Tafluprost, a new potent prostanoid receptor agonist: a dose-response study on pharmacodynamics and tolerability in healthy volunteers

Tafluprost: a novel prostaglandin analog for treatment of glaucoma

“…Similar observations were made in the second phase I study. 9 The authors stated that the overall rates of adverse effects were similar for the tafluprost 0.0001%, tafluprost 0.0025%, and latanoprost 0.005% groups, but rates of ocular hyperemia was significantly lower in eyes receiving latanoprost. All adverse events described in the first two phase I studies were mild to moderate and did not result in treatment discontinuation.…”

“…11 The systemic safety was similar for tafluprost, latanoprost, and placebo when administered topically. 8,9 The investigators did not observe clinically significant changes in laboratory parameters, vital signs, or electrocardiographic parameters in any of the 49 participants throughout the course of the first phase I study.…”

“…8,9 In the first phase I study, tafluprost 0.0025% and 0.005%, latanoprost 0.005%, and placebo were administered to healthy volunteers for 7 days.…”

“…The effect was maximal at 12 hours after administration and lasted throughout the duration of treatment (2 days). 9 After a subsequent dose-response phase II trial in Japan, the therapeutic concentration of tafluprost was set at 0.0015%, which was not used in phase I studies. 11 The systemic safety was similar for tafluprost, latanoprost, and placebo when administered topically.…”

Metabolism and Ocular Tissue Distribution of an Antiglaucoma Prostanoid, Tafluprost, After Ocular Instillation to Monkeys

“…2 In both animal models, maximal IOP reductions were dose dependent, and once-daily instillations of tafluprost at concentrations of 0.001%-0.005% for 5 days demonstrated greater IOP reduction at the trough time-point (24 h after dosing) when compared with placebo and 0.005% latanoprost in normotensive monkeys. 2 In clinical trials, dose-dependent IOP reduction was also observed in healthy Japanese and non-Japanese volunteers at concentrations of 0.0025% and 0.005% tafluprost, 3,4 and the efficacy and tolerability of tafluprost in patients were confirmed in phase III clinical studies at a concentration of 0.0015%, which is the pharmaceutical concentration of the commercial drug product. 5,6 Antiglaucoma PGF 2a ester analogs, including tafluprost, show meaningful high levels of efficacy in both human and monkey eyes.…”