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OTHERFDA ApprovedSEXUAL HEALTHLIBIDOMELANOCORTIN

Bremelanotide

Also known as: PT-141 · Vyleesi · PL-6983

21 views/week 443 citations 0 edits Updated 6/8/2026

Bremelanotide (PT-141 / Vyleesi) is an FDA-approved melanocortin receptor agonist used for hypoactive sexual desire disorder (HSDD) in premenopausal women. Unlike PDE5 inhibitors, it works centrally via the brain to increase sexual desire rather than through vascular mechanisms.

STRUCTURE

Molecular Composition

FORMULA

C₅₀H₆₈N₁₄O₁₀

MOL. WEIGHT

1,025.2 Da

CAS NUMBER

189691-06-3

TARGET

MC3R / MC4R

HALF-LIFE

~2.7 hours

FDA STATUS

Approved (2019)

AMINO ACID CHAIN VISUALIZATION

Nle-1

Oxidation-resistant Nle

—

NH-CO

His-3

MC4R binding residue

—

NH-CO

D-Phe-4

D-amino acid potency boost

—

NH-CO

Arg-5

Receptor contact point

—

NH-CO

Trp-6

Hydrophobic MC receptor core

—

NH-CO

Lys-7

Cyclic backbone closure

SEQUENCEN-H-F-R-W-K

MECHANISMS

How It Works

🧠

Central MC4R Activation for Sexual Desire

Bremelanotide activates MC4R in the hypothalamus and limbic system, the same regions governing sexual motivation. Unlike PDE5 inhibitors (which act on penile/vaginal blood flow), it directly modulates the CNS desire circuit — effective in both men and women regardless of hormonal status.

💫

Dopamine & Oxytocin Release

MC4R activation in the mesolimbic pathway stimulates dopamine release in the nucleus accumbens, enhancing motivational salience for sexual activity. Simultaneously, hypothalamic oxytocin release is upregulated, contributing to both desire and the subjective experience of intimacy.

⚗️

Hormone-Independent Mechanism

Bremelanotide does not alter testosterone, oestrogen, or other circulating sex hormone levels. This makes it uniquely applicable to HSDD in women where hormonal therapies are contraindicated or ineffective, and in men where low desire persists despite normal testosterone.

🔬

Cyclic Peptide Stability

The cyclic backbone (Asp-Lys disulfide mimic) and D-Phe substitution confer resistance to enzymatic degradation, extending activity vs linear MSH. The Nle₁ substitution prevents methionine oxidation, critical for storage stability in aqueous formulations.

OVERVIEW

Research Overview

Bremelanotide was FDA-approved in 2019 as Vyleesi for the treatment of HSDD in premenopausal women — the first non-hormonal, centrally acting treatment for female sexual dysfunction. Clinical trials showed significant improvements in sexual desire and reductions in distress associated with low desire. It is self-administered as a subcutaneous injection 45 minutes before anticipated sexual activity.

Mechanism of Action

Bremelanotide is a cyclic heptapeptide that activates melanocortin receptors MC1R, MC3R, and MC4R. MC4R activation in the hypothalamus and limbic system modulates dopaminergic and serotonergic pathways involved in sexual motivation and arousal. Unlike testosterone or oestrogen therapy, it does not alter circulating hormone levels but directly activates central desire circuits.

DOSAGE

Dosage & Administration

INJECTABLE (SUBCUTANEOUS) — FDA-APPROVED (VYLEESI)

DOSE

1.75 mg

FREQUENCY

As needed, 45 minutes before activity; max 1× per 24 hours

NOTES

Official FDA-approved dose. Self-injected into abdomen or thigh. Take antiemetic 30 min prior if nausea-prone. Avoid in uncontrolled hypertension.

Calculate dose in Peptide Calculator

INJECTABLE (SUBCUTANEOUS) — RESEARCH DOSING

DOSE

0.5–2 mg

FREQUENCY

As needed

NOTES

Research protocols vary; 1 mg is commonly used for men off-label. Higher doses increase nausea risk without proportional benefit.

Calculate dose in Peptide Calculator

FDA-approved as Vyleesi for HSDD in premenopausal women. Off-label use in men is well-documented in research. Transient blood pressure increase of 2–4 mmHg occurs — avoid in cardiovascular disease. Nausea in ~40% of users; ondansetron or ginger 30 minutes prior significantly reduces incidence. Skin hyperpigmentation can occur with frequent use due to MC1R activity.

CYCLING

Cycle Duration Guide

ON CYCLE

As needed (not cycled)

OFF CYCLE

Not applicable

Bremelanotide is used on-demand, not on a fixed cycle. No established cycling protocol. For research exploring chronic effects, limit frequency to avoid hyperpigmentation (MC1R activity) and blood pressure concerns.

View full Cycle Guide →

NOTES

Research Notes

FDA-approved (Vyleesi) for HSDD in premenopausal women. Off-label use in men for libido also studied. Transient blood pressure elevation common — not recommended with cardiovascular disease. Nausea can be reduced by taking an antiemetic 30 minutes beforehand.

◆Quick Reference

FORMULAC₅₀H₆₈N₁₄O₁₀

MOL. WEIGHT1,025.2 Da

LENGTH7 amino acids

ORIGINSynthetic melanocortin peptide; derived from alpha-MSH

HALF-LIFE~2.7 hours

SOLUBILITYSoluble in water at physiological pH

CAS NO.189691-06-3

STATUSFDA Approved

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