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Details

Stereochemistry ACHIRAL
Molecular Formula C29H34Cl2N6O3S2
Molecular Weight 649.6578
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AVATROMBOPAG

SMILES

C1CCC(CC1)N2CCN(CC2)c3c(-c4cc(cs4)Cl)nc(N=C(c5cc(c(nc5)N6CCC(CC6)C(=O)O)Cl)O)s3

InChI

InChIKey=OFZJKCQENFPZBH-UHFFFAOYSA-N
InChI=1S/C29H34Cl2N6O3S2/c30-20-15-23(41-17-20)24-27(37-12-10-35(11-13-37)21-4-2-1-3-5-21)42-29(33-24)34-26(38)19-14-22(31)25(32-16-19)36-8-6-18(7-9-36)28(39)40/h14-18,21H,1-13H2,(H,39,40)(H,33,34,38)

HIDE SMILES / InChI

Molecular Formula C29H34Cl2N6O3S2
Molecular Weight 649.6578
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Avatrombopag is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist that stimulates proliferation and differentiation of megakaryocytes from bone marrow progenitor cells resulting in increased production of platelets. Avatrombopag does not compete with TPO for binding to the TPO receptor and has an additive effect with TPO on platelet production. Avatrombopag was discovered by Yamanouchi Pharmaceutical, developed by AkaRx which late became acquired by Dova Pharmaceuticals. In 2018 avatrombopag was approved by the FDA for thrombocytopenia in adults with chronic liver disease scheduled to undergo a procedure.

Originator

Curator's Comment:: In April 2005, Astellas Pharmaceuticals was formed from the merger of Yamanouchi Pharmaceutical and Fujisawa Healthcare. In November 2005, AkaRx was formed as a spin out of Yamanouchi Pharma America (YPA), now part of Astellas Pharmaceuticals. Worldwide rights for AKR-501 have been licensed to AkaRx. In 2010 AkaRx became a wholly owned subsidiary of Eisai Inc, and in 2016 rights to the drug were acquired by Dova Pharmaceuticals.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P40238
Gene ID: 4352
Gene Symbol: MPL
Target Organism: Homo sapiens (Human)
3.29999999999999982 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
DOPTELET

Approved Use

Treatment of thrombocytopenia in adult patients with chronic liver disease who are scheduled to undergo a procedure.

Launch Date

1526774400000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
284 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
388 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
95.4 ng/mL
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
117 ng/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
183 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
164 ng/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
10000 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
10863.5 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3160 ng × h/mL
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
3340 ng × h/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
4840 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5900 ng × h/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
18.2 h
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
18 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
18.6 h
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
18 h
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AVATROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
Doses

