NO. 022 · REGEN
PT-141
Bremelanotide · MC4R Agonist · FDA Approved
ALIASES
Bremelanotide, PT-141, Vyleesi
CLASS
Cyclic melanocortin 3/4 receptor agonist · FDA-approved (Vyleesi)
FORMULA
C₅₀H₆₈N₁₄O₁₀
SEQUENCE
Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
HALF-LIFE
2.7 hours (subcutaneous)
ROUTES
Subcutaneous (FDA-approved Vyleesi formulation)
MECHANISM OF ACTION
Synthetic alpha-MSH analog acting as melanocortin MC4R agonist on hypothalamic CNS pathways. FDA-approved as Vyleesi (2019). Mechanism via central melanocortin receptor activation; side-effect profile includes melanocyte stimulation.
EVIDENCE GRADES
RECONNECT-1 and RECONNECT-2 Phase 3 trials met primary endpoint (improvement in FSFI desire score); FDA approval June 2019.
Phase 2 trials showed efficacy in men with ED but Palatin pivoted to female HSDD for regulatory reasons.
SAFETY
Side effects
- Nausea (most common)
- Facial flushing
- Headache
- Transient systolic BP elevation ~6 mmHg
Drug interactions
- Avoid in uncontrolled hypertension or known cardiovascular disease
Contraindications
- Uncontrolled hypertension
- Known cardiovascular disease
REGULATORY STATUS
FDA · FDA-approved as Vyleesi (bremelanotide) for HSDD in premenopausal women (June 2019).
WADA · Not currently listed on the WADA Prohibited List.
STORAGE
Lyophilized · -20 °C 24 months
Reconstituted · 2-8 °C 28 days
PEER-REVIEWED EVIDENCE
- Kingsberg SA, Clayton AH, et al.. Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials. Obstet Gynecol 2019. PMID 31022173. link →
- Clayton AH, et al.. Bremelanotide for female sexual dysfunctions in premenopausal women. Womens Health (Lond) 2016. PMID 27193591. link →
FAQ · 7 QUESTIONS
▶ What is PT-141?
PT-141 (bremelanotide, brand Vyleesi) is a cyclic 7-amino-acid peptide melanocortin 3/4 receptor agonist. FDA-approved June 2019 for hypoactive sexual desire disorder (HSDD) in premenopausal women.
▶ How does PT-141 differ from sildenafil?
PT-141 acts centrally on melanocortin receptors in the hypothalamus to drive arousal pathways (dopamine + oxytocin). Sildenafil acts peripherally on PDE-5 in the vasculature to facilitate erection. Different mechanism, different pathway.
▶ Is PT-141 FDA-approved?
Yes. FDA-approved as Vyleesi for HSDD in premenopausal women, June 2019. Distributed by Palatin Technologies/Cosette.
▶ What's the approved dose?
Single 1.75 mg subcutaneous injection administered at least 45 minutes before anticipated sexual activity. Per Vyleesi label.
▶ Side effects?
Most common: transient nausea (~40% incidence at the approved dose). Less common: facial flushing, headache, injection-site reactions, mild transient blood pressure increase.
▶ Who shouldn't use PT-141?
Vyleesi label contraindicates use in uncontrolled hypertension or known cardiovascular disease due to transient BP elevation in trials. Consult a healthcare provider for clinical use.
▶ Is PT-141 banned in sports?
Not currently listed on the WADA Prohibited List.
SIGNATURE MOVES
FDA-approved (Vyleesi). CNS pathway activation.
Side-effect: melanocyte stimulation.
SOURCED FROM GIGACOMPOUNDS
Reference compounds documented on this page are available as research-grade material at GigaCompounds · ≥99% purity · per-batch Certificate of Analysis. For laboratory research use only. No human dose is recommended by this wiki.
▶ LAST UPDATED · 2026-05-19