1. What is PT-141?
PT-141, also known as Bremelanotide, is a synthetic peptide derived from the melanocortin family. Unlike PDE-5 inhibitors (e.g., sildenafil) that act on vascular pathways, PT-141 works centrally by activating melanocortin receptors (MC3R/MC4R) in the brain. This mechanism enhances sexual desire and arousal through neural circuits linked to motivation and reward. It has been studied for both erectile dysfunction (ED) in men and hypoactive sexual desire disorder (HSDD) in women.
2. PT-141 Structure
Sequence: Ac-Nle-Asp(1)-His-D-Phe-Arg-Trp-Lys(1)
Molecular Formula: C₅₀H₆₈N₁₄O₁₀
Molecular Weight: 1025.16 g/mol
PubChem CID: 9941379
CAS Number: 189691-06-3
Synonyms: Bremelanotide, Vyleesi
3. PT-141 Research
Preclinical & Human Data
l In rodent and primate studies, PT-141 induced penile erections and activated hypothalamic neurons relevant to sexual behavior.
【1】
l Phase I/II clinical trials (intranasal) demonstrated safety, ~30 min onset, and effective erectile responses.
l Even PDE-5 non-responders showed significant improvements in erectile function scores.
【2】
Mechanistic Differentiation
l Works via MC4R in the CNS, modulating arousal and motivation—not direct vasodilation.
【3】
Women’s HSDD Trials
l FDA-approved as Vyleesi (1.75 mg SC, on-demand) for premenopausal women with HSDD.
【4】
l 52-week open-label data confirmed improved sexual desire and satisfaction with tolerability.
【5】
✅ Why Consider PT-141?
🌐 Central mechanism: Acts on brain pathways for desire and arousal.
🚀 Rapid onset (~30–45 min): Provides spontaneous, on-demand activity.
👥 Effective in PDE-5 non-responders: Expands treatment options for ED.
👩⚕️ FDA-approved (Vyleesi, 2019): For female HSDD.
🔄 Synergistic potential: Can be co-administered with PDE-5 inhibitors.
🛡 Safer profile: No nitrate contraindications compared to PDE-5 inhibitors.
4. Future PT-141 Research
· MC4R-Selective Analogues (e.g., PL-6983): Designed to reduce BP-related side effects.【6】
· Alternative Delivery Methods: Improved nasal sprays, oromucosal, and oral peptide delivery systems.
· Expanded Populations: Studies in diabetic men, older adults, and combination protocols with PDE-5 inhibitors.
· Female Sexual Dysfunction Expansion: Combining with oxytocin, kisspeptin, or neuromodulators for broader outcomes.
· Neurobiology Studies: fMRI, biomarkers, and CNS mapping to refine understanding of sexual motivation.
· Long-term Safety: Open-label trials (e.g., RECONNECT) are monitoring BP, pigmentation, and adherence.【7】
5. Application Areas
l Erectile Dysfunction: Particularly useful when PDE-5 inhibitors fail or are contraindicated.
l Female HSDD: On-demand treatment, improving desire and satisfaction.
l Performance Anxiety: Central action may reduce psychogenic arousal barriers.
l Combination Therapies: Co-use with sildenafil or tadalafil for additive benefits.
l Off-label Potential: Libido concerns, premature ejaculation, and psychosexual therapy adjuncts.
✅ Summary
PT-141 (Bremelanotide) provides a novel, centrally acting therapy for sexual dysfunction. By targeting MC4 receptors in the brain, it enhances sexual motivation and arousal rather than relying solely on vascular mechanisms. With FDA approval for female HSDD, efficacy in male PDE-5 non-responders, and ongoing research into safer analogues and new delivery methods, PT-141 represents an important advancement in sexual health therapeutics.
Disclaimer
ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATIONAL AND EDUCATIONAL PURPOSES ONLY.
The products offered on this website are furnished for in-vitro studies only (in vitro = outside of the body). These products are not medicines or drugs and have not been approved by the FDA to prevent, treat, or cure any medical condition, ailment, or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law.
