From the Guidelines
IV P2Y12 inhibitors, such as cangrelor, are recommended for use in patients undergoing PCI who are P2Y12 inhibitor naïve, to reduce periprocedural ischemic events, as supported by the 2021 ACC/AHA/SCAI guideline for coronary artery revascularization 1.
Key Characteristics of IV P2Y12 Inhibitors
- Cangrelor is a direct-acting, intravenous antagonist of the P2Y12 receptor, characterized by rapid and potent platelet inhibitory effects with restoration of platelet function occurring within 1 hour of drug discontinuation 1.
- It is administered as a 30 μg/kg bolus followed by a 4 μg/kg/min infusion, achieving almost immediate platelet inhibition within minutes of administration.
- Cangrelor has a very short half-life of 3-6 minutes, allowing platelet function to return to normal within 1-2 hours after stopping the infusion, making it useful for patients who might need urgent surgery.
Clinical Use and Recommendations
- IV P2Y12 inhibitors are particularly valuable in acute settings like primary percutaneous coronary intervention (PCI) for heart attacks when rapid antiplatelet effect is needed or when patients cannot take oral medications 1.
- The main side effects include bleeding complications, dyspnea, and allergic reactions.
- Typically, patients are transitioned to oral P2Y12 inhibitors before the IV infusion is discontinued to maintain antiplatelet therapy.
Comparison with Other Antiplatelet Agents
- Unlike oral P2Y12 inhibitors (clopidogrel, prasugrel, ticagrelor) which can take hours to achieve full effect, IV P2Y12 inhibitors work almost instantly 1.
- Cangrelor may be considered in patients who have not received P2Y12 receptor inhibitors, as stated in the 2017 ESC guidelines for the management of acute myocardial infarction in patients presenting with ST-segment elevation 1.
From the FDA Drug Label
KENGREAL is a direct-acting P2Y12 platelet receptor inhibitor that blocks adenosine diphosphate (ADP)-induced platelet activation and aggregation. Cangrelor is a direct P2Y12 platelet receptor inhibitor that blocks ADP-induced platelet activation and aggregation.
IV P2Y12 inhibitors are a class of drugs that inhibit platelet activation and aggregation by blocking the P2Y12 receptor.
- Examples of IV P2Y12 inhibitors include cangrelor.
- Key characteristics of cangrelor include:
From the Research
Definition and Mechanism of IV P2Y12 Inhibitors
- IV P2Y12 inhibitors are a class of antiplatelet drugs that work by inhibiting the P2Y12 receptor on platelets, thereby preventing platelet activation and aggregation [ 3, 4 ].
- Cangrelor is the only currently available intravenous platelet P2Y12 receptor inhibitor [ 4 ].
- It is characterized by potent, predictable, and rapidly reversible antiplatelet effects [ 4 ].
Clinical Use of IV P2Y12 Inhibitors
- Cangrelor is indicated for use in patients with coronary artery disease undergoing percutaneous coronary intervention [ 4 ].
- It has been shown to reduce periprocedural complications such as myocardial infarction, repeat coronary revascularization, and stent thrombosis in patients not yet treated with another P2Y12 inhibitor or glycoprotein IIb/IIIa inhibitor [ 3 ].
- IV P2Y12 inhibitors like cangrelor can also be used for antiplatelet bridging in patients who must discontinue their oral P2Y12 inhibitor before coronary artery bypass grafting [ 5, 6 ].
Safety and Efficacy of IV P2Y12 Inhibitors
- The safety and efficacy of cangrelor have been evaluated in several clinical trials, including the CHAMPION PHOENIX trial [ 4, 6 ].
- While cangrelor has been shown to be effective in reducing periprocedural complications, it has also been associated with a higher risk of bleeding, particularly in certain patient populations [ 5 ].
- The use of cangrelor requires careful consideration of the potential benefits and risks, particularly in patients with a high risk of bleeding [ 5 ].