CEDAR

Scientific Reference

PT-141 (Bremelanotide)

Evidence profile: Human Phase 3 evidence

PT-141 (Bremelanotide) is an FDA-approved synthetic peptide that acts as a melanocortin receptor agonist, specifically targeting MC3R and MC4R receptors in the central nervous system. Unlike traditional erectile dysfunction medications that work through vascular mechanisms, PT-141 directly influences sexual arousal pathways in the brain, making it effective for both male and female sexual dysfunction. Approved as Vyleesi for hypoactive sexual desire disorder (HSDD) in premenopausal women, PT-141 has also demonstrated efficacy in men with erectile dysfunction including those unresponsive to PDE5 inhibitors. Its central mechanism of action represents a fundamentally different therapeutic approach compared to sildenafil and related compounds.

Mechanism of Action

PT-141 activates melanocortin receptors (MC3R and MC4R) in the central nervous system, triggering sexual arousal pathways independent of vascular or hormonal mechanisms. Research confirmed selective binding to these receptors activates neural pathways involved in sexual desire and arousal without peripheral vasodilation. This central mechanism accounts for its efficacy across both male and female sexual dysfunction conditions.

Molecular Information

  • Type: Melanocortin receptor agonist (cyclic heptapeptide)
  • Length: 7 amino acids
  • Molecular weight: 1025.2 g/mol
  • Molecular formula: C50H68N14O10
  • CAS: 189691-06-3

Published Research

  • RECONNECT (Studies 301 and 302)

    Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials

    Kingsberg SA et al. · Obstetrics and gynecology · 2019 · Clinical

    PMID 31599840 — View on PubMed

  • Safety Profile of Bremelanotide Across the Clinical Development Program

    Clayton AH et al. · Journal of women's health (2002) · 2022 · Clinical

    PMID 35147466 — View on PubMed

  • Prespecified and Integrated Subgroup Analyses from the RECONNECT Phase 3 Studies of Bremelanotide

    Simon JA et al. · Journal of women's health (2002) · 2022 · Clinical

    PMID 35230162 — View on PubMed

  • The Patient Experience of Premenopausal Women Treated with Bremelanotide for Hypoactive Sexual Desire Disorder: RECONNECT Exit Study Results

    Koochaki P et al. · Journal of women's health (2002) · 2021 · Clinical

    PMID 33538638 — View on PubMed

  • Phase I Randomized Placebo-controlled, Double-blind Study of the Safety and Tolerability of Bremelanotide Coadministered With Ethanol in Healthy Male and Female Participants

    Clayton AH et al. · Clinical therapeutics · 2017 · Clinical

    PMID 28189361 — View on PubMed

  • Usefulness of ambulatory blood pressure monitoring to assess the melanocortin receptor agonist bremelanotide

    White WB et al. · Journal of hypertension · 2017 · Clinical

    PMID 27977473 — View on PubMed