#
Bexarotene (Systemic)
  • Professionals
  • AHFS Monographs

Bexarotene (Systemic)

Class: Antineoplastic Agents
VA Class: AN900
Chemical Name: 4-[1-(5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid
Molecular Formula: C24H28O2
CAS Number: 153559-49-0
Brands: Targretin

Medically reviewed by Drugs.com on Apr 21, 2022. Written by ASHP.

Warning

May cause birth defects in humans; teratogenicity and embryolethality demonstrated in animals. Contraindicated in pregnant women. See Fetal/Neonatal Morbidity and Mortality under Cautions.

Introduction

Antineoplastic agent; synthetic retinoid analog.

Uses for Bexarotene (Systemic)

Cutaneous T-cell Lymphoma

Treatment of skin manifestations of cutaneous T-cell lymphoma (CTCL) in patients who are refractory to at least one prior systemic therapy.

Bexarotene (Systemic) Dosage and Administration

Administration

Oral Administration

Administer orally once daily with a meal.

Dosage

Adults

CTCL
Oral

Initially, 300 mg/m2 daily.

If intolerable adverse effects occur, decrease dosage to 200 mg/m2 daily, then 100 mg/m2 daily, or temporarily discontinue. When toxicity is controlled, carefully readjust dosage upward.

If no tumor response is observed after 8 weeks and the 300-mg/m2 daily dosage is well tolerated, increase to 400 mg/m2 daily with careful monitoring.

Continue as long as benefit is derived from therapy. Optimum duration is not known.

Cautions for Bexarotene (Systemic)

Contraindications

  • Known or suspected pregnancy.

  • Known hypersensitivity to bexarotene or any ingredient in the formulation.

Warnings/Precautions

Warnings

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; teratogenicity and embryolethality demonstrated in animals.

Exclude pregnancy 1 week prior to initiation of therapy. Initiate therapy on second or third day of normal menstrual period. Repeat pregnancy tests monthly during therapy. To facilitate pregnancy test assessment and counseling, dispense no more than 1 month supply.

Use contraception (2 reliable forms, including at least 1 nonhormonal method) for 1 month before, during, and for 1 month after administration. Male patients should use condoms during sexual intercourse with women who are or may become pregnant.

If pregnancy occurs, immediately discontinue and apprise of potential fetal hazard.

Effects on Lipoproteins

Lipid abnormal...