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| Routes of administration | By mouth, topical |
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| Formula | C21H23N5S |
| Molar mass | 377.51 g·mol−1 |
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Talarozole (formerlyR115866, planned trade nameRambazole) was an investigational drug for the treatment ofacne,psoriasis and otherkeratinization disorders. Development for that purpose has been discontinued.[1] However, its effect in increasing retinoic acid is now being investigated in hand and knee osteoarthritis.[2]
Talarozole inhibits the metabolism ofretinoic acid by blockingcytochrome P450 enzyme CYP26isoenzymes (CYP26A1 and possibly alsoCYP26B1), retinoic acidhydroxylases.[3] Because of this mechanism, it is called aretinoic acid metabolism blocking agent (RAMBA).[3][4]
It has 750-fold higherpotency than the earlier drugliarozole as well as greaterselectivity, with more than 300-fold selectivity for inhibition of CYP26A1 over other steroid-metabolizing enzymes likeCYP17A1 (17α-hydroxylase/17,20-lyase) andaromatase (CYP19A1).[3][5]
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