Study summary · research use only
The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
This review discusses hypoactive sexual desire disorder (HSDD) in premenopausal women, describing it as estimated to affect approximately 10% of women in the United States and as suggested to involve imbalance of hormone and neurotransmitter levels including dopamine, norepinephrine, serotonin, estradiol, and testosterone. The authors describe current HSDD treatments as including psychotherapy and two FDA-approved medications, flibanserin and bremelanotide, a melanocortin receptor (MCR) agonist. Bremelanotide is described as nonselectively activating several MCR subtypes, with subtype 4 (MC4R) reported as most relevant at therapeutic doses and expressed in the medial preoptic area (mPOA) of the hypothalamus. Citing animal studies, the authors describe bremelanotide as potentially affecting sexual desire by activating presynaptic MC4Rs in the mPOA, increasing dopamine release.
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.
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