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Travoprost
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Travoprost is a synthetic lipophilic cloprostenol derivative. It is a prodrug of the active compound travoprost free acid, a prostaglandin F2α-analog with anti-glaucoma property. Upon administration, travoprost is hydrolyzed to the free acid by corneal esterases. It then selectively stimulates the prostaglandin F receptor, thereby increasing the uveoscleral outflow which leads to a reduction in intra-ocular pressure. Travoprost ophthalmic solution is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension (1).
A new look at the safety and tolerability of prostaglandin analogue eyedrops in glaucoma and ocular hypertension
Published in Expert Opinion on Drug Safety, 2022
Andreas Katsanos, Ivano Riva, Banu Bozkurt, Gábor Holló, Luciano Quaranta, Francesco Oddone, Murat Irkec, Gordon N. Dutton, Anastasios G. Konstas
Travoprost is a synthetic ester prodrug of prostaglandin F2α that was approved by the FDA in 2001 for the reduction of IOP in patients with glaucoma or OHT (Travatan® Alcon Laboratories, Ft Worth, USA). FDA approval was initially granted for patients who did not tolerate, or respond well to other available IOP-lowering agents, due to concerns about the long-term safety of travoprost and specifically due to the appearance of iris and periocular pigmentation associated with the topical administration of the drug. These restrictions were lifted in 2010 based on follow-up and post-marketing data which failed to identify cases of pigmentary glaucoma, or melanoma caused by the chronic use of travoprost [53]. The approved formulation of the drug (i.e. 0.004% travoprost preserved with BAK) was tested in large phase III registration trials against the BAK-containing formulations of travoprost 0.0015%, timolol 0.5% and latanoprost 0.005% [54–56]. The 0.004% concentration was selected for clinical use as representing the top of the dose-response curve from two previous unpublished studies by Alcon Laboratories, while 0.0015% was selected as an intermediate reference travoprost concentration [54].
Sustained release ocular drug delivery systems for glaucoma therapy
Published in Expert Opinion on Drug Delivery, 2023
Zinah K. Al-Qaysi, Ian G. Beadham, Sianne L. Schwikkard, Joseph C. Bear, Ali A. Al-Kinani, Raid G. Alany
ENV515/Travoprost XR (Envisia Therapeutics, Morrisville, NC, U.S.A) is an implant that is injected into the anterior chamber of the eye. It releases travoprost over a period of 6 months using a biodegradable system that requires a single injection. This implant provides IOP reduction over 6 months and can be manufactured from poly(esteramide) (PEA) using PRINT® technology. The polymer is printed, filled with the active ingredient, and injected or inserted into the appropriate ocular site through a suitably sized needle [56,122,123]. The PEA polymer is used to fabricate ENV515 as a rod-shaped implant to provide sustained drug delivery for the treatment of ophthalmic diseases. PEA degrades intravitreally, following zero-order kinetics, resulting in the slow release of travaprost [122,124,125]. In a preclinical study using normotensive beagle dogs, intracameral insertion of ENV515 resulted in an average decrease in IOP of 35 ± 3% to 6.4 ± 0.6 mm Hg from baseline over 24 weeks, with a favorable safety profile and good implant stability [126]. A further Phase IIa clinical study was carried out, recruiting patients with ocular hypertension who had previously been treated with topical prostaglandins. After a washout period, intracameral implantation of the ENV515 to the study eye and topical timolol ophthalmic solution 0.5% was applied once daily to the contralateral eye. After 11 months of receiving a single dose, a mean reduction in IOP of around 6.7 ± 3.7 mm Hg (25% from baseline) was recorded. The device was well tolerated, without serious adverse effects, although dose-related transient hyperemia and eye redness were noted on occasions [127].
Spanlastics nanovesicular ocular insert as a novel ocular delivery of travoprost: optimization using Box–Behnken design and in vivo evaluation
Published in Journal of Liposome Research, 2022
Marwa H. Shukr, Soha Ismail, Ghada G. El-Hossary, Amany H. El-Shazly
Prostaglandin analogs are commonly used to reduce IOP by increasing the uveoscleral and trabecular outflow of aqueous humor (Bean and Camras 2008). Travoprost (TRAVO) is a synthetic prostaglandin F2α analog, it is an ester prodrug penetrates the corneal epithelium and gets hydrolyzed by esterases into the biologically active form which is travoprost free acid. It was reported to be absorbed following ocular application with highest distribution in the cornea, followed by the conjunctiva, iris ciliary body, and finally the aqueous humor (Alcon Technical report 2000), then it gets eliminated following an initial elimination phase is followed by a slower beta elimination phase (Saati et al. 2010).