cangrelor 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
platelet aggregation inhibitors 5006 163706-06-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • canegrelor
  • cangrelor
  • cangrelor tetrasodium
  • kengreal
  • AR-C69931XX
  • AR-C69931MX
  • kengrexal
  • ARL69931
Cangrelor is a direct P2Y12 platelet receptor inhibitor that blocks ADP-induced platelet activation and aggregation. Cangrelor binds selectively and reversibly to the P2Y12 receptor to prevent further signaling and platelet activation.
  • Molecular weight: 776.35
  • Formula: C17H25Cl2F3N5O12P3S2
  • CLOGP: 2.23
  • LIPINSKI: 3
  • HAC: 17
  • HDO: 7
  • TPSA: 255.91
  • ALOGS: -2.25
  • ROTB: 16

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg P

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.04 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9.06 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.02 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.14 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
March 23, 2015 EMA
June 22, 2015 FDA MEDICINES CO

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AC25 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Platelet aggregation inhibitors excl. heparin
FDA PE N0000008832 Decreased Platelet Aggregation
MeSH PA D006401 Hematologic Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D010975 Platelet Aggregation Inhibitors
MeSH PA D058914 Purinergic Antagonists
MeSH PA D058919 Purinergic P2 Receptor Antagonists
MeSH PA D058921 Purinergic P2Y Receptor Antagonists
FDA EPC N0000182142 P2Y12 Platelet Inhibitor
FDA MoA N0000182143 P2Y12 Receptor Antagonists
CHEBI has role CHEBI:50427 platelet aggregation inhibitors
CHEBI has role CHEBI:68563 ADP receptor subtype P2Y12 antagonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Percutaneous coronary intervention indication 415070008




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 0.89 acidic
pKa2 4.72 acidic
pKa3 5.95 acidic
pKa4 11.94 acidic
pKa5 13.04 acidic
pKa6 3.26 Basic
pKa7 2.66 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
50MG/VIAL KENGREAL CHIESI N204958 June 22, 2015 RX POWDER INTRAVENOUS 6130208 June 29, 2023 P2Y12 PLATELET INHIBITOR FOR USE AS ADJUNCT TO PERCUTANEOUS CORONARY INTERVENTION TO REDUCE RISK OF VARIOUS DISEASES/CONDITIONS IN PATIENTS NOT TREATED WITH A P2Y12 PLATELET INHIBITOR AND NOT GIVEN A GLYCOPROTEIN IIB/IIIA INHIBITOR
50MG/VIAL KENGREAL CHIESI N204958 June 22, 2015 RX POWDER INTRAVENOUS 9925265 May 13, 2029 METHOD OF REDUCING THE RISK OF PERIPROCEDURAL MYOCARDIAL INFARCTION, AND STENT THROMBOSIS IN A PATIENT UNDERGOING PCI BY ADMINISTERING INTRAVENOUSLY 30 UG/KG BOLUS BEFORE PCI AND THEN A CONTINUOUS INFUSION
50MG/VIAL KENGREAL CHIESI N204958 June 22, 2015 RX POWDER INTRAVENOUS 9427448 Nov. 10, 2030 METHOD OF TREATING, REDUCING THE INCIDENCE OF, OR PREVENTING AN ISCHEMIC EVENT IN A PATIENT UNDERGOING PCI BY ADMINISTERING INTRAVENOUSLY 30 UG/KG BOLUS BEFORE PCI AND CONTINUOUS INFUSION OF 4 UG/KG/MIN FOR AT LEAST 2 HOURS OR THE DURATION OF THE PCI
50MG/VIAL KENGREAL CHIESI N204958 June 22, 2015 RX POWDER INTRAVENOUS 8680052 March 9, 2033 METHOD COMPRISING IV ADMINISTRATION OF CANGRELOR BEFORE PCI THEN CONTINUOUS INFUSION FOR AT LEAST 2 HOURS OR THE DURATION OF PCI AND, DURING OR AFTER CONTINUOUS INFUSION, ADMINISTRATION OF A LOADING DOSE OF TICAGRELOR, OR AN EQUIVALENT METHOD
50MG/VIAL KENGREAL CHIESI N204958 June 22, 2015 RX POWDER INTRAVENOUS 10039780 July 10, 2035 METHOD OF REDUCING THE RISK OF PERIPROCEDURAL MYOCARDIAL INFARCTION, AND STENT THROMBOSIS IN A PATIENT UNDERGOING PCI BY ADMINISTERING INTRAVENOUSLY 30 UG/KG BOLUS BEFORE PCI AND THEN A CONTINUOUS INFUSION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
P2Y purinoceptor 12 GPCR ANTAGONIST IC50 8.63 SCIENTIFIC LITERATURE DRUG LABEL
P2Y purinoceptor 13 GPCR ANTAGONIST IC50 8.30 IUPHAR
Uracil nucleotide/cysteinyl leukotriene receptor GPCR ANTAGONIST IC50 8.92 IUPHAR

External reference:

IDSource
D03359 KEGG_DRUG
4034569 VUID
N0000191733 NUI
4034569 VANDF
CHEBI:90841 CHEBI
CHEMBL334966 ChEMBL_ID
CHEMBL1097279 ChEMBL_ID
C117446 MESH_SUPPLEMENTAL_RECORD_UI
1776 IUPHAR_LIGAND_ID
7883 INN_ID
163706-36-3 SECONDARY_CAS_RN
DB06441 DRUGBANK_ID
6AQ1Y404U7 UNII
9854012 PUBCHEM_CID
1656051 RXNORM
234577 MMSL
31089 MMSL
31177 MMSL
d08365 MMSL
716118009 SNOMEDCT_US
763606005 SNOMEDCT_US
C1121991 UMLSCUI
016203 NDDF
016205 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
KENGREAL HUMAN PRESCRIPTION DRUG LABEL 1 10122-620 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 50 mg INTRAVENOUS NDA 24 sections