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American Journal of Clinical Dermatology

Published in:

01-07-2000 | Adis New Drug Profile

Bexarotene

Authors: Matthew N. Lowe, Greg L. Plosker

Published in: American Journal of Clinical Dermatology | Issue 4/2000

Abstract

▴ Bexarotene is a selective retinoid X receptor (RXR) agonist. It binds to, and activates RXRs which function as ligand-activated transcription factors that control gene expression. This leads to modulation of cell growth, apoptosis, and differentiation.

▴ In patients with refractory or persistent early stage cutaneous T cell lymphoma (CTCL), the overall response rate was 54% after oral bexarotene 300 mg/m²/day. The overall response rate in patients with refractory or persistent advanced stage CTCL was 45% at the same dosage.

▴ An overall response rate of 63% was reported after topical bexarotene 0.1 to 1% twice daily in patients with early stage CTCL. Another trial reported an overall response rate of 44% after topical bexarotene 1% once daily escalated up to 4 times daily.

▴ Plaque elevation was significantly reduced, and the severity of moderate to severe psoriasis was substantially improved in patients receiving oral bexarotene 0.5 to 2 mg/kg/day.

▴ At clinically relevant oral dosages, bexarotene significantly decreases levels of serum thyrotropin and free thyroxine.

▴ The most common adverse events associated with oral bexarotene are hypertriglyceridemia, hypercholesterolemia, central hypothyroidism and headache. Reversible acute pancreatitis has occurred during oral bexarotene therapy.

▴ Adverse events associated with the topical formulation are limited to rash, pruritus, and pain.

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Title: Bexarotene
Authors: Matthew N. Lowe
Greg L. Plosker
Publication date: 01-07-2000
Publisher: Springer International Publishing
Published in: American Journal of Clinical Dermatology / Issue 4/2000
Print ISSN: 1175-0561
Electronic ISSN: 1179-1888
DOI: https://doi.org/10.2165/00128071-200001040-00006

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