1607afa40e6b9303a8ec
dd63b15d38700dfaf140c3a9307a526a09592c4d39313d36bb3ba52838c0e2f9
n = 6; reference formulation used
In a study of healthy subjects receiving 30 mg of a reference formulation of seletalisib orally, the absolute oral bioavailability was found to be 97% (90% confidence interval 87, 107).
NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)CCC(=O)C3
69
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
69
percent
false
Samidorphan
absolute
healthy volunteers
null
null
null
vs iv
human
healthy volunteers | not specified | not specified | vs iv
31463821
starling
starling_oba
76923e17e9741439c95512ed88e5e9a5da967ef8e88d606c2cfdb1f9b75bdc13
103
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
76923e17e9741439c95512ed88e5e9a5da967ef8e88d606c2cfdb1f9b75bdc13
c6eb7284cc4d2600c83692e21aaed2771f2ed2393da4ec923d3701f775ee77bf
Sublingual administration showed an absolute bioavailability of 71%.
In study 1, which involved healthy volunteers, samidorphan was well-absorbed following oral administration and reached peak concentrations within 2 hours, with an absolute bioavailability of 69%.
C/C=C1\NC(=O)[C@H]2CSSCC/C=C/[C@H](CC(=O)N[C@H](C(C)C)C(=O)N2)OC(=O)[C@H](C(C)C)NC1=O
16
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
16
percent
false
Romidepsin
absolute
rats
50 mg/kg
p.o.
null
10 mg/kg iv
rodent
rats | p.o. | not specified | 10 mg/kg iv
28541045
starling
starling_oba
613854779ad0c3050f8d9be6daf62f6fe79bb495f775c4f4c155e3f9974175e8
104
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
613854779ad0c3050f8d9be6daf62f6fe79bb495f775c4f4c155e3f9974175e8
10c191584869f36e716d241fa2fc259a333ce5909d512002e6a32a1588dfd5b9
AUC = 19712 ± 9168 ng/mL·min
Romidepsin was significantly absorbed after oral administration to rats; at a dose of 50 mg/kg p.o., the absolute bioavailability (F) was 16 ± 7% with an AUC of 19712 ± 9168 ng/mL·min, compared to a 10 mg/kg iv dose.
CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
1.5
starling.oral_bioavailability.systemic_availability.percent
oral_bioavailability
systemic_availability
percent
rat
1.5
percent
false
3D53
systemic availability
rat
null
oral
null
null
rodent
rat | oral | not specified | not specified
28541045
starling
starling_oba
07d432862860b7d6fc90f8b33e994c9c7409c588e0b40e57e302c257fe907dba
105
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
07d432862860b7d6fc90f8b33e994c9c7409c588e0b40e57e302c257fe907dba
f1b93ee4eb6e88b30ea0d05e8446dfaac10b174639424bc465bfd4f5d91e5df1
The authors note that oral activity is observed despite this low bioavailability due to long receptor residence time.
Compound 3D53 (16) is described as having low oral bioavailability and low systemic availability (F = 1–2%) in rats.
O=C(c1ccc(NS(=O)(=O)c2cccc3cccnc23)cc1)N1CCN(CC2CC2)CC1
72.7
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
human
72.7
percent
false
Mitapivat
absolute
humans
null
oral
null
vs iv
human
humans | oral | not specified | vs iv
37596712
starling
starling_oba
fc4b95632c7bc3758c7eabcff4ddeff783dcb2dc35bbaba16a55f7723a381a40
106
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
fc4b95632c7bc3758c7eabcff4ddeff783dcb2dc35bbaba16a55f7723a381a40
3329432b97e80014a85c50702ea4c7ae471e2bf625aad8091ee1d2273e14bd72
8.80% CV
The absolute oral bioavailability of mitapivat in humans was high, reported as 72.7% (8.80% CV).
