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Bremelanotide

Medically reviewed by Drugs.com. Last updated on Apr 29, 2020.

Pronunciation

(BRE me LAN oh tide)

Index Terms

  • Bremelanotide Acetate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Auto-injector, Subcutaneous, as acetate [preservative free]:

Vyleesi: 1.75 mg/0.3 mL (0.3 mL)

Brand Names: U.S.

  • Vyleesi

Pharmacologic Category

  • Melanocortin Receptor Agonist

Pharmacology

Nonselective melanocortin receptor agonist that activates several receptor subtypes, most notably MC4R (present throughout the CNS) and MC1R (expressed on melanocytes). Mechanism for improvement of hypoactive sexual desire disorder is unknown.

Distribution

Vd: 25 ± 5.8 L

Metabolism

Primarily amide hydrolysis of the cyclic peptide

Excretion

Urine (64.8%); feces (22.8%)

Time to Peak

~1 hour

Half-Life Elimination

Terminal: ~2.7 hours (range: 1.9 to 4 hours)

Protein Binding

21%

Special Populations: Renal Function Impairment

In patients with mild (eGFR 60 to 89 mL/minute/1.73 m2), moderate (eGFR 30 to 59 mL/minute/1.73 m2), and severe (eGFR <30 mL/minute/1.73 m2) renal impairment, AUC increased by 1.2-, 1.5-, and 2-fold, respectively.

Special Populations: Hepatic Function Impairment

In patients with mild (Child-Pugh class A) and moderate (Child-Pugh class B) hepatic impairment, AUC increased by 1.2- and 1.7-fold, respectively.

Use: Labeled Indications

Hypoactive sexual desire disorder: 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 coexisting medical or psychiatric condition, problems with the relationship, or the effects of a medication or drug substance.

Limitations of use: Not indicated for the treatment of HSDD in postmenopausal women or in men or to enhance sexual performance.

Contraindications

Uncontrolled hypertension or known cardiovascular disease

Dosing: Adult

Note: Discontinue use of bremelanotide if no improvement in symptoms after 8 weeks.

Hypoactive sexual desire disorder: SubQ: 1.75 mg as needed, ≥45 minutes before sexual activity (maximum: 1.75 mg/24 hours). No more than 8 doses per month are recommended.

Dosing: Geriatric

Refer to adult dosing.

Administration

SubQ: Administer SubQ in the abdomen or thigh.

Storage

Store at ≤25°C (77°F). Do not freeze. Protect from light.

Drug Interactions

Indomethacin: Bremelanotide may decrease the serum concentration of Indomethacin. Monitor therapy

Naltrexone: Bremelanotide may decrease the serum concentration of Naltrexone. Avoid combination

Adverse Reactions

>10%:

Cardiovascular: Flushing (20%)

Central nervous system: Headache (11%)

Dermatologic: Skin hyperpigmentation (1% to 38%)

Gastrointestinal: Nausea (40%)

Local: Injection site reaction (13%)

1% to 10%:

Cardiovascular: Increased blood pressure (<2%)

Central nervous system: Fatigue (3%), paresthesia (3%), dizziness (2%), pain (<2%), restless leg syndrome (<2%)

Endocrine & metabolic: Hot flash (3%)

Gastrointestinal: Vomiting (5%), diarrhea (<2%), upper abdominal pain (<2%)

Neuromuscular & skeletal: Arthralgia (<2%), increased creatine phosphokinase in blood specimen (<2%), limb pain (<2%), myalgia (<2%)

Respiratory: Cough (3%), nasal congestion (2%), rhinorrhea (<2%)

Frequency not defined:

Cardiovascular: Decreased heart rate

Central nervous system: Hypoesthesia

Dermatologic: Injection site pruritus

Respiratory: Flu-like symptoms

Warnings/Precautions

Concerns related to adverse effects:

• Cardiovascular: A transient increase in blood pressure and reduction in heart rate may occur after each dose; peak effects occur 2 to 4 hours post-dose and typically return to baseline within 12 hours. Use is not recommended in patients at high risk for cardiovascular disease and is contraindicated in patients with uncontrolled hypertension or established cardiovascular disease.

• Focal hyperpigmentation: Focal hyperpigmentation, including involvement of the face, gingiva, and breasts, has been reported. May occur more frequently in patients with dark skin and with more frequent administration. Consider discontinuation if focal hyperpigmentation develops; may resolve in some patients.

• Gastrointestinal: Nausea, especially after the initial dose, has been reported. Onset usually occurs within 1 hour post-dose and may last approximately 2 hours. Incidence commonly decreases with subsequent doses. Use of an antiemetic may be effective; discontinuation of therapy may be considered for persistent or severe nausea.

Concurrent drug therapy issues:

• Delayed gastric emptying: May delay gastric emptying and reduce the rate and extent of absorption of concurrently administered oral drugs. Monitor for efficacy of concurrently administered oral drugs and consider discontinuation of bremelanotide if efficacy is affected. Additionally, concurrent use with oral drugs dependent on threshold concentrations for efficacy (eg, antibiotics) may need to be avoided.

Monitoring Parameters

Blood pressure and heart rate (if clinically indicated)

Reproductive Considerations

Females of reproductive potential should use effective contraception during bremelanotide therapy.

Pregnancy Considerations

Outcome information following maternal use of bremelanotide during pregnancy is limited. Discontinue if pregnancy is suspected.

Data collection to monitor pregnancy and infant outcomes following exposure to bremelanotide is ongoing. Health care providers are encouraged to enroll females exposed to bremelanotide during pregnancy in the Vyleesi Pregnancy Registry (1-877-411-2510).

Patient Education

What is this drug used for?

• It is used in some women to raise interest in sex.

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:

• Nausea

• Flushing

• Injection site irritation

• Vomiting

• Stuffy nose

• Cough

• Tingling

• Fatigue

• Weakness

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:

• Severe headache

• Severe dizziness

• Passing out

• Vision changes

• Slow heartbeat

• 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.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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