PT-141 (Bremelanotide)

An FDA-approved melanocortin receptor agonist originally derived from Melanotan II, developed specifically for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women. Unlike PDE5 inhibitors, it acts centrally on the nervous system to enhance sexual desire rather than targeting vascular mechanics.

• Agonizes melanocortin-4 receptors (MC4R) in the hypothalamus and limbic system to modulate sexual arousal pathways
• Activates central dopaminergic and oxytocinergic signaling involved in sexual motivation
• Does not act on peripheral vasculature like PDE5 inhibitors, instead targeting central nervous system desire pathways

• Uncontrolled hypertension or significant cardiovascular disease
• Concurrent use with naltrexone (opioid antagonist)
• Pregnancy or breastfeeding
• Known hypersensitivity to bremelanotide

Store at 2–8°C (36–46°F) for up to 6 months. Once reconstituted, refrigerate and use within 30 days. Pre-filled autoinjectors may be stored at room temperature (20–25°C (68–77°F)).

Reconstitute with bacteriostatic water. The FDA-approved autoinjector (Vyleesi) comes pre-filled at 1.75 mg per dose.

Bremelanotide was approved by the FDA in June 2019 under the brand name Vyleesi for HSDD in premenopausal women, following two Phase III RECONNECT trials. These studies showed statistically significant improvements in sexual desire and reductions in distress compared to placebo. Earlier Phase II research in men also demonstrated pro-erectile effects, though development focused on the female indication. It remains the only FDA-approved on-demand treatment for HSDD.