O=C(c1ccc(NS(=O)(=O)c2cccc3cccnc23)cc1)N1CCN(CC2CC2)CC1
65.3
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
human
65.3
percent
false
Mitapivat
absolute
humans
null
oral
null
vs iv
human
humans | oral | not specified | vs iv
37596712
starling
starling_oba
10f2441db29ce3960158eefa859e36e016e748c8b706efe7760ed0241b9802d6
107
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
10f2441db29ce3960158eefa859e36e016e748c8b706efe7760ed0241b9802d6
8df6e928875d23ebf4734c1219d7df83c3e1d8ba77c1fa251f1ff9c43f75cb75
Range for individual subjects based on AUC0–∞ or AUC0–last
For individual human subjects, the absolute bioavailability of mitapivat based on AUC0–∞ or AUC0–last ranged from 65.3% to 86.3%.
CN1CCc2nc(C(=O)N[C@@H]3C[C@@H](C(=O)N(C)C)CC[C@@H]3NC(=O)C(=O)Nc3ccc(Cl)cn3)sc2C1
62
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
62
percent
false
edoxaban
absolute
null
null
po
null
iv
null
null
27121940
starling
starling_oba
443cf1ffb3aea5b4d911e0c7fe6b3fd256ce3ceaf719c6972f3a7aea8129ceac
108
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
443cf1ffb3aea5b4d911e0c7fe6b3fd256ce3ceaf719c6972f3a7aea8129ceac
252adda099815605346b7bc59084233f91ed91fa4eba44a521599dd7efa4e9de
The drug was described as rapidly absorbed.
In conclusion, edoxaban is rapidly absorbed, and absolute bioavailability was almost 62% of the PO dose.
C[S+](CC[C@H](N)C(=O)O)C[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O
68.6
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
human
68.6
percent
false
SAM
absolute
humans
2 mg
oral
null
sublingual route
human
humans | oral | not specified | sublingual route
31463821
starling
starling_oba
73d4d61b64e78c106e02b2b25da89a767b6bcdfa4279c6bfbeb04199e5e98861
109
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
73d4d61b64e78c106e02b2b25da89a767b6bcdfa4279c6bfbeb04199e5e98861
60a640d8c91b4007656d1c11874abde6bad3e547767f2dd5926d8c26fe8c880e
n = 9
Following the administration of 2 mg SAM, the average absolute bioavailability for the oral route of administration was mean 68.6% (range 60.3–82.6%; n = 9), which was similar to the absolute bioavailability observed for the sublingual route (mean 71.2%; range 62.9–80.3%; n = 10).
COc1ccc(-c2cc3nccn3c(Nc3ncccc3C(N)=O)n2)cc1OC
54.6
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
human
54.6
percent
false
R406
absolute
humans
150 mg
tablet
null
14c-r406 (intravenous) 100 μg in solution
human
humans | tablet | not specified | 14c-r406 (intravenous) 100 µg in solution
27858108
starling
starling_oba
f79cff52c8d99cf652143b8e040937cd90c9b5e036e446db057bfc3fc5ca858c
110
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
f79cff52c8d99cf652143b8e040937cd90c9b5e036e446db057bfc3fc5ca858c
9905ae2fd8d06bd7dfd306850c020840e3f24d776f721473fceb2ef55b7b917a
Median value reported. Sample size: n=10 for oral and n=9 for intravenous.
In study 27, the oral bioavailability (F) of R406 following administration of a 150 mg tablet was 54.6 (42.4)%, with 14C-R406 (intravenous) 100 µg in solution used as the comparator.
CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21
66.1
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
66.1
percent
false
Sertraline
absolute
healthy subjects
null
null
null
vs iv
human
healthy subjects | not specified | not specified | vs iv
32430638
starling
starling_oba
57a8f025e9829b0b43b19fde0ad6656cdf2d69868cd056d3ab554dc3e2062537
111
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
57a8f025e9829b0b43b19fde0ad6656cdf2d69868cd056d3ab554dc3e2062537
bbd52a80b8fd893a2dcc860abcc21d8d807c407b40465e994bef65ea4d9be489
Fmax represents the maximum bioavailability within a nonlinear bioavailability-dose relationship estimated from clinical PK data.
In Table III, the maximum bioavailability (Fmax) for sertraline is reported with an estimate of 0.639 (8% RSE) and a SIR median of 0.661 (95% CI: 0.559–0.804).
