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PT-141 (Bremelanotide) 10mg

$45.00

PT-141, also known as Bremelanotide, is a synthetic cyclic heptapeptide lactam analogue of α-melanocyte-stimulating hormone (α-MSH). Its compact molecular size is noted for its ability to effectively cross the blood-brain barrier, which is essential for its mechanism of action as a melanocortin receptor agonist. It primarily targets central nervous system pathways involved in sexual arousal and desire, distinguishing it from traditional vasodilator agents. Bremelanotide serves as a compelling example of a peptide that successfully navigates the path from preclinical research to clinical approval, specifically targeting central nervous system pathways. While its primary indication is sexual function, its mechanism of action on the melanocortin system offers valuable insights into how peptides can modulate brain-mediated behaviors, which could inform strategies for other brain-related functions within a gut-brain product context.

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Data Sheet

Molecular Formula C₅₀H₆₈N₁₄O₁₀
CAS Number 189691-06-3
Molar Mass 1025.18 g/mol
Amino Acid Sequence Ac-Nle-Asp-His-D-Phe-Arg-Trp-Lys-OH
PubChem CID 9941379
Primary Research Area Sexual Desire/Arousal Enhancement
Hypoactive Sexual Desire Disorder (HSDD)
Sexual Dysfunction (men & women)
Melanocortin Receptor Agonism (MC3R, MC4R)
Central Nervous System (CNS) Modulation
Research Summary Description
Bremelanotide for the treatment of hypoactive sexual desire disorder: Two randomized phase 3 trials Summary: These were two identical Phase 3, randomized, double-blind, placebo-controlled, multicenter clinical trials (RECONNECT studies) evaluating bremelanotide 1.75 mg subcutaneously for premenopausal women with HSDD. Bremelanotide significantly increased sexual desire and reduced distress compared to placebo. Common adverse events included nausea, flushing, and headache.

Citation: Clayton, A. H., Althof, S. E., Kingsberg, S., DeRogatis, L. R., Kroll, R., Portman, D., DeRogatis, L. R.,... & Simon, J. A. (2019). Bremelanotide for the treatment of hypoactive sexual desire disorder: Two randomized phase 3 trials. Obstetrics & Gynecology, 133(4), 755-765.
Phase 2b, randomized, double-blind, placebo-controlled, dose-finding trial Summary: This trial involved 397 premenopausal women with HSDD or female sexual arousal disorder. Self-administered subcutaneous bremelanotide was taken as needed for up to 12 weeks. It showed dose-responsive improvements in desire, arousal, and associated distress with self-administered subcutaneous bremelanotide, leading to the selection of the 1.75 mg dose for further development.

Citation: Clayton, A. H., Althof, S. E., Kingsberg, S., DeRogatis, L. R., Kroll, R., Portman, D., DeRogatis, L. R.,... & Simon, J. A. (2019). Bremelanotide for the treatment of hypoactive sexual desire disorder: Two randomized phase 3 trials. Obstetrics & Gynecology, 133(4), 755-765.
PT-141 (Bremelanotide) for sexual dysfunction: clinical guide for physicians Summary: This article highlights that PT-141 activates melanocortin receptors MC3R and MC4R primarily within the hypothalamus, modulating pathways associated with sexual arousal, libido, and sexual satisfaction through central nervous system signaling rather than peripheral vasodilation.

Citation: Enavvi. (n.d.). PT-141 (Bremelanotide) for Sexual Dysfunction: Clinical Guide for Physicians.
PT-141: a melanocortin agonist for the treatment of sexual dysfunction Summary: This study investigated PT-141's effects in rats, nonhuman primates, and human clinical studies. It showed that PT-141 induced penile erections in animals and a rapid, dose-dependent increase in erectile activity in healthy men and those with erectile dysfunction.

Citation: Molinoff, P. B., Shadiack, A. M., Earle, D., Diamond, L. E., & Quon, C. Y. (2003). PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences, 994(1), 96-102.
Melanocortin-4 receptor agonism improves sexual brain processing in women with low sexual desire Summary: This clinical study investigated the effects of a melanocortin-4 receptor (MC4R) agonist (like bremelanotide) on brain activity related to sexual desire in premenopausal women with hypoactive sexual desire disorder (HSDD). Using functional MRI, psychometric measures, and hormonal analyses, the researchers found that MC4R agonism significantly increased sexual desire and enhanced brain regions involved in sexual processing (e.g., cerebellum, supplementary motor area, amygdala-insula connectivity) in response to erotic stimuli, compared to placebo. It also deactivated the secondary somatosensory cortex.

