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Talarozole
Systematic (IUPAC) name
N-(2-Benzothioazolyl)-N-[4-[2-ethyl-1-(1,2,4-triazo-1-yl)butyl]phenyl]amine
Identifiers
CAS number 201410-53-9
ATC code none
PubChem  ?
Chemical data
Formula C21H23N5S 
Mol. mass 377.505 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes oral, topical


Talarozole (formerly R115866, planned trade name Rambazole) is an investigational drug for the treatment of acne, psoriasis and other keratinization disorders.

Talarozole inhibits the metabolism of retinoic acid by blocking the cytochrome P450 enzyme isoform CYP26, a retinoic acid hydroxylase. Because of this mechanism, it is called a retinoic acid metabolism blocking agent (RAMBA).[1]

Talarozole, being developed by Barrier Therapeutics Inc under license from Johnson & Johnson, is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne. Phase II clinical trials of an oral formulation of talarozole in patients with psoriasis and with acne, and a phase I clinical trial of a topical formulation have been completed. At the time of publication, Barrier Therapeutics had suspended the development of talarozole as part of a series of cost-cutting initiatives; the company had also been acquired by Stiefel Laboratories Inc. No formal announcement had been made regarding the further development of talarozole.[2]

[edit] References

  1. ^ Giltaire, S; Herphelin F, Frankart A, Hérin M, Stoppie P, Poumay Y (11 December 2008). "The CYP26 inhibitor R115866 potentiates the effects of all-trans retinoic acid on cultured human epidermal keratinocytes". Br J Dermatol. PMID 19120344. 
  2. ^ Pubmed



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