Cc1ccc([C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)cc1Cc1ccc(-c2ccc(F)cc2)s1
65
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
65
percent
false
Canagliflozin
absolute
healthy participants
300 mg
tablet
fasted conditions
vs iv
human
healthy participants | tablet | fasted conditions | vs iv
27136910
starling
starling_oba
12ee1b2d7a4f65f71cd5802382d6e9b61b6c66adbd78f4b95c7f86b4823981ed
112
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
12ee1b2d7a4f65f71cd5802382d6e9b61b6c66adbd78f4b95c7f86b4823981ed
25342a364d76abb6b3ed1662613a5e395e0016c43403921003dd6e3f526ef2a9
Calculated as a geometric mean ratio of 65% for both AUC∞ and AUClast compared to dose-normalized intravenous [¹⁴C]-canagliflozin.
In healthy participants, the observed mean absolute oral bioavailability of canagliflozin was approximately 65% following a single-dose administration of a 300 mg tablet under fasted conditions.
O=C(NC[C@H]1CN(c2ccc(N3CCOCC3=O)cc2)C(=O)O1)c1ccc(Cl)s1
61.5
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
61.5
percent
false
5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide
absolute
rats
1-10 mg kg-1
oral dosing
null
null
rodent
rats | oral dosing | not specified | not specified
16308283
starling
starling_oba
5ed272e5404d3e9b5252730a74562ecd3c861111a8a67b0bae1d2ca4d8b606b5
113
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
5ed272e5404d3e9b5252730a74562ecd3c861111a8a67b0bae1d2ca4d8b606b5
0bcdda23e9811ea2f25f8cd4955939f8c97cf071212241831e6c2132682323e1
null
BAY 59-7939 was rapidly absorbed after oral dosing, with an absolute bioavailability of 57–66% in rats. Plasma pharmacokinetics of BAY 59-7939 were linear across the investigated dose range of 1–10 mg kg⁻¹ in rats.
O=C(NC[C@H]1CN(c2ccc(N3CCOCC3=O)cc2)C(=O)O1)c1ccc(Cl)s1
73
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
dog
73
percent
false
5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide
absolute
dogs
0.3-3 mg kg-1
oral dosing
null
null
dog
dogs | oral dosing | not specified | not specified
16308283
starling
starling_oba
72195098895ae7d9f656a3781033c4d2c3caee4eca88f453254cdbc5b3e176b0
114
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
72195098895ae7d9f656a3781033c4d2c3caee4eca88f453254cdbc5b3e176b0
c0b34627cfeae279e97c34af67025968f77286ad2b6907ad269f8b9c14527d23
null
BAY 59-7939 was rapidly absorbed after oral dosing, with an absolute bioavailability of 60–86% in dogs. Plasma pharmacokinetics of BAY 59-7939 were linear across the investigated dose range of 0.3–3 mg kg⁻¹ in dogs.
COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C
5.2
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
5.2
percent
false
Atorvastatin
absolute
rats
10 mg/kg
single oral dose
null
vs iv
rodent
rats | single oral dose | not specified | vs iv
16624870
starling
starling_oba
56eae95f3342a7bbb0e082b7a2194aa832deb793281ad5eb42418091d668a123
115
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
56eae95f3342a7bbb0e082b7a2194aa832deb793281ad5eb42418091d668a123
7140e34fe87c03827a0cd956f1ca17978e6b79a06ff89ca5c8f6ff47dec7f80f
Sample size n = 5; also described in text as 5.2%.
In rats (n = 5) receiving a single oral dose of 10 mg/kg atorvastatin (ATV) alone, the oral bioavailability (F) was 0.052 ± 0.020.
COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C
14
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
14
percent
false
Atorvastatin
absolute
rats
10 mg/kg
single oral dose
coadministered with bolus intravenous rifampicin (20 mg/kg)
vs iv
rodent
rats | single oral dose | coadministered with bolus intravenous rifampicin (20 mg/kg) | vs iv
16624870
starling
starling_oba
51420ca8b022df20e31dc9a6d428606dd965faf47dfebe6c05d4efe037140545
116
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
51420ca8b022df20e31dc9a6d428606dd965faf47dfebe6c05d4efe037140545
59ad69c5944e39e6e9ff3adaacf9c04e9044966befc662d5aa5cea921cf77050
Sample size n = 5; also described in text as 14%.
