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Melanocortin receptor agonist; synthetic cyclic analog of alpha-melanocyte-stimulating hormone (alpha-MSH)

PT-141 (Bremelanotide)

Approvedaka Bremelanotide, Vyleesi, PT-141

Bremelanotide is a synthetic cyclic analog of alpha-MSH that non-selectively activates melanocortin receptors. FDA approval rested on the two phase-3 RECONNECT randomized, double-blind, placebo-controlled trials; commonly reported adverse effects include nausea, flushing, injection-site reactions and headache, and it can cause transient increases in blood pressure.

Mechanism

Bremelanotide is a non-selective agonist of melanocortin receptors (MC1R-MC5R, with the exception of MC2R), acting principally at MC4R (and MC3R) within the central nervous system. Per the FDA prescribing information, the precise mechanism by which it improves sexual desire and reduces distress in HSDD is unknown.

Regulatory Status by Region

  • United States (FDA)Approved June 21, 2019 as Vyleesi (bremelanotide) for acquired, generalized HSDD in premenopausal women; prescription medicine.
  • Australia (TGA)Not registered on the ARTG; no approved bremelanotide/Vyleesi product in Australia. Compounded or imported PT-141 is unapproved.
  • European Union (EMA)No EMA marketing authorisation; not an approved medicine in the EU (European commercialisation rights licensed to Gedeon Richter were terminated in 2016 and no EU approval followed).
  • WADANot specifically named on the WADA Prohibited List. As an approved medicine it is not captured by the S0 non-approved-substances clause, and it does not fall within a listed prohibited class; athletes should nonetheless verify current status.

Key Studies

  • Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials (RECONNECT) (Kingsberg SA, et al. Obstet Gynecol. 2019 Nov;134(5):899-908. PMID: 31599840.)
  • VYLEESI (bremelanotide injection) US Prescribing Information (FDA label) (FDA, 2019, application 210557.)
  • Prespecified and Integrated Subgroup Analyses from the RECONNECT Phase 3 Studies of Bremelanotide (J Womens Health / related, PMID: 35230162.)