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Amlodipine

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Also known as AMLODIPINE COMPONENT OF CKD-330AmlodipinoAstudal 5HGP-0904HGP0904IstinNorvasNorvascSID29217715SID50111725SID124893198SID225144262C0164702AmiodipineAmlodipin

Summary

Amlodipine (CHEMBL1491) is an approved small-molecule antihypertensive agent (ATC C08CA01) targeting P2RX4, CACNA1C, and CACNA1D; indicated across 31 conditions including cardiovascular disorder and hypertensive disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C08CA01
  • Targets: 3 (P2RX4, CACNA1C, CACNA1D)
  • Indications: 31 conditions
  • Clinical trials: 377
  • Chemistry: 408.9 Da · C20H25ClN2O5

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1491
NameAmlodipine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID2162
ChEBICHEBI:2668
ATCC08CA01
Molecular formulaC20H25ClN2O5
Molecular weight408.9
InChIKeyHTIQEAQVCYTUBX-UHFFFAOYSA-N

SMILES: CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2Cl)C(=O)OC)C)COCCN

IUPAC name: 3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate

ChEBI definition: A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina.

Pharmacological roles (ChEBI): antihypertensive agent, calcium channel blocker, vasodilator agent.

Also known as: Amlodipine, AMLODIPINE COMPONENT OF CKD-330, Amlodipino, Astudal 5, HGP-0904, HGP0904, Istin, Norvas, Norvasc, SID29217715, SID50111725, SID124893198

Parent form; salt/anhydrous children: CHEMBL1200402, CHEMBL1200984, CHEMBL4594262

Patent coverage: 10,910 distinct patent families (39,495 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 39,488 (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).

GeneTargetActionpAffinityCancer dependencyUniProt
P2RX4P2X4Negative1.2%Q99571
CACNA1CCav1.29.30.1%Q13936
CACNA1DCav1.3Inhibition7.20.3%Q01668

Broader ChEMBL bioactivity targets: 38 (assay-derived). Sample: Nuclear receptor ROR-gamma, Ferritin light chain, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, 5-hydroxytryptamine receptor 3A, Alpha-2C adrenergic receptor, Voltage-dependent L-type calcium channel subunit alpha-1C, Histamine H2 receptor, Sodium channel protein type 5 subunit alpha, D(1A) dopamine receptor.

Bioactivity

ChEMBL activities: 39 potent at pChembl ≥ 5 of 60 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P220028.7Ki2nMCHEMBL_ACT_824014
P220026.96AC50110.1nMCHEMBL_ACT_25119543
ADRA2A6.65Ki226nMCHEMBL_ACT_7640494
ADRA2C6.58Ki261nMCHEMBL_ACT_7640498
KCNK26.4IC50400nMCHEMBL_ACT_12662607
KCNK26.37IC50430nMCHEMBL_ACT_29291075
O355056.24IC50570nMCHEMBL_ACT_15373193
ADRA2A6.22IC50602nMCHEMBL_ACT_7639292
OPRK15.94AC501155nMCHEMBL_ACT_25129369
CACNA1C5.92IC501200nMCHEMBL_ACT_15373195
HTR65.87Ki1346nMCHEMBL_ACT_7641982
KCNK25.82IC501520nMCHEMBL_ACT_29290947
ADRB25.75AC501800nMCHEMBL_ACT_25122820
ADRA2C5.75IC501800nMCHEMBL_ACT_7640497
ADRA1A5.72AC501889nMCHEMBL_ACT_25218921
HTR65.69AC502030nMCHEMBL_ACT_25118947
ADRA2A5.66AC502215nMCHEMBL_ACT_25156513
HTR3A5.64AC502300nMCHEMBL_ACT_25149061
ADRA1A5.63Ki2344nMCHEMBL_ACT_824011
DRD35.55AC502800nMCHEMBL_ACT_25193464
DRD25.54AC502900nMCHEMBL_ACT_25140269
HTR65.54IC502898nMCHEMBL_ACT_7641981
SLC6A35.51AC503088nMCHEMBL_ACT_25125043
SLC6A35.48AC503290nMCHEMBL_ACT_25123890
DRD35.46AC503453nMCHEMBL_ACT_25194606
CACNA1C5.39AC504100nMCHEMBL_ACT_25159090
CACNA1C5.38IC504200nMCHEMBL_ACT_15373194
HTR2B5.36AC504322nMCHEMBL_ACT_25164092
SLC6A35.36Ki4387nMCHEMBL_ACT_7640570
OPRD15.29AC505100nMCHEMBL_ACT_25154006

Target pathways

Aggregated over 3 target gene(s): P2RX4, CACNA1C, CACNA1D.

