PT-141, also called Bremelanotide (generic clinical name), is a heavily modified synthetic derivative of alpha-melanocyte-stimulating hormone. It has been tested in clinical trials as a treatment for both male/female hypoactive sexual desire disorder and acute hemorrhage. PT-141 is an agonist for the melanocortin-4 and melanocortin-1 receptors. Research shows that it promotes sexual arousal and stimulates the immune system.
PT-141 is a unique peptide that stimulates the MC-4R receptor in the central nervous system, which plays a role in sexual arousal and behavior. Preclinical studies in mice demonstrated that MC-4R activation increases sexual activity and mating in both males and females. Unlike traditional treatments such as sildenafil (Viagra), PT-141 works through a different pathway, making it a potential option for sexual arousal disorders not caused by restricted blood flow.
Clinical research in men with erectile dysfunction (ED) who did not respond to sildenafil found that approximately one-third achieved erections sufficient for intercourse following intranasal administration of PT-141. The effect was dose-dependent, suggesting clear therapeutic potential. These findings point to PT-141’s ability to address sexual dysfunction in cases where PDE5 inhibitors like sildenafil are less effective.
Although PT-141 showed promising results, it was initially withdrawn from development before FDA approval, despite data showing increased sexual events per month and decreased distress related to sexual dysfunction in women with female sexual dysfunction (FSD). Many experts believed these outcomes demonstrated significant benefit, but the lack of standardized trial designs and regulatory hurdles slowed progress. Renewed clinical studies were later launched, including trials using a subcutaneous form (branded as Rekynda in development) for female sexual dysfunction, with the potential for off-label use in treating both men and women.
In 2009, PT-141 was also investigated as a treatment for hemorrhagic shock. By binding to both MC-1R and MC-4R, it was found to reduce ischemia and protect against inadequate blood supply in preclinical models of hemorrhage. When given intravenously, it produced stabilization without significant side effects. The modified version developed for this purpose was referred to as LS-6683.
The MC-1R receptor, which PT-141 also targets, has been studied for its role in regulating immune responses and limiting the effects of certain infections. Early findings suggest PT-141 and related compounds may help control inflammatory pathways, which could make them valuable in treating specific infectious or inflammatory conditions.
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