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PT-141 (Bremelanotide)

Desire, reignited from within

Injection, Nasal · Prescription

Educational content. This page describes PT-141 (Bremelanotide) for informational purposes only and is not medical advice, diagnosis, or treatment. Consult a licensed provider before starting, stopping, or modifying any therapy.

Researched and maintained by the PepHookup team. Regulatory status last verified April 12, 2026.

Primary Use
A cyclic 7-residue melanocortin receptor agonist that acts centrally to drive arousal.
Administration
injection, nasal
Typical Cycle
Ongoing, as-needed
Legal Status
Legal
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Key Benefits

Restores Sexual Desire in Women

The two pivotal RECONNECT Phase 3 trials in 1,267 premenopausal women with HSDD showed statistically significant gains in sexual desire and reductions in the distress tied to low desire over 24 weeks.[1]

Works Through the Brain

Bremelanotide is a melanocortin receptor agonist that acts on MC4R in the hypothalamus. A 2022 brain-imaging study in women with HSDD showed it changes activity in brain regions that process sexual cues, confirming a central rather than peripheral mechanism.[4][5][7]

On-Demand Dosing

A single 1.75 mg subcutaneous dose is self-administered at least 45 minutes before anticipated activity. Absolute bioavailability is about 100% and there is no daily medication to take.[6]

Studied in Men Who Failed Viagra

In early subcutaneous studies, bremelanotide produced statistically significant erectile responses in men with ED, including those with an inadequate response to sildenafil. Use in men remains off-label and based on older, smaller trials.[9][10][11]

FDA-Approved with Extension Data

Approved by the FDA in 2019 as Vyleesi, with a 52-week open-label extension that showed sustained desire scores and no new safety signals. It is one of only two FDA-approved treatments for HSDD.[2][6]

What is PT-141 (Bremelanotide)?

PT-141 (bremelanotide, marketed as Vyleesi) is a synthetic cyclic 7-amino-acid peptide, a melanocortin receptor agonist modeled on alpha-melanocyte-stimulating hormone (alpha-MSH). In June 2019 the FDA approved it for acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women, the first and one of the few approved therapies that addresses desire through the central nervous system rather than peripheral blood flow.

Bremelanotide grew out of melanocortin research on melanotan II, when investigators noticed effects on sexual arousal that were separate from the tanning the compound was originally studied for. Palatin Technologies refined it into PT-141 and carried it through a clinical program that progressed from early intranasal studies to the subcutaneous formulation that ultimately reached approval.

How Does It Work?

Bremelanotide activates melanocortin-4 receptors (MC4R) in the hypothalamus, a region central to sexual motivation. Preclinical and pharmacology work links this MC4R activity to dopamine signaling in pathways that govern the desire, or appetitive, component of sexual behavior rather than the purely physical response.

A 2022 functional MRI study in women with HSDD found that an MC4R agonist altered activity in brain regions that process sexual stimuli, providing direct human evidence that the effect originates centrally. This contrasts with PDE5 inhibitors such as sildenafil, which act peripherally on the nitric oxide and cGMP pathway to support blood flow.

After a 1.75 mg subcutaneous dose, bremelanotide reaches peak plasma concentration at a median of about 1 hour with absolute bioavailability near 100%, and has a terminal half-life of roughly 2.7 hours. As a small peptide it is cleared by hydrolysis of its amide bonds, which fits the on-demand, take-as-needed dosing model.

Mechanism of Action

Bremelanotide is a melanocortin receptor agonist that activates MC4R in the hypothalamus, engaging dopamine-linked circuits that drive sexual desire and motivation. Unlike PDE5 inhibitors, which act on peripheral vasodilation, it addresses desire at its neurological source. Its broader melanocortin activity (including MC1R) explains the skin-pigmentation effect seen at higher or more frequent dosing.

PT-141MC4R ActivationHypothalamic mPOADopamine ReleasePresynaptic signalingMC1R BindingMelanocyte stimulationPVN / NO PathwayDescending neural signalsSexual DesireEnhanced appetitivesexual motivationCentral ArousalNeurological pathwayactivationMelanocyte EffectsMild tanning response(secondary)Erectile SupportNO-mediated peripheralvascular effectsCentral Nervous System Desire Enhancement

Clinical Evidence

RECONNECT Phase 3 Trials (Pivotal)

Two identical randomized, double-blind, placebo-controlled multicenter RCTs (NCT02333071, NCT02338960)1,267 premenopausal women with HSDD

Over 24 weeks, bremelanotide 1.75 mg significantly improved the FSFI desire-domain score (integrated effect 0.35, P<.001) and reduced sexual-desire-related distress on FSDS-DAO item 13 (integrated effect -0.33, P<.001) versus placebo.

