Travoprost: A potent ocular hypotensive agent

Travoprost (isopropyl (Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(1 E,3R)-3-hydroxy-4-[alpha,alpha,alpha,trifluoro-m-tolyl)oxy]- 1 butenyl]cyclopentyl]-5-heptenoate) is an isopropyl ester prodrug and a high-affinity, selective FP prostaglandin- receptor full agonist. This pro drug is a synthetic prostaglandin analogue, which in appropriate cases is administered topically for the treatment of glaucoma and ocular hypertension. The isopropyl ester prodrug is rapidly hydrolyzed by esterases in the cornea to the biologically active, free acid. Travoprost has demonstrated preferential affinity and full agonist activity for the FP receptor in the nanomolar range, with no meaningful affinity or activity at other receptors. Like other compounds of this class, the reduction of intraocular pressure by travoprost is due at least in part to increased uveoscleral outflow. Results from phase II and phase III pivotal studies for FDA approval in the United States have demonstrated that travoprost is an effective topical agent for treatment of elevated intraocular pressure in patients with open-angle glaucoma and ocular hypertension. Travoprost is a safe drug, with local side effects including hyperemia, eyelash growth and iris color change. The dosing is once per day in the evening, and storage does not require refrigeration. Travoprost will be a helpful new drug in the medical management of glaucoma. (C) Prous Science 2003. All rights reserved.