Cangrelor
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Also known as AR-C69931XXKengrealAdenosine triphosphate derivativeARL 69931MX
Summary
Cangrelor (CHEMBL334966) is an approved small-molecule platelet aggregation inhibitor (ATC B01AC25) targeting P2RY12, P2RY13, and GPR17; indicated across 7 conditions including thrombotic disease and myocardial infarction.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: B01AC25
- Targets: 3 (P2RY12, P2RY13, GPR17)
- Indications: 7 conditions
- Clinical trials: 30
- Chemistry: 776.4 Da · C17H25Cl2F3N5O12P3S2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL334966 |
| Name | Cangrelor |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 9854012 |
| ChEBI | CHEBI:90841 |
| ATC | B01AC25 |
| Molecular formula | C17H25Cl2F3N5O12P3S2 |
| Molecular weight | 776.4 |
| InChIKey | PAEBIVWUMLRPSK-IDTAVKCVSA-N |
SMILES: CSCCNC1=C2C(=NC(=N1)SCCC(F)(F)F)N(C=N2)[C@H]3[C@@H]([C@@H]([C@H](O3)COP(=O)(O)OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O)O
IUPAC name: [dichloro-[[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(2-methylsulfanylethylamino)-2-(3,3,3-trifluoropropylsulfanyl)purin-9-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]methyl]phosphonic acid
ChEBI definition: A nucleoside triphosphate analogue that is 5’-O-[({dichloro(phosphono)methylphosphoryl}oxy)(hydroxy)phosphoryl]adenosine carrying additional 2-(methylsulfanyl)ethyl and (3,3,3-trifluoropropyl)sulfanyl substituents at positions N6 and C2 respectively. Used (in the form of its tetrasodium salt) as an intravenous antiplatelet drug that prevents formation of harmful blood clots in the coronary arteries.
Pharmacological roles (ChEBI): platelet aggregation inhibitor, P2Y12 receptor antagonist.
Also known as: AR-C69931XX, Cangrelor, Kengreal, Adenosine triphosphate derivative, ARL 69931MX, CANGRELOR
Parent form; salt/anhydrous children: CHEMBL1097279
Patent coverage: 363 distinct patent families (900 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| P2RY12 | P2Y12 receptor | Antagonist | 8 | 0.5% | Q9H244 |
| P2RY13 | P2Y13 receptor | Antagonist | 8.3 | 0% | Q9BPV8 |
| GPR17 | GPR17 | Antagonist | 8.92 | 1.6% | Q13304 |
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: P2Y purinoceptor 12, P2Y purinoceptor 13.
Bioactivity
ChEMBL activities: 8 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P2RY12 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_16582134 |
| P2RY12 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_25089906 |
| P2RY12 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_26024767 |
| P2RY12 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_70413 |
| P2RY12 | 9.35 | IC50 | 0.45 | nM | CHEMBL_ACT_24689693 |
| P2RY12 | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_15642381 |
| P2RY12 | 7.74 | IC50 | 18.3 | nM | CHEMBL_ACT_16419569 |
| P2RY13 | 5.2 | EC50 | 6322 | nM | CHEMBL_ACT_27404942 |
Target pathways
Aggregated over 3 target gene(s): P2RY12, P2RY13, GPR17.
