Evidence Grade C — Moderate human evidence. 21 published studies, 18 human. 0 registered clinical trials.
Medically reviewed by a licensed medical professional
PT-141 is the research designation for bremelanotide, which is sold as the prescription medication Vyleesi for low sexual desire in premenopausal women. This entry covers its unregulated use beyond the prescribed indication. Self-administration outside of medical supervision bypasses the blood pressure monitoring and dosing limits built into the approved product.
PT-141 is also known by these brand and alternate names:
21 published studies: 18 human, 2 animal, 0 in-vitro, 6 reviews
PT-141 is the same molecule as bremelanotide, which is approved as Vyleesi (#40) exclusively for hypoactive sexual desire disorder in premenopausal women. Vyleesi is administered as a subcutaneous autoinjector under prescription.
PT-141 is available through unregulated channels for off-label purposes. Self-administration outside of prescribed use bypasses the medical evaluation that the approved product requires. The approved prescribing information includes a blood pressure monitoring requirement and limits use to one dose per 24 hours due to transient blood pressure increases. Products from unregulated sources lack pharmaceutical quality assurance and the dosing controls built into the approved delivery system.
PT-141 activates the MC4R melanocortin receptor in the hypothalamus, modulating dopaminergic pathways involved in sexual desire and arousal. This central brain mechanism is fundamentally different from PDE5 inhibitors (such as sildenafil), which act on blood vessels. The mechanism is established from the approved product's regulatory dossier.
Research suggests two large Phase III trials (1,267 participants total) established bremelanotide's efficacy for the approved indication (HSDD in premenopausal women), though effect sizes are modest. Small-scale off-label use data in men suggest effects on erectile function and desire, but no Phase III male data exist. The approved prescribing information includes dosing limits (one dose per 24 hours, eight per month) and blood pressure monitoring requirements. Unregulated use bypasses these safeguards. Nausea affects 40% of users. Potential skin darkening with repeated use may be permanent. Products from unregulated sources lack the dosing controls and quality assurance of the approved autoinjector.
PeptideTrace tracks 0 registered clinical trials for PT-141 sourced from ClinicalTrials.gov.
No trials registered on ClinicalTrials.gov for this compound.
FDA ORIG 1
FDA SUPPL 2
PT-141 (bremelanotide) is a cyclic heptapeptide melanocortin agonist, an active metabolite of Melanotan II differing by having a free carboxylic acid (-OH) at the C-terminus rather than an amide (-NH2). Sequence: Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-OH. Molecular weight: 1,025.2 Da. CAS: 189691-06-3. Molecular formula: C50H68N14O10. Half-life: 2.7 hours (range 1.9-4.0). Tmax approximately 1.0 hour. Brand name: Vyleesi (Palatin Technologies / AMAG Pharmaceuticals). FDA approved June 21, 2019 for hypoactive sexual desire disorder (HSDD) in premenopausal women. Dosing: 1.75 mg SC, at least 45 min before anticipated activity; max 1 dose/24h, 8 doses/month. Listed here as research_compound for grey-market context where it is used off-label.
Research suggests bremelanotide acts centrally in the brain through MC4R activation in the hypothalamus (particularly the medial preoptic area), modulating dopaminergic pathways involved in sexual desire and arousal. This is fundamentally different from PDE5 inhibitors, which act peripherally on the nitric oxide/cGMP vascular pathway. fMRI studies research suggests show improved connectivity between the amygdala and insula during visual sexual stimulation. MC1R binding accounts for the skin hyperpigmentation side effect. The FDA labeling states the exact mechanism by which it improves HSDD is unknown.
RECONNECT pivotal trials (Phase 3, two identical RCTs; total N=1,267): Co-primary endpoints were met. FSFI-Desire domain treatment difference: Study 301 +0.30 (P<0.001), Study 302 +0.42 (P<0.001), integrated +0.35 (P<0.0001). FSDS-DAO distress: integrated -0.33 (P<0.0001). Cohen's d effect sizes were 0.39 (desire) and 0.27 (distress). Responder rate approximately 25% vs 17% placebo. Male ED (Safarinejad 2008; N=342 sildenafil non-responders): 33.5% positive response vs 8.5% placebo (P=0.03) with intranasal PT-141. Safety: Nausea in 40.0% of patients, flushing 20.3%, injection site reactions 13.2%, headache 11.3%. Transient BP increases of approximately 6 mmHg systolic and 3 mmHg diastolic. Skin hyperpigmentation may occur with >8 doses/month and may not resolve. Contraindicated in uncontrolled hypertension or cardiovascular disease.
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This content is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before making decisions about your health.