Top Reactome pathways

19 total, by targets touching each:

PathwayTargetsGenes
Developmental Biology2CACNA1C, CACNA1D
Metabolism2CACNA1C, CACNA1D
Integration of energy metabolism2CACNA1C, CACNA1D
NCAM signaling for neurite out-growth2CACNA1C, CACNA1D
Adrenaline,noradrenaline inhibits insulin secretion2CACNA1C, CACNA1D
NCAM1 interactions2CACNA1C, CACNA1D
Regulation of insulin secretion2CACNA1C, CACNA1D
Axon guidance2CACNA1C, CACNA1D
Nervous system development2CACNA1C, CACNA1D
Elevation of cytosolic Ca2+ levels1P2RX4
Muscle contraction1CACNA1C
Platelet homeostasis1P2RX4
Cardiac conduction1CACNA1C
Phase 0 - rapid depolarisation1CACNA1C
Phase 2 - plateau phase1CACNA1C
Sensory processing of sound1CACNA1D
Purinergic signaling in leishmaniasis infection1P2RX4
Sensory processing of sound by inner hair cells of the cochlea1CACNA1D
Sensory Perception1CACNA1D

Dominant GO biological processes

GO termTargets
monoatomic ion transmembrane transport3
calcium ion transmembrane transport3
monoatomic ion transport3
positive regulation of calcium ion transport2
regulation of metal ion transport2
positive regulation of adenylate cyclase activity2
cardiac muscle cell action potential involved in contraction2
membrane depolarization during cardiac muscle cell action potential2
regulation of heart rate by cardiac conduction2
calcium ion import across plasma membrane2
calcium ion transport2
muscle contraction2
cell communication2
signaling2
transmembrane transport2

Indications & clinical

Indications

31 indications (1 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).

IndicationTrial phaseMONDOEFO
cardiovascular disorder4MONDO:0004995EFO:0000319
hypertensive disorder3MONDO:0005044EFO:0000537
heart failure3MONDO:0005252EFO:0003144
congestive heart failure3MONDO:0005009EFO:0000373
diabetes mellitus3MONDO:0005015EFO:0000400
myocardial infarction3MONDO:0005068EFO:0000612
atherosclerosis3MONDO:0005311EFO:0003914
myocardial ischemia3MONDO:0024644EFO:1001375
coronary artery disorder3MONDO:0005010EFO:0001645
depressive disorder3MONDO:0002050MONDO:0002050
essential hypertension3MONDO:0001134MONDO:0001134
type 2 diabetes mellitus3MONDO:0005148MONDO:0005148
abdominal aortic aneurysm2MONDO:0005350EFO:0004214
liver disorder2MONDO:0005154EFO:0001421
heart disorder2MONDO:0005267EFO:0003777
Raynaud disease2MONDO:0008364EFO:1001145
thalassemia2MONDO:0000984EFO:1001996
hypertrophic cardiomyopathy2MONDO:0005045EFO:0000538
dystonic disorder2MONDO:0003441MONDO:0000477
hyperaldosteronism2MONDO:0003009MONDO:0001422
aortic valve insufficiency2MONDO:0005648EFO:0007148
beta thalassemia2MONDO:0019402MONDO:0016486
vascular disorder2MONDO:0005385EFO:0004264
pancreatitis1MONDO:0004982EFO:0000278
HIV infectious disease1MONDO:0005109EFO:0000764
erectile dysfunction1MONDO:0005362EFO:0004234
kidney disorder1MONDO:0005240EFO:0003086
breast neoplasm1MONDO:0021100MONDO:0007254
hyperlipidemia1MONDO:0021187MONDO:0021187
neoplasm1MONDO:0005070EFO:0000616

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

Clinical trials

Total trials: 377.