Top Reactome pathways
5 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| P2Y receptors | 3 | GPR17, P2RY12, P2RY13 |
| G alpha (i) signalling events | 3 | GPR17, P2RY12, P2RY13 |
| Leukotriene receptors | 1 | GPR17 |
| ADP signalling through P2Y purinoceptor 12 | 1 | P2RY12 |
| G alpha (q) signalling events | 1 | GPR17 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| G protein-coupled receptor signaling pathway | 3 |
| signal transduction | 3 |
| G protein-coupled purinergic nucleotide receptor signaling pathway | 2 |
| monoatomic ion transport | 1 |
| substrate-dependent cell migration, cell extension | 1 |
| adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | 1 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 1 |
| hemostasis | 1 |
| calcium-mediated signaling | 1 |
| cerebral cortex radial glia-guided migration | 1 |
| cell projection organization | 1 |
| lamellipodium assembly | 1 |
| platelet activation | 1 |
| positive regulation of integrin activation by cell surface receptor linked signal transduction | 1 |
| positive regulation of cell adhesion mediated by integrin | 1 |
Indications & clinical
Indications
7 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| thrombotic disease | 4 | MONDO:0000831 | HP:0004419 |
| myocardial infarction | 4 | MONDO:0005068 | EFO:0000612 |
| ischemic disease | 3 | MONDO:0005053 | EFO:0000556 |
| acute coronary syndrome | 2 | MONDO:0005542 | EFO:0005672 |
| ST-elevation myocardial infarction | 2 | MONDO:0041656 | EFO:0008585 |
| coronary artery disorder | 2 | MONDO:0005010 | EFO:0001645 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 30.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 12 |
| PHASE2 | 7 |
| PHASE3 | 4 |
| Not specified | 4 |
| PHASE1 | 3 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06089577 | PHASE4 | RECRUITING | Effects of Cangrelor on MIcRovAscular Disfunction During Elective Percutaneous CORonary Intervention |
| NCT07225842 | PHASE4 | RECRUITING | The Bridging Antiplatelet Therapy With Cangrelor 2 Study |
| NCT02733341 | PHASE4 | COMPLETED | The Effect of IV Cangrelor and Oral Ticagrelor Study |
| NCT02943369 | PHASE4 | COMPLETED | Cangrelor Following Ticagrelor Loading vs Ticagrelor Loading Alone in STEMI |
| NCT02978040 | PHASE4 | COMPLETED | Randomized Comparison of Cangrelor, Tirofiban and Prasugrel in Patients With STEMI Referred for Primary PCI. |
| NCT03043274 | PHASE4 | TERMINATED | Cangrelor in ST-Elevation Myocardial Infarction to Decrease Infarct Size |
| NCT03247738 | PHASE4 | COMPLETED | Platelet Inhibition With Cangrelor and Crushed Ticagrelor in STEMI |
| NCT03273075 | PHASE4 | UNKNOWN | Add-on Cangrelor in STEMI-triggered Cardiac Arrest |
| NCT03551964 | PHASE4 | COMPLETED | Dual Antiplatelet Therapy For Shock Patients With Acute Myocardial Infarction |
| NCT04005729 | PHASE4 | COMPLETED | Cangrelor in Comatose Survivors of OHCA Undergoing Primary PCI |
| NCT04634162 | PHASE4 | COMPLETED | PD and PK Profiles of Switching Between Cangrelor and Ticagrelor Following Ticagrelor Pre-treatment |
| NCT04668144 | PHASE4 | COMPLETED | Pharmacodynamic and Pharmacokinetic of Switching From Cangrelor to Prasugrel in ACS Patients Undergoing PCI |
| NCT04667078 | PHASE3 | RECRUITING | REperfusion With P2Y12 Inhibitors in Addition to mEchanical thRombectomy for perFUsion Imaging Selected Acute Stroke patiEnts |
| NCT00305162 | PHASE3 | TERMINATED | A Clinical Trial to Demonstrate the Efficacy of Cangrelor |
