Overview
Bremelanotide (PT-141) is a synthetic melanocortin peptide developed from Melanotan II for the treatment of sexual dysfunction in both men and women. Early MT-II studies noted spontaneous erections in most male subjects, leading to PT-141’s development. Unlike PDE-5 inhibitors, PT-141 increases sexual desire and arousal via the central nervous system (CNS), not the vascular system. It has been evaluated in men with erectile dysfunction (ED) and in premenopausal women with hypoactive sexual desire disorder (HSDD), with over two decades of basic and clinical research.
Bremelanotide (PT-141) is a synthetic melanocortin peptide developed from Melanotan II for the treatment of sexual dysfunction in both men and women. Early MT-II studies noted spontaneous erections in most male subjects, leading to PT-141’s development. Unlike PDE-5 inhibitors, PT-141 increases sexual desire and arousal via the central nervous system (CNS), not the vascular system. It has been evaluated in men with erectile dysfunction (ED) and in premenopausal women with hypoactive sexual desire disorder (HSDD), with over two decades of basic and clinical research.
How It Works
PT-141 is an agonist at melanocortin receptors MC3R and MC4R in the CNS. Activation of these receptors modulates neural pathways related to sexual desire, arousal, mood, inflammation, and autonomic tone. Because it acts centrally, PT-141 may benefit patients who do not respond to vasodilatory agents.
PT-141 is an agonist at melanocortin receptors MC3R and MC4R in the CNS. Activation of these receptors modulates neural pathways related to sexual desire, arousal, mood, inflammation, and autonomic tone. Because it acts centrally, PT-141 may benefit patients who do not respond to vasodilatory agents.
Key Benefits
- Sexual Arousal & Desire: Increases libido and central arousal in men and women.
- ED Support (non-responders): Demonstrated benefit in a subset of men who did not respond to sildenafil.
- Female Sexual Function: Improved desire and reduced distress in premenopausal women with HSDD in phase 2/3 studies.
- Additional Exploratory Areas: Investigated for potential roles in hemorrhagic shock (tissue protection) and immune modulation.
Clinical Research (Highlights)
- ED Non-Responders: ~33% of sildenafil non-responding men achieved erections sufficient for intercourse with intranasal/subcutaneous PT-141 in controlled trials; dose-response observed.
- Female HSDD: Phase 2b and two Phase 3 (RECONNECT) trials showed significant improvements in sexual desire and reduced distress with 1.75 mg SC on demand (45 min pre-activity), with acceptable tolerability.
- Safety with Alcohol (Phase 1): No meaningful pharmacokinetic interaction when co-administered with ethanol in healthy volunteers (intranasal dosing).
Administration & Dosage (general guidance)
- Route: Subcutaneous injection to the abdomen or other fatty area; (other formats like nasal/oral strips have been explored).
- Typical Dose: 1.75 mg SC on demand, ~45 minutes before anticipated sexual activity.
- Frequency: Max 1 dose/24 h and no more than 8 doses/month.
- Practical Steps: Use sterile technique; clean site with alcohol; inject at 90°, depress plunger fully, dispose safely.
Some protocols describe titration in clinic settings. For men, clinical and compounding guidance may start around 1 mg SC and titrate; do not exceed clinic-directed limits.
Side Effects (most common to less common)
- Common: Nausea, flushing (face/skin), headache, injection-site reactions.
- Others reported: Dizziness, vomiting, increased sweating, hot flashes, transient blood pressure elevation, altered taste, nasal/post-nasal symptoms (non-SC routes).
- Rare/serious: Hypertension episodes; discontinue and seek care if severe reactions occur.
Contraindications & Interactions
- Avoid/Use with Caution: Uncontrolled hypertension, significant cardiovascular disease.
- Drug interactions: May reduce absorption of certain oral medications (e.g., naltrexone); avoid concurrent use where reduced efficacy would be harmful.
- General: Follow clinician guidance; discontinue if no meaningful benefit after an adequate trial (e.g., 8 weeks for on-demand SC).
Product Information
- Peptide Type: Cyclic heptapeptide, melanocortin receptor agonist
- Sequence (commonly cited): Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-NH₂
- Molecular Formula: C₅₀H₆₈N₁₄O₁₀
- Molecular Weight: ~1025.2 g/mol
- PubChem CID: 9941379 | CAS: 189691-06-3
- Storage: Store frozen until first use; then refrigerate at 2–8 °C (follow product-specific expiry; many pharmacies specify up to 56–90 days refrigerated).
Usage Notes (patient-facing summary)
- Take ~45 min before sexual activity. Effects may begin within minutes to a few hours and can last up to ~24 h.
- If no improvement in desire/arousal after an adequate trial, discuss discontinuation and alternatives with your clinician.
- Not a substitute for addressing relationship, psychological, or hormonal contributors—often used alongside those approaches.
Selected References
- Molinoff PB, et al. PT-141 for sexual dysfunction. Ann NY Acad Sci. 2003.
- Rosen RC, et al. SC PT-141 in healthy men & sildenafil non-responders. Int J Impot Res. 2004.
- Kingsberg SA, et al. Bremelanotide for HSDD: two Phase 3 trials. Obstet Gynecol. 2019.
- Clayton AH, et al. Dose-finding & responder analyses in women. J Sex Med. 2019.
- Clayton AH, et al. Phase 1 with ethanol co-administration. Clin Ther. 2017.
- AHFS/Drugs.com Monograph – Bremelanotide; DailyMed (Vyleesi) label.
- PubChem Compound Summary: Bremelanotide (CID 9941379).