Bremelanotide (PT-141)

PT-141, also known as Bremelanotide or Vyleesi, is a synthetic peptide derived from the melanocortin analog Melanotan II. It consists of seven amino acids and was originally developed to influence the melanocortin receptors involved in skin pigmentation and sexual arousal pathways.

Studies suggest that PT-141 may enhance sexual desire and performance by acting on the central nervous system rather than vascular pathways. It has been shown to increase libido and improve sexual function in both men and women by stimulating specific brain receptors associated with arousal and motivation.

Clinical studies of Bremelanotide (formerly PT‑141) have found that it can improve sexual desire and arousal in women with hypoactive sexual desire disorder (HSDD). In two phase 3 trials in premenopausal women, treatment led to statistically significant increases in desire domain scores of the Female Sexual Function Index and reductions in distress related to low sexual desire ¹. Animal and early human studies in men also showed enhancement of erectile responses through central nervous system pathways rather than purely vascular ones ². Overall these findings show Bremelanotide enhances sexual desire and arousal.

In men, clinical and pre-clinical data suggest that Bremelanotide may facilitate erectile function even in the absence of typical sexual stimuli. For example, one study of healthy male subjects found increased duration of base penile rigidity with doses of PT-141 compared to placebo ³. Thus, the main benefits of PT-141 include improved sexual desire in women with HSDD and enhanced erectile response in men. Together, these findings indicate that Bremelanotide acts as a centrally mediated sexual function enhancer for both men and women, targeting the brain’s melanocortin system rather than peripheral hormonal or vascular mechanisms.

The peptide known as Bremelanotide (formerly PT‑141) has been shown in human clinical trials to produce common adverse effects including nausea (occurring in around 40% of participants) and flushing (around 20%) ⁴. In addition, transient increases in blood pressure and corresponding decreases in heart rate have been documented after dosing ⁵.

Less frequent but potentially more serious side effects include skin darkening (especially of the face, gums, or breasts), and very rare reports of liver enzyme elevations and acute hepatitis in clinical trial settings ⁶. nimal or longer-term data remain limited, so the full safety profile over extended use is not fully characterized.

Bremelanotide (PT-141) is a melanocortin receptor agonist that nonselectively activates several melanocortin receptor subtypes and has high relevance at the MC4R in the brain. Activation of MC4R in medial preoptic and limbic regions modulates central sexual arousal pathways, appears to increase sexual imagery and responsiveness, and is thought to promote downstream dopaminergic signaling that enhances sexual desire ^{7, 8}. Animal studies show that PT-141 produces pro-erectile and pro-sexual behaviors through hypothalamic MC3R/MC4R stimulation and increases markers of neuronal activation in nuclei such as the paraventricular nucleus. Human imaging and clinical trial data support that MC4R agonism alters sexual brain processing and subjective sexual desire, which provides a mechanistic rationale for the drug’s clinical effects ^{9, 10}.

Bremelanotide is approved by the Food and Drug Administration (FDA) under the brand name Vyleesi for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. In sport, Bremelanotide is not currently on the World Anti-Doping Agency (WADA) Prohibited List and is therefore generally allowed in sports.