Tazarotene

What is tazarotene?

Tazarotene is a retinoid that binds selectively to retinoic acid receptors, specifically the β and γ subtypes, but does not bind to retinoid X receptors (R, R).

Does tazarotene get absorbed?

Tazarotene is available in gel, cream and foam formulations. Topical application delivers tazarotene directly into the skin. 10 hours after topical application of tazarotene gel, 4-6% of the dose was found in the stratum corneum and 2% in the viable epidermis and dermis (R).

What happens after tazarotene is absorbed?

Tazarotene is rapidly metabolised in the skin to tazarotenic acid, its primary and active metabolite (R, R). Although it accumulates after repeated dosing, reaching steady state concentrations after 2-3 weeks (R, R), its overall systemic bioavailability is still low at approximately 1% (R). The maximum average plasma concentration of tazarotenic acid after topical application of 0.1% tazarotene cream to the face was less than 0.25 µg/L (R). Dosing with tazarotene gel and foam also led to low plasma concentrations of tazarotenic acid, though the concentration is higher for the gel than the foam formulation (R).

Tazarotenic acid does not accumulate in adipose tissue, but undergoes further metabolism to its sulfoxide and to other polar metabolites and is rapidly eliminated via both urinary and faecal pathways with a terminal half-life of about 18 hours (R).