Description

Simple

A medication used to treat the narrowing of the arteries in the heart due to coronary artery disease, and prevent the occurrence of events in the heart during medical procedures.

Clinical

A P2Y12 platelet receptor antagonist used during percutaneous coronary intervention to reduce the risk for periprocedural myocardial infarction (MI), repeat coronary revascularization, and stent thrombosis (ST).

Overview

Cangrelor is an intravenous, direct-acting, reversible P2Y12 inhibitor for patients undergoing percutaneous coronary intervention (PCI) who have not been yet treated by oral P2Y12 inhibitors. An advantage Cangrelor provides over oral P2Y12 inhibitors (such as prasugrel, ticagrelor, and clopidogrel) is that it is an active drug not requiring metabolic conversion therefore providing a rapid onset and offset of action. Cangrelor was approved by the FDA in June 2015 for intravenous application.

Pharmacology

Indication

For use as an adjunct to percutaneous coronary intervention (PCI) for reducing the risk of periprocedural myocardial infarction (MI), repeat coronary revascularization, and stent thrombosis (ST) in patients in who have not been treated with a P2Y12 platelet inhibitor and are not being given a glycop... Read more

Pharmacodynamic

Information currently not available.

Mechanism of action

Cangrelor is a selective, reversible, P2Y12 platelet receptor antagonist which inhibits ADP platelet aggregation. ADP is typically released by damaged blood vessels, red blood cells, and/or platelets due to agonists stimulating platelet activity. ADP binds to P2Y12 to stimulate and complete platelet... Read more

Absorption

Information currently not available.

Protein binding

about 97-98%.

Volume of distribution

In a study in healthy volunteers administration at a dose of 30 mcg/kg bolus plus 4 mcg/kg/min showed a volume of distribution of 3.9 L.

Clearance

The mean clearance is about 43.2 L/h.

Half life

The average elimination half-life of cangrelor is about 3-6 minutes.

Route of elimination

Following IV administration of [3H] cangrelor, 58% of radioactivity was recovered in urine. The remaining 35% of radioactivity was in feces, presumably following biliary excretion.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Significant active bleeding
      • Drugbank Id: DBCOND0108443
      • Modification Of:
        • Condition Status: active
        • Base:
          • Name: Significant bleeding
          • Drugbank Id: DBCOND0108071

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(1,2,6,7-3H)Testosterone
(1,2,6,7-3H)Testosterone may increase the anticoagulant activities of Cangrelor.
(R)-warfarin
The risk or severity of bleeding can be increased when Cangrelor is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of bleeding can be increased when Cangrelor is combined with (S)-Warfarin.
1-Testosterone
1-Testosterone may increase the anticoagulant activities of Cangrelor.
18-methyl-19-nortestosterone
18-methyl-19-nortestosterone may increase the anticoagulant activities of Cangrelor.
3,5-Diiodotyrosine
3,5-Diiodotyrosine may increase the anticoagulant activities of Cangrelor.
4-hydroxycoumarin
The risk or severity of bleeding can be increased when Cangrelor is combined with 4-hydroxycoumarin.
4-Hydroxytestosterone
4-Hydroxytestosterone may increase the anticoagulant activities of Cangrelor.
5beta-dihydrotestosterone
5beta-dihydrotestosterone may increase the anticoagulant activities of Cangrelor.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of bleeding and hemorrhage can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Cangrelor.
Abciximab
The risk or severity of bleeding can be increased when Abciximab is combined with Cangrelor.
Aceclofenac
The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Cangrelor.
Acemetacin
The risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Cangrelor.
Acenocoumarol
The risk or severity of bleeding can be increased when Cangrelor is combined with Acenocoumarol.
Acetylsalicylic acid
Acetylsalicylic acid may increase the antiplatelet activities of Cangrelor.
Alaproclate
The risk or severity of hemorrhage can be increased when Alaproclate is combined with Cangrelor.
Albutrepenonacog alfa
The therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Cangrelor.
Alclofenac
The risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Cangrelor.
Aldesleukin
The risk or severity of bleeding can be increased when Cangrelor is combined with Aldesleukin.
Alemtuzumab
The risk or severity of bleeding can be increased when Cangrelor is combined with Alemtuzumab.
2 References
  1. 1 . Keating GM: Cangrelor: A Review in Percutaneous Coronary Intervention. Drugs. 2015 Aug;75(12):1425-34. doi: 10.1007/s40265-015-0445-3.PubMed: 26201463
  2. 2 . Fugate SE, Cudd LA: Cangrelor for treatment of coronary thrombosis. Ann Pharmacother. 2006 May;40(5):925-30. Epub 2006 Apr 4.PubMed: 16595568