Generic Name of Cangrelor
Cangrelor is the generic name of the drug marketed under the brand name KENGREAL®. 1
Pharmacological Characteristics
Cangrelor is an intravenous P2Y12 platelet inhibitor with the following key properties:
- It is an adenosine triphosphate analog that acts as a direct competitive inhibitor of the P2Y12 receptor 2
- Unlike thienopyridines (such as clopidogrel or prasugrel), cangrelor does not require hepatic conversion to an active metabolite 2
- It is administered intravenously and produces almost immediate and dose-proportional inhibition of ADP-induced platelet aggregation 2
- Cangrelor has a molecular weight of 776 and binds at the ADP binding site of the P2Y12 receptor 2
Pharmacokinetics and Pharmacodynamics
Cangrelor has distinctive pharmacokinetic properties that differentiate it from oral P2Y12 inhibitors:
- It has a very short half-life of 3-5 minutes 2
- The drug is rapidly inactivated by dephosphorylation 2
- Platelet function recovers within 60 minutes after discontinuation of therapy 2
- Elimination occurs through both renal (27%) and fecal (58%) routes 2
- Time to peak activity is approximately 30 minutes 2
Clinical Use and Administration
Cangrelor is FDA-approved as:
- An adjunct to percutaneous coronary intervention (PCI) for reducing the risk of periprocedural myocardial infarction, repeat coronary revascularization, and stent thrombosis 1
- Indicated specifically for patients who have not been treated with a P2Y12 platelet inhibitor and are not being given a glycoprotein IIb/IIIa inhibitor 1
The recommended dosage is:
- 30 mcg/kg intravenous bolus prior to PCI followed immediately by a 4 mcg/kg/min IV infusion 1
- The infusion should continue for at least 2 hours or for the duration of the procedure, whichever is longer 1
Clinical Considerations and Cautions
Important considerations when using cangrelor include:
- The interaction of cangrelor with P2Y12 prevents the binding of active metabolites of clopidogrel or prasugrel, which complicates transitioning patients from cangrelor to oral thienopyridines 2
- Oral P2Y12 inhibitors can only exert their effects once cangrelor dissociates from the P2Y12 receptor 2
- Contraindications include significant active bleeding and hypersensitivity to cangrelor or any component of the product 1
- Like other drugs that inhibit platelet P2Y12 function, cangrelor can increase the risk of bleeding 1
Clinical Evidence and Efficacy
Cangrelor has been evaluated in several clinical trials:
- The CHAMPION PHOENIX trial demonstrated that cangrelor significantly reduced the primary endpoint of all-cause death, MI, ischemia-driven revascularization, or stent thrombosis compared to clopidogrel in patients undergoing PCI for acute or stable coronary syndromes 2
- A patient-level pooled analysis of the CHAMPION trials showed that cangrelor was associated with a significant reduction in periprocedural ischemic events compared with control 2, 3
- The unique pharmacological properties of cangrelor make it particularly beneficial in clinical scenarios where absorption of orally administered P2Y12 inhibitors is impaired or not possible 2, 4