PT-141 (Bremelanotide)
approvedAlso known as: Bremelanotide, Vyleesi
**Mechanism of Action** PT-141 (bremelanotide) is a synthetic cyclic heptapeptide analog of α-melanocyte-stimulating hormone (α-MSH) that acts as a selective agonist at melanocortin receptors, primarily MC4R and, to a lesser extent, MC1R and MC3R. Its central mechanism involves activation of MC4R in the hypothalamus and limbic system, modulating dopaminergic and oxytocinergic pathways to enhance sexual arousal and desire without directly affecting peripheral vascular or hormonal systems. This distinguishes it from PDE5 inhibitors, as it does not rely on nitric oxide-mediated vasodilation. **Key Research Findings** Approved by the FDA in 2019 (Vyleesi) for premenopausal hypoactive sexual desire disorder (HSDD), bremelanotide demonstrated significant improvements in sexual desire and distress in two Phase III trials (RECONNECT studies). A 2020 meta-analysis of 1,267 women reported a 1.2-point increase in desire scores (Female Sexual Function Index) and a 30% reduction in distress vs. placebo. Common adverse effects include nausea (40%), flushing (20%), and transient blood pressure elevations. Notably, it shows no abuse liability and is administered subcutaneously 45 minutes before anticipated sexual activity. **Clinical Relevance** As the only FDA-approved centrally acting agent for HSDD, bremelanotide addresses an unmet need in women with acquired, generalized low sexual desire. Its rapid onset and on-demand dosing profile offer an alternative to daily flibanserin. Contraindications include uncontrolled hypertension and cardiovascular disease due to pressor effects. Ongoing research explores its utility in male sexual dysfunction (e.g., erectile dysfunction, anorgasmia) and neuropsychiatric conditions. For research purposes only — not medical advice.
Key data
C50H68N14O10Research & studies
Mindfulness-based CBT significantly improved total FSFI and subscales of desire, arousal, and orgasm.; Flibanserin improved total FSFI and desire, while bremelanotide improved total FSFI and desire and arousal subscales.; All three treatments (CBT, flibanserin, bremelanotide) reduced sexual distress.; No studies directly compared CBT to pharmacotherapy, and conclusions on other treatments were limited by study heterogeneity.
Biodegradable polymers were used to fabricate suction patches via a scalable mold casting process, with degradation confirmed in aqueous medium and simulated waste.; Ex vivo porcine buccal tissue testing showed enhanced permeation of a poorly permeable dye when combined with a chemical permeation enhancer.; In beagle dogs, the patch achieved substantially improved semaglutide bioavailability compared to a commercial tablet with only 10 minutes of application.; The patch achieved 26% relative bioavailability for bremelanotide compared to subcutaneous administration.
FDA-approved medications for HSDD include flibanserin and bremelanotide.; Investigational therapies include Lorexys and testosterone combinations.; The review provides guidance on diagnosis, patient selection, and side effect management.; Clinical strategies aim to improve treatment outcomes and patient satisfaction.
Continuous efficacy outcomes (FSFI, FSFI-D, FSDS-DAO, FSDS-DAO #13) have questionable validity evidence for women with HSDD.; No validity evidence was found for previously published categorical treatment response outcomes from the RECONNECT trials.; Effect sizes on 8 previously unpublished outcomes ranged from nil to small.; Nearly all modest apparent benefits were likely derived from post-hoc outcomes.
Bremelanotide is a melanocortin receptor agonist hypothesized to trigger excitatory brain pathways for sexual desire.; Most common adverse reaction is nausea (40%); overall safety and tolerability are moderate.; Clinical trials showed significant changes in validated questionnaires, but overall clinical benefit is modest.; Results are limited by high placebo effects and outcome measures susceptible to expectation biases.
Up to 45% of individuals assigned female at birth report sexual problems.; Pharmacologic options include local estrogen and testosterone for postmenopausal individuals and centrally-acting therapies for premenopausal individuals.; FDA-approved and off-label therapies have strengthened safety data from recent publications and systematic reviews.; Treatments like flibanserin, bremelanotide, and testosterone can safely improve sexual desire and satisfaction.
Frequently asked questions
What is PT-141 (Bremelanotide)?
**Mechanism of Action** PT-141 (bremelanotide) is a synthetic cyclic heptapeptide analog of α-melanocyte-stimulating hormone (α-MSH) that acts as a selective agonist at melanocortin receptors, primarily MC4R and, to a lesser extent, MC1R and MC3R. Its central mechanism involves activation of MC4R in the hypothalamus an
How does PT-141 (Bremelanotide) work?
Melanocortin MC4R agonist approved for hypoactive sexual desire disorder; acts centrally to increase sexual arousal.
What is the research status of PT-141 (Bremelanotide)?
PT-141 (Bremelanotide) is currently classified as approved, with 94 research references on record. This is for research purposes only and is not medical advice.
What is the molecular weight of PT-141 (Bremelanotide)?
PT-141 (Bremelanotide) has a molecular weight of approximately 1025.2 g/mol (formula C50H68N14O10).
Related peptides
KISS1R agonist decapeptide that triggers hypothalamic GnRH release, upstream regulator of reproductive hormone axis.
Non-selective melanocortin receptor agonist that stimulates melanogenesis (tanning) and increases libido via MC1R/MC4R.
Selective MC1R agonist approved (Scenesse) to prevent phototoxicity in erythropoietic protoporphyria by stimulating eumelanin.
Build on PT-141 (Bremelanotide) data programmatically
Structured peptide data, semantic search, and AI summaries via one API.
Get a free API key