Phase distribution

PhaseTrials
PHASE4131
PHASE3103
PHASE162
Not specified42
PHASE226
PHASE2/PHASE39
PHASE1/PHASE23
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03264352PHASE4RECRUITINGIntervention for High-normal Blood Pressure in Adults With Type 2 Diabetes
NCT04840342PHASE4ACTIVE_NOT_RECRUITINGMR Antagonist and LSD1
NCT04974138PHASE4RECRUITINGChina Stroke Primary Prevention Trial 2 for Participants With H-type Hypertension and MTHFR 677 CC/CT Genotype (CSPPT2-CC/CT)
NCT04974151PHASE4RECRUITINGChina Stroke Primary Prevention Trial 2 for Participants With Hypertension and MTHFR 677 TT Genotype
NCT05169021PHASE4NOT_YET_RECRUITINGFolic Acid and Intensive Antihypertensive Therapy for Hypertension With CSVD
NCT05416840PHASE4NOT_YET_RECRUITINGEffects and Safety of Clonidine Patch on Young and Middle-aged Smokers With Mild Hypertension
NCT05917275PHASE4RECRUITINGMulti-Omics to Predict the Blood Pressure Response to Antihypertensives
NCT06041529PHASE4ACTIVE_NOT_RECRUITINGStudy to Evaluate the Efficacy and Safety of TEL/AML/CTD in Elderly Patients With Essential Hypertension
NCT07241338PHASE4NOT_YET_RECRUITINGSacubitril/Allisartan for Hypertensive Patients With Overweight or Obesity
NCT00124969PHASE4COMPLETEDInfluence of Amlodipine on the Mortality of Patients With End-Stage Renal Failure
NCT00129233PHASE4COMPLETEDComparison of Valsartan With Amlodipine in Hypertensive Patients With Glucose Intolerance
NCT00136773PHASE4COMPLETEDEffects of Amlodipine/Benazepril on Albuminuria in Hypertensive Patients With Type 2 Diabetes Mellitus
NCT00139555PHASE4COMPLETEDEffects of Amlodipine/Benazepril in Reducing Left Ventricular Hypertrophy in Patients With High Risk Hypertension
NCT00143195PHASE4COMPLETEDAmlodipine vs Nitrates Study in Patients With Chronic Stable Angina
NCT00150384PHASE4COMPLETEDClinical Utility of Caduet in Achieving Blood Pressure and Lipid Endpoints in a Specific Patient Population
NCT00159692PHASE4COMPLETEDAmlodipine Diabetic Hypertension Efficacy Response Trial
NCT00159718PHASE4COMPLETEDDouble Blind Atorvastatin Amlodipine Study
NCT00171054PHASE4COMPLETEDEfficacy and Safety of Valsartan Versus Amlodipine in Postmenopausal Women With Hypertension
NCT00174304PHASE4COMPLETEDOpen Label Study To Assess The Effectiveness Of Amlodipine-Atorvastatin Combination In Hypertension And Dyslipidemia.
NCT00174330PHASE4COMPLETEDComparing Amlodipine/Atorvastatin Co-Administration To Amlodipine Alone In Patients With Hypertension And Dyslipidemia
NCT00185120PHASE4COMPLETEDTreatment of High Blood Pressure Using Olmesartan With Hydrochlorothiazide Compared to an ACE Inhibitor With a Calcium Channel Blocker
NCT00198562PHASE4UNKNOWNHypertension Control Based on Home Blood Pressure
NCT00202618PHASE4UNKNOWNRationale and Design for Shiga Microalbuminuria Reduction Trial
NCT00242814PHASE4COMPLETEDPhase IV, 9 Weeks Comparison Between MICARDIS 80 mg and Amlodipine 10 mg on Biological PPAR Gamma Activities
NCT00304226PHASE4COMPLETEDEffectiveness of a Valsartan Based Versus an Amlodipine Based Treatment Strategy in naïve Patients With Stage 1 or Stage 2 Hypertension or in Patients Uncontrolled on Current Monotherapy
NCT00338338PHASE4COMPLETEDThe Efficacy And Safety Of Lacidipine And Amlodipine Once-Daily Treatment In Hypertensive Adult Patients
NCT00351130PHASE4COMPLETEDEffectiveness of a Valsartan Based vs an Amlodipine Based Treatment Strategy in naïve Patients With Stage 1 or Stage 2 Hypertension or in Patients Uncontrolled on Current Monotherapy
NCT00367978PHASE4COMPLETEDEffects of Amlodipine/Benazepril in the Hypertensive African-American Population With Type 2 Diabetes Mellitus
NCT00400777PHASE4COMPLETEDEfficacy and Safety of Valsartan, Hydrochlorothiazide and Amlodipine Combination Therapy in Hypertension
NCT00421863PHASE4COMPLETEDItalian Study on the Cardiovascular Effects of Systolic Blood Pressure Control - CARDIOSIS Study
NCT00425997PHASE4COMPLETEDEfficacy of Valsartan/Hydrochlorothiazide Versus Amlodipine and Hydrochlorothiazide in Patients Hypertension
NCT00426478PHASE4COMPLETEDSafety and Efficacy of Valsartan Plus Hydrochlorothiazide and Amlodipine in Hypertensive Patients
NCT00439738PHASE4COMPLETEDSafety/Efficacy of Valsartan/Hydrochlorothiazide Combination Compared to Hydrochlorothiazide in Obese Hypertensive Adults
NCT00460915PHASE4COMPLETEDEfficacy and Safety of Lacidipine and Amlodipine on Blood Pressure in Korean ISH Patients Aged 60 to 80 Years
NCT00509470PHASE4COMPLETEDEvaluation of Effect of Combination With Telmisartan and Hydrochlorothiazide in Hypertensives Uncontrolled on Amlodipine
NCT00523549PHASE4COMPLETEDThe Effects of Systolic Blood Pressure Lowering on Diastolic Function Using Valsartan + Amlodipine in Patients With Hypertension and Diastolic Dysfunction
NCT00535925PHASE4COMPLETEDNephropathy In Type 2 Diabetes and Cardio-renal Events
NCT00538486PHASE4COMPLETEDA Randomized, Double-Blind, Active Control Trial Comparing Effects of Telmisartan, Candesartan and Amlodipine, Alone or Plus Metformin, on Non-Diabetic, Obese Hypertensive Patients
NCT00542269PHASE4TERMINATEDEfficacy and Safety of Aliskiren/Ramipril/Amlodipine Compared With Ramipril/Amlodipine and Aliskiren/Amlodipine in Patients With Metabolic Syndrome
NCT00637078PHASE4COMPLETEDSTITCH2 (Simplified Therapeutic Intervention to Control Hypertension and Hypercholesterolemia)

