VYLEESI (AUTOINJECTOR)

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VYLEESI (AUTOINJECTOR) (VYLEESI (AUTOINJECTOR)).

How it works

VYLEESI (bremelanotide) is a melanocortin receptor agonist, specifically activating the melanocortin-4 receptor (MC4R), which is involved in the central regulation of sexual desire and arousal. It is thought to modulate endogenous pathways in the brain that control sexual response.

What the body does with it

Metabolism	Primarily hydrolyzed by peptidases in plasma and tissues; minimal hepatic metabolism via CYP450 enzymes.
Excretion	Primarily renal (approximately 80% as unchanged drug) with minor fecal elimination (5-10%).
Half-life	Terminal elimination half-life is approximately 4 hours; clinically, steady-state is achieved within 1-2 days.
Protein binding	Approximately 60% bound primarily to albumin.
Volume of Distribution	Volume of distribution is approximately 0.4 L/kg, indicating distribution primarily in extracellular fluid.
Bioavailability	Subcutaneous injection: approximately 95%.
Onset of Action	Subcutaneous injection: onset within approximately 30 minutes.
Duration of Action	Duration of action is approximately 4-6 hours for the intended effect; effects peak at 1-2 hours post-dose.

Classification & Brands

Dosing & administration

1.5 mg subcutaneously as needed, at least 45 minutes prior to sexual activity, not to exceed one dose per 24 hours.

Dosage form	SOLUTION
Renal impairment	No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (eGFR <30 mL/min/1.73 m²).
Liver impairment	Contraindicated in severe hepatic impairment (Child-Pugh class C). No dose adjustment recommended for mild to moderate impairment (Child-Pugh class A or B).
Pediatric use	Not approved for use in pediatric patients. Safety and efficacy not established.
Geriatric use	No specific dose adjustment recommended, but consider lower starting dose due to potential increased sensitivity and comorbidities; clinical experience limited in patients >75 years.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for VYLEESI (AUTOINJECTOR) (VYLEESI (AUTOINJECTOR)).

Breastfeeding	No data are available on the presence of bremelanotide in human milk, its effects on the breastfed infant, or milk production. The M/P ratio is unknown. Because of the potential for serious adverse reactions in nursing infants, advise women not to breastfeed during treatment and for 48 hours after the last dose.
Teratogenic Risk	Vyleesi (bremelanotide) is contraindicated in pregnancy due to embryo-fetal toxicity. In animal studies, administration during organogenesis resulted in increased postimplantation loss and reduced fetal body weight. No data exist in pregnant women; therefore, avoid use in women who are or may become pregnant. If pregnancy occurs, discontinue immediately and report to the FDA.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Uncontrolled hypertension or known cardiovascular disease.","Concomitant use with naltrexone (opioid antagonist) due to potential reduced efficacy of naltrexone."]

Clinical Precautions

Precautions

["Hypertension: May increase blood pressure; contraindicated in patients with uncontrolled hypertension or cardiovascular disease.","Nausea: Commonly reported, especially at higher doses; may require dose reduction or discontinuation.","Injection site reactions.","Fetal risk: Not recommended during pregnancy; advise effective contraception.","Coadministration with alcohol may increase risk of hypotension and syncope."]

Clinical Tips & Counseling

Drug interactions

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VYLEESI (AUTOINJECTOR)

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VYLEESI (AUTOINJECTOR) (VYLEESI (AUTOINJECTOR)).

How it works

What the body does with it

Metabolism	Primarily hydrolyzed by peptidases in plasma and tissues; minimal hepatic metabolism via CYP450 enzymes.
Excretion	Primarily renal (approximately 80% as unchanged drug) with minor fecal elimination (5-10%).
Half-life	Terminal elimination half-life is approximately 4 hours; clinically, steady-state is achieved within 1-2 days.
Protein binding	Approximately 60% bound primarily to albumin.
Volume of Distribution	Volume of distribution is approximately 0.4 L/kg, indicating distribution primarily in extracellular fluid.
Bioavailability	Subcutaneous injection: approximately 95%.
Onset of Action	Subcutaneous injection: onset within approximately 30 minutes.
Duration of Action	Duration of action is approximately 4-6 hours for the intended effect; effects peak at 1-2 hours post-dose.

Classification & Brands

Dosing & administration

1.5 mg subcutaneously as needed, at least 45 minutes prior to sexual activity, not to exceed one dose per 24 hours.

Dosage form	SOLUTION
Renal impairment	No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (eGFR <30 mL/min/1.73 m²).
Liver impairment	Contraindicated in severe hepatic impairment (Child-Pugh class C). No dose adjustment recommended for mild to moderate impairment (Child-Pugh class A or B).
Pediatric use	Not approved for use in pediatric patients. Safety and efficacy not established.
Geriatric use	No specific dose adjustment recommended, but consider lower starting dose due to potential increased sensitivity and comorbidities; clinical experience limited in patients >75 years.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for VYLEESI (AUTOINJECTOR) (VYLEESI (AUTOINJECTOR)).

Breastfeeding	No data are available on the presence of bremelanotide in human milk, its effects on the breastfed infant, or milk production. The M/P ratio is unknown. Because of the potential for serious adverse reactions in nursing infants, advise women not to breastfeed during treatment and for 48 hours after the last dose.
Teratogenic Risk	Vyleesi (bremelanotide) is contraindicated in pregnancy due to embryo-fetal toxicity. In animal studies, administration during organogenesis resulted in increased postimplantation loss and reduced fetal body weight. No data exist in pregnant women; therefore, avoid use in women who are or may become pregnant. If pregnancy occurs, discontinue immediately and report to the FDA.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Uncontrolled hypertension or known cardiovascular disease.","Concomitant use with naltrexone (opioid antagonist) due to potential reduced efficacy of naltrexone."]