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Lusutrombopag

Medically reviewed by Drugs.com. Last updated on Sep 13, 2019.

Pronunciation

(loo soo TROM boe pag)

Index Terms

  • S-888711

Dosage Forms

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

Tablet, Oral:

Mulpleta: 3 mg

Brand Names: U.S.

  • Mulpleta

Pharmacologic Category

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

Pharmacology

Lusutrombopag is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist that stimulates proliferation and differentiation of megakaryocytes from bone marrow progenitor cells resulting in an increased platelet production.

Distribution

Vd: 39.5 L

Metabolism

Primarily metabolized by CYP4 enzymes, including CYP4A11

Excretion

Feces: 83% (16% as unchanged drug); Urine: ~1%

Onset of Action

The median time to reach the maximum platelet count was 12 days (range: 5 to 35 days)

Time to Peak

6 to 8 hours

Half-Life Elimination

~27 hours

Protein Binding

>99.9%

Special Populations: Hepatic Function Impairment

The mean observed lusutrombopag Cmax and AUC0-τ decreased by 20% to 30% in patients with severe hepatic impairment (Child-Pugh class C) compared to patients with Child-Pugh class A or B liver disease.

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 lusutrombopag to normalize platelet counts. Begin lusutrombopag 8 to 14 days prior to the scheduled procedure. Patients should undergo procedure 2 to 8 days after the last lusutrombopag dose. Obtain a platelet count prior to therapy administration and not more than 2 days before the procedure.

Chronic liver disease-associated thrombocytopenia: Oral: 3 mg once daily for 7 days

Missed doses: If a dose is missed, administer the dose as soon as possible on the same day. Return to the normal dosing schedule the next day.

Dosing: Geriatric

Refer to adult dosing.

Administration

Oral: Administer with or without 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 in original package.

Drug Interactions

There are no known significant interactions.

Adverse Reactions

1% to 10%: Central nervous system: Headache (5%)

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. Thromboses were not associated with a marked increase in platelet count. Due to the potential for increased thrombotic risks, 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). Lusutrombopag should only be used if the potential benefit justifies the risk in patients with ongoing or prior thrombosis or absence of hepatopetal blood flow. Do not administer to patients with chronic liver disease in an attempt to normalize platelet counts.

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 not more than 2 days before the scheduled procedure; monitor for signs/symptoms of thromboembolism. Monitor adherence.

Pregnancy Considerations

Adverse events were observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience headache. Have patient report immediately to prescriber signs of blood clots (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; fast heartbeat; or coughing up blood) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, 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. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Further information

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

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