Melanocortin Peptides Anti-aging Neuropeptides Weight Loss Hormonal Modulators Peptide Hormones Approved

PT-141 / Bremelanotide

Also known as: Vyleesi, PT-141, Bremelanotide

PT-141 (Bremelanotide, marketed as Vyleesi®) is a synthetic melanocortin MC4R receptor agonist. It is the only centrally-acting peptide approved by the FDA (2019) for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women, acting directly on brain centers controlling sexual motivation.

Mechanism of action

Cyclic heptapeptide derived from Melanotan II. Unlike peripheral vasodilation-based sexual dysfunction treatments (sildenafil), PT-141 acts centrally:

Agonist of MC3R and MC4R receptors in the central nervous system
Activates dopaminergic pathways associated with sexual motivation and reward
Does not primarily act on the peripheral vascular system

Uses & indications

Hypoactive sexual desire disorder (HSDD) in premenopausal women (FDA-approved indication)
Erectile dysfunction in men (off-label; effective even when PDE5i fail)
Psychogenic sexual dysfunction in both sexes

Effects

Beneficial effects: Significant increase in sexual desire and satisfaction (RECONNECT trials); effect onset 45–60 min, duration 24 h.

Adverse effects: Nausea (40% of patients, main discontinuation cause), transient facial hyperpigmentation, flushing, headache, vomiting. Transient blood pressure elevation.

Considerations & contraindications

Contraindicated with cardiovascular medications (may potentiate hypotension)
Do not use in severe cardiovascular disease or uncontrolled hypertension
Wait ≥2 h before consuming alcohol or other vasodilators
Do not use during pregnancy
Maximum 1 dose/24 h and 8 doses/month (Vyleesi® protocol)

Regulatory approval

FDA approved (2019): Vyleesi® (bremelanotide, 1.75 mg sc) for HSDD in premenopausal women. Manufactured by AMAG Pharmaceuticals (now Palatin Technologies).

Dosage

Vyleesi®: 1.75 mg sc, 45 min before sexual activity. Maximum 1 dose/24 h.

Storage

Vyleesi® pen: refrigerator until use; may be kept at room temperature <77°F (<25°C) for up to 90 days.

Technical data

Regulatory status Approved

Molecular weight 1025.21 Da

Half-life ~2.7 h

Administration routes Subcutánea (autoinyección abdominal o muslo)