PT-141: a melanocortin agonist for the treatment of sexual dysfunction.

Annals of the New York Academy of Sciences2003PMID: 12851303

Clinical TrialAnimal StudyPT-141

Plain Language Summary

The primary preclinical characterization paper for PT-141. Shows that PT-141 causes penile erection in rats and primates, activates hypothalamic neurons (c-Fos immunoreactivity) in areas innervating the corpus cavernosum, and produces rapid dose-dependent erection in men with and without ED. The foundational animal-to-human translational study establishing PT-141's mechanism and clinical promise.

Abstract

PT-141, a synthetic peptide analogue of alpha-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system. Administration of PT-141 to rats and nonhuman primates results in penile erections. Systemic administration of PT-141 to rats activates neurons in the hypothalamus as shown by an increase in c-Fos immunoreactivity. Neurons in the same region of the central nervous system take up pseudorabies virus injected into the corpus cavernosum of the rat penis. Administration of PT-141 to normal men and to patients with erectile dysfunction resulted in a rapid dose-dependent increase in erectile activity. The results suggest that PT-141 holds promise as a new treatment for sexual dysfunction.

Authors

Molinoff, P B; Shadiack, A M; Earle, D; Diamond, L E; Quon, C Y