Clopidogrel

Summary

Clopidogrel (CHEMBL1771) is an approved small-molecule platelet aggregation inhibitor (ATC B01AC04); indicated across 55 conditions including thrombotic disease and ischemic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: B01AC04
• Indications: 55 conditions
• Clinical trials: 572
• Chemistry: 321.8 Da · C16H16ClNO2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1771
Name	Clopidogrel
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	60606
ChEBI	CHEBI:37941
ATC	B01AC04
Molecular formula	C16H16ClNO2S
Molecular weight	321.8
InChIKey	GKTWGGQPFAXNFI-HNNXBMFYSA-N

SMILES: COC(=O)[C@H](C1=CC=CC=C1Cl)N2CCC3=C(C2)C=CS3

IUPAC name: methyl (2S)-2-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)acetate

ChEBI definition: A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks.

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

Also known as: Clopidogrel, NSC-758613, R 130964, R-130964, SR 25990, SR-25990, SID49666423, SID49666065, clopidogrel, CLOPIDOGREL, C0165035, CLOPIDOGREL SULFATE

Parent form; salt/anhydrous children: CHEMBL1083385, CHEMBL6068333, CHEMBL6068338, CHEMBL6068343

Patent coverage: 11,220 distinct patent families (40,370 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 40,357 (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

Broader ChEMBL bioactivity targets: 16 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, P2Y purinoceptor 12, D(1A) dopamine receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 2A, Sodium-dependent serotonin transporter, Mu-type opioid receptor, Kappa-type opioid receptor, Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 9 potent at pChembl ≥ 5 of 20 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CYP2B6	6.7	IC50	200	nM	CHEMBL_ACT_29116821
SLC6A4	6.52	Ki	299	nM	CHEMBL_ACT_7686876
CYP2B6	6.3	Ki	500	nM	CHEMBL_ACT_12163602
CYP2B6	6.3	Ki	500	nM	CHEMBL_ACT_6075029
SLC6A4	6.25	IC50	562	nM	CHEMBL_ACT_7686875
CYP2B6	5.96	Ki	1100	nM	CHEMBL_ACT_6075031
HTR2B	5.7	AC50	2000	nM	CHEMBL_ACT_25227787
P2RY12	5.62	IC50	2400	nM	CHEMBL_ACT_24689696
P15207	5.29	AC50	5100	nM	CHEMBL_ACT_25233006

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

55 indications (2 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
ischemic disease	3	MONDO:0005053	EFO:0000556
myocardial infarction	3	MONDO:0005068	EFO:0000612
coronary artery disorder	3	MONDO:0005010	EFO:0001645
internal carotid artery stenosis	3	MONDO:0005189	EFO:0002615
peripheral arterial disease	3	MONDO:0005386	EFO:0004265
acute coronary syndrome	3	MONDO:0005542	EFO:0005672
atrial fibrillation	3	MONDO:0004981	EFO:0000275
stroke disorder	3	MONDO:0005098	EFO:0000712
chronic kidney disease	3	MONDO:0005300	EFO:0003884
atherosclerosis	3	MONDO:0005311	EFO:0003914
heart failure	3	MONDO:0005252	EFO:0003144
vascular disorder	3	MONDO:0005385	EFO:0004264
aortic valve stenosis	3	MONDO:0042981	EFO:0000266
transient ischemic attack	3	MONDO:0005264	EFO:0003764
brain aneurysm	3	MONDO:0005291	EFO:0003870
cerebral atherosclerosis	3	MONDO:0006694	EFO:1000860
ST-elevation myocardial infarction	3	MONDO:0041656	EFO:0008585
arteriosclerosis disorder	3	MONDO:0002277	EFO:0009086
thrombophilia	3	MONDO:0002305	EFO:0009315
congenital heart disease	3	MONDO:0005453	HP:0030680
brain infarction	3	MONDO:0005394	EFO:0004277
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
acute myocardial infarction	3	MONDO:0004781	EFO:0008583
pneumonia	3	MONDO:0005249	EFO:0003106
influenza	3	MONDO:0005812	EFO:0007328
myocardial ischemia	3	MONDO:0024644	EFO:1001375
chronic obstructive pulmonary disease	3	MONDO:0005002	EFO:0000341
age-related macular degeneration	3	MONDO:0005150	EFO:0001365
exocrine pancreatic carcinoma	3	MONDO:0005192	EFO:0002618
malignant pancreatic neoplasm	3	MONDO:0009831	EFO:1000359
heart disorder	2	MONDO:0005267	EFO:0003777
HIV infectious disease	2	MONDO:0005109	EFO:0000180
peripheral vascular disease	2	MONDO:0005294	EFO:0003875
cardiovascular disorder	2	MONDO:0004995	EFO:0000319
pulmonary arterial hypertension	2	MONDO:0015924	EFO:0001361
acquired polycythemia vera	2	MONDO:0009891	EFO:0002429
intermittent vascular claudication	2	MONDO:0005295	EFO:0003876
venous thromboembolism	2	MONDO:0005399	EFO:0004286
viral pneumonia	2	MONDO:0006012	EFO:0007541
respiratory failure	2	MONDO:0021113	EFO:0009686
systemic sclerosis	2	MONDO:0005100	EFO:0000717
asthma	2	MONDO:0004979	MONDO:0004979
head and neck cancer	1	MONDO:0005627	EFO:0006859
major depressive disorder	1	MONDO:0002009	MONDO:0002009
type 2 diabetes mellitus	1	MONDO:0005148	MONDO:0005148
systemic lupus erythematosus	1	MONDO:0007915	MONDO:0007915

