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PT-141

Bremelanotide · Vyleesi

Sexual HealthPhase III
From$2.10/mgCompare prices
MW
1025.2g/mol
Formula
C50H68N14O10

PT-141, also known as Bremelanotide, is a cyclic heptapeptide and a synthetic analog of the melanocortin peptide PT-14. Researchers primarily study it for its potential applications in addressing erectile dysfunction (ED) and female sexual dysfunction. Key findings from clinical trials indicate that PT-141 may enhance sexual functionality in both males and females, with studies suggesting improved erectile responses when co-administered with phosphodiesterase type 5 inhibitors like sildenafil. Current research status includes completed phase IIb trials and plans for pivotal phase III trials to further evaluate its efficacy and safety.

Chemical Profile

Chemical Profile

Chemical structure
Chemical Structure
FormulaC50H68N14O10
Molecular Weight1025.2 g/mol
CAS Number189691-06-3
PubChem CID9941379
ChEMBL IDCHEMBL5315036

Half-Life

SCSubcutaneous

~2 to 4 hours

INIntranasal

Not applicable

POOral

Poor bioavailability

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

Mechanism

Mechanism of Action

PT-141 acts as a melanocortin receptor agonist, primarily targeting the melanocortin-4 receptor (MC4R) in the central nervous system, which is involved in the regulation of sexual arousal and erectile function. Its mechanism may involve the activation of the NO/cGMP signaling pathway, enhancing erectile response through increased nitric oxide production and subsequent vasodilation. Although the precise signaling pathways and biological processes are not fully understood, PT-141's efficacy suggests a complex interplay between central nervous system activation and peripheral vascular responses.

Research

17 Research Publications

802

Total Citations

6

Human/RCT

3.3

Avg. Influence

2023

Latest

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#01

Selective facilitation of sexual solicitation in the female rat by a melanocortin receptor agonist.

AnimalInfluence5.0
123
Researchers observed that PT-141 selectively stimulated solicitational behaviors in female rats without affecting other sexual behaviors, indicating its potential role in addressing female sexual desire disorders.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#02

Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction.

HumanInfluence3.0
119
The study demonstrated that PT-141 administration resulted in a significant erectile response in healthy males and patients with erectile dysfunction, with a favorable safety profile.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#03

An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist.

Human
111
The study demonstrated that bremelanotide (PT-141) positively affected sexual desire and arousal in premenopausal women with sexual arousal disorder, indicating its potential for further evaluation.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#04

PT-141: a melanocortin agonist for the treatment of sexual dysfunction.

HumanInfluence8.0
104
Researchers observed that PT-141 administration in humans resulted in a rapid, dose-dependent increase in erectile activity, supporting its potential for addressing sexual dysfunction.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#05

Evaluation of the safety, pharmacokinetics and pharmacodynamic effects of subcutaneously administered PT-141, a melanocortin receptor agonist, in healthy male subjects and in patients with an inadequate response to Viagra.

HumanInfluence2.0
90
Researchers observed that subcutaneous PT-141 administration elicited significant erectile responses in patients with inadequate response to Viagra, indicating its potential as an alternative treatment for erectile dysfunction.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#06

Melanocortins in the treatment of male and female sexual dysfunction.

ReviewInfluence1.0
57
Researchers observed that melanocortinergic agents, including PT-141, may effectively promote sexual desire and arousal in both male and female sexual dysfunction.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#07

Melanocortin receptors, melanotropic peptides and penile erection.

ReviewInfluence1.0
50
The review highlighted that activation of melanocortin receptors may facilitate penile erection, with PT-141 showing promise in phase II trials as a centrally mediated treatment for erectile dysfunction.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#08

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.

HumanInfluence3.0
44
The study demonstrated that co-administration of PT-141 and sildenafil significantly enhanced erectile response in men with erectile dysfunction compared to sildenafil alone.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#09

Medical Treatment of Female Sexual Dysfunction.

Nappi Rossella E, et al. · The Urologic clinics of North America · 2022

Review
33
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.

Key findings

  1. 01Researchers observed that flibanserin and bremelanotide are effective for premenopausal women with low sexual desire.
  2. 02Transdermal testosterone was noted to be effective for postmenopausal women experiencing similar issues.
  3. 03The study highlighted that menopause hormone therapy is crucial for managing symptoms in women during midlife.
PubMed
#10

Bremelanotide for Treatment of Female Hypoactive Sexual Desire.

Edinoff Amber N, et al. · Neurology international · 2022

Review
24
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.

Key findings

  1. 01Bremelanotide was recently approved by the FDA for treating HSDD in women.
  2. 02Researchers observed improvements in sexual desire and arousal after using bremelanotide.
  3. 03The treatment targets both biological and psychosocial factors related to HSDD.
PubMed
Safety

Safety & Handling

Research Gaps

While initial phase I/II trials for PT-141 have been conducted, there is a lack of large-scale randomized controlled trials specifically assessing its long-term safety and efficacy in diverse populations. Additionally, the precise mechanisms by which PT-141 exerts its effects on sexual functionality in both males and females remain unclear, necessitating further investigation into its pharmacodynamics and potential interactions with other ED treatments.

Solubility

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

Storage & Handling

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

Safety information is derived from published research and may not reflect all known risks. This is not medical advice.

Legal Status

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.

Community Insights

Community Insights

Publications per Year

15 total
2
03
5
04
2
05
2
06
2
07
1
25
1
26
Pricing

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Mechanism

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Mechanism

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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer