Products
Bremelanotide was approved in the United States in 2019 as an injection solution in an auto-injector pen (Vyleesi).
Structure and properties
Bremelanotide (C50H68N14O10, Mr = 1025.2 g/mol) is a synthetic cyclic peptide analog of α-melanocyte stimulating hormone (α-MSH) produced in the adenohypophysis. Bremelanotide consists of seven amino acids (heptapeptide) and is an active metabolite of melanotan-II. In the drug, it is present as bremelanotide acetate. Ac-Nle-cyclo-(Asp-His-D-Phe-Arg-Trp-Lys-OH) – x CH3COOH
Effects
Bremelanotide stimulates sexual desire. Effects are due to nonselective agonism at melanocortin receptors (MCRs) in the central nervous system. Melanocortin receptors are also localized on melanocytes. Therefore, activation of the receptors can lead to increased pigmentation. The half-life is approximately 2.7 hours. In has shown bremelanotide to have erection-promoting properties and could be used for erectile dysfunction therapy, but has not yet been approved for this purpose.
Indications
For the treatment of premenopausal women with hypoactive sexual desire disorder (HSDD).
Dosage
According to the SmPC. The drug is self-administered subcutaneously by the patient using an autoinjector. It is injected as needed at least 45 minutes before expected sexual activity and not regularly. No more than one dose should be administered within 24 hours. A maximum of 8 doses should be injected per month.
Contraindications
- Hypersensitivity
- Uncontrolled hypertension
- Cardiovascular diseases
For complete precautions, see the drug label.
Interactions
Bremelanotide may delay gastric emptying and thus affect the absorption of other drugs. Systemic exposure of naltrexone is significantly reduced by bremelanotide.
Adverse Effects
The most common potential adverse effects include nausea, vomiting, flushing, injection site reactions, and headache. Bremelanotide may temporarily increase blood pressure and reduce heart rate. It may cause local hyperpigmentation, for example, on the face, gums, and breasts.
