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Nicardipine

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Also known as Nicardipine (stn)NicardipinoPerpidineSID26755701SID26755702SID90340664SID104171201SID50111158SID50111159SID124880905SID144203762SID170465173Nicardipin

Summary

Nicardipine (CHEMBL1484) is an approved small molecule (ATC C08CA04) targeting ADORA3 and KCNA4; indicated across 9 conditions including cardiovascular disorder and hypertensive disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C08CA04
  • Targets: 2 (ADORA3, KCNA4)
  • Indications: 9 conditions
  • Clinical trials: 31
  • Chemistry: 479.5 Da · C26H29N3O6

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1484
NameNicardipine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID4474
ChEBICHEBI:180905
ATCC08CA04
Molecular formulaC26H29N3O6
Molecular weight479.5
InChIKeyZBBHBTPTTSWHBA-UHFFFAOYSA-N

SMILES: CC1=C(C(C(=C(N1)C)C(=O)OCCN(C)CC2=CC=CC=C2)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OC

IUPAC name: 5-O-[2-[benzyl(methyl)amino]ethyl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

ChEBI definition: A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively.

Also known as: Nicardipine, Nicardipine (stn), Nicardipino, Perpidine, nicardipine, SID26755701, SID26755702, SID90340664, SID104171201, SID50111158, SID50111159, SID124880905

Parent form; salt/anhydrous children: CHEMBL1200326

Patent coverage: 8,080 distinct patent families (30,866 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 30,763 (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
ADORA3A3 receptorAntagonist5.50%P0DMS8
KCNA4Kv1.46.10.7%P22459

Broader ChEMBL bioactivity targets: 50 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Transient receptor potential cation channel subfamily A member 1, Microtubule-associated protein tau, Survival motor neuron protein, Prelamin-A/C, Inositol monophosphatase 1, NPC intracellular cholesterol transporter 1, Ras-related protein Rab-9A, ATP-binding cassette sub-family C member 4, Alpha-2A adrenergic receptor.

Bioactivity

ChEMBL activities: 57 potent at pChembl ≥ 5 of 85 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P220029.08Ki0.84nMCHEMBL_ACT_933287
P220028.57IC502.66nMCHEMBL_ACT_407463
CACNA1C6.6IC50250nMCHEMBL_ACT_15373254
CYP2C96.55Ki280nMCHEMBL_ACT_389069
CYP2C96.42IC50378nMCHEMBL_ACT_15445914
CYP3A46.42IC50380nMCHEMBL_ACT_15450991
SLC6A26.4AC50397nMCHEMBL_ACT_25146252
CYP3A46.38IC50420nMCHEMBL_ACT_1150428
CHRM26.37AC50424.4nMCHEMBL_ACT_25195988
Q8BLA86.3EC50500nMCHEMBL_ACT_3301113
CYP2C196.25IC50560nMCHEMBL_ACT_15450931
CYP2C96.18IC50660nMCHEMBL_ACT_15450951
ADRA1A6.13AC50746.9nMCHEMBL_ACT_25219060
ABCB16.02IC50950nMCHEMBL_ACT_1150431
CHRM15.91AC501241nMCHEMBL_ACT_25210421
P193285.85IC501400nMCHEMBL_ACT_962939
PGR5.82AC501512nMCHEMBL_ACT_25204543
CYP2C85.81IC501560nMCHEMBL_ACT_15447387
CYP2D65.8IC501590nMCHEMBL_ACT_15445905
CYP2J25.77IC501690nMCHEMBL_ACT_15461598
ADORA35.77AC501696nMCHEMBL_ACT_25198914
CYP2D65.75IC501780nMCHEMBL_ACT_15450971
DRD15.72AC501883nMCHEMBL_ACT_25115462
LMNA5.7Potency1995nMCHEMBL_ACT_3653394
HTR1A5.66AC502175nMCHEMBL_ACT_25165276
ABCB15.64IC502300nMCHEMBL_ACT_11001309
ABCB15.64IC502300nMCHEMBL_ACT_1150434
P214475.6IC502500nMCHEMBL_ACT_11001319
P214475.6IC502500nMCHEMBL_ACT_1150432
SLC6A35.56AC502740nMCHEMBL_ACT_25125211

Target pathways

Aggregated over 2 target gene(s): ADORA3, KCNA4.

