KENGREAL® (cangrelor) Pharmacology

Rapid platelet inhibition with quick offset1

KENGREAL® (cangrelor) has onset within 2 minutes
  • IV administration
    • Bolus followed by infusion
  • Direct-acting
KENGREAL has offset within 1 hour after discontinuation
  • Binds reversibly to the P2Y12 receptor
  • Average elimination half-life of 3–6 minutes
  • Clearance independent of renal or hepatic function
KENGREAL delivers consistent pharmacokinetics

Consistent pharmacokinetics

Not influenced by age, gender, renal function, hepatic function, or patient presentation.1

The most common adverse reaction is bleeding.

Pathophysiology—Thrombosis after injury

Thrombotic response to laser-induced injury in mouse cremaster muscle arteriole.2,4

Information featured here includes in vitro data, the clinical significance of which has not been established.

KENGREAL is specifically designed as an adjunct to PCI1,3

KENGREAL rapidly inhibits platelet aggregation within 2 minutes and provides quick offset within 1 hour of discontinuation.

KENGREAL pharmacology
PK/PD chart shows KENGREAL platelet aggregation
98% inhibition of platelet aggregation in whole blood impedance aggregometery with KENGREAL
  • Pharmacology: >98% inhibition of platelet aggregation in whole blood impedance aggregometry4
  • Average elimination half-life: 3–6 minutes3

Phase I study in healthy volunteers (n=9); dose: 30 μg/kg IV bolus + 4 μg/kg/min IV infusion. KENGREAL blood levels and platelet activity were assessed over 150 minutes by whole blood impedance aggregometry in response to 20 μM of ADP.3

Infusion should be continued for at least 2 hours or the duration of the procedure, whichever is longer.1

KENGREAL does not require a several-day washout period
KENGREAL does not require a several-day washout period

Because of its offset within 1 hour,1 patients who need CABG or a valve replacement after PCI can proceed to surgery soon after KENGREAL discontinuation.

KENGREAL is appropriate for various patient types

Meet Kenneth and Rafael—two potential patients in whom KENGREAL may be appropriate

Evaluate their medical histories
IMPORTANT SAFETY INFORMATION

KENGREAL® (cangrelor) for Injection is contraindicated in patients with significant active bleeding.

KENGREAL® is contraindicated in patients with known hypersensitivity (e.g., anaphylaxis) to cangrelor or any component of the product.

Drugs that inhibit platelet P2Y12 function, including KENGREAL®, increase the risk of bleeding. In CHAMPION PHOENIX, bleeding events of all severities were more common with KENGREAL® than with clopidogrel. Bleeding complications with KENGREAL® were consistent across a variety of clinically important subgroups. Once KENGREAL® is discontinued, there is no antiplatelet effect after an hour.

The most common adverse reaction is bleeding.

INDICATION

KENGREAL® (cangrelor) for Injection is a P2Y12 platelet inhibitor indicated as an adjunct to percutaneous coronary intervention (PCI) to reduce the risk of periprocedural myocardial infarction (MI), repeat coronary revascularization, and stent thrombosis (ST) in patients who have not been treated with a P2Y12 platelet inhibitor and are not being given a glycoprotein IIb/IIIa inhibitor.

References: 1. KENGREAL® (cangrelor) Prescribing Information. 2016. 2. Stalker TJ, Traxler EA, Wu J, et al. Blood. 2013;121:1875-1885. 3. Akers WS, Oh JJ, Oestreich JH, Ferraris S, Wethington M, Steinhubl SR. Pharmacokinetics and pharmacodynamics of a bolus and infusion of cangrelor: a direct, parenteral P2Y12 receptor antagonist. J Clin Pharmacol. 2010;50(1):27-35. 4. Data on file. Chiesi USA, Inc.