Bremelanotide

PT-141, Vyleesi

Grade A: Approved and proven

TL;DR: Bremelanotide (Vyleesi) is FDA-approved for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women, based on two Phase 3 randomized controlled trials enrolling approximately 1,200 women. In those trials, statistically significant improvements were observed in desire scores and distress scores compared to placebo, though effect sizes were modest and the clinical meaningfulness of those differences has been debated in peer-reviewed commentary. The drug is indicated for on-demand use rather than continuous daily administration. Evidence in men or for other sexual dysfunction diagnoses is not FDA-supported; compounded PT-141 sold for other purposes has not been evaluated for safety or efficacy by the FDA. No long-term outcome data beyond the pivotal trial period are available.

Key Takeaways

Grade A: Approved and proven
FDA approved: FDA-approved (2019) for acquired, generalized HSDD in premenopausal women; not approved for use in men or for any other indication.
Compounding: Bremelanotide is FDA-approved as Vyleesi (subcutaneous injection) for premenopausal women with HSDD only. Compounded PT-141 is not FDA-approved for any indication, including use in men. Because an FDA-approved version exists, compounding is subject to restrictions; compounded preparations for uses other than the approved indication lack FDA evaluation of safety, efficacy, or manufacturing quality.

Bremelanotide chemical structure — Structure via PubChem CID 9941379

Mechanism

Bremelanotide is a melanocortin receptor agonist, primarily acting at MC4R in the central nervous system to modulate neural pathways involved in sexual desire.

Evidence

Bremelanotide (Vyleesi) is FDA-approved for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women, based on two Phase 3 randomized controlled trials enrolling approximately 1,200 women. In those trials, statistically significant improvements were observed in desire scores and distress scores compared to placebo, though effect sizes were modest and the clinical meaningfulness of those differences has been debated in peer-reviewed commentary. The drug is indicated for on-demand use rather than continuous daily administration. Evidence in men or for other sexual dysfunction diagnoses is not FDA-supported; compounded PT-141 sold for other purposes has not been evaluated for safety or efficacy by the FDA. No long-term outcome data beyond the pivotal trial period are available.

Safety and risks

Nausea is the most clinically significant adverse effect, occurring in approximately 40% of patients, requiring anti-emetic therapy in 13%, and causing treatment discontinuation in 8%; it was most severe at first injection and diminished with subsequent doses. Flushing occurred in approximately 20% of trial participants. Bremelanotide causes transient blood pressure increases peaking 2-4 hours post-dose, and the FDA label contraindicates use in patients with uncontrolled hypertension or known cardiovascular disease. Injection site reactions and headache are also commonly reported. Rare cases of hepatotoxicity with marked aminotransferase elevations have been reported post-approval, and the LiverTox database classifies bremelanotide as a possible rare cause of liver injury. Local hyperpigmentation at the injection site has been observed with repeated use. Compounded PT-141 lacks FDA oversight for purity, potency, or sterility, and is not approved for use in men.

Interactions

Contraindicated with use in patients on antihypertensive therapy where blood pressure is not well controlled; caution warranted with other medications that affect blood pressure or cardiovascular function. Concomitant use of drugs that slow gastric emptying may alter absorption of oral medications taken around the time of injection.

Federal compounding status

FDA-approved drug as of 2026-06-02.

An FDA-approved drug that should be obtained as the licensed product. It is not a 503A bulk-substance candidate; compounding from bulk is limited under federal rules and generally permitted only during a declared shortage.

Federal status only, from public FDA records. State pharmacy-board rules vary and are not covered here. This is regulatory reporting, not legal advice. All compounds.

Compounding legality

Bremelanotide is FDA-approved as Vyleesi (subcutaneous injection) for premenopausal women with HSDD only. Compounded PT-141 is not FDA-approved for any indication, including use in men. Because an FDA-approved version exists, compounding is subject to restrictions; compounded preparations for uses other than the approved indication lack FDA evaluation of safety, efficacy, or manufacturing quality.

Sources

Bremelanotide is FDA approved. PeptideGrids presents evidence and regulatory status for informational purposes only. We do not sell, supply, source, or help anyone obtain this compound, and we provide no dosing or administration guidance. This is not medical advice; consult a licensed clinician. Full disclaimer.

Last reviewed June 1, 2026 by PeptideGrids editorial team (independently audited).