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Libido5 cited studies

PT-141

Bremelanotide — central-acting MC4 agonist for hypoactive sexual desire and arousal disorders.

Also known as: PT 141 · Bremelanotide
SummaryMechanismDosingSafetyStudies
Research use only — not for human consumption.

What it is

PT-141 (Bremelanotide) is a synthetic peptide developed for sexual dysfunction, particularly low libido in men and women. Unlike vascular agents such as PDE5 inhibitors, PT-141 acts centrally via melanocortin receptors in the brain that drive sexual arousal — making it relevant when traditional agents are unsuitable or ineffective.

Mechanism of action

Central nervous system melanocortin receptor agonist with MC4 selectivity. MC4 activation in the hypothalamus modulates dopaminergic and other arousal pathways, producing increased sexual desire and arousal independent of peripheral blood flow.

Half-life: ~2 hours — onset within 30–60 minutes.

Evidence summary

Bremelanotide was FDA-approved in 2019 (Vyleesi) for premenopausal HSDD on the strength of two Phase 3 trials. Earlier pharmacokinetic / pharmacodynamic and proof-of-concept work in ED and arousal disorder support central mechanism and efficacy.

Typical dosing protocols

Typical dose
500–2000 mcg
Frequency
2x per week
Cycle length
4 weeks
  • 1.75 mg subcutaneous, on-demand, ~45 minutes before activity
  • Maximum 1 dose / 24 hours, 8 doses / month
  • Trial cycle of 8 weeks; reassess if no benefit

Side effects & safety

  • Nausea (most common), flushing, headache
  • Transient blood-pressure increase / heart-rate decrease
  • Focal hyperpigmentation with frequent / chronic use
Contraindications
  • • Uncontrolled hypertension or known cardiovascular disease
  • • History of melanoma

Cited studies

  1. (2003). PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences.
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  2. (2004). Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction. International Journal of Impotence Research.
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  3. (2004). Evaluation of the safety, pharmacokinetics and pharmacodynamic effects of subcutaneously administered PT-141, a melanocortin receptor agonist, in healthy male subjects and in patients with an inadequate response to Viagra. International Journal of Impotence Research.
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  4. (2006). An Effect on the Subjective Sexual Response in Premenopausal Women with Sexual Arousal Disorder by Bremelanotide (PT-141), a Melanocortin Receptor Agonist. The Journal of Sexual Medicine.
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  5. Kingsberg SA, Clayton AH, Portman D, et al. (2019). Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials. Obstetrics & Gynecology.
    PMID 31599840Read source ↗
Disclaimer

All content is for research and educational purposes. Peptides described are sold for laboratory research use only and are not intended to diagnose, treat, cure, or prevent any disease. Always consult a qualified healthcare professional before beginning any protocol.