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Sexual Health — MC4R Agonist✓ FDA Approved

PT-141

Also known as: Bremelanotide · Vyleesi

MW

1025.18 Da

Amino Acids

7 AA

Half-Life

2-3 hours

Route

SubQ

CAS

189691-06-3

Formula

C50H68N14O10

Amino Acid Sequence

Ac-Nle-cyclo(Asp-His-D-Phe-Arg-Trp-Lys)-OH

Mechanism of Action

PT-141 (Bremelanotide) is a cyclic heptapeptide melanocortin receptor agonist, primarily targeting MC4R. It is FDA-approved as Vyleesi for hypoactive sexual desire disorder (HSDD) in premenopausal women.

CENTRAL MECHANISM — MC4R ACTIVATION: Unlike PDE5 inhibitors (sildenafil, tadalafil) which work peripherally on penile blood vessels, PT-141 acts centrally in the brain. MC4R activation in the hypothalamic paraventricular nucleus → dopaminergic signaling in mesolimbic reward pathways → increased sexual desire and arousal.

BOTH SEXES: Works in both men and women by activating the same central arousal pathway. FDA approval is for women (HSDD), but Phase II data exists for male erectile dysfunction.

DERIVED FROM MT-2: PT-141 was developed from Melanotan II research after MT-2's pronounced sexual effects were discovered. PT-141 has improved MC4R selectivity — less tanning and fewer melanocortin side effects than MT-2, though some occur.

VASCULAR-INDEPENDENT: Because the mechanism is central (brain) rather than peripheral (blood vessels), PT-141 may work in patients who don't respond to PDE5 inhibitors.

Dosing Protocol

Low Dose

███ – ███ mcg/day

Standard Dose

███ mcg/day

High Dose

███ – ███ mcg/day

Dosing protocols are for paid members

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Frequency

As needed, ≥45 min before sexual activity.

Half-Life

2-3 hours

Reconstitution Guide

Full reconstitution protocol with BAC water volumes, concentration math, and units-to-draw per dose is available on the Clinical plan.

Unlock reconstitution guide →

Clinical Warnings

Nausea (40% in trials — most common side effect).

Transient blood pressure increase.

Facial flushing.

Hyperpigmentation with repeated use.

Not for uncontrolled hypertension/CV disease.

Max 8 doses/month per FDA.

Only approved for premenopausal women — male use off-label.

Contraindications

Absolute

Uncontrolled hypertension

Cardiovascular disease

Pregnancy

Relative Cautions

Controlled hypertension

Hepatic impairment

Renal impairment

Side Effect Profile

Mild

  • Nausea
  • Flushing
  • Headache
  • Injection site reactions

Moderate

  • Transient hypertension
  • Skin hyperpigmentation
  • Vomiting

Severe (Rare)

  • Severe hypertension
  • Cardiovascular events in at-risk patients

Synergistic Peptides

Melanotan IIKisspeptin

Common Stacks

Melanotan II

Research Status

FDA APPROVED (Vyleesi). PMID 31211618 (Clayton 2016): Phase III HSDD RCT — FDA approval basis. PMID 16417600 (Rosen 2004): Erectile function Phase II in men. One of few FDA-approved peptide therapeutics.

Frequently Asked Questions

How does PT-141 work?

PT-141 (Bremelanotide) is a cyclic heptapeptide melanocortin receptor agonist, primarily targeting MC4R. It is FDA-approved as Vyleesi for hypoactive sexual desire disorder (HSDD) in premenopausal women. CENTRAL MECHANISM — MC4R ACTIVATION: Unlike PDE5 inhibitors (sildenafil, tadalafil) which work peripherally on penile blood vessels, PT-141 acts centrally in the brain. MC4R activation in the hypothalamic paraventricular nucleus → dopaminergic signaling in mesolimbic reward pathways → increased

What is the standard dose of PT-141?

PT-141 dosing protocols are available with a ClinPep Clinical subscription. Dosing varies by indication and patient factors — consult a licensed healthcare provider. General frequency: As needed, ≥45 min before sexual activity.

What is the half-life of PT-141?

The half-life of PT-141 is 2-3 hours. This determines optimal dosing frequency and timing.

Who should not use PT-141?

PT-141 is absolutely contraindicated in: Uncontrolled hypertension; Cardiovascular disease; Pregnancy. Use with caution in: Controlled hypertension; Hepatic impairment; Renal impairment.

What are the side effects of PT-141?

Common mild side effects include: Nausea, Flushing, Headache, Injection site reactions. Moderate effects: Transient hypertension, Skin hyperpigmentation, Vomiting.

What peptides stack well with PT-141?

PT-141 is commonly stacked with: Melanotan II, Kisspeptin.

How do you reconstitute PT-141?

PT-141 is reconstituted with bacteriostatic water. Exact volumes, concentrations, and units-to-draw calculations are available in the ClinPep Clinical plan. Always follow your compounding pharmacy's instructions.

How long should you cycle PT-141?

PT-141 cycle protocols vary by indication. Detailed cycle length, on/off schedules, and monitoring guidelines are available with ClinPep Clinical access. Consult your healthcare provider for personalized cycling guidance.