Doses

DosePopulationAdverse events​
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 25.5 years
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Sources:
Other AEs: Dysgeusia, Flatulence...
Other AEs:
Dysgeusia (16.7%)
Flatulence (16.7%)
Dizziness (16.7%)
Headache (16.7%)
Diarrhoea (16.7%)
Sources:
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Other AEs: Pyrexia, Abdominal pain...
Other AEs:
Pyrexia (8%)
Abdominal pain (7%)
Nausea (7%)
Headache (7%)
Fatigue (3%)
Edema peripheral (4%)
Hyponatremia (serious, 8%)
Sources:
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Disc. AE: Anemia, Pyrexia...
Other AEs: Pyrexia, Abdominal pain...
AEs leading to
discontinuation/dose reduction:
Anemia (0.4%)
Pyrexia (0.4%)
Myalgia (0.4%)
Other AEs:
Pyrexia (11%)
Abdominal pain (6%)
Nausea (6%)
Headache (4%)
Fatigue (4%)
Edema peripheral (3%)
Hyponatremia (serious, 7%)
Sources:
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Other AEs: Gastrointestinal disorders, General disorders and administration site conditions...
Other AEs:
Gastrointestinal disorders (25.2%)
General disorders and administration site conditions (14.8%)
Nervous system disorders (7.8%)
Injury, poisoning and procedural complications (2.6%)
Infection (9.6%)
Infestation (9.6%)
Respiratory disorder (8.7%)
Thoracic disorders (excl lung and pleura) (8.7%)
Mediastinal disorders (8.7%)
Musculoskeletal disorder (5.2%)
Connective tissue disorders (5.2%)
Metabolism disorders NEC (5.2%)
General nutrition disorder (5.2%)
Skin disorder (1.7%)
Skin and subcutaneous tissue disorders (1.7%)
Blood disorder (3.5%)
Lymphatic system disorders NEC (3.5%)
Psychiatric disorders (4.3%)
Urinary tract disorder NOS (3.5%)
Renal disorder (3.5%)
Vascular disorders (0.9%)
Hepatobiliary disorders (1.7%)
Eye disorders (0.9%)
Cardiac disorders (0.9%)
Disorder ear (0.9%)
Labyrinthine disorders (0.9%)
Endocrine disorders (0.9%)
Sources:
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Other AEs: Gastrointestinal disorders, General disorders and administration site conditions...
Other AEs:
Gastrointestinal disorders (29.6%)
General disorders and administration site conditions (23.9%)
Nervous system disorders (8.8%)
Injury, poisoning and procedural complications (10.1%)
Infection (3.1%)
Infestation (3.1%)
Respiratory disorder (4.4%)
Thoracic disorders (excl lung and pleura) (4.4%)
Mediastinal disorders (4.4%)
Musculoskeletal disorder (6.9%)
Connective tissue disorders (6.9%)
Metabolism disorders NEC (3.8%)
General nutrition disorder (3.8%)
Skin disorder (5%)
Skin and subcutaneous tissue disorders (5%)
Blood disorder (3.8%)
Lymphatic system disorders NEC (3.8%)
Psychiatric disorders (3.1%)
Urinary tract disorder NOS (1.3%)
Renal disorder (1.3%)
Vascular disorders (2.5%)
Hepatobiliary disorders (1.9%)
Eye disorders (2.5%)
Cardiac disorders (0.6%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Diarrhoea 16.7%
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 25.5 years
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Sources:
Dizziness 16.7%
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 25.5 years
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Sources:
Dysgeusia 16.7%
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 25.5 years
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Sources:
Flatulence 16.7%
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 25.5 years
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Sources:
Headache 16.7%
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 25.5 years
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Sources:
Fatigue 3%
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Edema peripheral 4%
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Abdominal pain 7%
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Headache 7%
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Nausea 7%
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Pyrexia 8%
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Hyponatremia serious, 8%
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Anemia 0.4%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Myalgia 0.4%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Pyrexia 0.4%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Pyrexia 11%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Edema peripheral 3%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Fatigue 4%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Headache 4%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Abdominal pain 6%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Nausea 6%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Hyponatremia serious, 7%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Cardiac disorders 0.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Disorder ear 0.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Endocrine disorders 0.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Eye disorders 0.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Labyrinthine disorders 0.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Vascular disorders 0.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Hepatobiliary disorders 1.7%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Skin and subcutaneous tissue disorders 1.7%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Skin disorder 1.7%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
General disorders and administration site conditions 14.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Injury, poisoning and procedural complications 2.6%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Gastrointestinal disorders 25.2%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Blood disorder 3.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Lymphatic system disorders NEC 3.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Renal disorder 3.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Urinary tract disorder NOS 3.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Psychiatric disorders 4.3%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Connective tissue disorders 5.2%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
General nutrition disorder 5.2%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Metabolism disorders NEC 5.2%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Musculoskeletal disorder 5.2%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Nervous system disorders 7.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Mediastinal disorders 8.7%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Respiratory disorder 8.7%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Thoracic disorders (excl lung and pleura) 8.7%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Infection 9.6%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Infestation 9.6%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Cardiac disorders 0.6%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Renal disorder 1.3%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Urinary tract disorder NOS 1.3%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Hepatobiliary disorders 1.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Injury, poisoning and procedural complications 10.1%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Eye disorders 2.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Vascular disorders 2.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
General disorders and administration site conditions 23.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Gastrointestinal disorders 29.6%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Infection 3.1%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Infestation 3.1%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Psychiatric disorders 3.1%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Blood disorder 3.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
General nutrition disorder 3.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Lymphatic system disorders NEC 3.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Metabolism disorders NEC 3.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Mediastinal disorders 4.4%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Respiratory disorder 4.4%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Thoracic disorders (excl lung and pleura) 4.4%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Skin and subcutaneous tissue disorders 5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Skin disorder 5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Connective tissue disorders 6.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Musculoskeletal disorder 6.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
Nervous system disorders 8.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 58 years (range: 19-86 years)
Health Status: unhealthy
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
weak
weak
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
major
no
no
no
no
no
no
no
no
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Patents