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 9 clinical and 31 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

MoleculeSourceStatusShared targets
DULOXETINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, P2RX4
PAROXETINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, P2RX4
AMIODARONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
AMITRIPTYLINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
CHLORPROMAZINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
CILOSTAZOLChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
CLOZAPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
DIAZEPAMChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
DILTIAZEMChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
DOFETILIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
DONEPEZILChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
DROPERIDOLChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
FLECAINIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
HALOPERIDOLChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
IBUTILIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
IMIPRAMINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
ISRADIPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
LAMIVUDINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
LORATADINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
METHADONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
MEXILETINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
MITOXANTRONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
NIFEDIPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
NILOTINIBChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
NIMODIPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
NISOLDIPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
PHENYTOINChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
PIMOZIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
QUINIDINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
RISPERIDONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
SAQUINAVIRChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
SOLIFENACINChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
SUNITINIBChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
THIORIDAZINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
VERAPAMILChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
ASTEMIZOLEChEMBLPhase 4 (approved)CACNA1C, CACNA1D
BEPRIDILChEMBLPhase 4 (approved)CACNA1C, CACNA1D
CISAPRIDEChEMBLPhase 4 (approved)CACNA1C, CACNA1D
DASATINIBChEMBLPhase 4 (approved)CACNA1C, CACNA1D
HALOFANTRINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D
MIBEFRADILChEMBLPhase 4 (approved)CACNA1C, CACNA1D
SERTINDOLEChEMBLPhase 4 (approved)CACNA1C, CACNA1D
SPARFLOXACINChEMBLPhase 4 (approved)CACNA1C, CACNA1D
TACRINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D
TERFENADINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D
TERODILINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D
AJMALINEChEMBLPhase 3CACNA1C, CACNA1D
NITRENDIPINEChEMBLPhase 3CACNA1C, CACNA1D
CIFENLINEChEMBLPhase 2CACNA1C, CACNA1D
GALLOPAMILChEMBLPhase 2CACNA1C, CACNA1D
BelzutifanPubChemApprovedCACNA1C, CACNA1D
MoxifloxacinPubChemApprovedCACNA1C, CACNA1D
PaliperidonePubChemApprovedCACNA1C, CACNA1D
SILDENAFILChEMBL + PubChemPhase 4 (approved)CACNA1C
VARDENAFILChEMBL + PubChemPhase 4 (approved)CACNA1C
ALVIMOPANChEMBLPhase 4 (approved)CACNA1C
CLEMASTINEChEMBLPhase 4 (approved)CACNA1C
CLOTRIMAZOLEChEMBLPhase 4 (approved)CACNA1C
DIBUCAINEChEMBLPhase 4 (approved)CACNA1C
DORIPENEMChEMBLPhase 4 (approved)CACNA1C

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
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Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot