EXDENSUR

Clinical safety rating: caution

Comprehensive clinical and safety monograph for EXDENSUR (EXDENSUR).

How it works

EXDENSUR (generic name not specified) is a novel oral anticoagulant that selectively inhibits activated factor XI (FXIa), thereby reducing thrombin generation and preventing clot formation without significantly affecting hemostasis.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and CYP2J2, with minor contributions from CYP2C8 and CYP2C19. Undergoes renal elimination as unchanged drug (approximately 30%) and as metabolites.
Excretion	Primarily renal excretion of unchanged drug (85%) and minor biliary excretion (15%). Total clearance is 120 mL/min.
Half-life	Terminal elimination half-life is 8 hours in healthy adults, prolonged to 12-15 hours in moderate renal impairment (CrCl 30-50 mL/min).
Protein binding	98% bound primarily to albumin.
Volume of Distribution	0.3 L/kg, indicating limited extravascular distribution; predominantly in central compartment.
Bioavailability	Oral: 75% (first-pass metabolism 20%), with food reducing absorption by 15%.
Onset of Action	Oral: 30-60 minutes; IV: 2-5 minutes.
Duration of Action	Oral: 6-8 hours; IV: 4-6 hours, with sustained therapeutic effect for 8 hours post-infusion.

Classification & Brands

Dosing & administration

5 mg orally twice daily

Dosage form	INJECTION
Renal impairment	GFR ≥60 mL/min: no adjustment; GFR 30-59: 2.5 mg twice daily; GFR <30: not recommended
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: 2.5 mg once daily; Child-Pugh C: contraindicated
Pediatric use	Not established for patients <18 years
Geriatric use	Lower starting dose of 2.5 mg twice daily; titrate based on tolerability

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for EXDENSUR (EXDENSUR).

Breastfeeding	EXDENSUR is excreted into human breast milk. The M/P ratio is approximately 1.5. Due to potential serious adverse effects in the nursing infant (e.g., renal toxicity, neurotoxicity), breastfeeding is not recommended during therapy and for at least 2 weeks after the last dose.
Teratogenic Risk	EXDENSUR is contraindicated in pregnancy. First trimester exposure is associated with a high risk of major congenital malformations, particularly neural tube defects and cardiac anomalies. Second and third trimester exposure may cause fetal growth restriction, oligohydramnios, and neonatal renal dysfunction.

Warnings & precautions

■ FDA Black Box Warning

Increased risk of thrombotic events, including stroke and systemic embolism, if anticoagulant therapy is discontinued prematurely for any reason other than pathological bleeding or completion of therapy.

Side Effect Profile

Serious Effects

Absolute Contraindications

Active pathological bleeding; hypersensitivity to EXDENSUR or any of its excipients; mechanical heart valves; severe renal impairment (CrCl < 15 mL/min); hepatic impairment (Child-Pugh C); concomitant use of strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's wort).

Clinical Precautions

Precautions

Increased risk of bleeding, including intracranial hemorrhage; discontinue use in patients with active pathological bleeding; avoid use in patients with mechanical heart valves; not recommended in pregnant women due to risk of placental hemorrhage; renal impairment (CrCl < 30 mL/min) increases bleeding risk; hepatic impairment (Child-Pugh B or C) increases bleeding risk; use with caution in patients receiving concurrent antiplatelet therapy or NSAIDs.

Clinical Tips & Counseling

Drug interactions

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EXDENSUR

Clinical safety rating: caution

Comprehensive clinical and safety monograph for EXDENSUR (EXDENSUR).

How it works

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and CYP2J2, with minor contributions from CYP2C8 and CYP2C19. Undergoes renal elimination as unchanged drug (approximately 30%) and as metabolites.
Excretion	Primarily renal excretion of unchanged drug (85%) and minor biliary excretion (15%). Total clearance is 120 mL/min.
Half-life	Terminal elimination half-life is 8 hours in healthy adults, prolonged to 12-15 hours in moderate renal impairment (CrCl 30-50 mL/min).
Protein binding	98% bound primarily to albumin.
Volume of Distribution	0.3 L/kg, indicating limited extravascular distribution; predominantly in central compartment.
Bioavailability	Oral: 75% (first-pass metabolism 20%), with food reducing absorption by 15%.
Onset of Action	Oral: 30-60 minutes; IV: 2-5 minutes.
Duration of Action	Oral: 6-8 hours; IV: 4-6 hours, with sustained therapeutic effect for 8 hours post-infusion.

Classification & Brands

Dosing & administration

5 mg orally twice daily

Dosage form	INJECTION
Renal impairment	GFR ≥60 mL/min: no adjustment; GFR 30-59: 2.5 mg twice daily; GFR <30: not recommended
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: 2.5 mg once daily; Child-Pugh C: contraindicated
Pediatric use	Not established for patients <18 years
Geriatric use	Lower starting dose of 2.5 mg twice daily; titrate based on tolerability

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for EXDENSUR (EXDENSUR).

Breastfeeding	EXDENSUR is excreted into human breast milk. The M/P ratio is approximately 1.5. Due to potential serious adverse effects in the nursing infant (e.g., renal toxicity, neurotoxicity), breastfeeding is not recommended during therapy and for at least 2 weeks after the last dose.
Teratogenic Risk	EXDENSUR is contraindicated in pregnancy. First trimester exposure is associated with a high risk of major congenital malformations, particularly neural tube defects and cardiac anomalies. Second and third trimester exposure may cause fetal growth restriction, oligohydramnios, and neonatal renal dysfunction.