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Bexarotene

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American Journal of Clinical Dermatology Aims and scope Submit manuscript

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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  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand

    Matthew N. Lowe & Greg L. Plosker

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  1. Matthew N. Lowe
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  2. Greg L. Plosker
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Correspondence to Matthew N. Lowe.

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Lowe, M.N., Plosker, G.L. Bexarotene. Am J Clin Dermatol 1, 245–250 (2000). https://doi.org/10.2165/00128071-200001040-00006

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