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Details

Stereochemistry ACHIRAL
Molecular Formula C29H34Cl2N6O3S2
Molecular Weight 649.655
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AVATROMBOPAG

SMILES

OC(=O)C1CCN(CC1)C2=NC=C(C=C2Cl)C(=O)NC3=NC(C4=CC(Cl)=CS4)=C(S3)N5CCN(CC5)C6CCCCC6

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
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: 4352.0
Gene Symbol: MPL
Target Organism: Homo sapiens (Human)
3.3 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

2018
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
n = 6
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Population Size: 6
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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
n = 6
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Population Size: 6
Sources:
Dizziness 16.7%
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 25.5 years
n = 6
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Population Size: 6
Sources:
Dysgeusia 16.7%
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 25.5 years
n = 6
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Population Size: 6
Sources:
Flatulence 16.7%
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 25.5 years
n = 6
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Population Size: 6
Sources:
Headache 16.7%
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 25.5 years
n = 6
Health Status: healthy
Age Group: 25.5 years
Sex: M+F
Population Size: 6
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 115
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 115
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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)
n = 159
Health Status: unhealthy
Condition: thrombocytopenia
Age Group: 58 years (range: 19-86 years)
Sex: M+F
Population Size: 159
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

Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
AKR-501 (YM477) in combination with thrombopoietin enhances human megakaryocytopoiesis.
2008 Oct
AKR-501 (YM477) a novel orally-active thrombopoietin receptor agonist.
2009 Apr
Romiplostim: a second-generation thrombopoietin agonist.
2009 Mar
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.
Name Type Language
AVATROMBOPAG
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
YM-301477
Code English
avatrombopag [INN]
Common Name English
AKR-501
Common Name English
YM-477
Code English
AVATROMBOPAG [USAN]
Common Name English
Avatrombopag [WHO-DD]
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 Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
NCI_THESAURUS C78275
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
Code System Code Type Description
MERCK INDEX
m12070
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
DRUG CENTRAL
5285
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
PUBCHEM
9852519
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
INN
9571
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
CAS
570406-98-3
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
EVMPD
SUB121659
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
NCI_THESAURUS
C150559
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
DAILYMED
3H8GSZ4SQL
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
EPA CompTox
DTXSID30205667
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
WIKIPEDIA
Avatrombopag
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
RXCUI
2045726
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
FDA UNII
3H8GSZ4SQL
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
ChEMBL
CHEMBL2103883
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
USAN
YY-98
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
SMS_ID
100000144842
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY
DRUG BANK
DB11995
Created by admin on Fri Dec 15 16:35:11 GMT 2023 , Edited by admin on Fri Dec 15 16:35:11 GMT 2023
PRIMARY