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
Many premenopausal women with persistently low sexual desire want to know whether a medication can help, and what taking one might involve. Bremelanotide is one option specifically studied and approved for this concern.
Key takeaways
- Bremelanotide is 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 central nervous system, though the exact way this improves desire is not fully understood.
- It is not approved for postmenopausal women, for men, or for enhancing sexual performance.
- Across 10 registered trials, studies have examined bremelanotide alone and, more recently, in combination with other therapies.
- The most commonly reported reactions involve nausea, headache, and vomiting, based on FAERS reports rather than confirmed causation rates.
What Bremelanotide Is
Bremelanotide is a melanocortin receptor agonist, meaning it activates a family of receptors found throughout the central nervous system. It nonselectively engages several receptor subtypes, with MC1R and MC4R considered most relevant at the doses used in treatment. Neurons expressing MC4R are distributed across many brain regions, but the label states that the precise mechanism by which this activation improves HSDD symptoms is unknown.
What Bremelanotide Is Approved For
Vyleesi is indicated for acquired, generalized HSDD in premenopausal women, marked by low sexual desire causing notable distress or relationship difficulty. To qualify, this low desire must not stem from a coexisting medical or psychiatric condition, relationship problems, or the effects of another medication. "Acquired" means the change developed after a period of normal desire, and "generalized" means it occurs regardless of partner or situation. The label specifically excludes use in postmenopausal women, in men, or for enhancing sexual performance generally. No boxed warning is associated with this medication.
What the Evidence Shows
Bremelanotide has been studied across 10 registered clinical trials. A completed Phase 3 study evaluated its efficacy and safety in premenopausal women with HSDD, supporting its approved use. A completed Phase 4 trial further examined the role of the melanocortin-4 receptor in HSDD, while a separate, currently active Phase 2 study is investigating bremelanotide co-administered with tirzepatide for obesity, an application outside its approved indication.
Reported Side Effects
FAERS reports for bremelanotide are dominated by gastrointestinal and general reactions, led by nausea (432 reports), followed by headache (148) and vomiting (115). Flushing and general reports of illness or adverse drug reaction each appeared with lower frequency. A notable share of reports involved "drug ineffective" (202) or off label use (94), reflecting how the product is being used in practice rather than confirmed side effects. These figures represent counts of submitted reports, not confirmed incidence rates or established causation.
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 intended for low sexual desire that causes marked distress and is not explained by another medical condition, a relationship issue, or a medication's effects. It is not approved for postmenopausal women, men, or for enhancing sexual performance.
How does bremelanotide work?
Bremelanotide activates melanocortin receptors, a group of receptors found throughout the central nervous system, with the strongest relevant activity at MC1R and MC4R. Neurons carrying MC4R are present in many brain areas involved in regulating behavior. The label notes that the exact mechanism behind its effect on sexual desire is not fully understood.
Is bremelanotide the same as PT-141?
Bremelanotide is often referred to by its research name in scientific literature, but its FDA-approved form is marketed under the brand name Vyleesi. The approved product is indicated specifically for HSDD in premenopausal women under that labeling.
What are the most common side effects of bremelanotide?
The most frequently reported reactions in FAERS data are nausea, headache, and vomiting, with flushing also reported. These numbers reflect counts of submitted adverse event reports, not confirmed rates of occurrence or proof that the drug caused each reaction.
Is bremelanotide being studied for other uses?
Yes, beyond its approved HSDD indication, an active Phase 2 trial is evaluating bremelanotide combined with tirzepatide for obesity. This and other ongoing research fall outside the drug's current FDA-approved use.
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Content is editorial information, not medical advice. Talk to your doctor before any treatment decision.
Sources: FDA label (DailyMed) ClinicalTrials.gov FDA Adverse Event Reporting System (FAERS) PubChem CID 9941379
Updated 2026-09-26