In rats (n = 5) receiving a single oral dose of 10 mg/kg atorvastatin (ATV) with a bolus intravenous dose of 20 mg/kg rifampicin (RIF), the oral bioavailability (F) was 0.14 ± 0.03.
CCCCCCCCCCCCCCCCCC(=O)O.CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@](C)(O)C[C@@H](C)C(=O)[C@H](C)[C@@H](O)[C@]1(C)O
30
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
30
percent
false
erythromycin stearate
absolute
healthy volunteers
250 mg
film-coated tablets
1 h before meals
vs i.v. injections
human
healthy volunteers | film-coated tablets | 1 h before meals | vs i.v. injections
7306427
starling
starling_oba
9d4fdba01392558cd1c55a68352681aedf7b7c18551cdf9a74047b2ca4945a05
117
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
9d4fdba01392558cd1c55a68352681aedf7b7c18551cdf9a74047b2ca4945a05
b87ba8a1f9f0414893f070dfce6d0a03e4a45f4d656117964f2d0585cbe2754c
Dose 1; 24 healthy volunteers
In a study of 24 healthy volunteers, the absolute bioavailability of erythromycin stearate tablets (Regimen A), administered 1 hour before meals at a dose of 250 mg, was approximately 30% for Dose 1.
CCCCCCCCCCCCCCCCCC(=O)O.CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@](C)(O)C[C@@H](C)C(=O)[C@H](C)[C@@H](O)[C@]1(C)O
65
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
65
percent
false
erythromycin stearate
absolute
healthy volunteers
250 mg
film-coated tablets
1 h before meals
vs i.v. injections
human
healthy volunteers | film-coated tablets | 1 h before meals | vs i.v. injections
7306427
starling
starling_oba
f430e3b0f7637c827c18a55394f56cf13c2df4fbdaa391361ea7d37567e0c5e6
118
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
f430e3b0f7637c827c18a55394f56cf13c2df4fbdaa391361ea7d37567e0c5e6
875eca97ae00259cda9d8a4fc1c9d85ab71bfc614567afb07606d1c0eeb9b90b
Dose 9 (steady-state); 24 healthy volunteers
In a study of 24 healthy volunteers, the absolute bioavailability of erythromycin stearate tablets (Regimen A), administered 1 hour before meals at a dose of 250 mg, was 65% for Dose 9.
CCCCCCCCCCCCCCCCCC(=O)O.CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@](C)(O)C[C@@H](C)C(=O)[C@H](C)[C@@H](O)[C@]1(C)O
40
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
40
percent
false
erythromycin base
absolute
healthy volunteers
250 mg
enteric-coated capsules
30 min after start of meals
vs i.v. injections
human
healthy volunteers | enteric-coated capsules | 30 min after start of meals | vs i.v. injections
7306427
starling
starling_oba
8d3c6a2d085a8273adaf13446b40d3e91f74e69f77d4819b4958b106f39e5c86
119
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
8d3c6a2d085a8273adaf13446b40d3e91f74e69f77d4819b4958b106f39e5c86
5825010cb02fcaeb3ccf1921cd1dc41940b88d794f2a148ac25e7a37a9fac5f8
Reported for both Dose 1 and Dose 9; 24 healthy volunteers
For Regimen B, consisting of erythromycin base capsules administered 30 minutes after the start of meals at a dose of 250 mg, the absolute bioavailability was 40% for both Dose 1 and Dose 9 in 24 healthy volunteers.
CN(C)CCO[C@]1(c2ccccc2)C[C@H]2CC[C@]1(C)C2(C)C
56
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
56
percent
false
deramciclane
absolute
null
1 mg kg-1
oral
deramciclane fumarate
vs iv
null
null
9840215
starling
starling_oba
fd92e80256adf78afef91a6da0af495dce269356ae37a201c02e2ee799ba5505
122
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
fd92e80256adf78afef91a6da0af495dce269356ae37a201c02e2ee799ba5505
5855ce709b5779346100a61172b9c4f503437e5dc530eb84479884926862c2b4
null
The absolute bioavailabilities of deramciclane were 56 (10)% for a 1 mg kg⁻¹ dose.
