PT-141 (Bremelanotide)
approvedAlso known as: Bremelanotide, Vyleesi
**Mechanism of Action** PT-141 (bremelanotide) is a synthetic cyclic heptapeptide analog of α-melanocyte-stimulating hormone (α-MSH) that acts as a selective agonist at melanocortin receptors, primarily MC4R and, to a lesser extent, MC1R and MC3R. Its central mechanism involves activation of MC4R in the hypothalamus and limbic system, modulating dopaminergic and oxytocinergic pathways to enhance sexual arousal and desire without directly affecting peripheral vascular or hormonal systems. This distinguishes it from PDE5 inhibitors, as it does not rely on nitric oxide-mediated vasodilation. **Key Research Findings** Approved by the FDA in 2019 (Vyleesi) for premenopausal hypoactive sexual desire disorder (HSDD), bremelanotide demonstrated significant improvements in sexual desire and distress in two Phase III trials (RECONNECT studies). A 2020 meta-analysis of 1,267 women reported a 1.2-point increase in desire scores (Female Sexual Function Index) and a 30% reduction in distress vs. placebo. Common adverse effects include nausea (40%), flushing (20%), and transient blood pressure elevations. Notably, it shows no abuse liability and is administered subcutaneously 45 minutes before anticipated sexual activity. **Clinical Relevance** As the only FDA-approved centrally acting agent for HSDD, bremelanotide addresses an unmet need in women with acquired, generalized low sexual desire. Its rapid onset and on-demand dosing profile offer an alternative to daily flibanserin. Contraindications include uncontrolled hypertension and cardiovascular disease due to pressor effects. Ongoing research explores its utility in male sexual dysfunction (e.g., erectile dysfunction, anorgasmia) and neuropsychiatric conditions. For research purposes only — not medical advice.
Key data
C50H68N14O10Research & studies
Continuous efficacy outcomes (FSFI, FSFI-D, FSDS-DAO, FSDS-DAO #13) have questionable validity evidence for women with HSDD.; No validity evidence was found for previously published categorical treatment response outcomes from the RECONNECT trials.; Effect sizes on 8 previously unpublished outcomes ranged from nil to small.; Nearly all modest apparent benefits were likely derived from post-hoc outcomes.
Bremelanotide is a melanocortin receptor agonist hypothesized to trigger excitatory brain pathways for sexual desire.; Most common adverse reaction is nausea (40%); overall safety and tolerability are moderate.; Clinical trials showed significant changes in validated questionnaires, but overall clinical benefit is modest.; Results are limited by high placebo effects and outcome measures susceptible to expectation biases.
HSDD affects about 10% of U.S. women and is linked to neurotransmitter and hormone imbalances.; Bremelanotide nonselectively activates melanocortin receptors, with MC4R being most relevant at therapeutic doses.; MC4R is predominantly expressed in the medial preoptic area of the hypothalamus, important for female sexual function.; Animal studies indicate bremelanotide increases dopamine release by activating presynaptic MC4Rs, boosting sexual desire.
Flibanserin and bremelanotide are indicated for generalized acquired HSDD in premenopausal women.; Transdermal testosterone is effective for HSDD in postmenopausal women.; Menopause hormone therapy (systemic and local) is the mainstay for midlife women.; Bremelanotide should be used with caution during breastfeeding due to limited safety data.
Frequently asked questions
What is PT-141 (Bremelanotide)?
**Mechanism of Action** PT-141 (bremelanotide) is a synthetic cyclic heptapeptide analog of α-melanocyte-stimulating hormone (α-MSH) that acts as a selective agonist at melanocortin receptors, primarily MC4R and, to a lesser extent, MC1R and MC3R. Its central mechanism involves activation of MC4R in the hypothalamus an
How does PT-141 (Bremelanotide) work?
Melanocortin MC4R agonist approved for hypoactive sexual desire disorder; acts centrally to increase sexual arousal.
What is the research status of PT-141 (Bremelanotide)?
PT-141 (Bremelanotide) is currently classified as approved, with 94 research references on record. This is for research purposes only and is not medical advice.
What is the molecular weight of PT-141 (Bremelanotide)?
PT-141 (Bremelanotide) has a molecular weight of approximately 1025.2 g/mol (formula C50H68N14O10).
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