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cangrelor 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| platelet aggregation inhibitors | 5006 | 163706-06-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 50 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
| S (Water solubility) | 100 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -1.518 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 10.940 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.063 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 7.907 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 9.030 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 9.340 | % | High | 1 |
| herg | hERG pIC50 | 4.447 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.239 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.083 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 4.010 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAP3K21,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PIK3CD,PRKDC,TEK | 21 | |||
| kinase-selectivity-class | AXL,CDK16,CDK9,DYRK1B,EPHB4,ERBB2,GRK2,MAP2K6,MAPK7,PRKDC,STK33,SYK,TEK,ZAP70 | 14 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.472 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 35.563 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 19.490 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.205 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 | |||
| pppb | Pig plasma protein binding (% unbound) | 12.760 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 15.488 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 79.740 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 7.360 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 1000 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 22, 2015 | FDA | MEDICINES CO | |
| March 23, 2015 | EMA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Off label use | 113.23 | 82.04 | 55 | 153 | 638280 | 41982847 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Off label use | 97.60 | 86.99 | 58 | 284 | 1500127 | 109088830 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 | D010975 | Platelet Aggregation Inhibitors |
| MeSH PA | D018377 | Neurotransmitter Agents |
| 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:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:50249 | anticoagulant |
| CHEBI has role | CHEBI:50427 | platelet aggregation inhibitor |
| CHEBI has role | CHEBI:68563 | P2Y<small><sub>12</sub></small> receptor antagonist |
Related Drugs by ATC class:
B01AC Platelet aggregation inhibitors excl. heparin 24 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Percutaneous coronary intervention | indication | 415070008 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| D03359 | KEGG_DRUG |
| 4034569 | VUID |
| N0000191733 | NUI |
| 4034569 | VANDF |
| CHEBI:90841 | CHEBI |
| CHEMBL334966 | ChEMBL_ID |
| C117446 | MESH_SUPPLEMENTAL_RECORD_UI |
| 1776 | IUPHAR_LIGAND_ID |
| DB06441 | DRUGBANK_ID |
| 1656051 | RXNORM |
| 234577 | MMSL |
| 31089 | MMSL |
| 31177 | MMSL |
| d08365 | MMSL |
| 016203 | NDDF |
| 016205 | NDDF |
| 1217149008 | SNOMEDCT_US |
| 716118009 | SNOMEDCT_US |
| 763606005 | SNOMEDCT_US |
| C1121991 | UMLSCUI |
| CHEMBL1097279 | ChEMBL_ID |
| 7883 | INN_ID |
| 9854012 | PUBCHEM_CID |
| 163706-36-3 | SECONDARY_CAS_RN |
| 6AQ1Y404U7 | UNII |
| 6AQ1Y404U7 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| KENGREAL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10122-620 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | NDA | 24 sections |
| KENGREAL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10122-620 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | NDA | 24 sections |
| Cangrelor | Human Prescription Drug Label | 1 | 68083-412 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 24 sections |