Off-Label Use of Bremelanotide (PT-141) in Men: Insights on Libido, Erections, and Safety from Experts

madman

Super Moderator

In this episode, Dr. Brandon & Dr. Morgentaler talk about the off-label use of bremelanotide (Vyleesi/PT-141) in men—its potential benefits for libido/erections, origins, side effects (notably nausea), and how patients often access it via compounding pharmacies.




Chapters

00:05 – Dr. Brandon & Dr. Morgentaler dive into Bremelanotide and share how the Goldsteins have been pioneering its research.
02:08 – They laugh about the iconic Katz’s Deli “When Harry Met Sally” scene and its connection to sexual medicine history.
03:06 – The doctors explain how Bremelanotide works, how it’s used by both women and men, and why refills tell an important story.
08:43 – They tackle the criticism that women take these meds “for men,” pushing back and stressing women’s right to pleasure.
19:48 – Wrapping up, they encourage listeners to talk with their doctors or compounding pharmacies if they want to explore this option.
 
 


MELANOCORTINS

Melanocortins are another drug class with the potential to be pharmacologic treatment options for patients with HSDD.
In 2019, the FDA approved the bremelanotide therapeutic (Vyleesi) for the treatment of HSDD in premenopausal women. Early evidence suggests that bremelanotide, an analog of the neuropeptide a-melanocyte-stimulating hormone, acts on a multitude of melanocortin receptors that are involved in excitatory pathways that have been implicated in sexual desire and arousal.14 Similar to flibanserin, bremelanotide’s mechanism of action in improving sexual desire has still not been fully elucidated and more pre-clinical data will be necessary to better characterize these neural pathways. In addition, even less information exists regarding bremelanotide’s safety and efficacy in improving low sex drive in male HSDD patients. However, bremelanotide has been shown in pre-clinical and clinical studies to improve erectile function in men through stimulation of centrally-acting melanocortin receptors located in the hypothalamus, and some data suggest that activation of this pathway also may trigger oxytocin release that may be implicated in sexual function.15,16 Future investigation into bremelanotide may provide more information regarding its role in the treatment of low libido in men.
 

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Understanding Your Hormones

Estradiol (E2)

A form of estrogen produced from testosterone. Important for bone health, mood, and libido. Too high can cause side effects; too low can affect well-being.

DHT

Dihydrotestosterone is a potent androgen derived from testosterone. Affects hair growth, prostate health, and masculinization effects.

Free Testosterone

The biologically active form of testosterone not bound to proteins. Directly available for cellular uptake and biological effects.

Scientific Reference

Lakshman KM, Kaplan B, Travison TG, Basaria S, Knapp PE, Singh AB, LaValley MP, Mazer NA, Bhasin S. The effects of injected testosterone dose and age on the conversion of testosterone to estradiol and dihydrotestosterone in young and older men. J Clin Endocrinol Metab. 2010 Aug;95(8):3955-64.

DOI: 10.1210/jc.2010-0102 | PMID: 20534765 | PMCID: PMC2913038

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