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PT-141

Bremelanotide · Vyleesi

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

PT-141 is a synthetic cyclic heptapeptide analog of alpha-melanocyte-stimulating hormone (α-MSH) that functions as an agonist at melanocortin receptors, particularly MC3R and MC4R, in the central nervous system. Researchers primarily study PT-141 for its potential applications in addressing erectile dysfunction and female sexual dysfunction. Key findings from studies indicate that administration of PT-141 can lead to a dose-dependent increase in erectile activity in both healthy subjects and patients with erectile dysfunction, with effects observed within approximately 30 minutes of administration. Additionally, the peptide has demonstrated a favorable safety profile, with common side effects including flushing and nausea. Current research is focused on advancing PT-141 through clinical trials, with pivotal phase III studies planned 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 an agonist at melanocortin receptors, primarily MC3R and MC4R, which are expressed in the central nervous system. Its mechanism involves the activation of neuronal pathways in the hypothalamus, leading to increased sexual arousal and erectile function, although the precise signaling pathways involved remain to be fully elucidated. Unlike traditional erectile dysfunction treatments that target the NO/cGMP pathway, PT-141's effects are mediated through central nervous system mechanisms rather than peripheral vasodilation.

Research

18 Research Publications

900

Total Citations

6

Human/RCT

3.1

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
The study demonstrated that PT-141 selectively stimulates solicitational behaviors in female rats without affecting other sexual behaviors, indicating its potential role in regulating female sexual desire.
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 intranasal PT-141 significantly increased 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
112
Researchers observed that bremelanotide (PT-141) significantly increased reports of sexual desire in premenopausal women with sexual arousal disorder compared to placebo.
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.

AnimalInfluence8.0
105
The study demonstrated that PT-141 administration in rats and nonhuman primates resulted in a significant increase in erectile activity, indicating its potential as a treatment for sexual dysfunction.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#05

Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization.

ReviewInfluence2.0
96
Researchers observed that PT-141, a new melanocortin analog, has shown promise in initial clinical trials for improving sexual functionality in both males and females.
0.01 mg/kgsubcutaneous(human)2 consecutive weeks0.005 mg/kgsubcutaneous(human)2 consecutive weeks0.03 mg/kgsubcutaneous(human)2 consecutive weeks0.025 mg/kgsubcutaneous(human)2 consecutive weeks6 mgsubcutaneous(human)not mentioned0.1 mg/kgintravenous(rat)not mentioned0.3 mg/kgintravenous(rat)not mentioned1 mg/kgintravenous(rat)not mentioned0.1 µgwithin the paraventricular nucleus(rat)not mentioned1 µgwithin the paraventricular nucleus(rat)not mentioned3 mg/kgintraperitoneal(rat)not mentioned
PubMed
#06

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 administration of PT-141 resulted in significant erectile responses in patients with erectile dysfunction who had inadequate responses to Viagra.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#07

Melanocortins in the treatment of male and female sexual dysfunction.

ReviewInfluence1.0
57
The review discusses the potential of melanocortinergic agents, including PT-141, in addressing both male and female sexual dysfunction, supported by clinical trial data.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#08

Melanocortin receptors, melanotropic peptides and penile erection.

ReviewInfluence1.0
50
Researchers observed that activation of central melanocortin receptors may facilitate penile erection, suggesting that PT-141 could provide an alternative therapeutic approach for erectile dysfunction.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#09

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 resulted in a significantly enhanced erectile response compared to sildenafil alone in patients with erectile dysfunction.
7.5 mgintranasal(human)0.3 to 10 mgsubcutaneous(human)4 mg(human)6 mg(human)20 mgintranasal(human)
PubMed
#10

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
Safety

Safety & Handling

Research Gaps

While PT-141 has shown promise in short-term studies, there is a lack of long-term safety and efficacy data from extensive human trials, particularly regarding its effects on female sexual dysfunction. Additionally, the precise mechanisms by which PT-141 activates melanocortin receptors in the central nervous system and the potential for adverse effects with prolonged use remain unclear.

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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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