APA Citation:
Walpole, L., Ghosal, S., Koundal, S., Dhillo, W. S., & Le Roux, C. W. (2021). Melanocortin-4 receptor agonism improves sexual brain processing in women with low sexual desire. Endocrine Abstracts, 77, OC1.1.
Melanocortins in the treatment of male and female sexual dysfunction Summary: This review article provides a comprehensive overview of the role of melanocortinergic agents, including PT-141 (bremelanotide), in treating sexual dysfunction in both men and women. It highlights that the therapeutic investigations were sparked by the accidental discovery of penile erections caused by a synthetic alpha-MSH analog (Melanotan II). The review discusses how bremelanotide, specifically, has been clinically studied and shows promise for erectile dysfunction in men and promoting sexual desire and arousal in women by acting on central nervous system melanocortin receptors, particularly in the hypothalamus. It also notes that bremelanotide administration is generally well-tolerated and not associated with the hypotension seen with PDE-5 inhibitors.

APA Citation:
Diamond, L. E., & Earle, D. C. (2007). Melanocortins in the treatment of male and female sexual dysfunction. Current Topics in Medicinal Chemistry, 7(11), 1081-1087.

Bremelanotide for the treatment of hypoactive sexual desire disorder: Two randomized phase 3 trials

Summary: These were two identical Phase 3, randomized, double-blind, placebo-controlled, multicenter clinical trials (RECONNECT studies) evaluating bremelanotide 1.75 mg subcutaneously for premenopausal women with HSDD. Bremelanotide significantly increased sexual desire and reduced distress compared to placebo. Common adverse events included nausea, flushing, and headache.

Citation: Clayton, A. H., Althof, S. E., Kingsberg, S., DeRogatis, L. R., Kroll, R., Portman, D., DeRogatis, L. R.,... & Simon, J. A. (2019). Bremelanotide for the treatment of hypoactive sexual desire disorder: Two randomized phase 3 trials. Obstetrics & Gynecology, 133(4), 755-765.

Phase 2b, randomized, double-blind, placebo-controlled, dose-finding trial

Summary: This trial involved 397 premenopausal women with HSDD or female sexual arousal disorder. Self-administered subcutaneous bremelanotide was taken as needed for up to 12 weeks. It showed dose-responsive improvements in desire, arousal, and associated distress with self-administered subcutaneous bremelanotide, leading to the selection of the 1.75 mg dose for further development.

Citation: Clayton, A. H., Althof, S. E., Kingsberg, S., DeRogatis, L. R., Kroll, R., Portman, D., DeRogatis, L. R.,... & Simon, J. A. (2019). Bremelanotide for the treatment of hypoactive sexual desire disorder: Two randomized phase 3 trials. Obstetrics & Gynecology, 133(4), 755-765.

PT-141 (Bremelanotide) for sexual dysfunction: clinical guide for physicians

Summary: This article highlights that PT-141 activates melanocortin receptors MC3R and MC4R primarily within the hypothalamus, modulating pathways associated with sexual arousal, libido, and sexual satisfaction through central nervous system signaling rather than peripheral vasodilation.

Citation: Enavvi. (n.d.). PT-141 (Bremelanotide) for Sexual Dysfunction: Clinical Guide for Physicians.

PT-141: a melanocortin agonist for the treatment of sexual dysfunction

Summary: This study investigated PT-141's effects in rats, nonhuman primates, and human clinical studies. It showed that PT-141 induced penile erections in animals and a rapid, dose-dependent increase in erectile activity in healthy men and those with erectile dysfunction.

Citation: Molinoff, P. B., Shadiack, A. M., Earle, D., Diamond, L. E., & Quon, C. Y. (2003). PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences, 994(1), 96-102.

Melanocortin-4 receptor agonism improves sexual brain processing in women with low sexual desire

Summary: This clinical study investigated the effects of a melanocortin-4 receptor (MC4R) agonist (like bremelanotide) on brain activity related to sexual desire in premenopausal women with hypoactive sexual desire disorder (HSDD). Using functional MRI, psychometric measures, and hormonal analyses, the researchers found that MC4R agonism significantly increased sexual desire and enhanced brain regions involved in sexual processing (e.g., cerebellum, supplementary motor area, amygdala-insula connectivity) in response to erotic stimuli, compared to placebo. It also deactivated the secondary somatosensory cortex.

APA Citation:
Walpole, L., Ghosal, S., Koundal, S., Dhillo, W. S., & Le Roux, C. W. (2021). Melanocortin-4 receptor agonism improves sexual brain processing in women with low sexual desire. Endocrine Abstracts, 77, OC1.1.

Melanocortins in the treatment of male and female sexual dysfunction

Summary: This review article provides a comprehensive overview of the role of melanocortinergic agents, including PT-141 (bremelanotide), in treating sexual dysfunction in both men and women. It highlights that the therapeutic investigations were sparked by the accidental discovery of penile erections caused by a synthetic alpha-MSH analog (Melanotan II). The review discusses how bremelanotide, specifically, has been clinically studied and shows promise for erectile dysfunction in men and promoting sexual desire and arousal in women by acting on central nervous system melanocortin receptors, particularly in the hypothalamus. It also notes that bremelanotide administration is generally well-tolerated and not associated with the hypotension seen with PDE-5 inhibitors.

APA Citation:
Diamond, L. E., & Earle, D. C. (2007). Melanocortins in the treatment of male and female sexual dysfunction. Current Topics in Medicinal Chemistry, 7(11), 1081-1087.

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