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Cangrelor tetrasodium

Class: Platelet-aggregation Inhibitors
Chemical Name: N-[2-(Methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)thio]-5′-adenylic acid monoanhydride with (dichloromethylene)bis[phosphonic acid] tetrasodium salt
Molecular Formula: C17H21Cl2F3N5Na4O12P3S2
CAS Number: 163706-36-3
Brands: Kengreal

Medically reviewed on September 1, 2016


Platelet-activation and -aggregation inhibitor; nonthienopyridine, reversible, P2Y12 platelet adenosine diphosphate (ADP)-receptor antagonist. 1 2 6

Uses for Cangrelor tetrasodium

Acute Ischemic Complications of PCI

Used as an adjunct to PCI to reduce the risk of periprocedural MI, repeat coronary revascularization, and stent thrombosis in patients who have not been treated with a P2Y12-receptor antagonist and are not being given a glycoprotein IIb/IIIa (GP IIb/IIIa) inhibitor.1 2

Dual-drug antiplatelet therapy with a P2Y12-receptor antagonist and aspirin is part of the current standard of care in patients with acute coronary syndromes (ACS).5 9 12

Potential advantages of cangrelor include rapid onset and offset of effect and less interindividual variability in antiplatelet effect (i.e., compared with clopidogrel).6 7 8 9 20 21

Precise role of cangrelor in the management of ACS remains to be established.8 9 15

Cangrelor tetrasodium Dosage and Administration


  • Intended to be given to patients prior to PCI in conjunction with other standard-of-care therapy (e.g., aspirin, anticoagulants).1 5


IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Reconstituted drug requires further dilution prior to administration.1

Administer by rapid IV (“bolus”) injection (over <1 minute) from the prepared IV infusion bag via manual IV push or infusion pump, followed by IV infusion.1 9


Reconstitute vial containing 50 mg of lyophilized cangrelor with 5 mL of sterile water for injection (swirl gently).1


Dilute reconstituted solution in 250 mL of 5% dextrose or 0.9% sodium chloride injection to a final concentration of 200 mcg/mL for rapid IV injection and infusion.1

Rate of Administration

Rapid IV (“bolus”) injection: Administer over <1 minute.1

Continuous IV infusion: Administer for at least 2 hours or for duration of PCI, whichever is longer.1 2


Available as cangrelor tetrasodium; dosage expressed in terms of cangrelor.1


Acute Ischemic Complications of PCI

30 mcg/kg by rapid IV (“bolus”) injection prior to PCI, immediately followed by 4 mcg/kg per minute by continuous IV infusion for at least 2 hours or for the duration of the procedure, whichever is longer.1 2 13 14

Transitioning to Oral Therapy

After discontinuance of cangrelor infusion, administer an oral P2Y12-receptor antagonist (clopidogrel, prasugrel, or ticagrelor) to maintain platelet inhibition.1 16 17

If ticagrelor used, administer 180 mg any time during cangrelor infusion or immediately after discontinuance of the infusion.1

If clopidogrel used, administer 600 mg immediately after discontinuance of cangrelor infusion; do not administer concurrently with cangrelor.1 (See Specific Drugs under Interactions.)

If prasugrel used, administer 60 mg immediately after discontinuance of cangrelor infusion; do not administer concurrently with cangrelor.1 (See Specific Drugs under Interactions.)

Special Populations

Renal Impairment

Dosage adjustment not required.1

Hepatic Impairment

Dosage adjustment not required. 1 (See Hepatic Impairment under Cautions.)

Cautions for Cangrelor tetrasodium


  • Substantial active bleeding.1

  • Known hypersensitivity to cangrelor or any ingredient in the formulation.1



Possible bleeding, especially hematoma at the site of vascular access.1 2 3 4 6 8 9 10 11 (See Contraindications.)

In pivotal clinical trial, greater incidence of bleeding events of all severities with cangrelor compared with clopidogrel; however, rate of severe bleeding (per the Global Use of Strategies to Open Occluded Coronary Arteries [GUSTO] criteria) not substantially different between treatment groups.1 2 6

Antiplatelet effect negligible 1 hour after discontinuance of cangrelor infusion.1 6 11 14 16 18

Sensitivity Reactions


Hypersensitivity reactions (e.g., anaphylaxis, bronchospasm, angioedema, stridor) reported.1 (See Contraindications.)

