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Avatrombopag

Medically reviewed by Drugs.com. Last updated on Mar 4, 2019.

Pronunciation

(a va TROM boe PAG)

Index Terms

  • AKR501
  • Avatrombopag Maleate
  • Doptelet
  • E5501
  • YM477

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Doptelet: 20 mg

Brand Names: U.S.

  • Doptelet

Pharmacologic Category

  • Colony Stimulating Factor
  • Hematopoietic Agent
  • Thrombopoietic Agent
  • Thrombopoietin Receptor Agonist

Pharmacology

Avatrombopag is an orally bioavailable, small molecule TPO receptor agonist that stimulates proliferation and differentiation of megakaryocytes from bone marrow progenitor cells resulting in an increased platelet production. Avatrombopag does not compete with TPO for binding at the TPO receptor and has an additive effect with TPO on platelet production.

Distribution

Vd: ~180 L

Metabolism

Hepatic; primarily by CYP2C9 and CYP3A4

Excretion

Feces (88%; 34% as unchanged drug); urine (6%)

Onset of Action

Platelet count increase: 3 to 5 days after therapy initiation; peak effect observed after 10 to 13 days

Time to Peak

5 to 6 hours; delayed up to 2 hours when administered with a high-fat or low-fat meal

Duration of Action

Platelet count steadily declines within 7 days of procedure (Terrault 2018); platelet count return to baseline: 35 days

Half-Life Elimination

~19 hours

Protein Binding

>96% to human plasma proteins

Use: Labeled Indications

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

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Dosing: Adult

Note: Do not use avatrombopag to normalize platelet counts. Begin avatrombopag 10 to 13 days prior to the scheduled procedure. Patients should undergo procedure 5 to 8 days after the last avatrombopag dose. Obtain a platelet count prior to therapy administration and on the day of the procedure.

Chronic liver disease-associated thrombocytopenia: Oral:

Platelet count 40,000 to <50,000/mm3: 40 mg once daily for 5 consecutive days (Terrault 2018)

Platelet count <40,000/mm3: 60 mg once daily for 5 consecutive days (Terrault 2018)

Missed doses: If a dose is missed, administer the next dose as soon as it is remembered. Do not administer 2 doses at the same time to make up for a missed dose; take the next dose at the usual time the next day. Complete all 5 days of dosing.

Dosing: Geriatric

Refer to adult dosing.

Administration

Oral: Administer with food.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Store tablets in original package.

Drug Interactions

Enzalutamide: May decrease the serum concentration of Avatrombopag. Management: Management of this interaction varies based on avatrombopag indication. Dose adjustments are required for patients using avatrombopag for chronic immune thrombocytopenia. See monograph for details. Consider therapy modification

Fluconazole: May increase the serum concentration of Avatrombopag. Management: Management of this interaction varies based on avatrombopag indication. Dose adjustments are required for patients using avatrombopag for chronic immune thrombocytopenia. See monograph for details. Consider therapy modification

MiFEPRIStone: May increase the serum concentration of Avatrombopag. Management: Management of this interaction varies based on avatrombopag indication. Dose adjustments are required for patients using avatrombopag for chronic immune thrombocytopenia. See monograph for details. Consider therapy modification

RifAMPin: May decrease the serum concentration of Avatrombopag. Management: Management of this interaction varies based on avatrombopag indication. Dose adjustments are required for patients using avatrombopag for chronic immune thrombocytopenia. See monograph for details. Consider therapy modification

Adverse Reactions

Higher incidences reported with longer duration of use.

>10%:

Central nervous system: Headache (7% to 31%), fatigue (3% to 28%)

Gastrointestinal: Gingival hemorrhage (13%)

Hematologic & oncologic: Bruise (26%), petechia (11%)

Neuromuscular & skeletal: Arthralgia (13%)

Respiratory: Epistaxis (19%), upper respiratory tract infection (15%)

Miscellaneous: Fever (11%)

1% to 10%:

Cardiovascular: Arterial thromboembolism (≤7%), venous thromboembolism (≤7%), peripheral edema (3% to 4%)

Gastrointestinal: Abdominal pain (7%), nausea (7%)

Respiratory: Nasopharyngitis (10%)

<1%: Anemia, hyponatremia, myalgia, portal vein thrombosis

Warnings/Precautions

Concerns related to adverse effects:

• Thromboembolism: Thrombotic and thromboembolic complications with thrombopoietin receptor agonist use have occurred in patients with chronic liver disease. Use with caution in patients with known risk factors for thromboembolism (eg, Factor V Leiden, prothrombin 20210A, antithrombin deficiency or protein C or S deficiency). In clinical trials, treatment-emergent portal vein thrombosis was reported (rare). Do not administer to patients with chronic liver disease in an attempt to normalize platelet counts.

Dosage form specific issues:

• Lactose: Dosage form contains lactose monohydrate.

Other warnings/precautions:

• Appropriate use: Do not use to normalize platelet counts in patients with chronic liver disease.

Monitoring Parameters

Platelet count prior to therapy initiation and on the day of the scheduled procedure; monitor for signs/symptoms of thromboembolism. Monitor adherence.

Pregnancy Considerations

Adverse events were observed in animal reproduction studies.

Patient Education

What is this drug used for?

• It is used to raise platelet counts.

Frequently reported side effects of this drug

• Nausea

• Headache

• Loss of strength and energy

• Common cold symptoms

• Joint pain

• Rhinitis

• Pharyngitis

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

• Swelling of arms or legs

• Tachycardia

• Bruising

• Bleeding

• Petechiae

• Abdominal pain

• Blood clots like numbness or weakness on one side of the body; pain, redness, tenderness, warmth, or swelling in the arms or legs; change in color of an arm or leg; chest pain; shortness of breath; tachycardia; or coughing up blood

• Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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