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Melanocortin System

PT-141 (Bremelanotide)

FDA-approved (Vyleesi) on-demand melanocortin injection that boosts sexual desire by acting in the brain; nausea is common.

FDA approvedEvidence level 5 of 5: FDA-approved / large RCTsAlso: Bremelanotide, Vyleesi, PT 141

Overview

PT-141, or bremelanotide, is a cyclic seven-amino-acid peptide developed from Melanotan II after researchers noticed its libido effects. It mainly activates melanocortin-4 receptors in the brain, acting on the central circuits of desire and arousal rather than on blood flow like sildenafil. As Vyleesi, it is FDA-approved for premenopausal women with acquired, generalized low sexual desire that causes distress, taken as an as-needed injection about 45 minutes before sexual activity. In trials the benefit was real but modest. It is also used off-label in men, including those who do not respond to PDE5 inhibitors. Nausea is the most common side effect, blood pressure rises briefly after each dose, and frequent use can darken skin.

Classification
Synthetic cyclic heptapeptide (MC4R-preferring melanocortin agonist)
Route
Subcutaneous
Half-life
~2.7 hours (SC, Vyleesi label)

Mechanism of action

Primary targetMC4R (and MC3R) in the central nervous system
  1. On-demand SC injectionGiven roughly 45 minutes before sexual activity; peaks in about 1 hour.
  2. Crosses into the brainReaches hypothalamic and limbic regions controlling sexual motivation.
  3. MC4R activationStimulates melanocortin-4 receptors in the medial preoptic area.
  4. Dopamine releaseIncreases dopaminergic signaling in desire and reward circuits.
  5. Desire and arousal responseHeightened desire with downstream genital arousal or erection.
Downstream effects
  • Increased sexual desire
  • Reduced desire-related distress
  • Improved erectile response (off-label)

Researched for

  • Hypoactive sexual desire disorder (premenopausal women)
  • Erectile dysfunction
  • Female sexual arousal disorder
  • Postmenopausal low desire (off-label)

Research notes

  • RECONNECT Phase 3 trials (Kingsberg 2019): significant gains in desire and reduction in distress; no significant increase in satisfying sexual events.
  • About 40% of trial participants had nausea; ~18% discontinued for adverse events.
  • Phase 2 trials in men with ED, including PDE5-inhibitor non-responders, showed erectile responses.
  • The label caps how often it can be used; focal hyperpigmentation (face, gums, breasts) was seen with frequent dosing.

Reported side effects

  • Nausea (common)
  • Flushing
  • Headache
  • Transient blood-pressure rise and lower heart rate
  • Darkening of skin or gums with frequent use

Contraindications & cautions

  • Uncontrolled hypertension
  • Known cardiovascular disease or high CV risk
  • Pregnancy
  • Use with oral naltrexone (reduced naltrexone levels)
  • Personal history of melanoma (caution)

Lab monitoring

  • Blood pressure (seated and standing)
  • CBC, CMP
  • Lipid panel, fasting glucose/HbA1c
  • Testosterone, estradiol, prolactin, TSH (rule out other causes)
  • Baseline skin exam if frequent use

Dosing and pricing for PT-141 (Bremelanotide)

Dosing references and compound pricing are available to established patients in the secure portal after a medical evaluation.

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