Compound Overview
About the product
The sequence is Ac-Lys-Lys-Arg-Methyl-Trp-Gly-Trp-Pro-Val-NH₂, cyclized via a lactam bridge for receptor selectivity and metabolic stability. It includes N-terminal acetylation and C-terminal amidation to resist enzymatic degradation. No non-natural amino acids are present beyond these terminal modifications and the methylated tryptophan. Purity for clinical use exceeds 98 percent as confirmed by HPLC and mass spectrometry.
Bremelanotide acts as an agonist at the melanocortin-4 receptor (MC4R) in the central nervous system, modulating pathways that influence sexual desire and arousal. It does not activate the melanocortin-1 receptor, avoiding unwanted effects on skin pigmentation. Activation of MC4R leads to downstream signaling that enhances sexual motivation and response. Clinical pharmacology studies show central receptor engagement within an hour of subcutaneous administration.
The peptide is indicated for treatment of hypoactive sexual desire disorder in premenopausal women. In phase III trials, bremelanotide significantly increased satisfying sexual events and improved desire scores compared with placebo. Common benefits include enhanced sexual desire and reduced distress related to low sexual desire. Research is evaluating its use in other sexual-dysfunction populations.
The most frequently reported adverse events are nausea, flushing, headache, and injection-site reactions. Transient increases in blood pressure and reductions in heart rate have been observed; blood pressure should be monitored. It is contraindicated in patients with uncontrolled hypertension or cardiovascular disease. Safety data in pregnancy, lactation, and men are not available.
Bremelanotide is synthesized by Fmoc solid-phase peptide synthesis on a resin support, including on-resin cyclization to form its lactam bridge. After cleavage, the peptide is purified by preparative HPLC to > 98 percent purity. Mass spectrometry verifies molecular weight and sequence integrity. Manufacturing adheres to pharmaceutical-grade good manufacturing practices (GMP).
Bremelanotide (Vyleesi) is approved by the U.S. FDA for hypoactive sexual desire disorder and by comparable agencies in several other regions. It is available by prescription only and cannot be purchased over the counter. It is classified as a peptide therapeutic, subject to controlled manufacturing and distribution. No off-label cosmetic or non-sexual-health uses are authorized.
The recommended dose is 1.75 mg administered subcutaneously at least 45 minutes before anticipated sexual activity, with a maximum of eight doses per month. Each dose should be administered at least 24 hours apart. No loading doses are required. Dosing outside these parameters has not been studied.
Do follow the prescribed 1.75 mg subcutaneous dose and limit to eight doses per month.Do monitor blood pressure before and after administration.Don’t use if you have uncontrolled hypertension or cardiovascular disease.Don’t administer more frequently than once every 24 hours.
Q: How quickly does it work?A: Efficacy begins within about one hour of injection.Q: Can men use bremelanotide?A: No; it is approved only for premenopausal women.Q: Is daily use safe?A: No; dosing should not exceed once every 24 hours or eight times per month.
For research use only. Not approved for medical use.
