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Bremelanotide: Drug information

Bremelanotide: Drug information
(For additional information see "Bremelanotide: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Vyleesi
Pharmacologic Category
  • Melanocortin Receptor Agonist
Dosing: Adult

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

Hypoactive sexual desire disorder

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: Kidney Impairment: Adult

eGFR ≥30 mL/minute/1.73 m2: No dosage adjustment necessary.

eGFR <30 mL/minute/1.73 m2: Use with caution.

Dosing: Hepatic Impairment: Adult

Mild to moderate impairment (Child-Pugh class A and B): No dosage adjustment necessary.

Severe impairment (Child-Pugh class C): Use with caution (has not been studied).

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution Auto-injector, Subcutaneous, as acetate:

Vyleesi: 1.75 mg/0.3 mL (0.3 mL)

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

Vyleesi: 1.75 mg/0.3 mL (0.3 mL [DSC])

Generic Equivalent Available: US

No

Administration: Adult

SubQ: Administer SubQ in the abdomen or thigh.

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.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>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

Contraindications

Uncontrolled hypertension or known cardiovascular disease

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.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

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

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

Reproductive Considerations

Patients who may become pregnant 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 (800-972-5220).

Breastfeeding Considerations

It is not known if bremelanotide is present in breast milk.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Monitoring Parameters

Blood pressure and heart rate (if clinically indicated)

Mechanism of Action

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.

Pharmacokinetics

Distribution: Vd: 25 ± 5.8 L

Protein binding: 21%

Metabolism: Primarily amide hydrolysis of the cyclic peptide

Bioavailability: ~100%

Half-life elimination, terminal: ~2.7 hours (range: 1.9 to 4 hours)

Time to peak: ~1 hour

Excretion: Urine (64.8%); feces (22.8%)

Pharmacokinetics: Additional Considerations

Altered kidney function: 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.

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.

Pricing: US

Solution Auto-injector (Vyleesi Subcutaneous)

1.75 mg/0.3 mL (per 0.3 mL): $269.70

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

  1. Vyleesi (bremelanotide) [prescribing information]. Cranbury, NJ; Palatin Technologies, Inc; February 2021.
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