CANGRELOR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CANGRELOR (CANGRELOR).
Cangrelor is a reversible, direct-acting P2Y12 platelet receptor antagonist that inhibits ADP-induced platelet aggregation.
| Metabolism | Cangrelor is metabolized via dephosphorylation to its active metabolite, which is further metabolized by nucleotidases. It does not rely on hepatic CYP450 enzymes. |
| Excretion | Renal: 58% (as inactive metabolite), fecal: 35%, biliary: <5% |
| Half-life | 3-6 minutes (terminal elimination half-life of parent drug); after IV infusion cessation, platelet function recovers within 1-2 hours due to rapid deactivation |
| Protein binding | 97-98% (mainly to human serum albumin) |
| Volume of Distribution | 0.17-0.21 L/kg (primarily confined to extracellular fluid; low Vd indicates limited tissue distribution) |
| Bioavailability | Intravenous: 100%; oral: not available (only IV formulation) |
| Onset of Action | Intravenous: 2 minutes (platelet inhibition >80% at 2-4 min after bolus); oral: not applicable |
| Duration of Action | 1-2 hours after infusion discontinuation (platelet function returns to baseline); infusion maintains steady inhibition |
Initial IV bolus of 30 mcg/kg followed immediately by IV infusion of 4 mcg/kg/min for at least 2 hours or for duration of PCI, whichever is longer. Transition to oral P2Y12 inhibitor post-PCI.
| Dosage form | POWDER |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). For severe renal impairment (CrCl <30 mL/min) or dialysis, reduce infusion to 2 mcg/kg/min. Bolus dose remains 30 mcg/kg. |
| Liver impairment | No dose adjustment required for mild hepatic impairment (Child-Pugh Class A). For moderate to severe impairment (Child-Pugh Class B or C), reduce infusion to 2 mcg/kg/min. Bolus dose remains 30 mcg/kg. |
| Pediatric use | Safety and efficacy not established; no specific dosing guidelines available. |
| Geriatric use | No specific dose adjustment recommended solely for age. However, higher incidence of renal and hepatic impairment may necessitate dose reduction as per renal/hepatic guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CANGRELOR (CANGRELOR).
| Breastfeeding | No data on presence in human milk; M/P ratio unknown. Risk of bleeding in infant. Caution advised; consider discontinuing breastfeeding or drug based on importance to mother. |
| Teratogenic Risk | No adequate human studies; animal studies show no teratogenic effects at exposures 4-6 times human exposure. FDA Pregnancy Category C. Risk in first trimester unknown; avoid unless benefit outweighs risk. Second and third trimester: limited data, may cause fetal hemorrhage due to antiplatelet activity. |
| Fetal Monitoring |
■ FDA Black Box Warning
WARNING: BLEEDING RISK: Cangrelor increases the risk of bleeding, including fatal bleeding. Do not use in patients with active bleeding or a history of bleeding disorders.
| Serious Effects |
["Active bleeding","History of bleeding disorders","Severe hypersensitivity to cangrelor or any component of the formulation"]
| Precautions | ["Bleeding risk: Monitor for signs of bleeding; discontinue if active bleeding occurs","Thrombotic thrombocytopenic purpura (TTP): Rare reports","Hypersensitivity reactions: Including anaphylaxis","Renal impairment: Use with caution in severe renal impairment (CrCl <15 mL/min) as safety not established","Hepatic impairment: Use with caution in severe hepatic impairment"] |
| Food/Dietary | No significant food interactions. Avoid alcohol as it may increase bleeding risk. Maintain a balanced diet; no specific dietary restrictions. |
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| Monitor maternal platelet count, bleeding time, and signs of hemorrhage; fetal monitoring for signs of bleeding (e.g., unexplained fetal distress) if used near term. |
| Fertility Effects | No human data on fertility; animal studies show no impairment of fertility at exposures up to 6 times human exposure. |
| Clinical Pearls | Cangrelor is an intravenous, reversible P2Y12 platelet inhibitor with rapid onset and offset (half-life ~3-6 minutes). It is used in PCI to reduce thrombotic events. Contraindicated in active bleeding or severe hepatic impairment. Monitor for bleeding; discontinue 1 hour prior to CABG as platelet function recovers quickly. Dose adjustment not needed for renal impairment. Avoid concomitant use with oral P2Y12 inhibitors until cangrelor infusion is stopped. Infusion must be given via dedicated line; do not mix with other IV solutions. |
| Patient Advice | Cangrelor is given as an IV infusion during a heart procedure to prevent blood clots. · You will be monitored closely for any signs of bleeding (e.g., unusual bruising, dark stools). · Tell your doctor if you have any bleeding problems, liver disease, or a history of stroke. · Do not take other antiplatelet or anticoagulant medications unless prescribed. · Report any allergic reactions (rash, difficulty breathing) immediately. · The effects of cangrelor wear off quickly after the infusion is stopped. |