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

Clinical trials

Total trials: 572.

Phase distribution

Phase	Trials
PHASE4	239
PHASE3	109
Not specified	82
PHASE1	69
PHASE2	46
PHASE2/PHASE3	22
EARLY_PHASE1	3
PHASE1/PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03378934	PHASE4	RECRUITING	Anti-platelet Effect of Berberine in Patients After Percutaneous Coronary Intervention
NCT03568890	PHASE4	ACTIVE_NOT_RECRUITING	Short-Term Anticoagulation Versus Antiplatelet Therapy for Preventing Device Thrombosis Following Left Atrial Appendage Closure
NCT03947229	PHASE4	ACTIVE_NOT_RECRUITING	A Randomized Comparison of CLOpidogrel Monotherapy Versus Extended Dual-antiplatelet Therapy Beyond 12 Months After Implantation of Drug-eluting StEnts in High-risk Lesions or Patients; A-CLOSE Trial
NCT04250116	PHASE4	ACTIVE_NOT_RECRUITING	Appropriate Duration of Anti-Platelet and Thrombotic Strategy After 12 Months in Patients With Atrial Fibrillation Treated With Drug Eluting Stents
NCT04654052	PHASE4	ACTIVE_NOT_RECRUITING	VerifyNow to Optimise Platelet Inhibition in Coronary Acute Syndrome
NCT04698031	PHASE4	ACTIVE_NOT_RECRUITING	Efficacy of Clopidogrel on Incidence of Silent Brain Infarction
NCT04850417	PHASE4	NOT_YET_RECRUITING	Randomized Study of Beta-Blockers and Antiplatelets in Patients With Spontaneous Coronary Artery Dissection
NCT04937699	PHASE4	RECRUITING	Sequential MonotherApy of TicagrElor and Clopidogrel After Coronary Intervention
NCT05638867	PHASE4	RECRUITING	NOAC Therapy Guided by PARIS Risk Score and D-dimer in Patients With ACS After PCI
NCT05910125	PHASE4	NOT_YET_RECRUITING	Aspirin Combined With Clopidogrel Versus Intravenous Alteplase for Acute Minor Stroke
NCT06228456	PHASE4	RECRUITING	Effects of Low-dose Ticagrelor vs. Clopidogrel in Stable Patients Undergoing Elective Percutaneous Coronary Intervention
NCT06402747	PHASE4	RECRUITING	Clopidogrel Versus Cilostazol on Vessels
NCT06650488	PHASE4	RECRUITING	Clopidogrel vs. Aspirin for Cardiovascular Risk Reduction in Patients With S. Aureus Bacteremia
NCT06757764	PHASE4	RECRUITING	The Effect and Safety of Combined Anti-platelet Treatment in Acute Ischemic Stroke Due to Large Artery Atherosclerosis
NCT06763744	PHASE4	NOT_YET_RECRUITING	Genotype-Guided Abbreviated DAPT Versus Un-Guided De-escalation Therapy in Patients With ACS and HBR
NCT06821191	PHASE4	RECRUITING	Comparison of Dual Antiplatelet Therapy De-escalation by Dose Reduction Versus Switching in Patients Undergoing PCI: The Switching Antiplatelet-8 (SWAP-8) Study
NCT06901466	PHASE4	RECRUITING	STrategies for Antithrombotic tReatment Following Transcatheter Edge-to-Edge Repair in Patients With an Indication for Oral Anticoagulant
NCT07007143	PHASE4	RECRUITING	STrategies for Antithrombotic tReatment Following Transcatheter Edge-to-Edge Repair in Patients Without an Indication for Oral Anticoagulant
NCT07025148	PHASE4	RECRUITING	Dual Antiplatelet Therapy Escalation From Standard-dose Clopidogrel to Low-Dose Prasugrel in Patients With High Bleeding and Ischemic Risk Undergoing PCI: A Prospective, Randomized Pharmacodynamic Study (TAILOR-BLEED-2)
