Characteristics
| Molecular Formula | C50H68N14O10 |
| CAS Number | 189691-06-3 |
| Molar Mass | 1025.2 g/mol |
| Amino Acid Sequence | Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-OH |
| Synonyms | Bremelanotide, PT-141, PT141, PT 141 |
| Solubility | Water-soluble |
| Organoleptic Profile | White to off-white powder |
| Composition | Lyophilized powder - requires reconstitution |
How does PT-141 work?
PT-141 primarily acts as a melanocortin receptor agonist, with highest affinity for the melanocortin 4 receptor (MC4R) and melanocortin 1 receptor (MC1R). Research suggests the following mechanisms:
1. Central Nervous System: PT-141 activates MC4R in specific brain regions, particularly the hypothalamus and brainstem areas involved in sexual response. This activation is thought to influence neural pathways related to sexual desire and arousal.
2. Neurotransmitter Modulation: Studies indicate that PT-141 may increase dopamine release in the medial preoptic area, a region crucial for sexual motivation.
3. Peripheral Effects: PT-141's interaction with MC1R on melanocytes has been studied for potential effects on skin pigmentation.
Benefits
- HSDD in Premenopausal Women: Multiple Phase III clinical trials have evaluated PT-141's efficacy for HSDD. Studies typically measured changes in sexual desire and related distress using validated scales like the FSFI and FSDS-DAO. Research has examined various dosing regimens and administration methods.
- Male Sexual Function: Some studies have explored potential effects on erectile function, though this is not an FDA-approved use.
- Dermatology: Limited research has investigated PT-141's influence on melanogenesis and potential applications in pigmentation disorders.
- Cardiovascular Effects: Studies have examined PT-141's impact on blood pressure and heart rate, primarily for safety monitoring.
Side Effects
Based on the available preclinical data, the most common side effects associated with PT-141 treatment include:
- Nausea
- Flushing
- Headache
- Focal hyperpigmentation, which is generally reversible upon discontinuation of the drug
Note: The safety profile of PT-141 has not been fully established, and further clinical studies are needed to fully evaluate the potential for side effects and long-term safety of PT-141 in mammals.
Summary
PT-141 (Bremelanotide) is a synthetic peptide that has been the subject of extensive clinical research, particularly in the field of female sexual health. Its approved use for HSDD in premenopausal women represents a significant development in this therapeutic area. Ongoing studies continue to explore its mechanisms of action, potential applications, and long-term safety profile.
References
- Hedlund P. PT-141 Palatin. Curr Opin Investig Drugs. 2004.
- Ratnasiri MDK, Senarathna KW, Somarathne GPG, et al. Association between Bremelanotide and Hyponatremia; A Disproportionality Analysis of the WHO Pharmacovigilance Database. Curr Drug Saf. 2022.
- Van der Ploeg LH. Obesity: Neuropeptide targets for obesity treatment. Curr Opin Investig Drugs. 2003.
- Kingsberg SA, Schaffir J, Hatem C, et al. Efficacy, Safety, and Pharmacokinetics of Bremelanotide Self-Administered as Once-Weekly 2.75-mg Subcutaneous Injection. J Sex Med. 2023.
- Hadley ME, Dorr RT. Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization. Peptides. 2006.
- Safarinejad MR, Hosseini SY, Asgari MA, et al. A randomized, double-blind, placebo-controlled study of the efficacy and safety of bupropion for treating hypoactive sexual desire disorder in ovulating women. BJU Int. 2010.
- Kingsberg SA, Clayton AH, Pfaus JG. The Female Sexual Response: Current Models, Neurobiological Underpinnings and Agents Currently Approved or Under Investigation for the Treatment of HSDD. CNS Drugs. 2015.
- Thomas HN, Thurston RC. A biopsychosocial approach to women's sexual function and dysfunction at midlife: A narrative review. Maturitas. 2016.
- Simon JA, Kingsberg SA, Portman D, et al. Long-Term Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder. Obstet Gynecol. 2019.
- Poels S, Bloemers J, van Rooij K, et al. Two novel combined drug treatments for women with hypoactive sexual desire disorder. Pharmacol Biochem Behav. 2014.
- Diamond LE, Earle DC, Rosen RC, et al. Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141. Int J Impot Res. 2004.
- Altof SE, Stroberg P. The potential of bremelanotide for the treatment of hypoactive sexual desire disorder. Ther Adv Urol. 2013.
- Pfaus J, Giuliano F, Gelez H. Bremelanotide: an overview of preclinical CNS effects on female sexual function. J Sex Med. 2007.
- Pfaus JG. Pathways of sexual desire. J Sex Med. 2009.
- Safarinejad MR, Shafiei N, Safarinejad S. Evaluation of the efficacy and safety of bremelanotide in female subjects with arousal disorder. J Sex Med. 2008.
- Portman DJ, Edelson J, Jordan R, et al. Bremelanotide for hypoactive sexual desire disorder: analyses from a phase 2B dose-ranging study. J Women's Health. 2014.
Certificate of Analysis (COA)

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