A comparative, placebo-controlled study of prostanoid fluoroprostaglandin-receptor agonists tafluprost and latanoprost in healthy males.
OBJECTIVE
The aim of this study was to determine the safety, tolerability, and pharmaco-dynamics of a novel prostanoid fluoroprostaglandin (FP)-receptor agonist, tafluprost (AFP-168), in healthy males.


METHODS
This was a phase I study in healthy males 18-45 years of age (N = 49). Participants were randomized to receive 1 of 4 eye drops: tafluprost 0.0025% or 0.005%, latanoprost 0.005%, or a placebo, administered once-daily for 7 days, with 1 drop per eye. Safety and tolerability assessments and intraocular pressure (IOP) measurements were performed at defined intervals.


RESULTS
Tafluprost was generally well tolerated. No serious adverse events were reported and no participants withdrew owing to an adverse event. IOP decreased over time, compared with baseline, in all 4 treatment groups. Treatment with tafluprost 0.005% resulted in a significantly greater reduction in IOP, compared with either latanoprost 0.005% or a placebo, at various time points during treatment. Ocular hyperemia and photophobia were more common with tafluprost 0.0025% or 0.005%, compared with latanoprost 0.005%.


CONCLUSIONS
Tafluprost eye drops 0.0025% and 0.005% were generally well tolerated and safe. Tafluprost 0.005% reduced IOP more than placebo or latanoprost 0.005%. Therefore, tafluprost looks promising for further investigation.
Sutton
Andrew
A
Guildford Clinical Pharmacology Ltd., Guildford, Surrey, United Kingdom. asutton@gcpl.co.uk
Gilvarry
Anne
A
Ropo
Auli
A
D000287:Administration, Topical; D000293:Adolescent; D000328:Adult; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D006940:Hyperemia / Q000139:chemically induced; D007429:Intraocular Pressure / Q000187:drug effects*; D000077338:Latanoprost; D008297:Male; D008875:Middle Aged; D009883:Ophthalmic Solutions; D020795:Photophobia / Q000139:chemically induced; D011460:Prostaglandins F / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology*; D011461:Prostaglandins F, Synthetic / Q000009:adverse effects / Q000494:pharmacology*; D011982:Receptors, Prostaglandin / Q000378:metabolism