Bremelanotide

Bremelanotide is a synthetic cyclic heptapeptide melanocortin receptor agonist approved in the United States (Vyleesi) for on-demand treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. It is not approved for men, postmenopausal women, or sexual performance enhancement. The non-proprietary name bremelanotide is distinct from the unapproved research peptide melanotan II; the two differ at the C-terminus (carboxylate vs. amide) and in receptor-selectivity profile.

Bremelanotide has no current EMA, MHRA, Health Canada, or TGA marketing authorisation as of August 2026. A phase 2/3 study for HSDD was conducted but no application was submitted in the EU.

Melanocortin receptor agonist with selectivity for MC3R and MC4R over MC1R and MC2R. Activates central melanocortin pathways involved in sexual desire and arousal. Residual MC1R agonism accounts for melanogenic effects (hyperpigmentation). Subcutaneous absorption; peak plasma concentration at ~1 hour; elimination half-life ~2.7 hours. Slows gastric emptying, affecting absorption of co-administered oral drugs.

Approved labeled regimen

The label summary below is product-, indication-, and jurisdiction-specific; consult the full current label and a licensed clinician/pharmacist.

• Product: Vyleesi (bremelanotide injection) 1.75 mg/0.3 mL

• Route: Subcutaneous injection via autoinjector (abdomen or thigh)

• Dosing: 1.75 mg as needed, ≥45 min before anticipated sexual activity

• Maximum: 1 dose/24 hours; ≤8 doses/month

• Discontinue if no symptom improvement after 8 weeks

• Contraindicated in uncontrolled hypertension or known cardiovascular disease

Studied regimens (not recommendations)

• None beyond the approved regimen in registered clinical trials.

What is not established

No established or recommended human dose for men, postmenopausal women, sexual performance enhancement, or any indication other than HSDD.

Established label risks

• Transient blood pressure increase and heart rate decrease after each dose, resolving within ~12 hours; not recommended in patients at high cardiovascular risk.

• Nausea (40%), requiring anti-emetic therapy in 13%, leading to discontinuation in 8%.

• Focal hyperpigmentation (1%), including face, gingiva, breasts; higher risk with darker skin and daily dosing.

• Injection site reactions, flushing, headache, vomiting, cough, nasal congestion (incidence >2%).

• Drug interaction: May decrease systemic exposure of oral naltrexone; avoid co-administration with oral naltrexone-containing products.

Human-study signals

• Vasodilatory effects (flushing, hot flush).

Unknowns and product-quality risks

• Long-term cardiovascular safety and pigmentation outcomes not fully characterised.

• Not studied beyond 24 weeks in phase 3; open-label extension to 52 weeks only.

• Products sold online as "bremelanotide" or "PT-141" for research are unregulated and should not be assumed equivalent to Vyleesi.

• Oral drug absorption: May be reduced due to delayed gastric emptying.

• Naltrexone: Avoid with oral naltrexone.

• Pregnancy: Discontinue if pregnancy suspected; effective contraception advised.

• Renal/hepatic impairment: Not studied in moderate-to-severe impairment.

• US FDA: Prescription only (Vyleesi); no generic approved. NDA holder transferred from AMAG to Cosette Pharmaceuticals.

• Not scheduled under US Controlled Substances Act.

• WADA: Bremelanotide was not identified by exact name in the 2026 Prohibited List. Because it is an FDA-approved medicine, S0 does not apply on the basis of non-approval, and this review did not identify another matching class. Athletes should still verify the exact product and current status with their anti-doping organisation.

• Regulatory status: Not EMA/MHRA/Health Canada/TGA approved.

• Compounding: US federal compounding status depends on the source, facility type, prescription and applicable statutory conditions; this page does not establish that a particular preparation is lawful.

• Long-term safety beyond 1 year.

• Efficacy/safety in more diverse populations.

• Effects on sexual desire in women not in stable heterosexual relationships.

• Direct comparisons with other HSDD treatments.

• Mechanism of sustained benefit after discontinuation (if any).

• Databases and registries: DailyMed, Drugs@FDA, ClinicalTrials.gov, PubMed, EMA, WADA

• Search terms: bremelanotide, PT-141, Vyleesi, HSDD, melanocortin agonist

• Last searched: 2026-08-06

• Inclusion emphasis: FDA label, phase 3 RCTs, systematic reviews

1. Vyleesi Full Prescribing Information (Cosette Pharmaceuticals, revised 03/2024). https://vyleesi.com/docs/Vyleesi-Full-Prescribing-Information.pdf

2. DailyMed – VYLEESI (bremelanotide injection). https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f1d0c1b5-2f39-4bad-a6a4-0066e3ad5dcf

3. Kingsberg SA, et al. Bremelanotide for the treatment of hypoactive sexual desire disorder: two phase 3 trials (RECONNECT). J Sex Med. 2019;16(5):739-752. PMID 31003939.

4. ClinicalTrials.gov NCT02333071 and NCT02338960.

5. PubChem CID 9941379 (bremelanotide). https://pubchem.ncbi.nlm.nih.gov/compound/9941379

6. IUPHAR/BPS Guide to Pharmacology – bremelanotide ligand ID 10408. https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10408

7. WADA. 2026 Prohibited List. https://www.wada-ama.org/en/resources/world-anti-doping-program/prohibited-list