Bremelanotide (PT-141)

Classification

Melanocortin receptor agonist

Approval status

Approved medicine

Research status

Approved in the US (Vyleesi) for acquired, generalised hypoactive sexual desire disorder in premenopausal women, as labelled. PT-141 research-chemical products are not Vyleesi.

Molecular formula

Insufficient reliable evidence identified.

Molecular weight

Insufficient reliable evidence identified.

Sequence

Cyclic heptapeptide related to melanotan chemistry, developed as a sexual-dysfunction medicine in some markets.

Primary biological target

Melanocortin receptors (MC4R-preferring agonist as labelled)

Half-life

See Vyleesi USPI (hours-range after subcutaneous injection)

Routes investigated

Subcutaneous

Human evidence level

A — Approved clinical use / strong human evidence

A prescription melanocortin peptide in some countries for hypoactive sexual desire disorder. It is not a tanning product. Melanotan-II is a different, unapproved tanning peptide. Not sold here.

Synthetic cyclic heptapeptide melanocortin agonist; related historically to melanotan chemistry.

Established (labelled / textbook receptor pharmacology)

Bremelanotide is a melanocortin-receptor agonist; labelled sexual-desire effects are attributed primarily to central MC4R pathways. Peripheral tanning is not the labelled indication (contrast with unapproved melanotan products).

Affects sexual-response pathways in labelled use; also causes nausea and blood-pressure changes.

• Hypoactive sexual desire disorder

  A · Approved clinical use / strong human evidence

  Has been investigated and, in the US, approved for a defined premenopausal HSDD population.^[1]

Investigational findings are not proven clinical benefits unless an authority has labelled that indication.

Overall human evidence grade: A · Approved clinical use / strong human evidence

Animal, cell and in-vitro findings are listed separately from human effects.

Melanocortin biology.

This section does not provide personalised medical dosing. Values are those reported in papers or protocols. Animal mg/kg doses are not converted to human doses.

Doses reported in human studies

1. RECONNECT Phase 3

   Dose: 1.75 mg

   Route: Subcutaneous

   Frequency: As needed, with labelled maximum frequency

   Duration: 24 weeks core

   Population: Premenopausal women with HSDD

   Purpose: HSDD efficacy and safety

   ^[1]

Preclinical / animal study dosing

Insufficient reliable evidence identified.

Taken from regulator product information. This is not mixed with research-chemical schedules.

• FDA · United States

  Vyleesi (bremelanotide)

  Indication: Acquired, generalised HSDD in premenopausal women (see USPI limitations)

  Regimen: 1.75 mg subcutaneously as needed, no more than one dose in 24 hours and labelled monthly cap — verify current USPI.

  FDA Prescribing Information — Vyleesi

Half-life

See Vyleesi USPI (hours-range after subcutaneous injection)

Insufficient reliable evidence identified.

Nausea, flushing, injection-site reactions, headache. Transient blood-pressure increase.

Serious events. Focal hyperpigmentation reported; contraindicated in uncontrolled hypertension / CVD per label.

Pregnancy / lactation. Not indicated in pregnancy; see PI.

Unknowns. Absence of a published harm signal is not evidence of safety.

Contraindications. Cardiovascular cautions as per Product Information. Not for grey-market use.

Australia — TGA

Verify ARTG; US approval does not automatically confer Australian registration.

United States — FDA

Approved (Vyleesi) for a narrow HSDD indication.

European Union — EMA

Verify SmPC/register.

1. [1] Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder

   Kingsberg SA et al. Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder Obstet Gynecol. 2019. PMID 31599837

   PMID 31599837