Patents

Sample Use Guides

For patients with a platelet count 40000 to <50000/mm3: 40 mg once daily for 5 consecutive days, orally. For patients with platelet count below 40,000/mm3: 60 mg once daily for 5 consecutive days.
Route of Administration: Oral
Avatrombopag stimulated the proliferation of cells expressing the human thrombopoietin receptor (c-Mpl) with an EC50 value of 3.3 nM and promoted the differentiation of human hematopoietic progenitor cells (cord blood CD34+ cells) to megakaryocytes with an EC50 value of 25.0 nM.
Substance Class Chemical
Created
by admin
on Sat Jun 26 06:46:10 UTC 2021
Edited
by admin
on Sat Jun 26 06:46:10 UTC 2021
Record UNII
3H8GSZ4SQL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
AVATROMBOPAG
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
YM-301477
Code English
AVATROMBOPAG [INN]
Common Name English
AVATROMBOPAG [WHO-DD]
Common Name English
AKR-501
Common Name English
YM-477
Code English
AVATROMBOPAG [USAN]
Common Name English
E5501
Code English
E-5501
Code English
AVATROMBOPAG [MI]
Common Name English
1-(3-CHLORO-5-((4-(4-CHLOROTHIOPHEN-2-YL)-5-(4-CYCLOHEXYLPIPERAZIN-1-YL)THIAZOL-2-YL)CARBAMOYL)PYRIDIN-2-YL)PIPERIDINE-4-CARBOXYLIC ACID
Systematic Name English
1-(3-CHLORO-5-((4-(4-CHLOROTHIOPHEN-2-YL)-5-(4-CYCLOHEXYLPIPERAZIN-1-YL)THIAZOL-2-YL)CARBAMOYL)-2-PYRIDYL)PIPERIDINE-4-CARBOXYLIC ACID
Systematic Name English
Classification Tree Code System Code
WHO-ATC B02BX08
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
NCI_THESAURUS C78275
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
Code System Code Type Description
MERCK INDEX
M12070
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
DRUG CENTRAL
5285
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
PUBCHEM
9852519
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
INN
9571
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
CAS
570406-98-3
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
EVMPD
SUB121659
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
NCI_THESAURUS
C150559
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
EPA CompTox
570406-98-3
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
RXCUI
2045726
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
FDA UNII
3H8GSZ4SQL
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
ChEMBL
CHEMBL2103883
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
DRUG BANK
DB11995
Created by admin on Sat Jun 26 06:46:11 UTC 2021 , Edited by admin on Sat Jun 26 06:46:11 UTC 2021
PRIMARY
Related Record Type Details
TRANSPORTER -> INHIBITOR
IC50
EXCRETED UNCHANGED
FECAL
METABOLIC ENZYME -> INDUCER
WEAK
METABOLIC ENZYME -> SUBSTRATE
TARGET->IMAGING AGENT
METABOLIC ENZYME -> INDUCER
In vitro data suggests that avatrombopag weakly induces CYP2C8 and CYP2C9
WEAK
TRANSPORTER -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
BINDING
TRANSPORTER -> INHIBITOR
IC50
SALT/SOLVATE -> PARENT
Related Record Type Details
METABOLITE -> PARENT
Avatrombopag's metabolites were detected in feces. There were no metabolites detected in plasma.
METABOLITE -> PARENT
Avatrombopag's metabolites were detected in feces. There were no metabolites detected in plasma.
MAJOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC
Blood-to-Plasma Ratio PHARMACOKINETIC