Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction

被引:89
作者
Diamond, LE
Earle, DC
Rosen, RC
Willett, MS
Molinoff, PB
机构
[1] Palatin Technol Inc, Cranbury, NJ 08540 USA
[2] Univ Med & Dent New Jersey, Robert Wood Johnson Med Sch, Dept Psychiat, Piscataway, NJ 08854 USA
[3] Adv Biomed Res, Pennington, NJ USA
关键词
erectile dysfunction; melanocortin; PT-141;
D O I
10.1038/sj.ijir.3901139
中图分类号
R5 [内科学]; R69 [泌尿科学(泌尿生殖系疾病)];
学科分类号
1002 ; 100201 ;
摘要
PT-141, a cyclic heptapeptide melanocortin analog, was evaluated following intranasal administration in healthy male subjects and in Viagra-responsive erectile dysfunction (ED) patients. Erectile response was assessed by RigiScant(TM) in healthy subjects without visual sexual stimulation (VSS) and in Viagra(R)-responsive ED patients with VSS. In healthy subjects, mean C-max and AUC((0-t)) increased in a dose-dependent manner. Median T-max was 0.50 h and mean t(1/2) ranged from 1.85 to 2.09 h. In both studies, an erectile response induced by PT-141 administration was statistically significant, compared to placebo, at doses greater than 7 mg, with the onset of the first erection occurring in approximately 30 min. PT-141 was safely administered and well tolerated in both studies. A maximum-tolerated dose was not identified. Flushing and nausea were the most common adverse events reported in both studies and no clinically significant changes in vital signs, laboratory tests, ECGs, or physical exams were observed. Based upon its erectogenic potential and tolerability profile, PT-141 is a promising candidate for further evaluation as a treatment for male ED.
引用
收藏
页码:51 / 59
页数:9
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