Top Reactome pathways

11 total, by targets touching each:

PathwayTargetsGenes
Neuronal System1KCNA4
Potassium Channels1KCNA4
Voltage gated Potassium channels1KCNA4
Signal Transduction1ADORA3
Signaling by GPCR1ADORA3
Class A/1 (Rhodopsin-like receptors)1ADORA3
GPCR downstream signalling1ADORA3
Adenosine P1 receptors1ADORA3
Nucleotide-like (purinergic) receptors1ADORA3
G alpha (i) signalling events1ADORA3
GPCR ligand binding1ADORA3

Dominant GO biological processes

GO termTargets
G protein-coupled adenosine receptor signaling pathway1
inflammatory response1
signal transduction1
activation of adenylate cyclase activity1
regulation of heart contraction1
negative regulation of cell population proliferation1
response to wounding1
regulation of norepinephrine secretion1
negative regulation of cell migration1
obsolete negative regulation of NF-kappaB transcription factor activity1
presynaptic modulation of chemical synaptic transmission1
G protein-coupled receptor signaling pathway1
action potential1
potassium ion transport1
protein homooligomerization1

Indications & clinical

Indications

9 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
preeclampsia3MONDO:0005081EFO:0000668
thoracic aortic aneurysm2MONDO:0005396EFO:0004282
stroke disorder2MONDO:0005098EFO:0000712
subarachnoid hemorrhage2MONDO:0005099EFO:0000713
brain neoplasm1MONDO:0021211EFO:0003833
coronary artery disorder0MONDO:0005010EFO:0001645

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

Clinical trials

Total trials: 31.

Phase distribution

PhaseTrials
Not specified11
PHASE49
PHASE34
PHASE23
PHASE12
EARLY_PHASE12

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07044232PHASE4NOT_YET_RECRUITINGNICardipine for Fast Achievement of Systolic BP Targets in ICH
NCT07246629PHASE4NOT_YET_RECRUITINGLumbar Drain With Intrathecal Nicardipine in Aneurysmal Subarachnoid Hemorrhage
NCT00325793PHASE4UNKNOWNIV Double and Triple Concentrated Nicardipine for Stroke and ICH
NCT00765648PHASE4COMPLETEDEvaluation of Intravenous Cardene(Nicardipine)and Labetalol Use in the Emergency Department
NCT01171911PHASE4UNKNOWNComparison of Intravenous Injection of Calcium Antagonist and Beta-blockade on Endothelial Shear Stress of Coronary Artery
NCT01996436PHASE4TERMINATEDThe Intra-arterial Vasospasm Trial
NCT02271191PHASE4COMPLETEDEffect of Nicardipine on Renal Function in Deliberate Hypotension
NCT06093893PHASE4COMPLETEDHypotensive Anesthesia for Orthognathic Surgery
NCT07277283PHASE4COMPLETEDNicardipine vs. Labetalol
NCT00093925PHASE3COMPLETEDClevidipine in the Postoperative Treatment of Hypertension (ECLIPSE-NIC)
NCT00409253PHASE3UNKNOWNTreatment of Severe Hypertension During Pre-Eclampsia: A Preliminary Equivalence Study Between Urapidil and Nicardipine
NCT02558023PHASE3TERMINATEDThe Treatment of Hypertension Associated With Severe Preeclampsia (PE). A Trial of Urapidil Versus Nicardipine
NCT04538534PHASE3COMPLETEDNicardipine to Avoid Spasm in Trans Radial Percutaneous Coronary Intervention
NCT00508118PHASE2TERMINATEDNICardipine Neuroprotection in AortiC Surgery (NICNACS)
NCT04116112PHASE2COMPLETEDBlood Pressure After Endovascular Stroke Therapy-II
NCT04269408PHASE2COMPLETEDA Safety and Efficacy Study of NicaPlant® in Aneurysmal Subarachnoid Haemorrhage Patients Undergoing Aneurysm Clipping
NCT00415610PHASE1COMPLETEDAntihypertensive Treatment in Acute Cerebral Hemorrhage
NCT01951950PHASE1COMPLETEDNicardipine vs Esmolol Craniotomy Emergence
NCT03184155EARLY_PHASE1WITHDRAWNPrevention of Coronary Microvascular Dysfunction Post-PCI by Intracoronary Nicardipine
NCT05625503EARLY_PHASE1COMPLETEDDilution of Verapamil During Intraarterial Administration
NCT06329635Not specifiedRECRUITINGTreatment of Vasospasm of Aneurysmal Subarachnoid Hemorrhage With Intrathecal Nicardipine - FAST-IT Trial
NCT07603037Not specifiedNOT_YET_RECRUITINGEIT Evaluation of Different Antihypertensive Agents on the Ventilation-Perfusion Ratio in Patients With Acute Respiratory Failure
NCT00226096Not specifiedCOMPLETEDIntensive Blood Pressure Reduction in Acute Cerebral Haemorrhage
NCT00490464Not specifiedCOMPLETEDSafety and Efficacy of Nicardipine for the Control of Blood Pressure After SAH
NCT01041066Not specifiedUNKNOWNNicardipine Versus Labetalol During Intubation
NCT01175746Not specifiedCOMPLETEDThe Effect of Nicardipine on Kidney Function During Orthognathic Surgery Under Hypotensive Anesthesia
NCT03497351Not specifiedCOMPLETEDEffects of Different Kinds of Hypotensive Drugs on Dynamic Hemodynamic Changing in Patients Under Surgeries
NCT05586347Not specifiedCOMPLETEDRelationship Between Perioperative Carotid Blood Flow Monitoring and Cerebral Function Protection in Cardiac Surgery
NCT05920538Not specifiedUNKNOWNEffects of Subcutaneously Infiltrated Nicardipine on the Success Rate of Radial Artety Cannulation
NCT06130527Not specifiedUNKNOWNComparison of the Effects of Nicardipine and Remifentanil on Surgical Visual Field
NCT07364201Not specifiedCOMPLETEDA Comparison of Nicardipine and Labetalol for Blood Pressure Control in Intensive Care Patients After Hemorrhagic Stroke Brain Surgery

