Drug intelligence / Profile preview

etretinate

Development stage
Preclinical
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

Etretinate is a synthetic aromatic retinoid used primarily for the treatment of severe psoriasis. It acts by interfering with the terminal differentiation of keratinocytes and is thought to bind to retinoic acid receptors (RAR and RXR), thereby modulating gene expression involved in skin cell growth and differentiation. Etretinate is highly lipophilic with a long half-life due to storage in adipose tissue; it can remain detectable in plasma for up to three years after discontinuation. The drug was developed by Hoffmann–La Roche and approved by the FDA in 1986 but was withdrawn from markets such as Canada (1996) and the US (1998) due to its high risk of teratogenicity. In Japan it remains available under the brand name Tigason. Etretinate has been largely replaced by acitretin but may still be used for certain indications like T-cell lymphomas[1][2][3][5].

Brand names
TegisonTigason
Other names
2,4,6,8-nonatetraenoic acid, 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-, ethyl esterEtrinoate, Ethyl(2E,4E,6E,8E)-9-(4-Methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-nona-2,4,6,8-tetraenoic acid ethyl esterACITRETIN IMPURITY B
02

Targets

RARB (Retinoic acid receptor beta)RXRA (Retinoid X receptor alpha)RXRB (Retinoid X receptor beta)CRABP2 (Cellular retinoic acid-binding protein 2)RARG (Retinoic acid receptor gamma)RARA (Retinoic acid receptor alpha)RXRG (RXRγ)

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