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Bremelanotide
(PT-141)

Bremelanotide is approved under the commercial name Vyleesi as a treatment for hypoactive sexual desire disorder (HSDD) in premenopausal women. It is also used off-label to treat sexual dysfunction in men.

Bremelanotide is a peptide hormone and melanocortin receptor, agonist. It appears to have slightly better efficacy in women, but there is evidence showing positive outcomes in men suffering from erectile dysfunction (ED).

Increased Benefit

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In premenopausal women with female sexual dysfunctions, self-administered subcutaneous bremelanotide was found to be safe, effective, and well-tolerated.

 

Clayton AH, Althof SE, Kingsberg S, et al. Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial. Women's Health (Lond). 2016;12(3):325–337. doi:10.2217/whe-2016-0018

 

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Diabetic men with ED who were part of a phase IIB trial reported significant increases in the International Index of Erectile Function (IIEF) scores after receiving bremelanotide injections. 

 

Kaminetsky J, Zinner N, Gittleman M, et al: Phase IIb study of bremelanotide in the treatment of ED in non-diabetic males. Proceedings of the American Urology Association Annual Meeting; Anaheim, USA. 19–24, 2007

The History of Bremelanotide

Prior to its FDA approval, bremelanotide was available in some parts of the world and online. A limited population of men and women have long used bremelanotide to self-treat sexual dysfunction and/or improve sexual performance. Bremelanotide has positive reports from both men and women who have used it, but just like any pharmaceutical tool, it does not work for everyone. Some people report experiencing side effects.

Prior to the availability of regulated bremelanotide in the US, the quality of non-prescribed medication was never guaranteed. It’s difficult to know if illicit bremelanotide products used the quality controls necessary to produce a final product that maintains its stability for the duration of use, or if they even contained the active ingredients listed on the label.  Fortunately, there are now licensed US manufacturers and compounding pharmacies offering peptides produced under a high standard of quality control with final products going through third-party validation to confirm potency, sterility, and stability.

Melanocortin Agonist for the Treatment of Sexual Dysfunction

Melanocortins are peptide hormones produced in the pituitary gland that bind to melanocortin receptors located in the central nervous system. The resulting activation of melanocortin receptors produces effects on mood, cognition, skin pigmentation, and sexual response.

We still have a long way to go to fully understand the melanocortin system, but ongoing research has identified the melanocortin receptors and some of the effects these hormones can produce.  Melanocortin’s influence over sexual function was first reported during the 1960s. 

Several synthetic compounds have been investigated for their use as potential tanning, aphrodisiac, and anti-obesity agents by their interaction with melanocortin receptors. Two well-studied melanocortin receptor agonists are Melanotan II and bremelanotide.

Bremelanotide is a non-selective melanocortin receptor agonist that was developed after discovering the effects of another melanocortin agonist known as Melanotan-II. Melanotan-II is known as a tanning agent that can be used to darken skin but was also found to have sexual effects including increased arousal and physical response.

Studies revealed low tolerance for Melanotan-II in patients with a significant number of prohibitive side effects reported, in addition to experiencing uncontrollable delay and duration of sexual response. This led to the development of bremelanotide, which is designed to focus on aphrodisiac effects with a faster onset of action once administered.  Bremelanotide also appears to be better tolerated with side effects being experienced by fewer people. 

Most Common Side Effects

(less than 4% reported in Vyleesi trials)
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Nausea 

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Hypertension

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Priapism (men) 

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Injection site reactions 

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Headache 

 

Administration:

Bremelanotide is self-administered by subcutaneous injection as needed 45 minutes before sexual activity.

 

Access: 

We offer affordable access to pharmaceutical bremelanotide manufactured at FDA-registered US licensed facilities. Bremelanotide may not work for every patient, but it can be an important option for the challenging and often integrative treatment of sexual dysfunction.

Bremelanotide is available as a compounded nasal spray or self-administered injection.

Defy Medical offers expert physician-guided therapies with convenient, affordable access to your care team, pharmacy, and lab testing.

Contact our patient service team today to learn more about this treatment, including costs. 

 

Combination Therapies: 

Some patients may need a combination of two or more treatments to effectively improve sexual function. If there is a suspected hormone imbalance including low testosterone, hormone replacement therapy may be recommended by your physician to resolve the underlying sexual issues caused by a hormone imbalance. Combination therapy of premelanotide with sildenafil has been shown to enhance erectile response in some patients. Your practitioner will discuss all suitable options during your consultation. 

Diamond LE, Earle DC, Garcia WD, et al. : Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response. Urology. 2005;65(4):755–9. 10.1016/j.urology.2004.10.060  

 

 


References:

  • Clayton AH, Althof SE, Kingsberg S, et al. Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial. Women’s Health (Lond). 2016;12(3):325–337. doi:10.2217/whe-2016-0018
  • Patel CK, Bennett N. Advances in the treatment of erectile dysfunction: what's new and upcoming?. F1000Res. 2016;5:F1000 Faculty Rev-369. Published 2016 Mar 18. doi:10.12688/f1000research.7885.1
  • Shadiack, A. and Althof, S., Preclinical effects of melanocortins in male sexual dysfunction. International Journal of Impotence Research.
  • Kaminetsky J, Zinner N, Gittleman M, et al. : Phase IIb study of bremelanotide in the treatment of ED in non-diabetic males. Proceedings of the American Urology Association Annual Meeting; Anaheim, USA. 19–24 May 2007
  • com/history/vyleesi.html
  • Diamond LE, Earle DC, Garcia WD, et al. : Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response. Urology. 2005;65(4):755–9. 10.1016/j.urology.2004.10.060
  • Patel, D.P., et al., Emerging treatment options for ED: Hope or hype? Urology Times. 2019 May 17