Paragon Sports Medicine

PT-141

PT-141, also known as Bremelanotide, is a synthetic cyclic heptapeptide derived from alpha-melanocyte-stimulating hormone (α-MSH) that activates melanocortin receptors, including melanocortin-3 and melanocortin-4 receptors (MC3R/MC4R). Originally developed as a derivative of the tanning peptide Melanotan II, PT-141 represents a novel approach to sexual dysfunction treatment by targeting central nervous system pathways rather than peripheral vascular mechanisms. Through activation of melanocortin-3 and melanocortin-4 receptors (MC3R/MC4R) in the hypothalamus and limbic regions, PT-141 enhances sexual desire and arousal through neurogenic pathways.

This peptide has gained FDA approval as Vyleesi for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women and demonstrates significant efficacy in clinical studies for both male and female sexual dysfunction. PT-141's unique central mechanism of action, rapid onset of effects, and distinct pharmacological profile distinguish it from traditional sexual dysfunction treatments, making it a valuable therapeutic option for patients unresponsive to conventional therapies.

Chemical structure diagram of Bremelanotide showing its molecular bonds and elements.

Overview

PT-141 demonstrates high water solubility and excellent bioavailability via subcutaneous and intranasal administration routes. The peptide exhibits selective receptor binding affinity for melanocortin receptors, with minimal cross-reactivity to other receptor systems. It is metabolized primarily through hepatic pathways and eliminated via renal excretion within 24 hours post-administration.

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Chemical structure & Properties

  • Molecular Formula: C50H68N14O10
  • Molecular Weight: 1025.16 Da
  • Sequence: Cyclic heptapeptide: Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
  • Half-life: Approximately 2.5 hours (plasma elimination)
  • Stability: Stable synthetic peptide with resistance to enzymatic degradation

Mechanism of Action

PT-141 exerts its therapeutic effects through selective activation of melanocortin receptors in the central nervous system:

Safety Profile and Considerations

Clinical Safety Data

Extensive clinical trials across multiple populations demonstrate:

  • Generally well-tolerated with predictable side effect profile
  • Transient blood pressure increases and heart-rate decreases can occur after each dose. Vyleesi is contraindicated in uncontrolled hypertension and known cardiovascular disease.
  • Side effects are dose related, and only the 1.75 mg dose is approved
  • Bremelanotide slows gastric emptying and can reduce or delay absorption of oral medications; it should not be used with oral naltrexone

Common Side Effects

Common Effects at the Approved 1.75 mg Dose:

  • Nausea (most common, reported in approximately 40% of patients at the approved dose)
  • Facial flushing and transient blood pressure elevation
  • Headache and injection site reactions
  • Temporary loss of appetite

Unique Considerations:

  • Focal hyperpigmentation may occur and may not resolve after stopping.
  • Individual variation in nausea sensitivity
  • Single fixed 1.75 mg dose, with no titration. No more than one dose in 24 hours and no more than eight doses per month.

Potential Concerns

Cardiovascular Considerations:

  • Transient blood pressure effects requiring monitoring in cardiovascular patients
  • Potential interactions with antihypertensive medications
  • Caution advised in patients with unstable cardiovascular disease

Melanocortin System Effects:

  • Potential influence on appetite and weight regulation
  • Theoretical concerns about long-term melanocortin receptor stimulation
  • Limited data on extended use beyond approved treatment protocols

Contraindications

PT-141 should be avoided in:

  • Pregnancy and breastfeeding (known to cross placental barrier)
  • Uncontrolled hypertension or cardiovascular instability
  • Known hypersensitivity to melanocortin receptor agonists
  • Active eating disorders (due to appetite suppression effects)

Regulatory Status and Legal Considerations

Regulatory information current as of 28 August 2026. This is a summary, not legal or medical advice, and status can change.

FDA Status

  • Classification: Prescription medication (Vyleesi)
  • Approval Status: Approved for HSDD in premenopausal women (June 2019)
  • Indication: Treatment of hypoactive sexual desire disorder
  • Regulatory Position: Full FDA approval with established safety and efficacy profile

International Status

  • Other Jurisdictions: Regulatory submissions in progress in multiple countries
  • Off-Label Use: Permitted under physician supervision for approved indications

Legal Availability

  • Commercial Status: FDA approved as Vyleesi for one specific indication. Not approved for any other use.
  • Market Presence: Distributed through specialty pharmacies
  • Quality Control: Full pharmaceutical manufacturing and quality standards
  • Clinical Use: Approved for clinical use under medical supervision
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Conclusion

What the evidence supports

PT-141 (bremelanotide) is a melanocortin-receptor agonist that acts on central nervous system pathways involved in sexual desire. It is FDA approved as Vyleesi for hypoactive sexual desire disorder in premenopausal women, supported by controlled clinical trials; uses outside that indication are off-label and are not established by the same evidence. Nothing on this page is an offer to prescribe or supply. This page summarizes the published research and nothing further.

PT-141 SCIENTIFIC

DATA SUMMARY

Parameter
Molecular Weight
Amino Acid Length
Half-Life
Bioavailability
Detection Window
Value
1025.16 Da
7 residues (cyclic)
~2.5 hours (plasma)
High via SC and intranasal
Up to 24 hours (urine)
Application
Female HSDD
CNS Sexual Pathways
Reported outcome (model)
Significant desire improvement, reduced distress
Enhanced melanocortin receptor activation
Study Type
FDA Approval Trials
Population
1,247 premenopausal women
Results
Statistically significant HSDD improvement
Limitations
Limited to premenopausal women
Parameter
Acute Toxicity
Organ Toxicity
Adverse Events
Long-term Safety
Finding
Safety established at the approved 1.75 mg dose; higher doses are not approved
No significant organ toxicity reported
Nausea (40-50%), flushing, headache
24-week safety data established
Authority
FDA
WADA Status
DEA
Classification
Prescription Drug (Vyleesi)
Prescription medication
Unscheduled
Status
Approved for female HSDD (2019)
Not prohibited in sports
Not controlled substance

About this library

This library is published for education. It summarizes published research on compounds studied in this field. Many have no approved medical use, and several cannot lawfully be compounded in the United States. The presence of a page here does not mean Paragon offers that compound. Nothing on these pages is an offer to treat.

This page is general education about a compound studied in this field. Nothing here is medical advice, a recommendation, or an offer to prescribe or supply. A page appearing in this library does not mean Paragon Sports Medicine offers that compound.

Disclaimer: This information is provided for educational purposes only and does not constitute medical advice. PT-141 (Vyleesi) is FDA-approved for specific indications and requires prescription and medical supervision. Patients should consult with qualified healthcare providers before considering any peptide therapy.

Statements on this page have not been evaluated by the FDA and are not intended to diagnose, treat, cure, or prevent any disease. Many peptides described here are not FDA approved for the uses discussed, and some cannot lawfully be compounded in the United States. Nothing on this page is medical advice or a recommendation for any individual. Whether any therapy is appropriate depends on your history, your laboratory results, and a clinical evaluation. Individual results vary. This page is published for education. Use of this site does not create a physician-patient relationship.