Travoprost C화학적 특성, 용도, 생산
개요
Travoprost was launched in the US as Travatan?, an ophthalmic solution (0.004%)
administered topically for the treatment of elevated intraocular hypertension (lOP) through
open-angle glaucoma, a common optic neuropathy and a leading cause of blindness.
Travoprost is the isopropyl ester of (+)-fluprostenol, a new prostaglandin derivative
belonging to the PGF
2α, analog class. This compound can be prepared in 8 steps from a
bicyclic lactone aldehyde by a Wittig alkylidenation followed, after 2 ketonic reductions, by
a lactol opening to prostenoic acid while protecting and deprotecting appropriately.
Travoprost is a full agonist of FP receptors with a greater affinity than PGF
2α, (K
1 = 52 nM).
Pharmacologic studies in rabbits treated daily for a week demonstrated a significant
increase of the microvascular optic nerve head blood flow without significant alterations in
the systemic flow. In several placebo-controlled clinical studies with hundreds of patients
suffering from open-angle glaucoma or ocular hypertension, travoprost (1 to 4 pm daily)
dose-dependently reduced lOP (by about 30% at 4 pm); it was shown equal or superior to
latanoprost, another prostaglandin analog (5 pm daily) or the adrenergic ~-blocker timolol
(500 pm bid). In addition, travoprost was safe and well tolerated with a low incidence of
conjunctival hyperaemia.
화학적 성질
Colorless Oil
용도
Travoprost is a selective FP prostaglandin receptor agonist used to treat glaucoma (1,2).
정의
ChEBI: The isopropyl ester of prostaglandin F2alpha in which the pentyl group is replaced by a 3-(trifluoromethyl)phenoxymethyl group. A synthetic analogue of prostaglandin F2alpha, ophth
lmic solutions of travoprost are used as a topical medication for controlling the progression of open-angle glaucoma and ocular hypertension, by reducing intraocular pressure. It is a pro-drug; the isopropyl ester group is hydrolysed by esterases in the co
nea to the biologically active free acid, fluprostenol.
일반 설명
Travoprost (Travatan and Travatan-Z) is supplied asa 2.5- or 5.0-mL sterile 0.004% ophthalmic solution in a4.0- or 7.5-mL size container. Travoprost is claimed to bethe most potent and FP-specific analog in this product category. Cautions and side effects are similar to those givenpreviously.
Travoprost 준비 용품 및 원자재
원자재
준비 용품
