PT- 141

What is PT-141?

PT-141 is a melanocortin receptor agonist derived from the peptide hormone α-MSH. It has been the subject of significant research for its potential to modulate sexual behavior and neuroendocrine function. Studies suggest that PT-141 activates melanocortin-4 receptors (MC4R) in the hypothalamus, leading to increased sexual arousal independent of vascular pathways. PT-141 is intended solely for scientific investigation and is not approved for clinical or veterinary use.

Structure

• Chemical Formula: C50H68N14O10
• Synonyms: Bremelanotide

PT-141 Research

PT-141 and Female Sexual Dysfunction

PT-141 has been evaluated for its effects on premenopausal women with hypoactive sexual desire disorder (HSDD). In a 52-week open-label extension study, participants experienced improvements in sexual desire and satisfaction with a favorable safety profile. The most reported adverse events were mild nausea, flushing, and headache [1]. The mechanism of PT-141 through MC4R activation offers a targeted pathway for modulating sexual behavior.

PT-141 and Male Erectile Dysfunction

In male populations, PT-141 has demonstrated potential in treating erectile dysfunction (ED), particularly in cases where phosphodiesterase type 5 inhibitors like sildenafil are ineffective. A double-blind, placebo-controlled study showed statistically significant improvements in erectile response and satisfaction in men treated with PT-141 compared to placebo [2]. These results indicate its promise as an alternative mechanism-based therapy.

PT-141 in Combination Therapy

Research has investigated PT-141 in combination with sildenafil for synergistic effects. Co-administration resulted in a significantly enhanced erectile response compared to either drug alone [3]. This synergy is thought to stem from the central nervous system action of PT-141 complementing the vascular effects of sildenafil.

PT-141 Pharmacokinetics and Safety Profile

A Phase I clinical trial assessed the pharmacokinetics and tolerability of PT-141 in combination with PDE5 inhibitors. The study found that PT-141 was generally well-tolerated with mild to moderate adverse effects, primarily gastrointestinal in nature. These findings support continued study of PT-141 in combination treatments for sexual dysfunction [4].

Disclaimer

ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATIONAL AND EDUCATIONAL PURPOSES ONLY.

THIS PRODUCT IS INTENDED FOR LABORATORY RESEARCH USE ONLY. NOT FOR HUMAN OR ANIMAL CONSUMPTION.

Referenced Citations

1. Kingsberg SA, Clayton AH, Portman D, et al. “A Phase 3 Randomized Study of Bremelanotide for Hypoactive Sexual Desire Disorder in Premenopausal Women.” J Womens Health (Larchmt). 2019;28(2):173–180. doi:10.1089/jwh.2018.6997.
2. Safarinejad MR, et al. “Efficacy and safety of bremelanotide (PT-141) in men with erectile dysfunction: results of a double-blind, randomized, placebo-controlled study.” J Urol. 2008;179(3):1060–1065. doi:10.1016/j.juro.2007.10.063.
3. Diamond LE, Earle DC, Rosen RC, et al. “Double-blind, placebo-controlled evaluation of the safety and efficacy of a novel melanocortin receptor agonist in combination with sildenafil in men with erectile dysfunction.” J Sex Med. 2006;3(5):908–918. doi:10.1111/j.1743-6109.2006.00289.x.
4. Nappi RE, Palacios S, Bruyniks N, et al. “A phase I study of pharmacokinetics and safety of bremelanotide (PT-141) combined with a PDE5 inhibitor.” J Sex Med. 2017;14(3):354–362. doi:10.1016/j.jsxm.2016.12.237.