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
NCT07180472	PHASE4	NOT_YET_RECRUITING	Prevention of Stroke Recurrence and Disease Progression in Cerebral Small Vessel Disease With Cilostazol
NCT07237308	PHASE4	NOT_YET_RECRUITING	BEACON-AA: Apixaban With or Without Clopidogrel in Stroke Patients With Atrial Fibrillation and Cerebral Atherosclerosis
NCT07511257	PHASE4	RECRUITING	Multicenter Trial of Antithrombotic Strategies in Acute Coronary Syndrome With Coronary Artery Ectasia
NCT00130039	PHASE4	COMPLETED	Trial of Cilostazol in Symptomatic Intracranial Arterial Stenosis II
NCT00140465	PHASE4	COMPLETED	75 or 150 mg Clopidogrel Maintenance Doses Following PCI (ISAR-CHOICE-2)
NCT00152646	PHASE4	UNKNOWN	Platelets Induced Vasodilation, in Vitro and in Vivo Study
NCT00153062	PHASE4	COMPLETED	PRoFESS - Prevention Regimen For Effectively Avoiding Second Strokes
NCT00189618	PHASE4	COMPLETED	The Effects of Physical Training, ASA (Aspirin), and Clopidogrel on the Walking Capacity of Patients With Stage II Peripheral Arterial Disease (PAD)
NCT00222261	PHASE4	COMPLETED	Aspirin Non-responsiveness and Clopidogrel Endpoint Trial.
NCT00222573	PHASE4	COMPLETED	Efficacy and Safety of Adding Clopidogrel to Aspirin or Use of Metoprolol in Myocardial Infarction
NCT00235950	PHASE4	COMPLETED	Assessment of the Lipid Lowering Effect of Rosuvastatin Compared to Atorvastatin in Subjects With Coronary Heart Disease
NCT00296803	PHASE4	COMPLETED	PROCLAIM: Study Examining Effects of Clopidogrel Compared to Placebo on Inflammation in Subjects With Metabolic Syndrome
NCT00343876	PHASE4	COMPLETED	Clopidogrel and Aspirin Together: The Effect on C-Reactive Protein Trial
NCT00386191	PHASE4	COMPLETED	Safety and Efficacy of Clopidogrel for Cerebral Infarction Treatment
NCT00404053	PHASE4	COMPLETED	Clopidogrel Maintaining Dosage in Acute Coronary Syndrome After Drug Eluting Stent Implantation
NCT00404781	PHASE4	COMPLETED	Effects of Optimized Antiplatelet Treatment After Percutaneous Coronary Intervention
NCT00421252	PHASE4	TERMINATED	Role of Plavix in Hemorrhagic and Ischemic Complications of Catheterization.
NCT00433784	PHASE4	COMPLETED	H2 Haplotype and CYP3As Polymorphisms and the Antiplatelet Response to Clopidogrel
NCT00484926	PHASE4	COMPLETED	Association of Clopidogrel Therapy and Stent Thrombosis
NCT00513149	PHASE4	UNKNOWN	Platelet Function Assessment for Atherothrombotic Patients

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (4) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of CPIC Guideline for clopidogrel and CYP2C19	CPIC	CYP2C19		yes
Annotation of DPWG Guideline for clopidogrel and CYP2C19	DPWG	CYP2C19	yes	yes
Annotation of RNPGx Guideline for clopidogrel and CYP2C19	RNPGx	CYP2C19		yes
Annotation of AHA Guideline for clopidogrel and CYP2C19	AHA	CYP2C19		yes

PharmGKB also curates 51 clinical and 935 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).