Bexarotene Gel

Dosage form: gel
Drug class:Miscellaneous topical agents

Medically reviewed by Drugs.com. Last updated on Apr 1, 2022.

Bexarotene Gel Description

Bexarotene Gel, 1% contains bexarotene and is intended for topical application only. Bexarotene is a member of a subclass of retinoids that selectively activate retinoid X receptors (RXRs). These retinoid receptors have biologic activity distinct from that of retinoic acid receptors (RARs).

The chemical name is 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl] benzoic acid, and the structural formula is as follows:

Bexarotene is a white to off-white powder with a molecular weight of 348.478 and a molecular formula of C24H28O2. It is practically insoluble in water, slightly soluble in methanol, sparingly soluble in acetone, soluble in dimethyl sulfoxide, slightly soluble in ethanol and very slightly soluble in vegetable oil.

Bexarotene Gel, 1% is a clear gelled solution containing 1.0% (w/w) bexarotene in a base of dehydrated alcohol, polyethylene glycol 400, hydroxypropyl cellulose, and butylated hydroxytoluene.

Bexarotene Gel - Clinical Pharmacology

Mechanism of Action

Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRα, RXRβ, RXRγ). RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin D receptor, thyroid receptor, and peroxisome proliferator activator receptors (PPARs). Once activated, these receptors function as transcription factors that regulate the expression of genes that control cellular differentiation and proliferation. Bexarotene inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin. It also induces tumor regression in vivo in some animal models. The exact mechanism of action of bexarotene in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.

Pharmacokinetics

General

Plasma concentrations of bexarotene were determined d...