Kingsberg SA, Clayton AH, Portman D, et al. · Obstet Gynecol, 134(5):899-908 (2019) · PubMed

Long-Term Open-Label Extension

52-week open-label extension of the RECONNECT trialsRECONNECT completers who elected to continue

Desire improvements were sustained through the open-label phase with no new safety signals. The most common adverse events remained nausea, flushing, and headache, which tended to lessen over time.

Simon JA, Kingsberg SA, Portman D, et al. · Obstet Gynecol, 134(5):909-917 (2019) · PubMed

Phase 2b Dose-Finding Trial

Randomized, double-blind, placebo-controlled dose-ranging studyPremenopausal women with female sexual dysfunction (HSDD and/or FSAD)

Identified 1.75 mg subcutaneous as the dose carried into Phase 3, with improvements in the number of satisfying sexual events and in sexual function measures relative to placebo.

Clayton AH, Althof SE, Kingsberg SA, et al. · Womens Health (Lond), 12(3):325-37 (2016) · PubMed

Early Intranasal Study in Women

Placebo-controlled evaluation of subjective sexual responsePremenopausal women with female sexual arousal disorder

A single intranasal dose of bremelanotide, an alpha-MSH analog active at MC3R and MC4R, improved the subjective sexual response, an early signal from the intranasal development program that preceded the subcutaneous formulation.

Diamond LE, Earle DC, Heiman JR, et al. · J Sex Med, 3(4):628-638 (2006) · PubMed

Subcutaneous PK/PD Study in Men With ED

Dose-ranging study with RigiScan erectile assessmentHealthy men and men with ED who responded inadequately to Viagra

Subcutaneous PT-141 produced statistically significant erectile responses at doses above 1.0 mg, including in sildenafil non-responders, and was reported as safe and well tolerated. This is exploratory data; bremelanotide is not approved for men.

Rosen RC, Diamond LE, Earle DC, et al. · Int J Impot Res, 16(2):135-42 (2004) · PubMed

Dosing & Administration

Subcutaneous (FDA-approved, Vyleesi)

Dosage
1.75 mg via prefilled autoinjector
Frequency
As needed, at least 45 minutes before anticipated sexual activity
Cycle
Ongoing, as-needed

Subcutaneous (FDA-approved, Vyleesi): No more than one dose in any 24 hours; more than 8 doses per month is not recommended.

Dosing is set by a licensed prescriber. The FDA-approved dose is a single 1.75 mg subcutaneous injection into the abdomen or thigh, taken on an as-needed basis.

The duration of effect after a dose varies between individuals, so patients are guided to find their own optimal timing within the 45-minute-or-more window before activity.

Nausea is most pronounced with the first dose and improves for most people by the second; antiemetic therapy is an option for those who want to continue. Bremelanotide may slow gastric emptying and can markedly reduce the absorption of orally administered naltrexone, so that combination is avoided.

Side Effects & Safety

Common

  • Nausea: Reported by 40% in Phase 3 (vs 1.3% placebo); worst with the first dose, improves with continued use. About 13% used an antiemetic and about 8% discontinued.
  • Flushing: Warmth or redness, mostly of the face; reported by about 20% (vs 0.3% placebo) and generally transient.
  • Headache: Mild to moderate in most cases; reported by about 11% (vs 1.9% placebo).
  • Injection site reactions: Redness, swelling, or discomfort at the injection site; about 13% (vs 8.4% placebo).
  • Transient blood pressure increase: Maximal increases of about 6 mmHg systolic and 3 mmHg diastolic peaking 2-4 hours post-dose, with a small drop in heart rate; resolves within 12 hours.

Uncommon

  • Vomiting: Reported by about 5% (vs 0.2% placebo), generally alongside nausea.
  • Focal hyperpigmentation: Skin darkening from melanocortin activity, in about 1% at as-needed dosing; far more common with daily dosing. Resolution was not confirmed in all patients.

Safety Profile

In the pooled Phase 3 trials, the most common adverse reactions were nausea (40%), flushing (20%), injection site reactions (13%), and headache (11%), most of them mild to moderate and related to tolerability.

Bremelanotide transiently raises blood pressure (up to about 6 mmHg systolic, 3 mmHg diastolic) and slightly lowers heart rate after each dose, with values returning to baseline within 12 hours. It is contraindicated in uncontrolled hypertension or known cardiovascular disease, and is not recommended for those at high cardiovascular risk.

