Bremelanotide
Melanocortin receptor agonist
Status
Approved
FDA approved bremelanotide (Vyleesi) in June 2019 for acquired, generalized hypoactive sexual desire disorder in premenopausal women; the label states it is not indicated for postmenopausal women, men, or to enhance sexual performance.
Evidence
Strong
Two identical phase 3 randomized trials in about 1,250 women met both co-primary endpoints, although the average improvement was modest and satisfying sexual events did not increase.
Bremelanotide is a small ring-shaped peptide that activates melanocortin receptors, including in the brain. It is FDA-approved as an as-needed injection (Vyleesi) for premenopausal women with distressing low sexual desire that has no other identifiable cause.
Structure
7 residuesPoint at a bead, or focus the chain and use the arrow keys, to name it. Pick a chemistry to highlight it.
D-form (mirror image), shown in lower case
Sequence as text
Ac-Nle-D-H-D-Phe-R-W-K-OH
What it is used for
- Acquired, generalized hypoactive sexual desire disorder in premenopausal women (approved)
- Low sexual desire in postmenopausal women or men (claimed, unproven)
- Enhancing sexual performance (claimed, unproven)
How it works
Bremelanotide activates several melanocortin receptors without strong selectivity; at approved doses, binding to MC4R, found on neurons throughout the central nervous system, and to MC1R on pigment cells is most relevant. The label states that how it improves low sexual desire in women is unknown. MC1R activation increases melanin, which explains the skin and gum darkening reported with frequent use.
How strong the evidence is
Strong
The RECONNECT programme comprised two identical 24-week phase 3 trials that randomized 1,267 premenopausal women with HSDD to bremelanotide or placebo used as needed (Kingsberg 2019). Women on bremelanotide had statistically significant gains in the desire score of the Female Sexual Function Index (integrated difference 0.35 points) and reductions in distress about low desire (difference -0.33) compared with placebo. The number of satisfying sexual events, a secondary endpoint, did not differ significantly (label). Nausea, flushing and headache each affected at least 10% of users in both studies.
Risks and side effects
- Nausea in about 40% of users, sometimes needing anti-nausea medicine
- Transient rise in blood pressure and fall in heart rate after each dose; not for people with uncontrolled hypertension or cardiovascular disease
- Focal darkening of the face, gums or breasts, which may not resolve
- Flushing, headache, vomiting and injection-site reactions
- Can reduce absorption of oral naltrexone and slow absorption of other oral medicines
Label dosing
Label: 1.75 mg injected under the skin of the abdomen or thigh at least 45 minutes before anticipated sexual activity, no more than one dose in 24 hours and no more than 8 doses a month.
Regulatory status
| Region | Year | Approved for |
|---|---|---|
| USFDA | 2019 | Acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women |
Status by country
| Jurisdiction | Status | Source |
|---|---|---|
| USUnited States | Authorised medicine | Source 2 |
| EUEuropean Union | No authorised medicine | Source 6 |
| UKUnited Kingdom | No authorised medicine | Source 7 |
| AUAustralia | No authorised medicine | Source 8 |
| CACanada | No authorised medicine | Source 9 |
Timeline
2026
2019
- Approved, US (FDA)Acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women
Sources
- 01VYLEESI (bremelanotide injection) label(opens the source in a new tab)
- 02VYLEESI NDA 210557: approval history(opens the source in a new tab)
- 03Bremelanotide for the treatment of hypoactive sexual desire disorder: two randomized phase 3 trials(opens the source in a new tab)
- 04Bremelanotide: first approval(opens the source in a new tab)
- 05Bremelanotide (CID 9941379)(opens the source in a new tab)
- 06Find medicine: centrally authorised medicines(opens the source in a new tab)
- 07MHRA Products: active substances beginning with B(opens the source in a new tab)
- 08Australian Register of Therapeutic Goods (ARTG)(opens the source in a new tab)
- 09Unauthorized injectable peptide drugs seized and sold by Canada Peptide may pose serious health risks(opens the source in a new tab)
Educational information, not medical advice. Talk to a licensed clinician before starting, stopping or changing any medicine.