lusutrombopag (Rx)

Brand and Other Names:Mulpleta
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 3mg

Thrombocytopenia

Indicated for thrombocytopenia in adults with chronic liver disease who are scheduled to undergo a procedure

Begin dosing 8-14 days prior to scheduled procedure

Patients should undergo their procedure 2-8 days after the last dose

Recommended dose: 3 mg PO qDay for 7 days

Also see Administration

Dosage Modifications

Renal impairment

  • Mild-to-moderate (CrCl 30-90 mL/min): No clinically meaningful effects on the pharmacokinetics
  • Severe (CrCl <30 mL/min) or hemodialysis: Limited data

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A or B): No clinically meaningful effects on the pharmacokinetics
  • Severe (Child-Pugh C): Mean observed peak plasma concentration and AUC decreased by 20-30% in patients (compared with patients with Child-Pugh A and B); however, ranges for peak plasma concentration and AUC overlapped among patients with Child-Pugh class A, B, and C liver disease

Dosing Considerations

Investigated only as a single 7‐day, once-daily dosing regimen in clinical trials in patients with chronic liver disease

Not to be administered to patients with chronic liver disease in an attempt to normalize platelet counts

Monitoring

  • Obtain a platelet count prior to initiating and not more than 2 days before the procedure

Safety and efficacy not established

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Interactions

Interaction Checker

and lusutrombopag

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Headache (5%)

            Portal vein thrombosis (1%)

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            Warnings

            Contraindications

            None

            Cautions

            Thrombotic or thromboembolic complications

            • Thrombopoietin (TPO) receptor agonists, such as lusutrombopag, have been associated with thrombotic and thromboembolic complications (eg, portal vein thrombosis) in patients with chronic liver disease
            • Consider the potential increased thrombotic risk when administering drug to patients with known risk factors for thromboembolism (eg, genetic prothrombotic conditions [factor V Leiden, prothrombin 20210A, antithrombin deficiency, or protein C or S deficiency])
            • In patients with ongoing or prior thrombosis or absence of hepatopetal blood flow, use lusutrombopag if the potential benefit justifies the potential risk
            • Should not be administered to patients with chronic liver disease in an attempt to normalize platelet counts
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            Pregnancy

            Pregnancy

            There are no available data on use in pregnant women to inform a drug-associated risk

            Animal data

            • In animal reproduction studies, oral administration of lusutrombopag to pregnant rats during organogenesis and the lactation period resulted in adverse developmental outcomes
            • These finding were observed at exposures based on AUC that were substantially higher than the AUC observed in patients (~89 times) at the recommended clinical dose of 3 mg qDay; advise pregnant women of the potential risk to a fetus

            Lactation

            There is no information on the presence of lusutrombopag in human milk, the effects on the breastfed child, and the effects on milk production

            Drug was present in the milk of lactating rats

            Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

            Clinical considerations

            • Lactating women should interrupt breastfeeding and pump and discard breast milk during treatment and for 28 days after the last dose in order to minimize exposure to a breastfed child

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Thrombopoietin (TPO) receptor agonist

            Orally bioavailable, small molecule that interacts with the transmembrane domain of human TPO receptors expressed on megakaryocytes to induce the proliferation and differentiation of megakaryocytic progenitor cells from hematopoietic stem cells and megakaryocyte maturation

            Absorption

            Peak plasma concentration: 111 ng/mL

            Peak plasma time: 6-8 hr

            AUC: 2931 ng·hr/mL

            Food effect

            • AUC and peak plasma concentration were not affected when coadministered with a high‐fat meal (~900 calories [total calories], with 500, 250, and 150 calories from fat, carbohydrate, and protein, respectively)

            Distribution

            Vd: 39.5 L

            Protein binding: >99.9%

            Metabolism

            Metabolized by CYP4 enzymes, including CYP4A11

            Elimination

            Half-life: 27 hr

            Clearance: 1.1 L/hr

            Excretion: Feces (83%, 16% [unchanged]); Urine (~1%)

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            Administration

            Oral Administration

            Administer orally once a day with or without food for 7 days

            Missed dose: Take the missed dose as soon as possible on the same day and return to the normal schedule the following day

            Storage

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

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            Formulary

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.