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
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)
Molecular Formula | C29H34Cl2N6O3S2 |
Molecular Weight | 649.655 |
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
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P40238 Gene ID: 4352.0 Gene Symbol: MPL Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/19183407 |
3.3 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | DOPTELET Approved UseTreatment of thrombocytopenia in adult patients with chronic liver disease who are scheduled to undergo a procedure. Launch Date2018 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
284 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30203841 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
10000 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30203841 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
18.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30203841 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28339166/ |
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
Dose | Population | Adverse events |
---|---|---|
100 mg single, oral |
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%) Sources: Flatulence (16.7%) Dizziness (16.7%) Headache (16.7%) Diarrhoea (16.7%) |
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: |
Other AEs: Pyrexia, Abdominal pain... Other AEs: Pyrexia (8%) Sources: Abdominal pain (7%) Nausea (7%) Headache (7%) Fatigue (3%) Edema peripheral (4%) Hyponatremia (serious, 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: |
Disc. AE: Anemia, Pyrexia... Other AEs: Pyrexia, Abdominal pain... AEs leading to discontinuation/dose reduction: Anemia (0.4%) Other AEs:Pyrexia (0.4%) Myalgia (0.4%) Pyrexia (11%) Sources: Abdominal pain (6%) Nausea (6%) Headache (4%) Fatigue (4%) Edema peripheral (3%) 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 = 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%) Sources: 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%) |
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%) Sources: 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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Diarrhoea | 16.7% | 100 mg single, oral |
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 |
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 |
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 |
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 |
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: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
weak | ||||
weak | ||||
yes | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | ||||
major | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/ppa/avatrombopag.html
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
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:35:11 GMT 2023
by
admin
on
Fri Dec 15 16:35:11 GMT 2023
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Record UNII |
3H8GSZ4SQL
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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WHO-ATC |
B02BX08
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NCI_THESAURUS |
C78275
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m12070
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SUB121659
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DTXSID30205667
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Avatrombopag
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2045726
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3H8GSZ4SQL
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CHEMBL2103883
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YY-98
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100000144842
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DB11995
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Related Record | Type | Details | ||
---|---|---|---|---|
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TRANSPORTER -> INHIBITOR |
IC50
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EXCRETED UNCHANGED |
FECAL
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METABOLIC ENZYME -> INDUCER |
WEAK
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METABOLIC ENZYME -> SUBSTRATE |
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TARGET -> AGONIST |
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METABOLIC ENZYME -> INDUCER |
In vitro data suggests that avatrombopag weakly induces CYP2C8 and CYP2C9
WEAK
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TRANSPORTER -> SUBSTRATE |
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METABOLIC ENZYME -> SUBSTRATE |
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BINDER->LIGAND |
BINDING
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TRANSPORTER -> INHIBITOR |
IC50
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SALT/SOLVATE -> PARENT |
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Related Record | Type | Details | ||
---|---|---|---|---|
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METABOLITE -> PARENT |
Avatrombopag's metabolites were detected in feces. There were no metabolites detected in plasma.
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METABOLITE -> PARENT |
Avatrombopag's metabolites were detected in feces. There were no metabolites detected in plasma.
MAJOR
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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Blood-to-Plasma Ratio | PHARMACOKINETIC |
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