Drug intelligence / Profile preview

talarozole

Development stage
Phase 2
Lead developer
Stiefel
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

Talarozole is a small molecule drug and highly potent, selective azole derivative that acts as a retinoic acid metabolism blocking agent (RAMBA). It inhibits the cytochrome P450 enzyme isoforms CYP26A1 and possibly CYP26B1, which are responsible for the breakdown of all-trans retinoic acid. By blocking these enzymes, talarozole increases endogenous levels of retinoic acid, thereby modulating epithelial differentiation and growth through activation of nuclear RA receptors. Originally developed for acne, psoriasis, and other keratinization disorders (development discontinued), it is now being investigated as a potential disease-modifying therapy for hand and knee osteoarthritis due to its ability to suppress inflammation and cartilage damage in preclinical models[1][2][4][5][7].

Brand names
Rambazole
Other names
talarozole(+)-talarozole201410-53-9
02

Targets

CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP26A1 (Cytochrome P450 26A1)CYP26B1 (Cytochrome P450 26B1)CYP3A4 (Cytochrome P450 3A4)

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