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PT-141

Sexual Health
BremelanotideVyleesi

Overview

PT-141, also known as Bremelanotide or Vyleesi, is a synthetic peptide developed from the melanocortin receptor agonist family. It is structurally related to the alpha-melanocyte-stimulating hormone (α-MSH) and was initially synthesized for its potential effects on sexual arousal. The compound is typically synthesized through solid-phase peptide synthesis, a method that allows for the precise assembly of amino acids into the desired peptide sequence. Researchers have primarily investigated PT-141 for its effects on sexual dysfunction, particularly in premenopausal women with hypoactive sexual desire disorder (HSDD). Studies have shown that PT-141 can enhance sexual desire and arousal, leading to its approval for use in certain populations. It has also been explored for potential applications in male erectile dysfunction, although this is not its primary indication. The mechanism of action of PT-141 involves the activation of melanocortin receptors, particularly MC3R and MC4R, in the central nervous system. This activation is believed to influence pathways associated with sexual arousal and desire, although the exact neural mechanisms remain an area of active research. Pharmacokinetically, PT-141 has a half-life of approximately 2 to 4 hours when administered subcutaneously. It is known for its rapid onset of action, with effects typically observed within 30 minutes to an hour. The compound is stable when stored appropriately, but its bioavailability is limited when administered orally. Currently, PT-141 is approved by the FDA for the treatment of HSDD in premenopausal women under the brand name Vyleesi. It is not approved for use in men or for other indications. Ongoing research continues to explore its broader therapeutic potential and long-term safety profile.

Mechanism of Action

PT-141 acts primarily through the activation of melanocortin receptors MC3R and MC4R in the central nervous system. This activation is thought to modulate pathways involved in sexual arousal and desire, although the precise neural circuits remain under investigation.

Molecular Data

FormulaC50H68N14O10
Molecular Weight1025.2 g/mol
CAS Number189691-06-3
PubChem CID9941379

Half-Life

Subcutaneous~2 to 4 hours
IntranasalNot applicable
OralPoor bioavailability

The pharmacokinetic profile is characterized by rapid absorption and onset of action when administered subcutaneously.

Storage

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Solubility

PT-141 is soluble in water and DMSO, with limited solubility in organic solvents like acetonitrile.

Legal Status

🇩🇪DE

Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.

🇺🇸US

Approved by the FDA for treatment of HSDD in premenopausal women. Not scheduled by the DEA.

🇦🇺AU

Data limited

🇬🇧UK

Data limited

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

7 Research Publications

Targeting the central melanocortin system for the treatment of metabolic disorders.

Review

Nature reviews. Endocrinology · 2023

Researchers observed that the central melanocortin system could be a valuable target for treating metabolic disorders like obesity and anorexia. The FDA has approved several drugs that interact with this system, indicating its potential for safe therapeutic use. This review discusses the system's anatomy, its role in various conditions, and the ongoing development of related treatments.

  • Researchers found that the central melanocortin system is linked to metabolic disorders such as obesity and cachexia.
  • The FDA approved setmelanotide in 2020 for specific types of syndromic obesity, highlighting the system's therapeutic potential.
  • The review outlines both the progress made and challenges faced in developing drugs that target melanocortin receptors.
PubMed

An evaluation of bremelanotide injection for the treatment of hypoactive sexual desire disorder.

Review

Expert opinion on pharmacotherapy · 2023

Researchers evaluated the effectiveness and safety of bremelanotide (Vyleesi) for women with hypoactive sexual desire disorder (HSDD). They found that while bremelanotide can lead to some improvement in sexual desire, the overall benefits are modest and the most common side effect is nausea.

  • Bremelanotide was observed to moderately enhance sexual desire in premenopausal women with HSDD.
  • The most common side effect reported was nausea, affecting about 40% of users.
  • The overall clinical benefit of bremelanotide appears to be modest, influenced by challenges in clinical trial design.
PubMed

Medical Treatment of Female Sexual Dysfunction.

Review

The Urologic clinics of North America · 2022

Researchers reviewed various treatments for female sexual dysfunction (FSD), which involves multiple overlapping disorders influenced by biological, psychological, and social factors. They found that healthcare providers can screen for FSD and offer initial counseling before referring patients to specialists, with a range of treatment options available for different stages of life.

  • Researchers observed that flibanserin and bremelanotide are effective for premenopausal women with low sexual desire.
  • Transdermal testosterone was noted to be effective for postmenopausal women experiencing similar issues.
  • The study highlighted that menopause hormone therapy is crucial for managing symptoms in women during midlife.
PubMed

Bremelanotide for Treatment of Female Hypoactive Sexual Desire.

Review

Neurology international · 2022

Researchers studied bremelanotide, a new treatment for women with hypoactive sexual desire disorder (HSDD), which causes a significant lack of sexual desire and distress. The study found that bremelanotide improved sexual desire, arousal, and orgasm scores when used before sexual activity compared to a placebo.

  • Bremelanotide was recently approved by the FDA for treating HSDD in women.
  • Researchers observed improvements in sexual desire and arousal after using bremelanotide.
  • The treatment targets both biological and psychosocial factors related to HSDD.
PubMed

Hypoactive Sexual Desire Disorder in Women: Physiology, Assessment, Diagnosis, and Treatment.

Review

Journal of midwifery & women's health · 2021

Researchers found that nearly half of women in the U.S. experience sexual function issues, with hypoactive sexual desire disorder (HSDD) being the most common. This study provides an overview of HSDD, including its symptoms, assessment methods, and treatment options, highlighting the need for healthcare providers to address this often-overlooked condition.

  • HSDD is characterized by a lack of sexual thoughts and feelings that causes personal distress and has been present for at least six months.
  • The study emphasizes the importance of using validated screening tools and a comprehensive assessment approach in diagnosing HSDD.
  • Researchers reviewed two recently approved medications for HSDD and discussed additional off-label treatment options.
PubMed

Bremelanotide: First Approval.

Review

Drugs · 2019

Researchers observed that bremelanotide, a new medication approved in the USA, is designed for premenopausal women experiencing low sexual desire that causes distress. This self-administered treatment works by targeting specific brain pathways related to sexual response. The study highlights the development journey of bremelanotide leading to its regulatory approval.

  • Bremelanotide is approved for women with acquired, generalized hypoactive sexual desire disorder (HSDD).
  • The drug is administered through a self-injection and is used on-demand.
  • Bremelanotide mimics a natural hormone that influences sexual function by acting on brain receptors.
PubMed

PT-141 Palatin.

Review

Current opinion in investigational drugs (London, England : 2000) · 2004

Researchers observed that PT-141, a nasal spray developed by Palatin, is a modified version of a peptide aimed at addressing erectile dysfunction (ED) and female sexual dysfunction. The study reviewed the progress of PT-141, noting that it had completed a phase IIb trial and was preparing for phase III trials.

  • Researchers found that PT-141 is a synthetic analog of the peptide PT-14.
  • The study noted that a phase IIb trial for ED was completed in September 2003.
  • Palatin planned to initiate phase III trials for PT-141 in early 2005.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.