Kengreal (cangrelor tetrasodium)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Cangrelor tetrasodium, a nonthienopyridine, reversible P2Y12 platelet adenosine diphosphate (ADP)-receptor antagonist, is a platelet-activation and -aggregation inhibitor.

Cangrelor is a nonthienopyridine, direct-acting, P2Y12 ADP-receptor antagonist. Unlike the thienopyridine prodrugs clopidogrel and prasugrel but like ticagrelor, cangrelor does not require hepatic transformation to exert its pharmacologic effects. Cangrelor, like ticagrelor, binds reversibly to the P2Y12 platelet ADP receptor, preventing signal transduction of the cyclic adenosine monophosphate (cAMP) pathway.

This action results in reduced exposure of fibrinogen binding sites to the platelet glycoprotein IIb/IIIa complex and subsequent inhibition of platelet activation and aggregation.

After administration of a 30-mcg/kg IV loading dose followed by a 4-mcg/kg per minute IV infusion, peak plasma concentrations of cangrelor are reached within 2 minutes. Unlike clopidogrel, cangrelor does not require metabolic activation and as a result is not associated with interindividual variability in plasma concentrations. Cangrelor is deactivated rapidly in circulation by dephosphorylation to its primary metabolite, a nucleoside, which has negligible antiplatelet activity.

Cangrelor is eliminated principally in urine (58% of the dose) and to a lesser extent in feces (35%). Because of its short half-life (3-6 minutes) and reversible binding to the P2Y12 receptor, cangrelor has a rapid offset of effect that allows recovery of platelet function within 1 hour after cessation of IV infusion.

Generic name: cangrelor tetrasodium

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Kengreal:

  • Percutaneous Coronary Intervention Adjunct For Thrombosis Prevention

Dosing

Dosage of cangrelor tetrasodium is expressed in terms of cangrelor. Cangrelor is intended to be given to patients prior to PCI in conjunction with other standard-of-care therapy (e.g., aspirin, anticoagulants). Upon discontinuance of the cangrelor infusion, patients should be transitioned to an oral P2Y12 inhibitor to maintain platelet inhibition.

Drug interactions

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Contraindications

Cangrelor is contraindicated in patients with substantial active bleeding and in those with known hypersensitivity to the drug or any ingredient in the formulation.

Adverse reactions

The most common adverse effect of cangrelor reported in clinical trials was bleeding. Cases of transient dyspnea were also reported during clinical trials.

Precautions

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ICD codes

No ICD codes are available for this drug.

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data