Tafluprost Acid is a derivative of Tafluprost (T004820), a novel prostanoid used in the treatment of glaucoma and is the first prostanoid to be released in a preservative free-formula.
A number of 17-phenyl trinor prostaglandin F2α (17-phenyl trinor PGF2α) derivatives have been approved for the treatment of glaucoma. Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects. Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile. Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. Tafluprost (free acid) is a very potent FP receptor agonist, with a Ki of 0.4 nM. The ester prodrug forms of tafluprost are also potent ocular hypotensives in monkeys.
Chemical Name:
7-[2-(3,3-difluoro-4-phenoxybut-1-enyl)-3,5-dihydroxycyclopentyl]hept-5-enoic acid
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