Sutton Andrew, Gilvarry Anne, Ropo Auli
Guildford Clinical Pharmacology Ltd., Guildford, Surrey, United Kingdom.
J Ocul Pharmacol Ther. 2007 Aug;23(4):359-65. doi: 10.1089/jop.2006.0061.
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.
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.
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%.
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.
本研究旨在确定新型前列腺素氟前列素（FP）受体激动剂他氟前列素（AFP - 168）在健康男性中的安全性、耐受性和药效学。
这是一项针对18至45岁健康男性的I期研究（N = 49）。参与者被随机分配接受4种滴眼液中的一种：0.0025%或0.005%的他氟前列素、0.005%的拉坦前列素或安慰剂，每天滴眼一次，共7天，每眼一滴。在规定的时间间隔进行安全性和耐受性评估以及眼压（IOP）测量。
他氟前列素总体耐受性良好。未报告严重不良事件，也没有参与者因不良事件退出研究。与基线相比，所有4个治疗组的眼压均随时间下降。在治疗期间的各个时间点，0.005%的他氟前列素治疗导致眼压下降幅度明显大于0.005%的拉坦前列素或安慰剂。与0.005%的拉坦前列素相比，0.0025%或0.005%的他氟前列素引起的眼部充血和畏光更为常见。
0.0025%和0.005%的他氟前列素滴眼液总体耐受性良好且安全。0.005%的他氟前列素降低眼压的效果优于安慰剂或0.005%的拉坦前列素。因此，他氟前列素在进一步研究中前景广阔。
