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PT-141 (Bremelanotide)

Also known as: Bremelanotide, Vyleesi, PT-141 Acetate, Rekynda

FDA Approved

Molecular Formula

C50 H68 N14 O10

Molecular Weight

1,025.2 Da

Half-Life

2.7 hours (range 1.9–4.0 hours)

Sequence

Ac-Nle-cyclo-OH

Clinical Applications & Evidence

Mechanism of Action

PT-141 acts as an agonist across multiple melanocortin receptors (MC1R-MC5R). Its efficacy in addressing sexual dysfunction is driven primarily by MC4R activation in the medial preoptic area (mPOA) of the hypothalamus. This presynaptic binding initiates an intracellular cascade that stimulates the release of dopamine into mesolimbic reward circuits, fundamentally shifting the neurobiological balance toward sexual excitation.

Investigated Uses

  • Hypoactive sexual desire disorder (HSDD) in women
  • Erectile dysfunction (investigational in men)
  • Sexual arousal disorders
Extensive Clinical Data

Regulatory & Safety Status

FDA Status

FDA Approved

WADA / Athletic Status

Prohibited in Competition

Known Side Effects

Nausea (40.0%)Flushing (20.3%)Injection site reactions (13.2%)Headache (11.3%)Vomiting (4.8%)Focal hyperpigmentation (1.0%)

Contraindications

  • Uncontrolled hypertension
  • Known cardiovascular disease

Drug Interactions

  • Naltrexone (oral administration)
  • Indomethacin
  • Concomitant oral medications dependent on rapid absorption (due to delayed gastric emptying)

Citations & Clinical Trials

FDA Bremelanotide (Vyleesi) Approval PubMed RECONNECT Phase 3 Trials