PT-141
PT-141 (Vyleesi) is a synthetic heptapeptide derived from alpha-MSH (sequence: Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH), acting as a non-hormonal melanocortin receptor agonist (MC3R/MC4R). FDA-approved (2019) for premenopausal HSDD (hypoactive sexual desire disorder), it boosts libido via central nervous system pathways—unlike Viagra’s vascular focus. Research extends to erectile dysfunction, mood, and neuroprotection.
Unique: Nasal/subQ; works in SSRI-failed cases; 45min onset.
Mechanism
- MC4R in Brain: Hypothalamus → dopamine/NO release → arousal.
- Sexual Dimorphism: Women (desire), men (erection + desire).
- No Vascular Dependence: Brain-mediated; effective in diabetes.
- Bonus: Anti-inflammatory MC3R.
PK: Nasal half-life 2h; subQ 2.7h.
Clinical Evidence
| Indication | Studies/Outcomes |
|---|---|
| HSDD (Women) | +0.5 satisfying events/month (Phase 3, RECONNECT, J Sex Med 2019). |
| ED (Men) | 80% response rate (Phase 2); rivals sildenafil. |
| SSRI ED | 68% success (urology trials). |
| Neuro | Stroke recovery models (MC4R). |
Protocols
| Use Case | Dose | Route/Frequency | Notes |
|---|---|---|---|
| Libido (Women) | 1.75mg | SubQ 45min pre | Max 8/month |
| ED (Men) | 1–2mg | Nasal/subQ PRN | 2h window |
| Wellness | 0.5–1mg | 1–2x/week | Microdose |
| Research Stack | 1mg + PT-141 | w/ Kisspeptin | Synergy |
- Nasal: 10–20mg spray.
- Sides Management: Nausea prophylaxis (ondansetron).
Benefits
- Sexual Wellness: Desire + arousal (both sexes).
- Refractory Cases: Post-SSRI, diabetes, psychogenic.
- Rapid: 30–60min peak.
- Neuro/Mood: Dopamine modulation.
Side Effects
| Common (30–40%) | Manageable | Rare |
|---|---|---|
| Nausea, flushing | Headache, injection site | Hyperpigmentation (cumulative) |
| Fatigue | HTN transient | Priapism (low) |
- Nausea: 40%; pre-treat antiemetic.
Comparisons
| Drug | Mechanism | Onset | HSDD? | Sides |
|---|---|---|---|---|
| PT-141 | CNS MC4R | 45min | Yes | Nausea |
| Sildenafil | PDE5 Vasc | 60min | No | Headache |
| Addyi | Serotonin | Days | Yes | Sedation |
| Kisspeptin | GnRH | Acute | Yes | Hormonal |
Status & Access
- FDA: Vyleesi subQ auto-injector (women).
- Research: Nasal/oral analogs; male ED off-label.
- UK: Private clinics; research chemical.
Disclaimer: Prescription/research; MD-supervised.
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