Overview
11 DESCRIPTION VYLEESI (bremelanotide injection) contains bremelanotide, a melanocortin receptor agonist for subcutaneous administration via an autoinjector. Bremelanotide acetate is a synthetic, cyclic heptapeptide with a free acid at the carboxyl terminus and an acetylated amino group at the amino terminus of the peptide with the following structure: Ac-Nle-cyclo-(Asp-His-D-Phe-Arg-Trp-Lys-OH)...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Bremelanotide is a melanocortin receptor (MCR) agonist that nonselectively activates several receptor subtypes with the following order of potency: MC1R, MC4R, MC3R, MC5R, MC2R. At therapeutic dose levels, binding to MC1R and MC4R is most relevant. Neurons expressing MC4R are present in many areas of the central nervous system (CNS). The mechanism by which VYLEESI improves HSDD in women is unknown. The MC1R is expressed on melanocytes; binding at this receptor leads to melanin expression and increased pigmentation. 12.2 Pharmacodynamics Transient Increases in Blood Pressure In an open-label ambulatory blood pressure monitoring study of 127 premenopausal women receiving VYLEESI once daily, there was a mean increase of 1.9 mmHg (95% CI: 1.
Indications
- 1 INDICATIONS AND USAGE VYLEESI is indicated for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD), as characterized by low sexual desire that causes marked distress or interpersonal difficulty and is NOT due to: A co-existing medical or psychiatric condition, Problems with the relationship, or The effects of a medication or drug substance. Acquired HSDD refers to HSDD that develops in a patient who previously had no problems with sexual desire.
Common Doses
- 1.75 mg
Dosage
2 DOSAGE AND ADMINISTRATION Inject 1.75 mg subcutaneously via the autoinjector to the abdomen or thigh, as needed, at least 45 minutes before anticipated sexual activity. ( 2.1 ) Do not administer more than one dose within 24 hours. ( 2.1 ) More than 8 doses per month is not recommended. ( 2.1 ) 2.1 Recommended Dosage The recommended dosage of VYLEESI is 1.75 mg administered subcutaneously in the abdomen or thigh, as needed, at least 45 minutes before anticipated sexual activity.
Contraindications
- 4 CONTRAINDICATIONS VYLEESI is contraindicated in patients who have uncontrolled hypertension or known cardiovascular disease [see Warnings and Precautions ( 5.1 )]. Uncontrolled hypertension or known cardiovascular disease. ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following adverse reactions are discussed in greater detail elsewhere in labeling: Transient increases in blood pressure and reductions in heart rate [ see Warnings and Precautions ( 5.1 ) and Clinical Pharmacology ( 12.2 ) ] Focal hyperpigmentation [ see Warnings and Precautions ( 5.2 )] Nausea [ see Warnings and Precautions ( 5.3 ) ] Most common adverse reactions (incidence > 4%) are nausea, flushing, injection site reactions, headache, and vomiting. ( 6.
Interactions
- 7 DRUG INTERACTIONS VYLEESI may slow gastric emptying and impact absorption of concomitantly administered oral medications. ( 7.1 ) VYLEESI may significantly decrease the systemic exposure of orally-administered naltrexone; avoid use with orally administered naltrexone-containing products intended to treat alcohol or opioid addiction. ( 7.2 ) 7.1 Effect of VYLEESI on Other Drugs VYLEESI may slow gastric emptying and thus has the potential to reduce the rate and extent of absorption of concomitantly administered oral medications.