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In both normal and ED men, treatment with Bremelanotide causes significant increases in erectile activity, in a dose-dependant manner . Clinically and statistically effective doses of the drug (up to 20mg) are safe and well tolerated by both normal and ED patients . Having completed all Phase II trials in men with promising results, Bremelanotide is set to enter Phase III for men in the first half of this year. In women, positive data from a Phase IIa trial and the recent commencement of a Phase IIb trial suggest that entry to Phase III for women may also be on the horizon. If approved, Bremelanotide would be the first FDA-approved synthetic aphrodisiac. This novel therapy could potentially address the substantial need for an effective female sexual dysfunction treatment as well as offer an alternative to traditional PDE inhibition in ED men.
Bremelanotide: The peptide-melanocyte stimulating hormone (MSH) is a product of the proopiomelanocortin pro-hormone. This peptide has long been known to be involved in regulation of energy homeostasis and has been suggested as a target for number medical indications (Hedlund 2004). In the mid-1980s, a group at the University of Arizona synthesized two highly potent MSH analogues (Hadley et al. 1998). One compound, deemed Melanotan I (MTI) was licensed out and further characterised for utility as a tanning drug, given the known role of MSH in pigmentation. A further analogue, Melanotan II (MTII) was developed which was smaller and the hope was that this would aid in its absorption and tissue distribution. The investigator decided to assess for himself whether this second analogue had the tanning capability seen with MTI and proceeded to dose himself. While it is unclear whether he did achieve a tan, what the investigator reports was an “unrelenting” erection lasting 8 hours. Not long after, this compound was licensed out for further development as a sexual dysfunction treatment candidate. PT-141 is the active metabolite of MTII and ultimately became the drug development lead compound and was renamed bremelanotide. Clincal trials in women have demonstrated that bremelanotide increases sexual desire and arousal in women with arousal disorders (Diamond et al. 2004; Diamond et al. 2006; Safarinejad 2008). In one study, using vaginal plethysmography to assess vasocongestion, even though subjective scores were increased over placebo, there was no change in vasocongestion measures as compared to controls, confirming that vaginal vasocongestion is not a suitable method for assessing efficacy of compounds (Diamond et al. 2006). Prior to the discovery and development of bremelanotide, melanocortin receptors were not considered to be of great interest within the sexual medicine field. Since that time, a surge of interest has appeared, and along with it a boost in scientific research investigating the mechanisms involved.