DENAVIR

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DENAVIR (DENAVIR).

How it works

DENAVIR is a synthetic peptide that inhibits viral replication by preventing the fusion of the viral envelope with the host cell membrane. It specifically targets the HIV-1 envelope glycoprotein gp41, blocking the conformational changes required for membrane fusion.

What the body does with it

Metabolism	DENAVIR is not significantly metabolized; it is excreted unchanged primarily via the kidneys.
Excretion	Renal excretion of unchanged drug accounts for approximately 90% of the administered dose via glomerular filtration and tubular secretion. Biliary/fecal elimination is minimal (<5%).
Half-life	Terminal elimination half-life is 2.5–3.5 hours in patients with normal renal function. Prolonged to 20–40 hours in severe renal impairment (CrCl <30 mL/min).
Protein binding	Approximately 70–80% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Volume of distribution is 0.8–1.2 L/kg, indicating wide distribution into total body water and tissues.
Bioavailability	Oral bioavailability is approximately 80–85% following administration with food, which enhances absorption. Absolute bioavailability is 80%.
Onset of Action	Oral: Onset of action occurs within 1–2 hours post-dose. Intravenous: Onset is immediate upon completion of infusion.
Duration of Action	Duration of antiviral effect is approximately 8–12 hours based on trough plasma concentrations above EC50. Clinical dosing interval is every 12 hours for oral and every 24 hours for IV in renal impairment.

Classification & Brands

Dosing & administration

5 mg applied topically to affected area once daily for 4 weeks.

Dosage form	CREAM
Renal impairment	No adjustment required; drug is not significantly renally excreted.
Liver impairment	No adjustment required for mild to moderate hepatic impairment; safety not established in severe impairment.
Pediatric use	Not approved for pediatric use; safety and efficacy not established.
Geriatric use	No specific adjustment; use with caution due to potential age-related skin barrier changes.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DENAVIR (DENAVIR).

Breastfeeding	Excreted in human milk in low concentrations; M/P ratio unknown. Caution in breastfeeding due to potential for adverse effects in infant (e.g., bleeding risk).
Teratogenic Risk	FDA Pregnancy Category C. In first trimester, no adequate human studies; animal studies show embryotoxicity at high doses. Second and third trimesters: risk of fetal hemorrhage due to inhibition of platelet aggregation; avoid near term. Use only if potential benefit outweighs risk.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to DENAVIR or any of its components"]

Clinical Precautions

Precautions	["Hypersensitivity reactions","Local injection site reactions","Increased risk of infections"]
Food/Dietary	No known food interactions. Maintain a balanced diet to support immune function.

Clinical Tips & Counseling

Clinical Pearls

Apply within 48 hours of lesion onset for efficacy. Use a finger cot or gloves to prevent autoinoculation. Avoid application to mucous membranes or eyes.

Drug interactions

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DENAVIR

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DENAVIR (DENAVIR).

How it works

What the body does with it

Metabolism	DENAVIR is not significantly metabolized; it is excreted unchanged primarily via the kidneys.
Excretion	Renal excretion of unchanged drug accounts for approximately 90% of the administered dose via glomerular filtration and tubular secretion. Biliary/fecal elimination is minimal (<5%).
Half-life	Terminal elimination half-life is 2.5–3.5 hours in patients with normal renal function. Prolonged to 20–40 hours in severe renal impairment (CrCl <30 mL/min).
Protein binding	Approximately 70–80% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Volume of distribution is 0.8–1.2 L/kg, indicating wide distribution into total body water and tissues.
Bioavailability	Oral bioavailability is approximately 80–85% following administration with food, which enhances absorption. Absolute bioavailability is 80%.
Onset of Action	Oral: Onset of action occurs within 1–2 hours post-dose. Intravenous: Onset is immediate upon completion of infusion.
Duration of Action	Duration of antiviral effect is approximately 8–12 hours based on trough plasma concentrations above EC50. Clinical dosing interval is every 12 hours for oral and every 24 hours for IV in renal impairment.

Classification & Brands

Dosing & administration

5 mg applied topically to affected area once daily for 4 weeks.

Dosage form	CREAM
Renal impairment	No adjustment required; drug is not significantly renally excreted.
Liver impairment	No adjustment required for mild to moderate hepatic impairment; safety not established in severe impairment.
Pediatric use	Not approved for pediatric use; safety and efficacy not established.
Geriatric use	No specific adjustment; use with caution due to potential age-related skin barrier changes.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DENAVIR (DENAVIR).

Breastfeeding	Excreted in human milk in low concentrations; M/P ratio unknown. Caution in breastfeeding due to potential for adverse effects in infant (e.g., bleeding risk).
Teratogenic Risk	FDA Pregnancy Category C. In first trimester, no adequate human studies; animal studies show embryotoxicity at high doses. Second and third trimesters: risk of fetal hemorrhage due to inhibition of platelet aggregation; avoid near term. Use only if potential benefit outweighs risk.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to DENAVIR or any of its components"]

Clinical Precautions

Precautions	["Hypersensitivity reactions","Local injection site reactions","Increased risk of infections"]
Food/Dietary	No known food interactions. Maintain a balanced diet to support immune function.

Clinical Tips & Counseling

Clinical Pearls

Apply within 48 hours of lesion onset for efficacy. Use a finger cot or gloves to prevent autoinoculation. Avoid application to mucous membranes or eyes.

Drug interactions

Loading safety data…