Bremelanotide
Cyclic seven-residue melanocortin receptor agonist with preference for MC4R; central activation in the medial preoptic area and paraventricular nucleus is associated with downstream pro-sexual signaling.
Bremelanotide is a cyclic seven-residue analog of the endogenous melanocortin α-melanocyte-stimulating hormone (α-MSH). The molecule was originally synthesized as part of the broader Melanotan research program at the University of Arizona in the 1980s and 90s, and was later optimized for selectivity at the melanocortin-4 receptor (MC4R) relative to MC1R.
The therapeutic interest in MC4R agonism derives from the receptor’s central role in hypothalamic regulation of sexual function, appetite, and energy balance. In contrast with peripherally targeted treatments for sexual dysfunction, Bremelanotide acts primarily within the medial preoptic area and paraventricular nucleus to modulate downstream pro-sexual circuitry, including dopaminergic projections to the nucleus accumbens.
Bremelanotide is FDA-approved (Vyleesi, 2019) for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. Common adverse effects include nausea, flushing, transient blood-pressure elevation, and focal hyperpigmentation in some patients. It is included in the PharmaKinetics database for research and reference purposes.