Bremelanotide

Summary

Bremelanotide (Vyleesi) is an FDA-approved subcutaneous injectable peptide for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women. It is administered on-demand prior to anticipated sexual activity and works centrally via melanocortin receptor agonism to increase sexual desire.

Mechanism of Action

Selectively activates melanocortin receptors MC1R, MC3R, MC4R, and MC5R in the central nervous system, particularly MC4R in the hypothalamus, modulating dopaminergic and serotonergic pathways to enhance sexual desire and arousal independent of gonadal hormones or vascular effects.

Routes of Administration

Goals & Uses

• Melanocortin-related skin tanningDermatology / CosmeticLow
• Male sexual dysfunction / erectile dysfunctionSexual HealthLow
• Female sexual arousal disorderSexual DysfunctionModerate
• Hypoactive Sexual Desire Disorder (HSDD) treatmentSexual DysfunctionHigh
• Increased sexual desire/libidoSexual HealthHigh

Contraindications

• Known cardiovascular diseaseCardiovascularHigh
• Hypersensitivity to bremelanotide or excipientsAllergic/immunologicHigh
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Use in postmenopausal womenEndocrine/hormonalModerate
• Uncontrolled hypertensionCardiovascularHigh

Adverse Effects

• Injection site reactionsLocalCommon
• HeadacheNeurologicCommonPain in the head or upper neck
• Transient hypertensionCardiovascularCommon
• FlushingVascularCommonWarmth and redness of the skin
• NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
• Hyperpigmentation (focal)DermatologicUncommon

Drug Interactions

• Antihypertensive agentsModerate
• Indomethacin and NSAIDsLow
• NaltrexoneModerate

Population Constraints

• Severe renal impairmentOrgan ImpairmentRelative
• Pediatric patientsAgeAbsolute
• Premenopausal women onlyAge/reproductive StatusAbsolute
• Severe hepatic impairmentOrgan ImpairmentRelative

Regulatory Status

• European UnionUnapprovedNot approved by the European Medicines Agency as of current data; no marketing authorization in the EU.
• United StatesApprovedApproved: Hypoactive sexual desire disorder (HSDD) in premenopausal womenFDA approved June 21, 2019 under brand name Vyleesi. NDA 210557. On-demand subcutaneous injection.
• United KingdomUnapprovedNot approved by MHRA in the UK; not available as a licensed medicine.

FDA approved in June 2019 for HSDD in premenopausal women. Not approved for postmenopausal women or men. Not intended for daily use; maximum one dose per 24 hours recommended. Carries a warning regarding transient blood pressure increases and flushing.

Evidence & Sources

No sources recorded yet.