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Lusutrombopag

Class: Hematopoietic Agents
Chemical Name: (E)-3-[2,6-dichloro-4-[[4-[3-[(1S)-1-hexoxyethyl]-2-methoxyphenyl]-1,3-thiazol-2-yl]carbamoyl]phenyl]-2-methylprop-2-enoic acid
Molecular Formula: C29H32Cl2N2O5S
CAS Number: 1110766-97-6
Brands: Mulpleta

Medically reviewed by Drugs.com on Aug 24, 2020. Written by ASHP.

Introduction

Lusutrombopag is a hematopoietic agent.

Uses for Lusutrombopag

Lusutrombopag has the following uses:

Lusutrombopag is a thrombopoietin receptor agonist indicated for the treatment of thrombocytopenia in adult patients with chronic liver disease who are scheduled to undergo a procedure.

Lusutrombopag Dosage and Administration

General

Lusutrombopag is available in the following dosage form(s) and strength(s):

Tablet: 3 mg.

Dosage

It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

Adults

Dosage & Administration
  • Begin lusutrombopag dosing 8-14 days prior to a scheduled procedure.

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

  • Recommended Dosage: 3 mg orally once daily with or without food for 7 days.

Cautions for Lusutrombopag

Contraindications

  • None.

Warnings/Precautions

Thrombotic/Thromboembolic Complications

Lusutrombopag is a thrombopoietin (TPO) receptor agonist, and TPO receptor agonists have been associated with thrombotic and thromboembolic complications in patients with chronic liver disease. Portal vein thrombosis has been reported in patients with chronic liver disease treated with TPO receptor agonists. Portal vein thrombosis was reported in 1% (2 of 171) of lusutrombopag-treated patients and 1% (2 of 170) of placebo-treated patients in 3 randomized, double-blind trials and was identified post-procedure in protocol-specified imaging. The thromboses were not associated with a marked increase in platelet count.

Consider the potential increased thrombotic risk when administering lusutrombopag to patients with known risk factors for thromboembolism, including genetic pro-thrombotic 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, lusutrombopag should only be used if the potential benefit to the patient justifies the potential risk.

Lusutrombopag should not be administered to patients with chronic liver disease in an attempt to normalize platelet counts.

Specific Populations

Pregnancy

Risk Summary: There are no available data on lusutrombopag in pregnant women to inform the drug-associated risk. In animal reproduction studies, oral administration of lusutrombopag to pregnant rats during organogenesis and the lactation period resulted in adverse developmental outcomes. These findings were observed at exposures based on AUC that were substantially higher than the AUC observed in patients (approximately 89 times) at the recommended clinical dose of 3 mg once daily. Advise pregnant women of the potential risk to a fetus.

The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the general population in the United States, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Animal Data: In an embryo-fetal development study in rats, lusutrombopag was orally administered during organogenesis at doses of 4, 12.5, 40, and 80 mg/kg/day. Low body weight and a decrease in the number of ossified sternebrae were noted in fetuses at 80 mg/kg/day (approximately 251 times the AUC observed in patients at the recommended clinical dose of 3 mg once daily). Minor skeletal variations (supernumerary ribs) were observed at doses of 4 mg/kg/day (approximately 23 times the AUC observed in patients at the recommended clinical dose of 3 mg once daily).

In an embryo-fetal development study in rabbits following oral administration of lusutrombopag at doses up to 1000 mg/kg/day, no effect of lusutrombopag was observed on any parameter of embryo-fetal development.

In a pre- and postnatal development study in rats at oral doses of 1, 4, 12.5, and 40 mg/kg/day, there were adverse effects of lusutrombopag on postnatal development at 40 mg/kg/day (approximately 230 times the AUC observed in patients at the recommended clinical dose of 3 mg once daily). The effects included prolongation of the gestation period in dams, low viability before weaning, delayed postnatal growth (delayed negative geotaxis, delayed eyelid opening, or low pup body weight), abnormal clinical signs (prominent annular rings on the tail after weaning), low fertility index, a low number of corpora lutea or implantations, and increased pre-implantation loss. The incidence of short thoracolumbar supernumerary ribs on postnatal Day 4 of F1 pups was high at doses of 12.5 mg/kg/day or more (approximately 89 times the AUC observed in patients at the recommended clinical dose of 3 mg once daily).

Lactation

There is no information regarding the presence of lusutrombopag in human milk, the effects on the breastfed child, and the effects on milk production. Lusutrombopag was present in the milk of lactating rats. Due to the potential for serious adverse reactions in a breastfed child, breastfeeding is not recommended during treatment with lusutrombopag and for at least 28 days after the last dose.

A lactating woman should interrupt breastfeeding and pump and discard breast milk during lusutrombopag treatment and for 28 days after the last dose of lusutrombopag in order to minimize exposure to a breastfed child.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

Clinical studies of lusutrombopag did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

Common Adverse Effects

The most common adverse reaction (≥3%): headache.

Drug Interactions

Specific Drugs

It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

Please see product labeling for drug interaction information.

Actions

Mechanism of Action

Lusutrombopag is an orally bioavailable, small molecule TPO receptor agonist 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.

Advice to Patients

Advise the patient to read the FDA-approved patient labeling (Patient Information).

Prior to treatment, patients should fully understand and be informed of the following risks and considerations for lusutrombopag.

Thrombotic/Thromboembolic Complications

Lusutrombopag is a thrombopoietin (TPO) receptor agonist, and TPO receptor agonists have been associated with thrombotic and thromboembolic complications in patients with chronic liver disease. Portal vein thrombosis has been reported in patients with chronic liver disease treated with TPO receptor agonists.

Pregnancy

Advise women of reproductive potential who become pregnant or are planning to become pregnant that lusutrombopag should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.

Lactation

Advise women not to breastfeed during treatment with lusutrombopag and for 28 days after the last dose of lusutrombopag. Advise women to pump and discard breast milk during this period.

Additional Information

AHFSfirstRelease. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Lusutrombopag

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablet, Film Coated

3 mg

Mulpleta

SHIONOGI INC.

AHFS Drug Information. © Copyright 2021, Selected Revisions September 3, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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