What Is PT-141 (Bremelanotide)?
PT-141 (bremelanotide) is a synthetic melanocortin agonist developed from melanotan II with structural modifications designed to target sexual function pathways while reducing cardiovascular side effects associated with its parent compound. In 2019, PT-141 received FDA approval under the brand name Vyleesi® for hypoactive sexual desire disorder (HSDD) in premenopausal women — making it the first non-hormonal, centrally acting treatment for female sexual dysfunction to receive FDA approval.
PT-141 is notable for its central rather than peripheral mechanism of action. Unlike PDE5 inhibitors (sildenafil, tadalafil) which work through peripheral vascular mechanisms, PT-141 activates melanocortin receptors in the CNS — specifically in hypothalamic regions involved in sexual motivation and arousal — producing a fundamentally different pharmacological profile that has attracted significant research interest.
Mechanism of Action
- MC4R Agonism (primary): Activates melanocortin-4 receptors in the hypothalamus, particularly the paraventricular nucleus (PVN), the brain region most directly linked to sexual motivation
- MC3R Agonism: Contributes to appetite modulation and neuroendocrine signaling
- Central Arousal Pathways: Increases dopaminergic tone in limbic reward circuits, enhancing motivational components of sexual behavior in research models
- Nitric Oxide: Downstream MC4R activation increases hypothalamic NO production, which contributes to genital engorgement responses in both sexes
- MC1R (minimal): Some melanin-stimulating effects, lower than melanotan II due to structural differences
Research and Clinical Data
Phase 3 RECONNECT Trials (leading to FDA approval)
- Two Phase 3 trials enrolled over 1,200 premenopausal women with HSDD
- Significant improvement in satisfying sexual events (SSEs) vs. placebo across both trials
- Female Sexual Function Index (FSFI) desire domain scores improved significantly
- Effect observed within 45 minutes of administration, peak at 1–2 hours
Male Sexual Function Research
- Phase 2 trials demonstrated dose-dependent erection facilitation in men with erectile dysfunction, including non-responders to PDE5 inhibitors
- Psychogenic ED research shows particularly strong response, as the central mechanism targets motivation rather than purely vascular function
Melanocortin System Research (Broader)
- PT-141 used as a research tool to investigate MC4R function in feeding, metabolic, and pain research
- Documented analgesic effects in rodent pain models (MC4R expressed in pain-modulating regions)
Dosage Reference for Research
| Context | Dose | Route | Notes |
|---|---|---|---|
| FDA-approved (HSDD) | 1.75 mg | SC auto-injector | As needed, ≤1× per 24h |
| Phase 2 (male ED) | 4–20 mg | SC | Dose-finding studies |
| Rodent models | 0.1–1 mg/kg | SC or IP | Behavioral and metabolic studies |

HPLC Verified
PT-141 (Bremelanotide) 10mg
Research Disclaimer: This product is sold strictly for in vitro research and laboratory use only. Not for human consumption. Not medical advice.