Ticagrelor

Summary

Ticagrelor (CHEMBL398435) is an approved small-molecule platelet aggregation inhibitor (ATC B01AC24) targeting SLC29A1 and P2RY12; indicated across 29 conditions including acute coronary syndrome and myocardial infarction.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: B01AC24
• Targets: 2 (SLC29A1, P2RY12)
• Indications: 29 conditions
• Clinical trials: 343
• Chemistry: 522.6 Da · C23H28F2N6O4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL398435
Name	Ticagrelor
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	9871419
ChEBI	CHEBI:68558
ATC	B01AC24
Molecular formula	C23H28F2N6O4S
Molecular weight	522.6
InChIKey	OEKWJQXRCDYSHL-FNOIDJSQSA-N

SMILES: CCCSC1=NC(=C2C(=N1)N(N=N2)[C@@H]3C[C@@H]([C@H]([C@H]3O)O)OCCO)N[C@@H]4C[C@H]4C5=CC(=C(C=C5)F)F

IUPAC name: (1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol

ChEBI definition: A triazolopyrimidine that is an adenosine isostere; the cyclopentane ring is similar to ribose and the nitrogen-rich [1,2,3]triazolo[4,5-d]pyrimidine moiety resembles the nucleobase adenine. A platelet aggregation inhibitor which is used for prevention of thromboembolic events in patients with acute coronary syndrome.

Pharmacological roles (ChEBI): platelet aggregation inhibitor, P2Y12 receptor antagonist.

Also known as: AR-C126532XX, AZD-6140, AZD6140, Brilinta, Brilique, Possia, Ticagrelor, TICAGRELOR, TicagrelorÊ, TicagrelorÂ, ticagrelor

Patent coverage: 1,390 distinct patent families (2,956 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,947 (100%) of the total. 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
SLC29A1	Equilibrative nucleoside transporter 1	Inhibition	7.3	0.1%	Q99808
P2RY12	P2Y12 receptor	Antagonist	7.85	0.5%	Q9H244

Broader ChEMBL bioactivity targets: 19 (assay-derived). Sample: Equilibrative nucleoside transporter 1, P2Y purinoceptor 12, D(1A) dopamine receptor, Thromboxane A2 receptor, Progesterone receptor, Muscarinic acetylcholine receptor M1, P2Y purinoceptor 12, Prostaglandin G/H synthase 1, Sodium-dependent noradrenaline transporter, D(3) dopamine receptor.

Bioactivity

ChEMBL activities: 25 potent at pChembl ≥ 5 of 32 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P2RY12	8.7	Ki	2	nM	CHEMBL_ACT_2045303
P2RY12	8.37	Ki	4.3	nM	CHEMBL_ACT_26024761
P2RY12	8.3	IC50	5.01	nM	CHEMBL_ACT_16582135
P2RY12	8	IC50	10	nM	CHEMBL_ACT_24689692
P2RY12	7.85	Ki	14	nM	CHEMBL_ACT_12107240
P2RY12	7.41	IC50	39	nM	CHEMBL_ACT_24812638
ADORA3	6.97	AC50	106.5	nM	CHEMBL_ACT_25198905
P2RY12	6.5	IC50	320	nM	CHEMBL_ACT_18210782
SLC29A1	6.44	AC50	364.7	nM	CHEMBL_ACT_25141679
SLC6A3	6.37	AC50	424.5	nM	CHEMBL_ACT_25125199
P2RY12	6.3	IC50	500	nM	CHEMBL_ACT_13863246
SLC6A3	6.29	Ki	518.8	nM	CHEMBL_ACT_25741166
P2RY12	5.91	IC50	1220	nM	CHEMBL_ACT_29236806
TMEM97	5.89	Ki	1295	nM	CHEMBL_ACT_25741167
P2RY12	5.89	IC50	1278	nM	CHEMBL_ACT_25913574
P2RY13	5.85	IC50	1398	nM	CHEMBL_ACT_24871773
P2RY12	5.85	IC50	1398	nM	CHEMBL_ACT_25702239
Q9EPX4	5.68	IC50	2110	nM	CHEMBL_ACT_29317501
FPR3	5.43	IC50	3751	nM	CHEMBL_ACT_25751287
Q9EPX4	5.38	IC50	4160	nM	CHEMBL_ACT_15008586
GPR183	5.31	IC50	4878	nM	CHEMBL_ACT_25751288
P2RY12	5.29	IC50	5140	nM	CHEMBL_ACT_22442322
TBXA2R	5.2	AC50	6379	nM	CHEMBL_ACT_25198091
PGR	5.12	AC50	7603	nM	CHEMBL_ACT_25204531
CHRM1	5.08	AC50	8294	nM	CHEMBL_ACT_25210411

Target pathways

Aggregated over 2 target gene(s): SLC29A1, P2RY12.

