AQVESME

Clinical safety rating: caution

Comprehensive clinical and safety monograph for AQVESME (AQVESME).

How it works

AQVESME is a phospholipase A2 inhibitor that reduces the hydrolysis of phospholipids into lysophospholipids and free fatty acids, thereby attenuating the release of inflammatory mediators and decreasing blood-brain barrier permeability. It also exhibits antioxidant and anti-apoptotic properties.

What the body does with it

Metabolism	Primarily metabolized by cytochrome P450 enzymes, specifically CYP3A4 and CYP2C9, with minor contributions from CYP2C19. Metabolites are excreted in urine (approximately 60%) and feces (approximately 30%).
Excretion	Primarily renal (70-80% as unchanged drug), with 20-30% biliary/fecal elimination.
Half-life	Terminal elimination half-life is approximately 12-15 hours in adults with normal renal function; extended to 24-36 hours in moderate renal impairment (CrCl 30-50 mL/min).
Protein binding	98% bound primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.3-0.5 L/kg, indicating limited extravascular distribution.
Bioavailability	Oral: 60-70% (due to first-pass metabolism); IM: 100%.
Onset of Action	IV: 5-10 minutes; Oral: 30-60 minutes.
Duration of Action	IV: 4-6 hours; Oral: 6-8 hours, prolonged in hepatic impairment.

Classification & Brands

Dosing & administration

5 mg/kg via IV infusion over 1 hour every 2 weeks

Dosage form	TABLET
Renal impairment	No dose adjustment required for mild to moderate renal impairment (GFR ≥30 mL/min). For severe impairment (GFR <30 mL/min), reduce dose to 2.5 mg/kg via IV infusion over 1 hour every 2 weeks.
Liver impairment	Child-Pugh Class A: No adjustment. Child-Pugh Class B: Reduce dose to 2.5 mg/kg via IV infusion over 1 hour every 2 weeks. Child-Pugh Class C: Not recommended (no clinical data).
Pediatric use	Children 2 years and older: 5 mg/kg via IV infusion over 1 hour every 2 weeks; for weight <10 kg, dose based on body surface area (BSA): 150 mg/m² via IV infusion over 1 hour every 2 weeks.
Geriatric use	No specific dose adjustment required for elderly patients based on age alone; monitor renal function and adjust per renal criteria.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for AQVESME (AQVESME).

Breastfeeding	No data on excretion in human milk; M/P ratio unknown. Based on molecular weight (<500 Da), low-level excretion is possible. Caution recommended; consider alternative agents with more safety data.
Teratogenic Risk	First trimester: No adequate human data; animal studies show no evidence of teratogenicity at clinically relevant doses. Second and third trimesters: Potential risk of fetal growth restriction and oligohydramnios due to placental hypoperfusion from maternal hypotension. Avoid use unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

None reported by FDA for AQVESME as of current labeling.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to AQVESME or any component of the formulation. Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage). Severe hepatic impairment (Child-Pugh class C).

Clinical Precautions

Precautions	Monitor liver function tests; risk of hepatotoxicity. May cause gastrointestinal bleeding, especially in patients on anticoagulants. Use with caution in patients with renal impairment. Potential for drug interactions with CYP3A4 inhibitors or inducers.
Food/Dietary	Avoid grapefruit and grapefruit juice during treatment as they may increase drug levels. No specific food restrictions otherwise.

Clinical Tips & Counseling

Drug interactions

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AQVESME

Clinical safety rating: caution

Comprehensive clinical and safety monograph for AQVESME (AQVESME).

How it works

What the body does with it

Metabolism	Primarily metabolized by cytochrome P450 enzymes, specifically CYP3A4 and CYP2C9, with minor contributions from CYP2C19. Metabolites are excreted in urine (approximately 60%) and feces (approximately 30%).
Excretion	Primarily renal (70-80% as unchanged drug), with 20-30% biliary/fecal elimination.
Half-life	Terminal elimination half-life is approximately 12-15 hours in adults with normal renal function; extended to 24-36 hours in moderate renal impairment (CrCl 30-50 mL/min).
Protein binding	98% bound primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.3-0.5 L/kg, indicating limited extravascular distribution.
Bioavailability	Oral: 60-70% (due to first-pass metabolism); IM: 100%.
Onset of Action	IV: 5-10 minutes; Oral: 30-60 minutes.
Duration of Action	IV: 4-6 hours; Oral: 6-8 hours, prolonged in hepatic impairment.

Classification & Brands

Dosing & administration

5 mg/kg via IV infusion over 1 hour every 2 weeks

Dosage form	TABLET
Renal impairment	No dose adjustment required for mild to moderate renal impairment (GFR ≥30 mL/min). For severe impairment (GFR <30 mL/min), reduce dose to 2.5 mg/kg via IV infusion over 1 hour every 2 weeks.
Liver impairment	Child-Pugh Class A: No adjustment. Child-Pugh Class B: Reduce dose to 2.5 mg/kg via IV infusion over 1 hour every 2 weeks. Child-Pugh Class C: Not recommended (no clinical data).
Pediatric use	Children 2 years and older: 5 mg/kg via IV infusion over 1 hour every 2 weeks; for weight <10 kg, dose based on body surface area (BSA): 150 mg/m² via IV infusion over 1 hour every 2 weeks.
Geriatric use	No specific dose adjustment required for elderly patients based on age alone; monitor renal function and adjust per renal criteria.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for AQVESME (AQVESME).

Breastfeeding	No data on excretion in human milk; M/P ratio unknown. Based on molecular weight (<500 Da), low-level excretion is possible. Caution recommended; consider alternative agents with more safety data.
Teratogenic Risk	First trimester: No adequate human data; animal studies show no evidence of teratogenicity at clinically relevant doses. Second and third trimesters: Potential risk of fetal growth restriction and oligohydramnios due to placental hypoperfusion from maternal hypotension. Avoid use unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

None reported by FDA for AQVESME as of current labeling.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to AQVESME or any component of the formulation. Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage). Severe hepatic impairment (Child-Pugh class C).

Clinical Precautions

Precautions	Monitor liver function tests; risk of hepatotoxicity. May cause gastrointestinal bleeding, especially in patients on anticoagulants. Use with caution in patients with renal impairment. Potential for drug interactions with CYP3A4 inhibitors or inducers.
Food/Dietary	Avoid grapefruit and grapefruit juice during treatment as they may increase drug levels. No specific food restrictions otherwise.

Clinical Tips & Counseling

Drug interactions

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