Bremelanotide (Vyleesi): Uses, Evidence, and Side Effects

Many premenopausal women who experience a persistent drop in sexual desire wonder whether a medication can help, and what that treatment actually involves. Bremelanotide, sold under the brand name Vyleesi, is one FDA-approved option developed specifically for this concern.

Key takeaways

• Bremelanotide (Vyleesi) is approved for acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women.
• It works by activating melanocortin receptors in the central nervous system, though its exact mechanism for improving HSDD is unknown.
• It is not approved for postmenopausal women, men, or for enhancing sexual performance.
• Ten registered clinical trials have studied bremelanotide, including completed Phase 2 studies in sexual arousal and desire disorders.
• Reported side effects in FDA adverse event data are led by nausea, along with headache, vomiting, and flushing.

What Bremelanotide Is

Bremelanotide is a melanocortin receptor agonist, meaning it activates a family of receptors found throughout the central nervous system. It nonselectively stimulates several receptor subtypes, with MC1R and MC4R considered most relevant at the doses used in treatment. Neurons expressing MC4R are widespread in the brain, but the label states that the precise way bremelanotide improves HSDD symptoms is not fully understood.

What Bremelanotide Is Approved For

Under the brand name Vyleesi, bremelanotide is indicated for acquired, generalized HSDD in premenopausal women. Acquired HSDD means desire that has declined after a period of normal sexual interest, and generalized means the low desire occurs regardless of partner or situation. The label specifies that it is not intended for cases explained by a co-existing medical or psychiatric condition, relationship problems, or medication effects. It is not indicated for HSDD in postmenopausal women or in men, and it is not intended to enhance sexual performance. No boxed warning is listed for this medication.

What the Evidence Shows

Ten clinical trials involving bremelanotide are registered, spanning different areas of investigation. A completed Phase 2 study examined bremelanotide in premenopausal women with female sexual arousal disorder and hypoactive sexual desire disorder. Another completed Phase 2 trial evaluated its safety and efficacy specifically in women with female sexual arousal disorder.

Reported Side Effects

Adverse event reports submitted to FDA's system show nausea as by far the most common reaction, followed by headache, vomiting, and flushing. These are counts of submitted reports, not confirmed rates of incidence, and they do not establish that the drug caused each event. Some reports also cited drug ineffectiveness or off-label use rather than a physical symptom.