PT-141 (Bremelanotide)

approved

Also 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

Category
Sexual Health
Molecular weight
1025.2 g/mol
Molecular formula
C50H68N14O10
CAS number
189691-06-3
Administration
subcutaneous, intranasal
Research status
approved
References
95
Tags
melanocortin, libido, approved

Research & studies

Therapeutic peptides in gerontology: mechanisms and applications for healthy aging
Frontiers in aging · 2026 · PubMed

Nine peptides were identified targeting diverse aging mechanisms including metabolic restoration, telomere biology, tissue repair, and neuroprotection.; FDA-approved peptides demonstrated robust safety profiles from large-scale trials, whereas non-approved peptides lack long-term safety data.; Significant knowledge gaps exist in optimal dosing regimens, combination therapy effects, and biomarkers for monitoring efficacy.

Female Sexual Desire, Arousal, and Orgasmic Dysfunctions: A Systematic Review and Meta-Analysis of Treatment Options
Journal of minimally invasive gynecology · 2026 · PubMed

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.

Polymorphism of Melanocortin Receptor Genes-Association with Inflammatory Traits and Diseases
Diseases (Basel, Switzerland) · 2025 · PubMed

MCRs regulate diverse functions including pigmentation, appetite, stress response, steroid synthesis, energy balance, and immunomodulation, with tissue distribution in brain, limbic system, adrenal cortex, neutrophils, monocytes, and macrophages.; Mutations in MC1R, MC2R, MC3R, and MC4R are associated with melanoma, familial glucocorticoid deficiency, obesity, and type 2 diabetes mellitus, respectively; MC1R, MC2R, and MC5R are linked to major depressive disorder risk.; MCRs are involved in inflammatory disorders such as atopic dermatitis, autoimmune uveitis, sarcoidosis, respiratory diseases, multiple sclerosis, scleroderma, inflammatory bowel disease, amyotrophic lateral sclerosis, Alzheimer's disease, arthritis, and reperfusion injury.; FDA-approved MCR-related therapies include repository corticotropin injection for sarcoidosis, Bremelanotide for hypoactive sexual desire disorder, Afamelanotide for erythropoietic protoporphyria, and Setmelanotide for obesity due to pro-opiomelanocortin and leptin receptor deficiency.

A biodegradable suction patch for sustainable transbuccal peptide delivery
Journal of controlled release : official journal of the Controlled Release Society · 2025 · PubMed

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.

2024 SOGC, 2024 NCCN, 2022 ESO-ESMO, and 2018 ASCO: a comparison of female cancer survivorship guidelines for the management of sexual health concerns
Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2025 · PubMed

All guidelines strongly recommend non-hormonal therapies (lubricants or moisturizers) as first-line for vaginal dryness, with low-dose estrogen as second-line if unsuccessful.; Multidisciplinary care including psychosocial and relationship counselling, specialist referrals, and cognitive behavioral therapy is recommended by all guidelines for psychological concerns.; ASCO, NCCN, and SOGC recommend vaginal dilators and pelvic physical therapy for pain; ASCO recommends any kind of stimulation for sexual response, while NCCN and SOGC recommend sexual aids (e.g., vibrators) for arousal.; All guidelines except ESO-ESMO include recommendations for androgens, bupropion, flibanserin, bremelanotide, and buspirone for low sex drive, but evidence is limited.

Novel Pharmacologic Treatments of Female Sexual Dysfunction
Clinical obstetrics and gynecology · 2025 · PubMed

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.

Bremelanotide
2025 · PubMed
Small Effects, Questionable Outcomes: Bremelanotide for Hypoactive Sexual Desire Disorder
Journal of sex research · 2024 · PubMed

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.

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 95 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

Build on PT-141 (Bremelanotide) data programmatically

Structured peptide data, semantic search, and AI summaries via one API.

Get a free API key