References & Citations

10 PubMed studies · 3 clinical trials

Strategies for Treating Sexual Health Concerns After Breast and Gynecologic Cancer.

Mihulka Olivia, Curran Melissa, Narasimhan Raksha M, Moore Jessica F et al.. Journal of minimally invasive gynecology. 2025

PubMed: 41419078DOI ↗C — Research Article

Sexual dysfunction is a common but underrecognized sequelae of breast and gynecologic cancer treatment. Many patients experience symptoms of genitourinary syndrome of menopause, including vaginal dryn

Practical considerations and emerging approaches for the management of vasomotor and sexual symptoms in breast cancer patients on endocrine therapies.

Fuhrman Jessica, Yun Jina, Indorf Amy. Expert review of clinical pharmacology. 2025

PubMed: 41088800DOI ↗C — Research Article

Vasomotor symptoms (VMS) and decreased libido are common menopausal symptoms. Patients with breast cancer receiving endocrine therapy experience new or worsening menopausal symptoms. Pharmacologic the

Female Sexual Desire, Arousal, and Orgasmic Dysfunctions: A Systematic Review and Meta-Analysis of Treatment Options.

Toledo Rafaela Germano, Winkelman William D, Reyes-Gonzalez Daniela, Bergeron Sophie et al.. Journal of minimally invasive gynecology. 2026

PubMed: 40543759DOI ↗C — Research Article

To conduct a systematic review and meta-analysis of treatments for female sexual desire, arousal, and orgasmic dysfunction in patients without sexual pain conditions. MEDLINE, Embase, Web of Science,

2024 SOGC, 2024 NCCN, 2022 ESO-ESMO, and 2018 ASCO: a comparison of female cancer survivorship guidelines for the management of sexual health concerns.

Bhinder Jashmira K, Kennedy Samantha K F, Faouk Al Aadah Carmen, Al-Khaifi Muna. Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer. 2025

PubMed: 40518469DOI ↗C — Research Article

Female cancer survivors often experience sexual dysfunction, which is a significant and increasingly recognized aspect of survivorship. This review compares guidelines from the American Society of Cli

Novel Pharmacologic Treatments of Female Sexual Dysfunction.

How Andrew, Jowdy Christopher, Novatcheva Elli, Clayton Anita H. Clinical obstetrics and gynecology. 2025

PubMed: 39846877DOI ↗C — Research Article

This review evaluates pharmacologic treatments for female sexual dysfunction (FSD), focusing on hypoactive sexual desire disorder (HSDD). We provide clinically relevant applications for Food and Drug

Female Syrian hamster analyses of bremelanotide, a US FDA approved drug for the treatment of female hypoactive sexual desire disorder.

Borland Johnathan M, Kohut-Jackson Abigail L, Peyla Anna C, Hall Megan Al et al.. Neuropharmacology. 2025

PubMed: 39793696DOI ↗C — Research Article

Hypoactive sexual desire disorder (HSDD) is the most reported sexual dysfunction among premenopausal women worldwide. Bremelanotide, trade name Vyleesi, has been approved by the United States Food and

Gap in Sexual Dysfunction Management Between Male and Female Patients Seen in Primary Care: An Observational Study.

Stanley Elizabeth E, Pfoh Elizabeth, Lipold Laura, Martinez Kathryn. Journal of general internal medicine. 2025

PubMed: 39231849DOI ↗C — Research Article

Female sexual dysfunction (FSD), defined as clinically distressing problems with desire, arousal, orgasm, or pain, affects 12% of US women. Despite availability of medications for FSD, primary care ph

Understanding the Interplay Between Premenstrual Dysphoric Disorder (PMDD) and Female Sexual Dysfunction (FSD).

Gollapudi Mahati, Thomas Angelica, Yogarajah Angelina, Ospina David et al.. Cureus. 2024

PubMed: 39036127DOI ↗C — Research Article

Premenstrual dysphoric disorder (PMDD) is a severe variant of premenstrual syndrome (PMS), categorized as a mood disorder due to marked symptoms of depression and anxiety, compounded with severe physi

Registered Clinical Trials

Bremelanotide in Premenopausal Women With Female Sexual Arousal Disorder and/or Hypoactive Sexual Desire Disorder

NCT01382719COMPLETEDPHASE2

A Phase 3, Bridging, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group Trial to Evaluate the Efficacy and Safety of Subcutaneously Administered Bremelanotide in Premenopausal Women With Hypoactive Sexual Desire Disorder (With or Without Decreased Arousal)

NCT04943068COMPLETEDPHASE3

A Phase IIb, Multicenter, Open-Label, Prospective Study of Bremelanotide in Diabetic Kidney Disease

NCT05709444COMPLETEDPHASE2

Symptom Indications

Low libidoErectile dysfunctionHypoactive sexual desire disorderFemale sexual dysfunction

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Complete PT-141 Protocol

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This information is for educational and research reference purposes only. ClinPep does not provide medical advice, diagnosis, or treatment recommendations. All protocols should be reviewed by a licensed healthcare provider.