CN(C)CCO[C@]1(c2ccccc2)C[C@H]2CC[C@]1(C)C2(C)C
45
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
45
percent
false
deramciclane
absolute
null
3 mg kg-1
oral
deramciclane fumarate
vs iv
null
null
9840215
starling
starling_oba
5c5a99dcbbb3ad37a6eebf7e679beccfb3e1725dfd16b733d2ab2eb112425143
123
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
5c5a99dcbbb3ad37a6eebf7e679beccfb3e1725dfd16b733d2ab2eb112425143
2cf3564109ae919f976f81186edd5b9848d542c4de758c890038c5639aa93de4
null
The absolute bioavailabilities of deramciclane were 45 (5.9)% for a 3 mg kg⁻¹ dose.
CN(C)CCO[C@]1(c2ccccc2)C[C@H]2CC[C@]1(C)C2(C)C
61
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
61
percent
false
deramciclane
absolute
null
6 mg kg-1
oral
deramciclane fumarate
vs iv
null
null
9840215
starling
starling_oba
27ee03713de102a991e21e62a13cb03e5c6032909e383cf61b3ef280a76eef74
124
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
27ee03713de102a991e21e62a13cb03e5c6032909e383cf61b3ef280a76eef74
fb0a4f865dc9b229ef91d31b51928a403727d0b7f3968b2d2f08589f692204c1
null
The absolute bioavailabilities of deramciclane were 61 (14)% for a 6 mg kg⁻¹ dose.
Cc1ccc(-c2ncc(Cl)cc2-c2ccc(S(C)(=O)=O)cc2)cn1
100
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
100
percent
false
Etoricoxib
absolute
healthy subjects
120 mg
tablet
null
null
human
healthy subjects | tablet | not specified | not specified
12638395
starling
starling_oba
aeb4c3c7211ddc04d987bacbb9afdd4110cae8885e0641c80a9aade9b1e69c52
125
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
aeb4c3c7211ddc04d987bacbb9afdd4110cae8885e0641c80a9aade9b1e69c52
0523bf6d41a22e86130df6559843184adf2acf06b321800b011bc49c140789f7
Reported for the highest dose-strength tablet; authors infer that lower dose-strength tablets (60, 90 mg) are also completely absorbed.
Etoricoxib was found to be essentially completely absorbed and available following administration of the highest dose-strength tablet (120 mg), with an estimated absolute bioavailability of approximately 100% in healthy subjects.
Cc1ccc(-c2ncc(Cl)cc2-c2ccc(S(C)(=O)=O)cc2)cn1
100
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
null
100
percent
false
Etoricoxib
absolute
healthy subjects
120 mg
tablet
high-fat meal
null
human
healthy subjects | tablet | high-fat meal | not specified
12638395
starling
starling_oba
7442ff3254b3ec66e6a8d9f0afedd5b3efb89e2b68a55ea75387117ff9f064ec
126
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
7442ff3254b3ec66e6a8d9f0afedd5b3efb89e2b68a55ea75387117ff9f064ec
22ff0ba43a564641831513e59f556b85e06ca2d38236951a9b794b3b77308f89
High-fat meal decreased the rate of absorption (Cmax 36% lower and delayed) but did not affect the extent of absorption (AUC infinity).
Administration of the 120-mg tablet of etoricoxib following a high-fat meal had no effect on the extent of absorption, consistent with the compound's 100% bioavailability.
CC12CCCC(O)(C1)C1CC(C)(C)C1CC2
1.17
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
1.17
percent
false
$\beta$-caryophyllene alcohol
absolute
rats
null
solution
null
vs iv
rodent
rats | solution | not specified | vs iv
28891397
starling
starling_oba
05220e6912b94bfb7c2bc85e907a97d5bc20d2d5c0a35dce5c5479bac2e3720c
129
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
05220e6912b94bfb7c2bc85e907a97d5bc20d2d5c0a35dce5c5479bac2e3720c
90cdb0b6259f7a0e66e54509b65b4bfb1dd0c1383a3b173d0a64f8b88ac6db61
described as low
In rats, the measured oral bioavailability of $\beta$-caryophyllene alcohol (BCPA) was low for the solution formulation, reported as 1.17 ± 0.78%.
