OtherPeptideEvidence B3 cited

PT-141

Bremelanotide

aka Bremelanotide · Vyleesi · PT141

A melanocortin receptor agonist researched for enhancing sexual desire via central nervous system pathways.

Molecular wt

1025.2g/mol

Formula

C50H68N14O10

CAS

189691-06-3

Half-life

2.7 h

clinical

Tmax

1 h

PubChem

9941379

Sequence

Read this before quoting the sequence

Cyclic synthetic heptapeptide analogue of alpha-MSH. The VYLEESI label gives the structure as 'Ac-Nle-cyclo-(Asp-His-D-Phe-Arg-Trp-Lys)-OH'. A one-letter string is not given because the peptide contains norleucine and a D-amino acid and is cyclised through an Asp-Lys lactam bridge.

Source ↗

Mechanism of action

PT-141, also known as Bremelanotide, works by activating melanocortin receptors in the central nervous system. This activation leads to increased sexual arousal and desire by modulating neurotransmitter release. It primarily targets the MC3 and MC4 receptors, which are involved in sexual function regulation.

What the evidence actually shows

Grade B

There are several human clinical trials demonstrating PT-141's efficacy in enhancing sexual desire and function, particularly in women with hypoactive sexual desire disorder (HSDD). These studies show significant improvements in sexual desire scores compared to placebo. However, more research is needed to fully understand long-term safety and efficacy.

Regulatory status

Status

Approved prescription medicine (US).

Approved as

VYLEESI (bremelanotide) injection, indicated for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD).

Clinical stage

Marketed / approved.

prescription_only

In the UK, PT-141 is available by prescription only for the treatment of hypoactive sexual desire disorder.

Source ↗

Pharmacokinetics

Half-life

2.7 h

Tmax

1 h

Absorption

subcutaneous

Elimination

renal

Washout

2 days

Low-confidence pharmacokinetics

These figures are recorded as clinical rather than measured in a published PK study. Treat them as an order of magnitude. Anything downstream of them — accumulation, steady state, washout — inherits that uncertainty.

Dosing — what backs each figure

PT-141 (bremelanotide) is FDA-approved as VYLEESI at a fixed 1.75 mg subcutaneous dose taken at least 45 minutes before anticipated sexual activity, capped at one dose per 24 hours and eight per month, for premenopausal women with acquired generalized HSDD. There is no approved dose for men, for postmenopausal women, or for any performance indication, and the label directs discontinuation at 8 weeks without benefit.

ClinicalApproved labelling or a published human trial

1.75 mg subcutaneously in the abdomen or thigh, at least 45 minutes before anticipated sexual activity; no more than one dose in 24 hours and no more than 8 doses per month; discontinue after 8 weeks if symptoms have not improved
premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD); explicitly not indicated for postmenopausal women, men, or performance enhancement · subcutaneous
FDA label VYLEESI (bremelanotide injection), NDA 210557, initial US approval 2019 ↗

Handling and storage

Lyophilized

No compound-specific data documented

Reconstituted

Not applicable — VYLEESI is supplied as a ready-to-use single-dose autoinjector.

VYLEESI label, Storage and Handling: 'Store at or below 25 °C (77 °F). Do not freeze. Protect from light.' No refrigeration is required and no lyophilised presentation is marketed.

Source ↗

→ Reconstitution walkthrough → Reconstitution calculator

Safety

Commonly reported

·Nausea
·Flushing
·Headache

Rarely reported

·Severe hypertension
·Cardiovascular events

Contraindications

·Uncontrolled hypertension
·Cardiovascular disease

Drug interactions

·Naltrexone - may reduce PT-141 efficacy due to opioid receptor interactions

Nausea, flushing, headache, transient blood-pressure rise

Reported combinations

Reported as synergistic

·L-arginine - may enhance vasodilation effects

Reported as antagonistic

·Alcohol - may increase risk of adverse effects

Combination claims in this dataset are largely unsourced and should be treated as folk knowledge until a citation appears beside them.

References (3)

Kingsberg SA, Clayton AH, Portman D, et al. (2019) Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials. ↗
Obstetrics & GynecologyPMID 31599840DOI
The two RECONNECT Phase 3 randomised placebo-controlled trials in premenopausal women with HSDD; the pivotal evidence supporting FDA approval of bremelanotide.
Clayton AH, Lucas J, DeRogatis LR, Jordan R (2017) Phase I Randomized Placebo-controlled, Double-blind Study of the Safety and Tolerability of Bremelanotide Coadministered With Ethanol in Healthy Male and Female Participants. ↗
Clinical TherapeuticsPMID 28189361DOI
Phase 1 study showing subcutaneous bremelanotide co-administered with ethanol did not produce clinically meaningful additional blood-pressure or orthostatic effects.
Sauter M, Uhl P, Burhenne J, Haefeli WE (2020) Ultra-sensitive quantification of the therapeutic cyclic peptide bremelanotide utilizing UHPLC-MS/MS for evaluation of its oral plasma pharmacokinetics. ↗
Journal of Pharmaceutical and Biomedical AnalysisPMID 32353679DOI
Validated UHPLC-MS/MS assay for bremelanotide in plasma, used to characterise its plasma pharmacokinetics.

Data provenance

Chemistry and citations on this page were checked against primary sources on 2026-08-14. Values that could not be verified were left blank rather than filled with a plausible guess.

Could not verify
regulatory.wada

Research use only

This profile is educational reference material. It is not medical advice, not a prescription, and not an endorsement of self-administration. Compounds discussed here are research chemicals and most are not approved for human therapeutic use.

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