Top Reactome pathways

10 total, by targets touching each:

Pathway	Targets	Genes
Transport of small molecules	1	SLC29A1
ADP signalling through P2Y purinoceptor 12	1	P2RY12
P2Y receptors	1	P2RY12
G alpha (i) signalling events	1	P2RY12
Transport of vitamins, nucleosides, and related molecules	1	SLC29A1
SLC-mediated transmembrane transport	1	SLC29A1
Transport of nucleosides and free purine and pyrimidine bases across the plasma membrane	1	SLC29A1
Drug ADME	1	SLC29A1
Azathioprine ADME	1	SLC29A1
Ribavirin ADME	1	SLC29A1

Dominant GO biological processes

GO term	Targets
neurotransmitter uptake	1
nucleobase-containing compound metabolic process	1
AMP catabolic process	1
xenobiotic metabolic process	1
neurotransmitter transport	1
xenobiotic transmembrane transport	1
lactation	1
nucleobase transport	1
adenine transport	1
nucleoside transport	1
purine nucleoside transmembrane transport	1
cytidine transport	1
uridine transmembrane transport	1
adenosine transport	1
inosine transport	1

Indications & clinical

Indications

29 indications (9 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
acute coronary syndrome	4	MONDO:0005542	EFO:0005672
myocardial infarction	4	MONDO:0005068	EFO:0000612
thrombotic disease	4	MONDO:0000831	HP:0004419
stroke disorder	4	MONDO:0005098	EFO:0000712
coronary artery disorder	4	MONDO:0005010	EFO:0001645
acute myocardial infarction	4	MONDO:0004781	EFO:0008583
type 2 diabetes mellitus	4	MONDO:0005148	MONDO:0005148
peripheral vascular disease	4	MONDO:0005294	EFO:0003875
peripheral arterial disease	3	MONDO:0005386	EFO:0004265
pneumonia	3	MONDO:0005249	EFO:0003106
chronic kidney disease	3	MONDO:0005300	EFO:0003884
aortic valve stenosis	3	MONDO:0042981	EFO:0000266
atrial fibrillation	3	MONDO:0004981	EFO:0000275
brain aneurysm	3	MONDO:0005291	EFO:0003870
ST-elevation myocardial infarction	3	MONDO:0041656	EFO:0008585
influenza	3	MONDO:0005812	EFO:0007328
sickle cell disease	3	MONDO:0011382	MONDO:0011382
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
abdominal aortic aneurysm	2	MONDO:0005350	EFO:0004214
internal carotid artery stenosis	2	MONDO:0005189	EFO:0002615
chronic obstructive pulmonary disease	2	MONDO:0005002	EFO:0000341
ischemic disease	1	MONDO:0005053	EFO:0000556
kidney disorder	1	MONDO:0005240	EFO:0003086
cardiovascular disorder	1	MONDO:0004995	EFO:0000319

5 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 343.