Liver injury is rare: clinical trials showed no clinically significant lab changes, and the NIH LiverTox database rates bremelanotide as a possible but rare cause of clinically apparent liver injury, with no reported cases of acute liver failure.

Contraindications

  • Uncontrolled or poorly managed hypertension (absolute)
  • History of stroke or myocardial infarction
  • Concurrent organic nitrate medications
  • Pregnancy or breastfeeding (adverse fetal effects in animals)
  • Not approved for postmenopausal women or men

Compare with Similar Peptides

PeptidePrimary UseAdministrationCycle LengthKey Differentiator
PT-141 (Bremelanotide)Sexual HealthInjection (as-needed)Ongoing as-neededThe only FDA-approved on-demand HSDD treatment that works centrally through melanocortin and dopamine pathways rather than peripheral blood flow
Melanotan 2Pigmentation and sexual function (no approved use)Subcutaneous injectionAbout 2 weeks in published trialsNon-selective melanocortin agonist that produces tanning, sexual arousal, and appetite suppression together, paired with safety concerns that kept it from approval and led regulators to flag it

Regulatory Status

FDA-Approved

Prescription

This peptide is an FDA-approved drug available via standard prescription.

Regulatory Detail

FDA-approved as Vyleesi for hypoactive sexual desire disorder (HSDD) in premenopausal women. Available via standard prescription.

FDA Action History

What do these terms mean?
503A compounding
Licensed pharmacies that prepare custom prescriptions for individual patients based on a physician's order. 503A is the section of the federal law that governs them.
503B outsourcing
FDA-registered facilities that compound in larger batches under stricter federal oversight (closer to a manufacturer than a pharmacy). Used mostly by hospitals and clinics.
Bulk drug substance
The active pharmaceutical ingredient a compounder starts with, before it's made into a finished medication.
Category 1
Interim bucket for bulk substances that have been nominated and don't appear to present significant safety risks. 503A pharmacies may compound them under FDA enforcement discretion while the agency continues its review. Not the same as FDA approval.
Category 2
Bulk substances the FDA has flagged for significant safety risks. 503A compounding carries FDA enforcement risk, so most pharmacies decline to prepare them and many physicians hesitate to prescribe them.
PCAC
Pharmacy Compounding Advisory Committee. The FDA advisory committee that reviews nominated bulk substances and recommends whether they belong in Category 1, Category 2, or on the final 503A Bulks List.

Last verified April 12, 2026. PepHookup tracks public FDA actions. This is not legal or medical advice.

Frequently Asked Questions

Research & References

  1. 1

    Kingsberg SA, Clayton AH, Portman D, et al. Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials.” Obstet Gynecol, 134(5):899-908 (2019)

  2. 2

    Simon JA, Kingsberg SA, Portman D, et al. Long-Term Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder.” Obstet Gynecol, 134(5):909-917 (2019)

  3. 3

    Clayton AH, Althof SE, Kingsberg SA, et al. Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial.” Womens Health (Lond), 12(3):325-37 (2016)

  4. 4

    Pfaus JG, Sadiq A, Spana C, Clayton AH The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women.” CNS Spectr, 27(3):281-289 (2022)

  5. 5

    Thurston L, Hunjan T, Mills EG, et al. Melanocortin 4 receptor agonism enhances sexual brain processing in women with hypoactive sexual desire disorder.” J Clin Invest, 132(19):e152341 (2022)

  6. 6

    Dhillon S, Keam SJ Bremelanotide: First Approval.” Drugs, 79(14):1599-1606 (2019)

  7. 7

    Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY PT-141: a melanocortin agonist for the treatment of sexual dysfunction.” Ann N Y Acad Sci, 994:96-102 (2003)

  8. 8

    Diamond LE, Earle DC, Heiman JR, et al. An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist.” J Sex Med, 3(4):628-638 (2006)

  9. 9

    Diamond LE, Earle DC, Rosen RC, Willett MS, Molinoff PB 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.” Int J Impot Res, 16(1):51-9 (2004)

  10. 10

    Rosen RC, Diamond LE, Earle DC, et al. 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.” Int J Impot Res, 16(2):135-42 (2004)

  11. 11

    Safarinejad MR, Hosseini SY Salvage of sildenafil failures with bremelanotide: a randomized, double-blind, placebo controlled study.” J Urol, 179(3):1066-71 (2008)

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