Specific Populations


Category C.1

No adequate and well-controlled studies of cangrelor in pregnant women.1 In animal studies, cangrelor produced dose-related fetal growth retardation and increased incidences of abortion and/or intrauterine losses, but did not produce malformations; not considered to be a teratogen.1


Not known whether cangrelor is distributed into human milk; discontinue nursing or the drug.1

Pediatric Use

Safety and efficacy not established.1 2

Geriatric Use

No substantial differences in safety or efficacy relative to younger adults.1

Renal Impairment

No dosage adjustment required; however, worsening renal function reported in some patients with severe renal impairment (Clcr <30 mL/minute) receiving cangrelor in clinical studies.1 (See Renal Impairment under Dosage and Administration.)

Hepatic Impairment

Safety and efficacy not established in patients with hepatic impairment.1 Hepatic impairment not expected to affect pharmacokinetics because metabolism not dependent on hepatic function.1 11

Common Adverse Effects

Bleeding; transient dyspnea reported in some patients.1 2 3 4 16

Interactions for Cangrelor tetrasodium

Drugs Metabolized by Hepatic Microsomal Enzymes

Neither cangrelor nor its major metabolites inhibit activity of the hepatic CYP isoenzymes at therapeutic concentrations in vitro.1 Cangrelor not expected to interact with drugs metabolized by these microsomal enzymes.1

Specific Drugs





No effect on pharmacokinetics or pharmacodynamics of cangrelor1 11


No clinically detectable interactions1


No effect on pharmacokinetics or pharmacodynamics of cangrelor1 11

Heparin, low molecular weight

No clinically detectable interactions1 11


No effect on pharmacokinetics or pharmacodynamics of cangrelor1


Antiplatelet effect of ticagrelor 180 mg not substantially altered when given during cangrelor infusion1 11 16

Administer ticagrelor at any time during or immediately after cangrelor infusion1

Thienopyridines (clopidogrel, prasugrel)

Decreased antiplatelet effect of clopidogrel 600 mg or prasugrel 60 mg when given during cangrelor infusion1 6 16

Do not administer clopidogrel or prasugrel until cangrelor infusion discontinued1

Cangrelor tetrasodium Pharmacokinetics



Peak plasma concentrations achieved within 2 minutes after administration of rapid IV (“bolus”) injection followed by continuous infusion.1 9


Immediate antiplatelet effect.1 9


Platelet function returns to normal within 1 hour after discontinuance of infusion.1 9 18



Not known whether the drug is distributed into human milk.1

Plasma Protein Binding

Approximately 97–98%.1



Rapidly deactivated in circulation by dephosphorylation to its primary metabolite, which has negligible antiplatelet activity.1 9 11 16

Elimination Route

Excreted in urine (58%) and feces (35%).1 11


3–6 minutes.1 6 11 14 16 18

Special Populations

Pharmacokinetics not affected by gender, age, renal status, or hepatic function.1 11 Body weight has effect on pharmacokinetics but accounted for by weight-based infusion regimen.1 11




Powder for Injection

20–25°C (may be exposed to 15–30°C).1

Diluted IV solutions (200 mcg/mL) are stable at room temperature for ≤12 hours in 5% dextrose injection and 24 hours in 0.9% sodium chloride injection.1


For information on systemic interactions resulting from concomitant use, see Interactions.


Solution Compatibility1


Dextrose 5% in water

Sodium chloride 0.9%


  • Nonthienopyridine, direct-acting P2Y12 platelet ADP-receptor antagonist; unlike thienopyridines (e.g., clopidogrel, prasugrel), but like ticagrelor, cangrelor binds reversibly to P2Y12 receptor and does not require hepatic transformation to exert its pharmacologic effects.1 2 6 9 13

  • Prevents signal transduction of the cyclic adenosine monophosphate (cAMP) pathway, resulting in reduced exposure of fibrinogen binding sites to the GP IIb/IIIa complex and subsequent inhibition of platelet activation and aggregation.13 19

  • Compared with clopidogrel, cangrelor produces more rapid and effective inhibition of platelet aggregation and has a faster onset and offset of action.1 18 20

Advice to Patients

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of patients informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant diseases.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Cangrelor Tetrasodium


Dosage Forms


Brand Names



For injection, for IV use

50 mg (of cangrelor)


Medicines Company

AHFS DI Essentials. © Copyright 2018, Selected Revisions September 1, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.