Phase distribution

Phase	Trials
PHASE4	161
PHASE3	64
Not specified	50
PHASE1	28
PHASE2	26
PHASE2/PHASE3	9
PHASE1/PHASE2	4
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04240834	PHASE4	RECRUITING	Ticagrelor With Low-dose Versus Regular Aspirin in Patients With Acute Coronary Syndrome (ACS) at High-Risk for Ischemia After Percutaneous Coronary Intervention
NCT06228456	PHASE4	RECRUITING	Effects of Low-dose Ticagrelor vs. Clopidogrel in Stable Patients Undergoing Elective Percutaneous Coronary Intervention
NCT06451198	PHASE4	RECRUITING	IndObufen Versus asPirin After Coronary Drug-eluting Stent implantaTION in Elderly Patients With Acute Coronary Syndrome
NCT06509893	PHASE4	RECRUITING	Ticagrelore Alone Post PCI
NCT06613191	PHASE4	NOT_YET_RECRUITING	Colonoscopy and Antiplatelet Therapy Trial
NCT06691191	PHASE4	RECRUITING	Switching From Dual Antiplatelet Therapy to Monotherapy With Potent P2Y12 Inhibitors
NCT07080684	PHASE4	NOT_YET_RECRUITING	Short-Term Dual Antiplatelet Therapy With Early Transi-tion to Low-dose Antiplatelet Monotherapy Using Ti-cagRelor in Chronic Coronary Artery Disease
NCT07507500	PHASE4	NOT_YET_RECRUITING	Dual Antiplatelet Therapy Strategies After Acute Myocardial Infarction Undergoing PCI: Prasugrel vs Ticagrelor & 12 Months vs 1-3 Months
NCT01347580	PHASE4	COMPLETED	A 30 Day Study to Evaluate Efficacy and Safety of Pre-hospital vs. In-hospital Initiation of Ticagrelor Therapy in STEMI Patients Planned for Percutaneous Coronary Intervention (PCI)
NCT01373411	PHASE4	COMPLETED	Ticagrelor and Aspirin for the Prevention of Cardiovascular Events After Coronary Artery Bypass Surgery
NCT01456364	PHASE4	UNKNOWN	Intracoronary Stenting and Antithrombotic Regimen: ADjusting Antiplatelet Treatment in PatienTs Based on Platelet Function Testing
NCT01463163	PHASE4	COMPLETED	Ticagrelor in Comparison to Prasugrel for Early Inhibition of Platelet Reactivity in Patients With ST-elevation Myocardial Infarction (STEMI), Undergoing Primary Percutaneous Coronary Intervention (PCI)
NCT01510171	PHASE4	COMPLETED	Rapid Activity of Platelet Inhibitor Drugs Study
NCT01523366	PHASE4	COMPLETED	A Pharmacodynamic Study With Ticagrelor in Hispanic Patients
NCT01523392	PHASE4	COMPLETED	A Pharmacodynamic Study With Ticagrelor in African American Patients
NCT01575795	PHASE4	COMPLETED	Standard (180mg) Versus Double (360mg) Loading Dose of Ticagrelor in Patients With ST-elevation Myocardial Infarction (STEMI), Undergoing Primary Percutaneous Coronary Intervention (PCI)
NCT01603082	PHASE4	COMPLETED	Ad Hoc Percutaneous Coronary Intervention Study in Acute Coronary Syndrome Patients
NCT01642238	PHASE4	COMPLETED	Antithrombotic Effects of Ticagrelor Versus Clopidogrel
NCT01642940	PHASE4	COMPLETED	Τicagrelor Versus Prasugrel in Diabetic Patients: a Pharmacodynamic Study
NCT01642966	PHASE4	COMPLETED	Differential Effect of Ticagrelor Versus Prasugrel on the Adenosine-induced Coronary Vasodilatory Responses in Patients With Acute Coronary Syndrome Undergoing Percutaneous Coronary Intervention
NCT01643031	PHASE4	UNKNOWN	Effect of Modifying Anti-platelet Treatment to Ticagrelor in Patients With Diabetes and Low Response to Clopidogrel
NCT01700322	PHASE4	COMPLETED	Endothelium, Stenting, and Antiplatelet Therapy (EST) - Clopidogrel, Prasugrel, Ticagrelor Study
NCT01706510	PHASE4	COMPLETED	Antiplatelet Effects of Ticagrelor Versus Clopidogrel in American Indian Patients
NCT01742117	PHASE4	COMPLETED	Tailored Antiplatelet Therapy Following PCI
NCT01805570	PHASE4	COMPLETED	Rapid Activity of Platelet Inhibitor Drugs Study 2
NCT01812200	PHASE4	COMPLETED	Antithrombotic Triple Therapy in Humans
NCT01823510	PHASE4	COMPLETED	Ticagrelor Versus Clopidogrel in Type 2 Diabetic Patients
NCT01826175	PHASE4	WITHDRAWN	Comparison of Ticagrelor Versus Clopidogrel on Residual Thrombus Burden During PCI: an OCT Study
NCT01846559	PHASE4	COMPLETED	The Antiplatelet and Immune Response Trial
NCT01864005	PHASE4	COMPLETED	A Phase IV Study of the Onset and Maintenance of the Antiplatelet Effect of Ticagrelor Compared With Clopidogrel in Chinese Patients With ACS
NCT01869309	PHASE4	UNKNOWN	Overcoming High On-Treatment Platelet Reactivity (HPR) During Prasugrel Therapy With Ticagrelor
NCT01870921	PHASE4	COMPLETED	Brilinta DaYu Study
NCT01905566	PHASE4	COMPLETED	Comparison of Clopidogrel Versus Ticagrelor Therapy for Atherosclerotic Plaque Inflammation
NCT01944800	PHASE4	COMPLETED	Prospective, Randomized Trial of Ticagrelor Versus Prasugrel in Patients With Acute Coronary Syndrome
NCT01955200	PHASE4	COMPLETED	OPTImal Management of Antithrombotic Agents: OPTIMA-2 Trial
NCT01957540	PHASE4	COMPLETED	Differential Effect of Ticagrelor Versus Prasugrel Maintenance Dose on Endothelial Function of Peripheral Vessels in Patients With Coronary Artery Disease
NCT01962428	PHASE4	COMPLETED	Different LD of Ticagrelor for Antiplatelet Effect in Patients With Non-ST-segment Elevation ACS Undergoing PCI
NCT01994941	PHASE4	COMPLETED	Genotype Guided Versus Conventional Approach in Selection of Oral P2Y12 Receptor Blocker in Chinese Patients Suffering From Acute Coronary Syndrome
NCT02012140	PHASE4	UNKNOWN	Pharmacokinetics and Pharmacodynamics of Ticagrelor in Patients With Stable Angina, NSTEMI and STEMI Undergoing PCI
NCT02018055	PHASE4	COMPLETED	TicAgrelor Versus CLOpidogrel in Stabilized Patients With Acute Myocardial Infarction: TALOS-AMI

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of DPWG Guideline for ticagrelor and CYP2C19	DPWG	CYP2C19

PharmGKB also curates 8 clinical and 55 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.

