MECHANISM OF ACTION
PT-141 (bremelanotide) is a cyclic heptapeptide analogue of α-MSH that acts as a selective agonist at MC3R and MC4R in the CNS. Unlike PDE5 inhibitors (Viagra, Cialis) which act peripherally on vascular smooth muscle, PT-141 acts centrally via hypothalamic pathways that regulate sexual arousal and desire. This distinction makes it effective for disorders of sexual desire rather than purely mechanical dysfunction. FDA approved (Vyleesi, AMAG Pharmaceuticals) specifically for premenopausal women with HSDD - representing the first centrally-acting approved treatment for female sexual dysfunction.
RESEARCH APPLICATIONS
- Hypoactive Sexual Desire Disorder (HSDD) - FDA approved indication (women)
- Male erectile dysfunction (MC4R mechanism, off-label research)
- Central sexual arousal pathway (hypothalamic MC3R/MC4R) research
- Melanocortin receptor comparative pharmacology
- Post-menopausal sexual function research
RESEARCH HIGHLIGHTS
FDA Approval for HSDD in Women
2019Phase III RECONNECT trials demonstrated significantly improved satisfying sexual events and decreased personal distress in premenopausal women with HSDD vs. placebo.
Ref: Simon et al., Obstet Gynecol
Central vs. Peripheral Mechanism
2006Distinct from PDE5 inhibitors - PT-141 activates desire via hypothalamic MC4R signalling rather than peripheral vascular effects, effective in subjects non-responsive to peripheral agents.
Ref: Diamond et al., J Sex Med
RESEARCH PROTOCOL NOTES
Chemical Identity
Storage & Stability
Lyophilised: -20°C. Reconstituted: 2–8°C, 21 days. Protect from light. Approved auto-injector pens: room temperature storage.
Regulatory Status
FDA approved (Vyleesi) for premenopausal HSDD. Not SA SAHPRA registered - importable via named patient pathway. Research vials available. Not WADA prohibited.