Bremelanotide
Melanocortin receptor agonist peptide for hypoactive sexual desire disorder in premenopausal women.
Chemical Identity
| Property | Value |
|---|---|
| Chemical Formula | C50H68N14O10 |
| Molecular Weight | 1025.2 Da |
| CAS Number | 189691-06-3 |
| Peptide Class | Cyclic Heptapeptide (Melanocortin Agonist) |
| Route | SC injection |
Structure
Bremelanotide (Vyleesi) is a synthetic cyclic heptapeptide analog of alpha-melanocyte-stimulating hormone (alpha-MSH). It contains D-phenylalanine and N-methylated residues that provide metabolic stability and oral bioavailability in early development, though the approved formulation is subcutaneous.
Mechanism of Action
Bremelanotide activates melanocortin receptors MC3R and MC4R in the central nervous system, particularly in the hypothalamus. These receptors modulate sexual arousal and desire through dopaminergic and oxytocinergic pathways. Unlike flibanserin, it acts on desire pathways rather than neurotransmitter balance.
Clinical Applications
- Hypoactive sexual desire disorder: Premenopausal women (Vyleesi)
- On-demand dosing: Self-administered SC at least 45 minutes before anticipated sexual activity
- RECONNECT trials: Demonstrated significant improvement in desire scores
- Not for postmenopausal women: Safety not established
Pharmacokinetics
- Half-life: 2.7 hours
- Tmax: 1 hour (SC)
- Bioavailability: ~100% (SC)
- Metabolism: Hepatic
- Route: SC injection (abdomen or thigh)
Safety and Side Effects
Nausea (40%, most common), flushing, headache, injection site reactions, and transient blood pressure increase (mean 3 mmHg). Contraindicated in uncontrolled hypertension and cardiovascular disease.
References
- Kingsberg, S.A., et al. (2019). RECONNECT trials: bremelanotide for HSDD. Lancet, 394, 1009-1018.
- Pfaus, J.G., et al. (2019). Melanocortin pathways in sexual desire. Journal of Sexual Medicine, 16, 431-444.
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