PT-141
Also sold as Vyleesi
About
About PT-141
A synthetic cyclic heptapeptide melanocortin receptor agonist, bremelanotide (PT-141) acts primarily on MC4 receptors in the central nervous system to modulate sexual arousal pathways. The compound increases sexual desire through direct neurological mechanisms rather than peripheral vascular effects. Its primary clinical application is the treatment of hypoactive sexual desire disorder in premenopausal women.
Science
Mechanism of Action
PT-141 activates melanocortin receptor subtypes MC3R and MC4R in the hypothalamus and other brain regions involved in sexual behavior. MC4R activation in the paraventricular nucleus of the hypothalamus initiates downstream signaling pathways (dopamine, oxytocin) that produce sexual arousal and desire. Unlike PDE5 inhibitors, this mechanism is centrally mediated and functions independently of vascular response, explaining its efficacy for libido rather than purely mechanical erectile function.
Dosing
Typical Protocol
Subcutaneous injection: 1.75 mg (FDA-approved dose) administered 45 minutes before sexual activity. Compounded dosing: 0.5–2 mg SC as needed, not more than once per 24 hours. Maximum frequency: No more than 2 doses per week recommended. Nasal spray: 0.3–0.6 mg per nostril (compounded formulation). Anti-nausea pretreatment: Ondansetron 4–8 mg 30 minutes prior can reduce GI side effects.
⚠ Protocol information is for educational purposes only. Dosing must be determined by a licensed physician based on individual health status and goals.
Regulatory
Legal Status in 2026
This compound has completed clinical trials and received formal FDA approval for one or more indications. It can be legally prescribed by licensed physicians, filled at any licensed pharmacy, and may be covered by insurance. Off-label use by physicians is also legal. This is the highest level of regulatory clearance available in the US.
Evidence
Evidence Tier
Supported by the clinical trial data required for FDA approval, representing the highest evidence bar. Safety and efficacy have been established in multiple phases of human clinical trials.
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