KENGREAL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for KENGREAL (KENGREAL).
Cangrelor is a reversible, direct-acting P2Y12 platelet receptor antagonist that inhibits ADP-mediated platelet activation and aggregation.
| Metabolism | Cangrelor is rapidly deactivated by dephosphorylation via ectonucleotidases to its major metabolite, a nucleoside triphosphate analogue, without involvement of cytochrome P450 enzymes. |
| Excretion | Cangrelor is metabolized via rapid dephosphorylation to its major metabolite, a nucleoside, which is further degraded; approximately 58% of the dose is excreted in urine as unchanged cangrelor and metabolites, with <35% in feces. |
| Half-life | Terminal elimination half-life is approximately 3–6 minutes (mean 3.3 minutes), allowing rapid recovery of platelet function within 60 minutes of infusion cessation. |
| Protein binding | 97–98% bound, primarily to serum albumin. |
| Volume of Distribution | Volume of distribution at steady state is approximately 3.7 L, correlating to ~0.05 L/kg, indicating minimal extravascular distribution. |
| Bioavailability | Not applicable; only intravenous administration (bioavailability 100% by IV route). |
| Onset of Action | Intravenous: immediate inhibition of platelet aggregation within 2 minutes of bolus administration. |
| Duration of Action | Duration of action is short: platelet function returns to >50% of baseline within 1 hour after stopping infusion. Note: Requires rebolus if restarted after interruption. |
10 mcg/kg intravenous bolus over 1-2 minutes, followed by 0.1 mcg/kg/min continuous intravenous infusion for 2-4 hours.
| Dosage form | POWDER |
| Renal impairment | No dose adjustment required for renal impairment (including end-stage renal disease). |
| Liver impairment | No dose adjustment required for mild or moderate hepatic impairment (Child-Pugh class A or B). Not studied in severe hepatic impairment (Child-Pugh class C). |
| Pediatric use | Not established; safety and efficacy in pediatric patients have not been studied. |
| Geriatric use | No specific dose adjustment recommended; clinical studies included patients aged 65 and older with no overall differences in safety or efficacy observed. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for KENGREAL (KENGREAL).
| Breastfeeding | It is unknown whether cangrelor is excreted in human milk. In lactating rats, cangrelor and its metabolites were present in milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from KENGREAL, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. M/P ratio not established in humans. |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. In animal studies, no teratogenicity was observed at doses up to 3 times the recommended human dose. However, because animal reproduction studies are not always predictive of human response, KENGREAL should be used during pregnancy only if clearly needed. In the first trimester, potential risks of maternal bleeding and fetal hemorrhage due to antiplatelet effect. In the second trimester, similar risks. In the third trimester, increased risk of maternal bleeding during delivery and potential for fetal intracranial hemorrhage. |
■ FDA Black Box Warning
WARNING: BLEEDING RISK - KENGREAL increases the risk of bleeding. Significant bleeding may be fatal, intracranial, or gastrointestinal. Risk factors include older age, renal impairment, low body weight, and concomitant use of anticoagulants.
| Serious Effects |
Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage), history of intracranial hemorrhage, severe hepatic impairment, known hypersensitivity to cangrelor or any component of the product.
| Precautions | Bleeding risk (including fatal bleeding), thrombotic thrombocytopenic purpura (TTP), hypersensitivity reactions (including anaphylaxis and angioedema), renal impairment (increases drug exposure), and need for transition to oral P2Y12 inhibitor (administer after infusion discontinuation). |
| Food/Dietary | No significant food interactions. Patients may eat normally. However, avoid excessive alcohol consumption as it may increase bleeding risk. |
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| Fetal Monitoring | Monitor for signs of bleeding in mother and fetus, including fetal distress via electronic fetal monitoring if indicated. Assess maternal complete blood count (CBC) with platelet count periodically. Monitor for hypersensitivity reactions, including angioedema, bronchospasm, and anaphylaxis. For pregnant patients, consider fetal ultrasound to assess for intracranial hemorrhage if maternal bleeding occurs. |
| Fertility Effects | No studies on fertility effects in humans. In animal studies, no impairment of fertility was observed in male or female rats at doses up to 3 times the recommended human dose. However, antiplatelet therapy may theoretically affect reproductive functions due to potential bleeding during implantation or ovulation. Insufficient data to determine clinical impact on fertility. |
| Clinical Pearls | Cangrelor (KENGREAL) is an intravenous, reversible P2Y12 inhibitor with rapid onset and offset. It is used primarily during percutaneous coronary intervention (PCI) to prevent thrombotic complications. Its half-life is approximately 3-6 minutes, and platelet function returns to normal within 1 hour after discontinuation. It should not be administered concurrently with oral P2Y12 inhibitors; transition to oral therapy (e.g., prasugrel or ticagrelor) should occur after infusion ends. Avoid use in patients with active bleeding or history of intracranial hemorrhage. Monitor for bleeding, especially at vascular access sites. |
| Patient Advice | KENGREAL is given as an IV infusion during heart procedures to prevent blood clots. · You may bruise or bleed more easily while receiving this medication. Report any unusual bleeding or bruising to your healthcare team. · Do not take aspirin or other blood thinners without your doctor's approval. · Tell your doctor if you have a history of bleeding problems, liver disease, or recent surgery. · This medication is short-acting; your bleeding risk returns to normal quickly after the infusion stops. |