CC12CCCC(O)(C1)C1CC(C)(C)C1CC2
1.21
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
1.21
percent
false
$\beta$-caryophyllene alcohol
absolute
rats
null
suspension
null
vs iv
rodent
rats | suspension | not specified | vs iv
28891397
starling
starling_oba
391e57ff610898c94dc2dbebad54c59a54aaf19db50df824e082ac5c9cf87314
130
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
391e57ff610898c94dc2dbebad54c59a54aaf19db50df824e082ac5c9cf87314
35030ecbbfd71943907d6a0371a4f9897e53a1bd4f2abcd260ba91cd31cae995
described as low
In rats, the measured oral bioavailability of $\beta$-caryophyllene alcohol (BCPA) was low for the suspension formulation, reported as 1.21 ± 0.33%.
CC12CCCC(O)(C1)C1CC(C)(C)C1CC2
6.22
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
rat
6.22
percent
false
$\beta$-caryophyllene alcohol
absolute
rats
null
peg formulation
null
vs iv
rodent
rats | peg formulation | not specified | vs iv
28891397
starling
starling_oba
c74d90c7e7f7a7c6f326b9321b6a11b2bed7d51b42fc8c8bfc3b280c9efaa0dc
131
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
c74d90c7e7f7a7c6f326b9321b6a11b2bed7d51b42fc8c8bfc3b280c9efaa0dc
322da4c82f29e9794c5df71a9162a183f7b9d1d2485460ee8960c48e05cdf00f
described as low
In rats, the measured oral bioavailability of $\beta$-caryophyllene alcohol (BCPA) was low for the PEG formulation, reported as 6.22 ± 2.63%.
CC12CCCC(O)(C1)C1CC(C)(C)C1CC2
0.12
oral_bioavailability.absolute.percent
oral_bioavailability
absolute
percent
dog
0.12
percent
false
$\beta$-caryophyllene alcohol
absolute
dogs
null
solution
null
vs iv
dog
dogs | solution | not specified | vs iv
28891397
starling
starling_oba
98064657b1c53d616ed24f8b2ff60ec735afa561bf58665e96ab991f17f76089
132
2068cd431e76155d0c7f61a9eb45a2ba64eaa8d77c7a19c966a70a294079dceb
98064657b1c53d616ed24f8b2ff60ec735afa561bf58665e96ab991f17f76089
51c51301ab7fbc37cb1a41c19bd203911b9e8c9bac29ba2923123757e1b1f76a
reported as lower than in rats
The bioavailability of $\beta$-caryophyllene alcohol was lower in dogs for the solution formulation, reported as 0.12 ± 0.05%.
End of preview. Expand in Data Studio

Starling Oba Cleaned

This dataset contains 27,640 accepted finite scalar measurement children from the versioned canonical-base pipeline. A parent row with several unambiguous measurements can produce several child rows. Rejected, malformed, ambiguous, bounded, range-only, TDC-overlapping, and endpoint-unassignable records are not published here.

Cleaning

The following source columns are replaced in place with validated canonical or lexical normalizations:

  • smilescanonical_smiles
  • bioavailability_report_typebioavailability_report_type_normalized
  • species_or_populationspecies_or_population_mechanical_normalized
  • dosedose_normalized
  • oral_exposure_modeoral_exposure_mode_normalized
  • qualifying_conditionsqualifying_conditions_normalized
  • comparatorcomparator_normalized
  • oral_bioavailability_valuescalar_value

The public column names on the left are retained; the names on the right identify the validated internal values used to replace them. Columns omitted from this dataset:

  • direction: all_null_in_dataset
  • target: all_null_in_dataset
  • kinetic_parameter: all_null_in_dataset
  • auc_window: all_null_in_dataset
  • defining_timepoint: all_null_in_dataset
  • variation_value: all_null_in_dataset
  • variation_type: all_null_in_dataset
  • accompanying_interval_lower: all_null_in_dataset
  • accompanying_interval_upper: all_null_in_dataset

canonical_endpoint_key is the endpoint identity field. No condition_key is added. species_exact is populated only for explicit, unambiguous species references. Narrative and other source fields without a validated normalization remain source text.

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