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PT-141

Bremelanotide, Vyleesi

Quick Stats
Studies 74
Trials 10
Score 3
2021 pubmed

The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women.

Pfaus. James G JG; Sadiq. Amama A; Spana. Carl C; Clayton. Anita H AH

Key Findings

  • HSDD may stem from hormone and neurotransmitter imbalances affecting brain excitation and inhibition
  • Bremelanotide is a melanocortin receptor agonist that primarily activates MC4R in the hypothalamus
  • MC4R activation in the medial preoptic area increases dopamine release, which can raise sexual desire

Practical Outcomes

  • The review clarifies that bremelanotide’s effect comes from MC4R‑driven dopamine release, supporting its use for HSDD. However, it offers no dosing guidance or safety data, so enthusiasts should treat it as a clinically‑approved drug that requires medical supervision rather than a DIY protocol.

Summary

Bremelanotide (pt‑141) is a drug that activates certain brain receptors (MC4R) linked to sexual desire, boosting dopamine release in a key hypothalamic area, which may help women with low sexual desire, but the paper only explains how it works, not how to use it.

Abstract

Hypoactive sexual desire disorder (HSDD) is a common female sexual dysfunction and is estimated to affect approximately 10% of women in the United States. It has been suggested that HSDD is associated with an imbalance of hormone and neurotransmitter levels in the brain, resulting in decreased excitation, increased inhibition, or a combination of both. Evidence suggests neurotransmitters, including dopamine (DA), norepinephrine, and serotonin, as well as hormones such as estradiol and testosterone, contribute to female sexual desire and response. Current treatments for HSDD include psychotherapy, and two US Food and Drug Administration-approved medications for premenopausal women: flibanserin, a serotonin mixed agonist and antagonist, and bremelanotide, a melanocortin receptor (MCR) agonist. Melanocortins are endogenous neuropeptides associated with the excitatory pathway of the female sexual response system. MCRs are found throughout the body, including the brain. Bremelanotide is an MCR agonist that nonselectively activates several of the receptor subtypes, of which subtype 4 (MC4R) is the most relevant at therapeutic doses. MC4R is predominantly expressed in the medial preoptic area (mPOA) of the hypothalamus in the brain, and is important for female sexual function. Animal studies suggest that bremelanotide may affect female sexual desire by activating presynaptic MC4Rs on neurons in the mPOA of the hypothalamus, leading to increased release of DA, an excitatory neurotransmitter that increases sexual desire. This review presents what is known about the mechanism of action of bremelanotide in the context of treating HSDD.

Study Information

Provider

pubmed

Year

2021

Date

2021-01-18T00:00:00.000Z

DOI

10.1017/s109285292100002x