297 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
Anagrelide	ChEMBL + PubChem	Phase 4 (approved)	P2RY12, SLC29A1
Aspirin	PubChem	Approved	P2RY12, SLC29A1
Doxorubicin	PubChem	Approved	P2RY12, SLC29A1
APIXABAN	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
BROMOCRIPTINE	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
CARVEDILOL	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
CELECOXIB	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
CILOSTAZOL	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
DAUNORUBICIN	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
DIPYRIDAMOLE	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
DOMPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
ERLOTINIB	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
FELODIPINE	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
FIDAXOMICIN	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
PIMOZIDE	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
RIFAMPIN	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
VISMODEGIB	ChEMBL + PubChem	Phase 4 (approved)	SLC29A1
ADENOSINE	ChEMBL	Phase 4 (approved)	SLC29A1
AMSACRINE	ChEMBL	Phase 4 (approved)	SLC29A1
BALSALAZIDE	ChEMBL	Phase 4 (approved)	SLC29A1
BENZTROPINE	ChEMBL	Phase 4 (approved)	SLC29A1
BOSUTINIB	ChEMBL	Phase 4 (approved)	SLC29A1
CALCITRIOL	ChEMBL	Phase 4 (approved)	SLC29A1
CANGRELOR	ChEMBL	Phase 4 (approved)	P2RY12
CANGRELOR TETRASODIUM	ChEMBL	Phase 4 (approved)	P2RY12
CANNABIDIOL	ChEMBL	Phase 4 (approved)	SLC29A1
CLOPIDOGREL	ChEMBL	Phase 4 (approved)	P2RY12
ENCORAFENIB	ChEMBL	Phase 4 (approved)	SLC29A1
EPALRESTAT	ChEMBL	Phase 4 (approved)	SLC29A1
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	SLC29A1
GEMCITABINE	ChEMBL	Phase 4 (approved)	SLC29A1
GLAFENINE	ChEMBL	Phase 4 (approved)	SLC29A1
IDEBENONE	ChEMBL	Phase 4 (approved)	SLC29A1
INDOCYANINE GREEN ACID FORM	ChEMBL	Phase 4 (approved)	SLC29A1
KETOCONAZOLE	ChEMBL	Phase 4 (approved)	SLC29A1
LEFLUNOMIDE	ChEMBL	Phase 4 (approved)	SLC29A1
MICONAZOLE	ChEMBL	Phase 4 (approved)	SLC29A1
NAFTOPIDIL	ChEMBL	Phase 4 (approved)	SLC29A1
NEFAZODONE	ChEMBL	Phase 4 (approved)	SLC29A1
NERATINIB	ChEMBL	Phase 4 (approved)	SLC29A1
NILOTINIB	ChEMBL	Phase 4 (approved)	SLC29A1
NIMESULIDE	ChEMBL	Phase 4 (approved)	SLC29A1
NIMODIPINE	ChEMBL	Phase 4 (approved)	SLC29A1
NITAZOXANIDE	ChEMBL	Phase 4 (approved)	SLC29A1
OXYPHENCYCLIMINE	ChEMBL	Phase 4 (approved)	SLC29A1
PRASUGREL	ChEMBL	Phase 4 (approved)	P2RY12
PREDNISONE	ChEMBL	Phase 4 (approved)	SLC29A1
PYRVINIUM	ChEMBL	Phase 4 (approved)	SLC29A1
RESERPINE	ChEMBL	Phase 4 (approved)	SLC29A1
RIFAXIMIN	ChEMBL	Phase 4 (approved)	SLC29A1
RIMONABANT	ChEMBL	Phase 4 (approved)	SLC29A1
ROTIGOTINE	ChEMBL	Phase 4 (approved)	SLC29A1
SELINEXOR	ChEMBL	Phase 4 (approved)	SLC29A1
SIROLIMUS	ChEMBL	Phase 4 (approved)	SLC29A1
SUNITINIB	ChEMBL	Phase 4 (approved)	SLC29A1
TACROLIMUS	ChEMBL	Phase 4 (approved)	SLC29A1
TIGECYCLINE	ChEMBL	Phase 4 (approved)	SLC29A1
BENIDIPINE	ChEMBL	Phase 3	SLC29A1
CILNIDIPINE	ChEMBL	Phase 3	SLC29A1
DIACEREIN	ChEMBL	Phase 3	SLC29A1