| NCT00385138 | PHASE3 | TERMINATED | Cangrelor Versus Standard Therapy to Achieve Optimal Management of Platelet Inhibition. |
| NCT01156571 | PHASE3 | COMPLETED | A Clinical Trial Comparing Cangrelor to Clopidogrel Standard Therapy in Subjects Who Require Percutaneous Coronary Intervention (PCI) (CHAMPION PHOENIX) |
| NCT06792643 | PHASE2 | RECRUITING | Cangrelor on Top of anticoagUlation in Patients With myocaRdial Infarction-related Cardiogenic Shock/Cardiac Arrest receiVIng VA-ECMO |
| NCT00767507 | PHASE2 | COMPLETED | Maintenance of Platelet Inhibition With Cangrelor |
| NCT01766466 | PHASE2 | COMPLETED | Cangrelor Ticagrelor Transition Study |
| NCT01852019 | PHASE2 | COMPLETED | Cangrelor Prasugrel Transition Study |
| NCT01979445 | PHASE2 | COMPLETED | Cangrelor to Clopidogrel or Prasugrel Transition Study |
| NCT03102723 | PHASE2 | UNKNOWN | Platelet Inhibition to Target Reperfusion Injury |
| NCT03862651 | PHASE2 | UNKNOWN | Maintenance Of aNtiplatElet Therapy in Patients With Coronary Stenting Undergoing Surgery (MONET BRIDGE) |
| NCT00102674 | PHASE1 | COMPLETED | Pharmacokinetics/Pharmacodynamics (PK/PD) of Cangrelor |
| NCT00699504 | PHASE1 | COMPLETED | Assess the Effect of Cangrelor at the Therapeutic Dose and a Supratherapeutic Dose Level on the QT/QTc Interval in Healthy Volunteers |
| NCT02765633 | PHASE1 | COMPLETED | Cangrelor Neonatal PK/PD and Safety Study |
| NCT03048019 | Not specified | TERMINATED | Antiplatelet Effects of Tirofiban vs. Cangrelor N-STEMI Patients Undergoing Percutaneous Coronary Intervention |
| NCT04138641 | Not specified | COMPLETED | Dutch Cangrelor Registry |
| NCT04790032 | Not specified | COMPLETED | Pharmacodynamic Effects of Cangrelor in ACS or CCS Patients Undergoing PCI (POMPEII Registry) |
| NCT05505591 | Not specified | UNKNOWN | Intravenous CAngrelor in High-bleeding Risk Patients Undergoing percutaneouS Coronary Intervention (ICARUS) Registry |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 2 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
20 molecules share ≥1 primary target. Top 20 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| TICAGRELOR | ChEMBL + PubChem | Phase 4 (approved) | P2RY12, P2RY13 |
| ANAGRELIDE | ChEMBL + PubChem | Phase 4 (approved) | P2RY12 |
| INDOMETHACIN | ChEMBL + PubChem | Phase 4 (approved) | GPR17 |
| MONTELUKAST | ChEMBL + PubChem | Phase 4 (approved) | GPR17 |
| CLOPIDOGREL | ChEMBL | Phase 4 (approved) | P2RY12 |
| PRANLUKAST | ChEMBL | Phase 4 (approved) | GPR17 |
| PRASUGREL | ChEMBL | Phase 4 (approved) | P2RY12 |
| SELATOGREL | ChEMBL | Phase 3 | P2RY12 |
| SURAMIN HEXASODIUM | ChEMBL | Phase 3 | P2RY13 |
| ELINOGREL | ChEMBL | Phase 2 | P2RY12 |
| GAVESTINEL | ChEMBL | Phase 2 | GPR17 |
| LIXAZINONE | ChEMBL | Phase 2 | P2RY12 |
| REGRELOR | ChEMBL | Phase 2 | P2RY12 |
| REGRELOR DISODIUM | ChEMBL | Phase 2 | P2RY12 |
| Aspirin | PubChem | Approved | P2RY12 |
| Doxorubicin | PubChem | Approved | P2RY12 |
| Mitoxantrone | PubChem | Approved | P2RY12 |
| Rizatriptan | PubChem | Approved | GPR17 |
| tryptophan | PubChem | Approved | GPR17 |
| Zileuton | PubChem | Approved | GPR17 |
Related Atlas pages
- Genes: P2RY12, P2RY13, GPR17
- Diseases: thrombotic disease, myocardial infarction, ischemic disease
- Drugs: Ticagrelor, Anagrelide, Indomethacin, Montelukast, Clopidogrel, Pranlukast, Prasugrel, Selatogrel, Aspirin, Doxorubicin, Mitoxantrone, Rizatriptan, tryptophan, Zileuton