Bremelanotide (Vyleesi): A Comprehensive Pharmacological and Clinical Review

Executive Summary

Bremelanotide, marketed as Vyleesi, is a first-in-class melanocortin receptor agonist approved for the treatment of acquired, generalized Hypoactive Sexual Desire Disorder (HSDD) in premenopausal women.[1] It represents a novel therapeutic approach, acting centrally on brain pathways associated with sexual desire, in contrast to peripherally acting agents that target vascular response.[3] Administered as an on-demand subcutaneous injection, Bremelanotide offers a distinct alternative to daily oral therapies.[4] Its approval was based on the pivotal RECONNECT Phase 3 clinical trials, which demonstrated statistically significant, albeit modest, improvements in sexual desire and reductions in the distress associated with HSDD when compared to placebo.[5] The safety and tolerability profile is characterized primarily by a high incidence of nausea, transient increases in blood pressure, and a risk of focal hyperpigmentation with frequent use.[1] This report provides a comprehensive review of Bremelanotide, detailing its chemical properties, mechanism of action, clinical evidence, administration protocols, and safety profile, while contextualizing its unique position relative to its main therapeutic alternative, Flibanserin (Addyi).

Section 1: Foundational Profile of Bremelanotide

This section establishes the fundamental scientific identity of Bremelanotide, detailing its chemical nature, pharmacological properties, and pharmacokinetic profile. This foundational knowledge is crucial for understanding its therapeutic effects and side effect profile discussed in later sections.

1.1. Chemical Identity and Structure