Preclinical efficacy of travoprost, a potent and selective FP prostaglandin receptor agonist

Travoprost is the isopropyl ester prodrug of a high affinity, selective FP prostaglandin full receptor agonist. In contrast to travoprost acid's high affinity and efficacy at the FP receptor, there is only sub-micromolar affi nity for the DP, EP1, EP3, EP4, IP, and TP receptors. Travoprost produced a lower incidence of ocular irritation than PGF(2 alpha) isopropyl ester at a dose of 1 mug in the New Zealand albino (NZA) rabbit. Topical ocular appl ication of travoprost produced a marked miotic effect in cats following dos es of 0.01, 0.03 and 0.1 mug. In the ocular hypertensive monkey, b.i.d. app lication of 0.1 and 0.3 mug of travoprost afforded peak reduction in intrao cular pressure (IOP) of 22.7% and 28.6%, respectively. Topical application of travoprost was well tolerated in rabbits, cats and monkeys, causing no o cular irritation or discomfort at doses up to 1 mug. Travoprost is a promis ing ocular hypotensive prostaglandin FP derivative that has the ocular hypo tensive efficacy of PGF(2 alpha) isopropyl ester but with less severe ocula r side effects.