1. The Medicines Company. Kengreal (cangrelor) for injection prescribing information. Parsippany, NJ; 2015 Jun.

2. Bhatt DL, Stone GW, Mahaffey KW et al. Effect of platelet inhibition with cangrelor during PCI on ischemic events. N Engl J Med. 2013; 368:1303-13.

3. Harrington RA, Stone GW, McNulty S et al. Platelet inhibition with cangrelor in patients undergoing PCI. N Engl J Med. 2009; 361:2318-29.

4. Bhatt DL, Lincoff AM, Gibson CM et al. Intravenous platelet blockade with cangrelor during PCI. N Engl J Med. 2009; 361:2330-41.

5. Levine GN, Bates ER, Blankenship JC et al. 2011 ACCF/AHA/SCAI Guideline for Percutaneous Coronary Intervention. A report of the American College of Cardiology Foundation/American Heart Association Task Force on Practice Guidelines and the Society for Cardiovascular Angiography and Interventions. J Am Coll Cardiol. 2011; 58:e44-122.

6. Franchi F, Rollini F, Muñiz-Lozano A et al. Cangrelor: a review on pharmacology and clinical trial development. Expert Rev Cardiovasc Ther. 2013; 11:1279-91.

7. Kastrati A, Ndrepepa G. Cangrelor - a champion lost in translation?. N Engl J Med. 2009; 361:2382-4.

8. Mehta SR. Cangrelor: a new CHAMPION for percutaneous coronary intervention. Lancet. 2013; 382:1960-2.

9. Oestreich JH, Dobesh PP. Cangrelor for treatment during percutaneous coronary intervention. Future Cardiol. 2014; 10:201-13.

10. Steg PG, Bhatt DL, Hamm CW et al. Effect of cangrelor on periprocedural outcomes in percutaneous coronary interventions: a pooled analysis of patient-level data. Lancet. 2013; 382:1981-92.

11. Waite LH, Phan YL, Spinler SA. Cangrelor: a novel intravenous antiplatelet agent with a questionable future. Pharmacotherapy. 2014; 34:1061-76.

12. Hamm CW, Bassand JP, Agewall S et al. ESC Guidelines for the management of acute coronary syndromes in patients presenting without persistent ST-segment elevation: The Task Force for the management of acute coronary syndromes (ACS) in patients presenting without persistent ST-segment elevation of the European Society of Cardiology (ESC). Eur Heart J. 2011; 32:2999-3054.

13. Wallentin L. P2Y(12) inhibitors: differences in properties and mechanisms of action and potential consequences for clinical use. Eur Heart J. 2009; 30:1964-77.

14. Bonadei I, Sciatti E, Vizzardi E et al. New frontiers in the management of acute coronary syndromes: cangrelor and elinogrel. Recent Pat Cardiovasc Drug Discov. 2014; 9:22-7.

15. Lange RA, Hillis LD. The duel between dual antiplatelet therapies. N Engl J Med. 2013; 368:1356-7.

16. Kubica J, Kozinski M, Navarese EP et al. Cangrelor: an emerging therapeutic option for patients with coronary artery disease. Curr Med Res Opin. 2014; 30:813-28.

17. Schneider DJ, Seecheran N, Raza SS et al. Pharmacodynamic effects during the transition between cangrelor and prasugrel. Coron Artery Dis. 2015; 26:42-8.

18. Lhermusier T, Baker NC, Waksman R. Overview of the 2014 Food and Drug Administration Cardiovascular and Renal Drugs Advisory Committee meeting regarding cangrelor. Am J Cardiol. 2015; 115:1154-61.

19. Angiolillo DJ, Capranzano P. Pharmacology of emerging novel platelet inhibitors. Am Heart J. 2008; 156(2 Suppl):S10-5.

20. Tang Y, Zhang YC, Chen Y et al. Efficacy and safety of cangrelor for patients with coronary artery disease: a meta-analysis of four randomized trials. Int J Clin Exp Med. 2015; 8:800-8.

21. Cattaneo M. New P2Y(12) inhibitors. Circulation. 2010; 121:171-9.