PT-141 (Bremelanotide) - (Female Viagra)
PT-141, also known as Bremelanotide, is an FDA-approved peptide designed to address sexual dysfunction in both men and women. Often referred to as "Female Viagra," PT-141 was originally derived from Melanotan II, a hormone known for its skin tanning effects. It was discovered to enhance sexual arousal and function, leading to its development as a treatment for sexual dysfunction.
Key Benefits:
Enhanced Sexual Desire: PT-141 effectively
increases sexual arousal in both men and women, offering a solution for those
experiencing low sexual desire.
Improved Sensation: It helps address issues
such as decreased sensation during intercourse and difficulty achieving orgasm.
Emotional Well-being: PT-141 can also
assist with emotional issues related to sexual dysfunction, helping to restore
confidence and pleasure.
Clinical Background: PT-141 was initially tested at the University of Arizona, where it demonstrated significant effects on sexual arousal in a majority of male volunteers. This discovery led to further research, revealing its broader potential in treating sexual dysfunction by affecting the central nervous system.
Current Use:
Female Sexual Arousal Disorder: PT-141 is
marketed under the brand name Vyleesi and is the first FDA-approved treatment
specifically for premenopausal women with acquired, generalized hypoactive
sexual desire disorder (HSDD).
Male Sexual Dysfunction: While initially
discovered through male studies, PT-141 is also used to address similar sexual
issues in men.
Additional Benefits:
Physical Health: Increased sexual activity
induced by PT-141 may offer additional benefits such as improved immune
function, enhanced pelvic floor muscle strength, and better bladder control in
women.
Well-being: PT-141 can contribute to
overall mental and physical well-being, including effects similar to regular
exercise such as fat burning, lower blood pressure, and reduced stress levels.
Conclusion: PT-141 offers a novel approach to treating sexual dysfunction, focusing on enhancing arousal and addressing emotional and physical aspects of sexual health. Its unique mechanism of action and broad benefits make it a valuable option for individuals struggling with sexual desire and related issues.
PT-141 (Bremelanotide) and Sexual Arousal
PT-141 is distinguished as a unique peptide due to its activation of the MC-4R receptor, which is known for inducing sexual arousal in the central nervous system and influencing sexual behavior [1], [2]. Studies in mice have shown that binding to MC-4R via an agonist results in sexual arousal and increased mating behavior in both male and female subjects [3], [4]. PT-141 operates through a different mechanism compared to medications like Viagra, offering a potential treatment for sexual arousal disorders in both genders, including cases not related to reduced blood flow to the genital organs.
In a study involving men with erectile dysfunction (ED) who did not respond to sildenafil (Viagra), about one-third of participants achieved sufficient erections for sexual activity with PT-141 administered via a nasal spray. The trial also demonstrated a dose-dependent effect, highlighting PT-141's potential efficacy in specific cases []. These results suggest that PT-141 might be a valuable alternative for treating ED when sildenafil fails, and could offer insights into central causes of decreased sexual desire.
PT-141, a promising drug for treating women with hypoactive sexual desire disorder (HSDD), was unexpectedly excluded from clinical trials before approval. Although it showed significant improvements in the number of satisfactory sexual events per month and a reduction in sexual distress scores in women without major side effects [6], it was not approved for this use. Many experts in female sexual dysfunction were disheartened by this decision, attributing it to a lack of established criteria for FSD trials and socio-cultural biases against female sexual health. These obstacles have delayed the approval of necessary treatments like PT-141 [7].
Experts are calling for more focus on this issue and the establishment of clearer FDA guidelines for evaluating effective therapies like PT-141. They also regret that pharmacological treatments were not tested alongside other established methods for sexual dysfunction, believing that combined therapies might have a synergistic effect. Additionally, they view peptides like PT-141 as valuable for overcoming initial barriers and initiating psychological treatment approaches.
In response to concerns over the termination of previous trials in 2017, Phase II clinical trials named Reconnect have been launched, utilizing subcutaneous injections of PT-141 for treating FSD. The latest version of PT-141, known as Rekynda, is anticipated soon in the U.S., allowing PT-141 to be used off-label for treating sexual dysfunction in both men and women [8]. These new trials have adjusted endpoints, which is welcomed by FSD experts as it increases the likelihood of approval for such treatments.
PT-141 and Hemorrhage
In 2009, PT-141 underwent minor modifications and was evaluated as a potential treatment for hemorrhagic shock. Given its binding affinity for both MC-1R and MC-4R, PT-141 demonstrated the ability to reduce ischemia and protect tissues from insufficient blood supply in cases of hypovolemic (hemorrhagic) shock. Intravenous administration of the drug resulted in minimal side effects. The modified variant, now known as PL-6983, has been assessed in Phase IIb clinical trials.
PT-141 and Infections
In a rat model of a specific fungal infection, MC-1R was found to exhibit significant antifungal and anti-inflammatory properties [9]. This finding is particularly significant as current antifungal treatments have limitations in their mechanisms and often result in severe side effects for certain individuals. Exploring alternative approaches to treating fungal infections could greatly impact by reducing both morbidity and mortality, especially among patients with weakened immune systems.
PT-141 and Cancer
The MC-1R receptor is crucial for activating DNA repair pathways, making it an important target in cancer treatment and prevention [10]. Research indicates that individuals with variants of MC-1R have an increased risk of basal cell and squamous cell skin cancers [11]. Modified PT-141 shows potential in addressing issues related to these variants, providing possible pathways for preventing or treating these types of cancer.
Research Directions
Currently, PT-141 is gaining significant attention as a treatment for sexual dysfunctions. However, its potential extends beyond sexual issues and hemorrhage, offering possibilities for various research applications. For example, MC-4R, the target of PT-141, is associated with certain cases of obesity, potentially contributing to up to 6% of early-onset obesity cases. Investigating PT-141's effects on this specific cause of obesity could reveal new intervention strategies. Additionally, MC-1R, another receptor affected by PT-141, plays roles in pain, inflammation, kidney pathology, and infection spread, presenting diverse research opportunities.
It is important to note that PT-141 shows minimal side effects and excellent bioavailability when administered subcutaneously in mice. However, dosage adjustments should be considered when transitioning from animal studies to human use.
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