Bremelanotide

What is Bremelanotide?

• Bremelanotide (Vyleesi) is a prescription medicine used to treat hypoactive sexual desire disorder (HSDD) in women.

Bremelanotide

Bremelanotide structure

What are the uses of this medicine?

It is used in:

• Women who have not gone through menopause
• Women who have not had problems with low sexual desire in the past
• Those that have low sexual desire no matter the type of sexual activity, the situation, or the sexual partner.

What is hypoactive sexual disorder?

Women with HSDD have low sexual desire that is bothersome to them. This low sexual desire is not due to:

• a medical or mental health problem
• problems in the relationship
• medicine or other drug use

How does this medicine work?

• Bremelanotide is a melanocortin receptor (MCR) agonist that nonselectively activates several receptor subtypes incluing MC1R, MC4R, MC3R, MC5R, MC2R of which 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.

Who should not use this medicine?

This medicine cannot be used if you have:

• high blood pressure that is not controlled (uncontrolled hypertension)
• known heart (cardiovascular) disease
• Before using Vyleesi, tell your healthcare provider about all of your medical conditions, including if you:
• have high blood pressure.
• have heart problems.
• have kidney problems.
• have liver problems.
• are pregnant or plan to become pregnant.
• currently nursing

Is this medicine FDA approved?

• It was approved for use in the United States in 2019 under brand name Vyleesi.

How should this medicine be administered?

• Use Vyleesi exactly as prescribed by your healthcare provider.
• Vyleesi comes in an autoinjector that you or your caregiver may use at home to give injections.
• Vyleesi is given as an injection under the skin (subcutaneous injection), in your thighs or stomach area (abdomen).
• Inject Vyleesi at least 45 minutes before you think that you will begin sexual activity.
• Do not inject more than 1 dose of Vyleesi within 24 hours of your last dose.
• Do not inject more than 8 doses of Vyleesi within a month.
• Tell your healthcare provider if your symptoms of HSDD have not improved after you have used Vyleesi for 8 weeks.

What are the dosage forms and brand names of this medicine?

• It comes as a Subcutaneous injection: 1.75 mg/0.3 mL clear solution in a single-dose autoinjector.
• 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.
• The duration of efficacy after each dose is unknown and the optimal window for Vyleesi administration has not been fully characterized and it is recommended that no more than one dose be taken in 24 hours.

What side effects can this medication cause?

Most common possible side effects of this medicine include:

• flushing
• vomiting
• hot flush
• nasal congestion
• injection site reactions
• cough
• tingling
• headache
• fatigue
• dizziness

These are not all the possible side effects of Vyleesi and other or more serious side effects can occur. Call your healthcare provider for medical advice about side effects.

What special precautions should I follow?

• Vyleesi transiently increases blood pressure and reduces heart rate after each dose, therefore caution is advised if you have high blood pressure.
• In the phase 3 placebo-controlled trials, focal hyperpigmentation, including involvement of the face, gingiva, and breasts, was reported in 1% of patients who received up to 8 doses per month of Vyleesi compared to no placebo-treated patients.
• In the phase 3 placebo-controlled trials, nausea was the most commonly reported adverse reaction, reported in 40% of Vyleesi-treated patients, requiring anti-emetic therapy in 13% of Vyleesi-treated patients and leading to premature discontinuation from the trials for 8% of Vyleesi-treated patients. Nausea improves for most patients with the second dose

What to do in case of emergency/overdose?

• No reports of overdosage with Vyleesi have been reported.
• Nausea, focal hyperpigmentation and more pronounced blood pressure increases are more likely with higher doses.
• In the event of overdosage, treatment should address the symptoms with supportive measures, as needed.

Can this medicine be used in pregnancy?

• Use of Vyleesi during pregnancy is not recommended.
• Advise females of reproductive potential to use effective contraception while taking Vyleesi, and to discontinue Vyleesi if pregnancy is suspected.

Can this medicine be used in children?

• The safety and effectiveness of Vyleesi have not been established in pediatric patients.

What should I know about storage of this medication?

• Store at or below 77°F (25°C).
• Do not freeze.
• Protect from light.
• Keep Vyleesi and all medicines out of the reach of children.

What are the active and inactive ingredients in this medicine?

• Active ingredient: bremelanotide
• Inactive ingredients: 2.5% glycerin, sterile water for injection, and hydrochloric acid or sodium hydroxide is added to adjust the pH.

Who manufactures and distributes this medicine?

• Vyleesi is a trademark of AMAG Pharmaceuticals, Inc.
• Manufactured for: AMAG Pharmaceuticals, Inc.

• Dailymed label info on Bremelanotide
• FDA Bremelanotide