cangrelor 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: 1.56
  • 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

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 purinergic receptor subtype p2y12 antagonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Percutaneous coronary intervention indication 415070008

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)

None

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 Unclassified ANTAGONIST IC50 8.92 IUPHAR

External reference:

IDSource
D03359 KEGG_DRUG
4034569 VUID
N0000191733 NUI
163706-36-3 SECONDARY_CAS_RN
4034569 VANDF
C0763767 UMLSCUI
CHEBI:90841 CHEBI
CHEMBL1097279 ChEMBL_ID
CHEMBL334966 ChEMBL_ID
DB06441 DRUGBANK_ID
10260031 PUBCHEM_CID
7883 INN_ID
C117446 MESH_SUPPLEMENTAL_RECORD_UI
1776 IUPHAR_LIGAND_ID
6AQ1Y404U7 UNII
1656051 RXNORM
234577 MMSL
31089 MMSL
31177 MMSL
d08365 MMSL
016203 NDDF
016205 NDDF
716118009 SNOMEDCT_US
763606005 SNOMEDCT_US

Pharmaceutical products:

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