R2 Medical Clinic

PT-141 (Bremelanotide)

What Is PT-141?

PT-141, also known as Bremelanotide, is a synthetic cyclic heptapeptide and melanocortin receptor agonist originally developed from the peptide melanotan II. Unlike medications such as sildenafil or tadalafil, which improve genital blood flow through vascular mechanisms, PT-141 works primarily within the central nervous system by activating melanocortin receptors involved in sexual desire and arousal.

PT-141 (Bremelanotide) — a cyclic melanocortin peptide (C₅₀H₆₈N₁₄O₁₀).

The FDA-approved form of bremelanotide is marketed as Vyleesi® and is approved only for acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women.

Mechanism of Action

PT-141 primarily activates melanocortin-4 receptors (MC4R) and, to a lesser extent, melanocortin-3 receptors (MC3R) in the brain.

This may result in:

  • Increased sexual desire
  • Increased sexual arousal
  • Modulation of dopamine-mediated reward pathways
  • Central nervous system stimulation of sexual motivation
  • Sexual effects independent of direct genital blood-flow mechanisms

Potential Benefits

Potential benefits may include:

  • Increased sexual desire
  • Improved sexual arousal
  • Reduced distress related to low sexual desire
  • Improved sexual satisfaction in selected patients
  • Possible benefit in male sexual dysfunction, though this remains investigational

Risks & Side Effects

Potential side effects include:

  • Nausea
  • Vomiting
  • Flushing
  • Headache
  • Injection-site reactions
  • Fatigue
  • Dizziness
  • Nasal congestion
  • Hyperpigmentation with repeated use
  • Temporary increases in blood pressure
  • Decreased heart rate
  • Abdominal discomfort

Contraindications

PT-141 should generally be avoided in individuals with:

  • Uncontrolled hypertension
  • Known cardiovascular disease
  • Pregnancy
  • Known hypersensitivity to bremelanotide
  • Severe hepatic impairment
  • Severe renal impairment

Caution is also appropriate in patients taking oral medications that require rapid absorption because bremelanotide may delay gastric emptying.

FDA Approval Status

Bremelanotide/Vyleesi® is FDA-approved for:

  • Acquired, generalized HSDD in premenopausal women

It is not FDA-approved for:

  • Erectile dysfunction
  • Male sexual dysfunction
  • Testosterone deficiency
  • Hormone optimization
  • Athletic performance
  • Bodybuilding
  • Anti-aging
  • Weight loss
  • General sexual enhancement

Human & Animal Studies

Human Studies

PT-141 has been studied in humans for female hypoactive sexual desire disorder, female sexual arousal disorder, erectile dysfunction, and sexual arousal physiology.

Two large Phase III randomized trials demonstrated improvements in sexual desire and reductions in distress in premenopausal women with acquired, generalized HSDD, leading to FDA approval of Vyleesi®.

Animal & Preclinical Studies

Animal studies have shown that PT-141 may:

  • Activate melanocortin receptors in the brain
  • Increase sexual motivation
  • Facilitate sexual behavior
  • Influence dopamine signaling
  • Affect appetite regulation
  • Modulate autonomic nervous system activity

Published Studies

  1. Kingsberg SA, et al. Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase III Trials
    https://pubmed.ncbi.nlm.nih.gov/31599840/
  2. Bremelanotide for Female Hypoactive Sexual Desire Disorder: Review of Clinical Development
    https://pmc.ncbi.nlm.nih.gov/articles/PMC8788464/
  3. New Drug Approved for Treating Hypoactive Sexual Desire Disorder in Premenopausal Women
    https://pubmed.ncbi.nlm.nih.gov/31893927/
  4. ClinicalTrials.gov – Bremelanotide Clinical Studies
    https://clinicaltrials.gov/search?term=bremelanotide

The information provided on this page is intended for educational and informational purposes only and should not be considered medical advice, diagnosis, or treatment.

This content was generated with the assistance of artificial intelligence (AI) and should be reviewed by a qualified medical professional before publication or clinical use. AI-generated medical content may contain errors, omissions, outdated information, or incomplete interpretations of the available scientific literature.

PT-141/bremelanotide is FDA-approved only as Vyleesi® for acquired, generalized HSDD in premenopausal women. Other uses are not FDA-approved. Individual results vary, and no specific outcome or benefit can be guaranteed.

R2 Medical Clinic uses medications sourced from compounding pharmacies. Compounded medications are not approved by the U.S. Food and Drug Administration (FDA). Unlike FDA-approved medications, compounded drugs have not undergone FDA review for safety, effectiveness, or efficacy through the FDA drug approval process. While 503B outsourcing facilities are registered with and inspected by the FDA and must comply with Current Good Manufacturing Practice (CGMP) requirements, the compounded medications they produce are not individually approved by the FDA. Similarly, compounded medications prepared by 503A pharmacies are not FDA-approved and are primarily regulated by state boards of pharmacy, with FDA oversight under applicable federal law.

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