Generic name: bremelanotide
Brand name: Vyleesi
Dosage form: subcutaneous solution (1.75 mg/0.3 mL)
Drug class: Melanocortin receptor agonists
What is bremelanotide?
Bremelanotide is a prescription medicine that is used in some women to raise interest in sex.
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) • xCH3COOH
The molecular formula of bremelanotide acetate is C50H68N14O10 • xCH3COOH (1≤ x ≤ 2) and the molecular weight is 1025.2 (free base).
VYLEESI (bremelanotide injection) is supplied as a sterile, clear solution in a pre-filled syringe contained in a single-dose autoinjector for subcutaneous administration. Each pre-filled syringe contains 1.75 mg of bremelanotide (equivalent to 1.89 mg bremelanotide acetate) in 0.3 mL solution. Inactive ingredients consist of 2.5% glycerin, sterile water for injection, and hydrochloric acid or sodium hydroxide added to adjust the pH.
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.
Before taking bremelanotide, tell your doctor:
- If you are allergic to bremelanotide; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
- If you have any of these health problems: Heart disease or high blood pressure.
- If you are taking naltrexone.
- If you are pregnant or may be pregnant. Do not take bremelanotide if you are pregnant.
This is not a list of all drugs or health problems that interact with bremelanotide.
Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take bremelanotide with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.
What are some things I need to know or do while I take bremelanotide?
- Tell all of your health care providers that you take bremelanotide. This includes your doctors, nurses, pharmacists, and dentists.
- High blood pressure and slow heartbeat have happened with bremelanotide. Most of the time, these effects go away within 12 hours after a dose. If you have questions, talk with your doctor.
- Darkened skin on the face, gums, and breast has happened with bremelanotide. The risk is higher in people with darker skin color. The risk is higher if used every day. Do not take more than 8 doses in a month. Darkened skin may not go back to normal even after bremelanotide is stopped. If you have questions or concerns, talk with your doctor.
- This medicine may cause harm to an unborn baby. Women must use birth control while taking bremelanotide. If you get pregnant, call your doctor right away.
- Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.
How is bremelanotide best taken?
Use bremelanotide as ordered by your doctor. Read all information given to you. Follow all instructions closely.
- It is given as a shot into the fatty part of the skin on the top of the thigh or the belly area.
- If you will be giving yourself the shot, your doctor or nurse will teach you how to give the shot.
- Take a dose at least 45 minutes before you think you will have sex. If it does not seem to be working well, talk with your doctor. You may need to take bremelanotide at a different time.
- Do not use if the solution is cloudy, leaking, or has particles.
- Do not use if solution changes color.
- Throw away needles in a needle/sharp disposal box. Do not reuse needles or other items. When the box is full, follow all local rules for getting rid of it. Talk with a doctor or pharmacist if you have any questions.
What do I do if I miss a dose?
- This medicine is taken on an as needed basis. Do not take more often than every 24 hours unless told to do so by your doctor.
What are the side effects of bremelanotide that I need to call my doctor about immediately?
WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:
- Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
- Signs of high blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
- Slow heartbeat.
What are some other side effects of bremelanotide?
All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
- Upset stomach. Most of the time, this happens after the first dose but can happen after any dose. This usually lasts for about 2 hours. If upset stomach is severe or does not go away, talk with your doctor.
- Irritation where the shot is given.
- Throwing up.
- Stuffy nose.
- Feeling dizzy, tired, or weak.
These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.
You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.
If overdose is suspected:
If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.
How do I store and/or throw out bremelanotide?
- Store at room temperature. Do not freeze.
- Protect from light.
- Store in a dry place. Do not store in a bathroom.
- Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
- Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.
PRINCIPAL DISPLAY PANEL – NDC: 64011-701-04 – AUTOINJECTOR CARTON LABEL
SRC: NLM .