Source: FDA label
| Molecular formula | C50H68N14O10 |
|---|---|
| Molecular weight | 1025.2 g/mol |
| Registered trials | 10 |
| PubChem CID | 9941379 |
| Brand names | Vyleesi |
Mechanism of Action
12.1 Mechanism of Action Bremelanotide is a melanocortin receptor (MCR) agonist that nonselectively activates several receptor subtypes with the following order of potency: MC1R, MC4R, MC3R, MC5R, MC2R. At therapeutic dose levels, binding to MC1R and MC4R is most relevant. Neurons expressing MC4R are present in many areas of the central nervous system (CNS). The mechanism by which VYLEESI improves HSDD in women is unknown. The MC1R is expressed on melanocytes; binding at this receptor leads to m
Key takeaways
- Bremelanotide is FDA-approved under the brand name Vyleesi for acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women.
- It works by activating melanocortin receptors in the brain, though the exact way this improves desire is not fully understood.
- It is not approved for postmenopausal women, men, or for enhancing sexual performance.
- Ten registered trials have studied bremelanotide, including completed Phase 2 work in sexual arousal and desire disorders.
- Nausea is by far the most reported side effect, followed by 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. At the doses used in treatment, its effects are most tied to two receptor subtypes, MC1R and MC4R. Neurons carrying MC4R are widespread in the brain, and this receptor is believed to play the larger role in how the drug affects sexual desire, although the label states the precise mechanism behind its effect on HSDD is unknown.
What Bremelanotide Is Approved For
Bremelanotide is approved, under the brand name Vyleesi, for premenopausal women with acquired, generalized hypoactive sexual desire disorder. This condition involves low sexual desire that causes real distress or relationship difficulty, and it must not be explained by another medical or psychiatric condition, a relationship problem, or a medication side effect. "Acquired" means the low desire developed after a period of normal sexual desire, and "generalized" means it happens regardless of the partner or situation. The label is explicit that Vyleesi is not indicated for HSDD in postmenopausal women or in men, and it is not intended to enhance sexual performance.
What The Evidence Shows
Bremelanotide has been studied across 10 registered clinical trials. A completed Phase 2 trial evaluated its safety and efficacy in women with female sexual arousal disorder, and a separate completed Phase 2 study examined its effects in premenopausal women with arousal disorder and, or hypoactive sexual desire disorder. The compound has also been explored outside its approved indication, including a completed Phase 2 study in diabetic kidney disease.
Reported Side Effects
Reported side effect data reflect counts of adverse event reports submitted to a surveillance database, not confirmed rates of incidence or proof that the drug caused the reaction. The most frequently reported reaction by far is nausea, followed at a distance by reports of the drug being ineffective, headache, and vomiting. Flushing and general reports of illness or adverse drug reaction also appear, along with a smaller number of reports describing off label use.
FAQ
What is bremelanotide used for?
Bremelanotide, sold as Vyleesi, is approved to treat acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. It is meant for low sexual desire causing distress that is not explained by another medical condition, relationship issue, or medication effect. It is not approved for postmenopausal women, men, or for improving sexual performance generally.
How does bremelanotide work?
Bremelanotide activates melanocortin receptors found throughout the central nervous system, most notably MC1R and MC4R at typical doses. MC4R is present on neurons in many brain regions and is thought to be most relevant to its effect on desire. The exact mechanism by which this improves HSDD symptoms has not been established.
What are the most common side effects of bremelanotide?
The most frequently reported side effect is nausea, followed by headache, vomiting, and flushing. These figures come from adverse event report counts, which reflect how often a reaction was reported rather than a confirmed rate or proof the drug caused it. Reports of the drug being ineffective and general illness have also been logged.
Has bremelanotide been studied for other conditions?
Yes. Beyond its approved use in HSDD, bremelanotide has been studied in a completed Phase 2 trial for diabetic kidney disease and in earlier trials for female sexual arousal disorder. In total, it has been evaluated across 10 registered clinical trials.
Is bremelanotide approved for men or postmenopausal women?
No. The approved label for Vyleesi specifically limits its use to premenopausal women with acquired, generalized HSDD. It is not indicated for postmenopausal women, for men, or as a general enhancer of sexual performance.
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Sources: DailyMed label (Vyleesi) ClinicalTrials.gov FAERS adverse event reports PubChem
Updated 2026-08-03