Review Of Potential Role Of Bremelanotide (Pt-141) In Treating Female Sexual Dysfunction

Introduction. Bremelanotide is a synthetic peptide analog of α-melanocyte stimulating hormone and is an agonist at melanocortin receptors MC3R and MC4R.This review examines research to date regarding the potential use of bremelanotide for the treatment of female sexual dysfunction (FSD). Results. Six distinct research paths suggest a potential role for bremelanotide in FSD treatment: 1) Clinical trials have demonstrated induction of significant erectile activity in healthy male volunteers and patients with erectile dysfunction, supporting the hypothesis that bremelanotide is a central initiator of sexual arousal in men. Anatomical similarities between genders suggest similar benefits may accrue to women. 2) Preclinical research demonstrated effects of bremelanotide on proceptive sexual behaviors in ovariectomized female rats. Appetitive behavior in female rats may have a human analog in sexual interest, desire, or arousal. 3) Thirty-two healthy women were treated with either placebo or subcutaneous bremelanotide. Bremelanotide was safe and well tolerated. 4) An in-clinic, double-blind, placebo-controlled, crossover study of two concurrent doses of 10 mg intranasal bremelanotide in 18 premenopausal patients with female sexual arousal disorder found that more women reported moderate or high sexual desire after bremelanotide than placebo and there was a correlation between positive desire responses and increased genital arousal. 5) A similar study enrolling postmenopausal women with FSD was recently completed and results comparable to the premenopausal data were suggested. 6) An at-home, multi-site clinical trial enrolling both premenopausal and postmenopausal women with FSD is underway. Conclusions. Collectively, these preclinical and clinical data evoke a cautious optimism and strong recommendation for continued assessment of bremelanotide for the treatment of FSD. Additionally, contextual sensitivity of female sexual response may require combination treatment, where sexual pharmaceuticals and sex coaching is integrated more frequently for women than it has been for men.

Conflict of Interest: Dr. Perelman Has Served As A Consultant For Palatin Technologies, Inc.
Financial Support/Funding: Research Funded By Palatin Technologies, Inc.
Sydney, Australia, April 2007