PT-141 (Bremelanotide)

Approved as VYLEESI (bremelanotide) for hypoactive sexual desire disorder (HSDD) in premenopausal women, FDA approval 2019.

PubChem CID9941379

FormulaC50H68N14O10

Mol. Weight1025.2 g/mol

Sequence

Mechanism of Action

Bremelanotide is a synthetic cyclic heptapeptide analogue of alpha-MSH that acts as a nonselective melanocortin receptor agonist, with activity at both MC4R and MC3R. Central MC4R activation is understood to modulate hypothalamic circuits implicated in sexual arousal and desire, distinguishing its mechanism from peripheral vascular-acting agents. It has an unusually deep human clinical trial record among research peptides, including a 52-week long-term safety extension.

Melanocortin-4 receptor (MC4R)Melanocortin-3 receptor (MC3R)

Research Literature

Bremelanotide: First Approval

Other

Drugs · 2019

Documents bremelanotide's 2019 FDA approval as the first melanocortin receptor agonist for HSDD in premenopausal women.

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Long-Term Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder

Human Trial

Obstetrics & Gynecology · 2019

52-week open-label extension of the pivotal trials found no new safety signals, with sustained desire improvements; nausea, flushing, and headache were the most common adverse effects.

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An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist

Human Trial

Journal of Sexual Medicine · 2006

Crossover study found more women reported moderate-to-high desire after intranasal bremelanotide versus placebo during erotic video exposure, though vaginal vasocongestion was not significantly changed.

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