PT-141
FDA-approved Bremelanotide (Vyleesi 2019) — acts via central nervous system melanocortin pathways.
Mechanism of Action
Bioregulator compound with targeted biochemical activity.
Evidence Chain
PT-141
COMPOUND
1 Research Goal
• Skin & Cosmetic
Evidence Strength
2 articles sourced
Knowledge Graph
(3 connections)Research Evidence
(2)Melanotan II: α-MSH Analog Pharmacology, Clinical History, and Safety Profile
Melanotan II is a synthetic analog of α-melanocyte-stimulating hormone investigated in early-phase clinical trials for tanning and sexual dysfunction. This review summarizes its clinical evidence and notable safety concerns.
PT-141 / Bremelanotide: Melanocortin Agonist for Hypoactive Sexual Desire Disorder — Regulatory and Clinical Evidence
PT-141, developed as bremelanotide, is a melanocortin receptor agonist FDA-approved (Vyleesi) for premenopausal women with hypoactive sexual desire disorder. This review summarizes the registrational clinical evidence.
Overview
PT-141 (Bremelanotide) is a synthetic peptide analog of alpha-melanocyte-stimulating hormone (alpha-MSH) that acts on the central nervous system to influence sexual arousal. Approved by the FDA in 2019 under the brand name Vyleesi for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD), PT-141 represents a novel CNS-acting approach to sexual dysfunction — distinct from peripheral-acting medications like sildenafil.
Mechanism of Action
PT-141 acts as an agonist at melanocortin receptors, particularly MC4R, in the central nervous system. Unlike sildenafil and other PDE5 inhibitors that act on peripheral vascular mechanisms, PT-141 acts on the central nervous system pathways that regulate sexual desire and arousal. The MC4R activation in the hypothalamus and other brain regions influences the neural circuits controlling sexual behavior and arousal. This central mechanism makes PT-141 effective for desire-based sexual dysfunction, which is not addressed by peripheral-acting medications.
Research Highlights
Clinical trials demonstrated PT-141's efficacy in improving sexual desire and reducing distress associated with HSDD in premenopausal women. The RECONNECT trials showed significant improvements in desire scores and satisfying sexual events. Research explored its potential in both female and male sexual dysfunction, with studies in erectile dysfunction showing efficacy in patients who did not respond to sildenafil. The central mechanism of action represents a paradigm shift in sexual dysfunction treatment, addressing desire rather than just physical response.
Dosage & Administration
FDA-approved dosing is 1.75 mg administered via subcutaneous injection in the abdomen or thigh at least 45 minutes before anticipated sexual activity. Maximum frequency is one dose per day and no more than eight doses per month. For research use only (RUO) — this information is provided for educational purposes only.
Safety Profile
Common side effects include nausea (40% of patients), flushing, injection site reactions, and headache. Contraindicated in patients with uncontrolled hypertension or cardiovascular disease due to transient blood pressure increases. Not recommended for use with nitrates. Does not cause priapism in clinical trials. The high rate of nausea is the primary tolerability concern.
References
Kingsberg SA, et al. Bremelanotide for HSDD (RECONNECT). Obstet Gynecol. 2019. Clayton AH, et al. Bremelanotide efficacy. J Sex Med. 2018. FDA Vyleesi prescribing information. All content is for educational and research purposes only.
Related Compounds
Synergy & Compatibility
(5)Computational assessment of bio-regulatory compatibility with compounds sharing research goals. Scores reflect half-life alignment, receptor target overlap, and bioavailability data.
Highest Compatibility
PT-141 + Dutasteride
Moderate Compatibility
Shared targets: mc3r, mc4r
Computational assessment based on available pharmacology data. Does not account for individual variability, dose-dependent effects, or unstudied interactions. For research use only.
Community Observations
(0)Qualitative, self-reported researcher observations. Distinct from peer-reviewed evidence — not medical advice.
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For research use only. Not medical advice.