|Trade names||Kengreal, Kengrexal, Canreal|
|Drug class||P2Y12 inhibitor|
|Main uses||Those undergoing percutaneous coronary intervention (PCI)|
|Side effects||Bleeding, shortness of breath|
|Metabolism||Rapid deactivation in the circulation (independent of CYP system)|
|Elimination half-life||~3–6 minutes|
|Excretion||Kidney (58%), Bile duct (35%)|
|Chemical and physical data|
|Molar mass||776.35 g·mol−1|
|3D model (JSmol)|
Cangrelor, sold under the brand name Kengreal among others, is a medication used in those undergoing percutaneous coronary intervention (PCI) to prevent blood clots. It is used with aspirin. It is given by injection into a vein.
Common side effects include bleeding and shortness of breath. Other side effects may include allergic reactions. Safety in pregnancy is unclear. It is a P2Y12 inhibitor which blocks platelets from sticking together.
Cangrelor was approved for medical use in the United States and Europe in 2015. In the United Kingdom 50 mg costs the NHS about £250 as of 2021. This amount in the United States costs about 830 USD.
According to recent phase 3 randomized trials, a cangrelor–clopidogrel combination is safe and has been found to be more effective than standard clopidogrel treatment at reducing ischemic events in the heart, without increasing major bleeding in the treatment of stenotic coronary arteries. The advantages of this drug combination are most prominent in patients with myocardial infarction.
Available antiplatelet drugs have delayed onset and offset of action. Since cangrelor’s effects are immediate and quickly reversed, it is a more desirable drug for elective treatment of stenotic coronary arteries, high risk acute coronary syndromes treated with immediate coronary stenting, and for bridging those surgery patients who require P2Y12 inhibition.
Current evidence regarding cangrelor therapy is limited by the lack studies assessing cangrelor administration in conjunction with either prasugrel or ticagrelor.
Poor interim results led to the abandonment of the two CHAMPION clinical trials in mid-2009. The BRIDGE study, for short term use prior to surgery, continues. The CHAMPION PHOENIX trial was a randomized study of over 11,000 patients published in 2013. It found usefulness of cangrelor in people getting cardiac stents. Compared with clopidogrel given around the time of stenting, intravenous cangrelor reduced the rate of stent thrombosis and myocardial infarction. Reviewers have questioned the methodology of the trial.
It is given at an initial dose of 30 micrograms per kilogram followed by an infusion at a rate of 4 micrograms per kilogram per minute. It is continued for at least 2 hours following the procedure. Medications by mouth such as clopidogrel, ticagrelor, or prasugrel are than used.
Despite fewer bleeding events during cardiac surgery, cangrelor carries the risk of potential autoimmune reactions manifesting as breathlessness. Potential mechanisms for dyspnea following cangrelor treatment include: repeated binding and unbinding cycles, impaired platelet turnover, and lung sequestration or apoptosis of overloaded destructive platelets. The dyspnea risks following cangrelor treatment, suggest a common mechanism linking transfusion-related acute lung injury, dyspnea, and reversible platelet inhibition.
The risk of breathlessness after intravenous cangrelor is smaller when compared with other reversible platelet P2Y12 receptor inhibitors, however, it is still significantly higher when compared to irreversible oral antiplatelet drugs or intravenous glycoprotein IIb/IIIa inhibitors; which do not increase the incidence of breathlessness at all.
Cangrelor is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. It does not require metabolic conversion to an active metabolite. This allows cangrelor’s immediate effect after infusion, and the therapeutic effects can be maintained with continuous infusion. The pharmacokinetics of cangrelor has allow it to rapidly achieve steady-state concentrations with a clearance of 50 L/h and a half-life of 2.6 to 3.3 minutes. Cessation of its administration is associated with rapid removal, and normal platelet function is restored within 1 hour.
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