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 2 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.

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

MoleculeSourceStatusShared targets
FIDAXOMICINChEMBL + PubChemPhase 4 (approved)ADORA3
LINAGLIPTINChEMBL + PubChemPhase 4 (approved)ADORA3
PYRAZINAMIDEChEMBL + PubChemPhase 4 (approved)ADORA3
VORAPAXARChEMBL + PubChemPhase 4 (approved)ADORA3
ACALABRUTINIBChEMBLPhase 4 (approved)ADORA3
ADENOSINEChEMBLPhase 4 (approved)ADORA3
ALECTINIBChEMBLPhase 4 (approved)ADORA3
ALFACALCIDOLChEMBLPhase 4 (approved)ADORA3
ALPIDEMChEMBLPhase 4 (approved)ADORA3
AMIODARONEChEMBLPhase 4 (approved)ADORA3
AMITRIPTYLINEChEMBLPhase 4 (approved)ADORA3
AMLODIPINEChEMBLPhase 4 (approved)ADORA3
AMOROLFINEChEMBLPhase 4 (approved)ADORA3
AMOXAPINEChEMBLPhase 4 (approved)ADORA3
ANTAZOLINEChEMBLPhase 4 (approved)ADORA3
APOMORPHINEChEMBLPhase 4 (approved)ADORA3
ARIPIPRAZOLEChEMBLPhase 4 (approved)ADORA3
ASTEMIZOLEChEMBLPhase 4 (approved)ADORA3
AURANOFINChEMBLPhase 4 (approved)ADORA3
AXITINIBChEMBLPhase 4 (approved)ADORA3
BACLOFENChEMBLPhase 4 (approved)ADORA3
BALSALAZIDEChEMBLPhase 4 (approved)ADORA3
BAZEDOXIFENEChEMBLPhase 4 (approved)ADORA3
BECLOMETHASONE DIPROPIONATEChEMBLPhase 4 (approved)ADORA3
BENFLUOREXChEMBLPhase 4 (approved)ADORA3
BENZBROMARONEChEMBLPhase 4 (approved)ADORA3
BEPRIDILChEMBLPhase 4 (approved)ADORA3
BETAMETHASONE DIPROPIONATEChEMBLPhase 4 (approved)ADORA3
BEXAROTENEChEMBLPhase 4 (approved)ADORA3
BITHIONOLChEMBLPhase 4 (approved)ADORA3
BOSUTINIBChEMBLPhase 4 (approved)ADORA3
BROMHEXINEChEMBLPhase 4 (approved)ADORA3
BROMOCRIPTINEChEMBLPhase 4 (approved)ADORA3
BUCLIZINEChEMBLPhase 4 (approved)ADORA3
BUTOCONAZOLEChEMBLPhase 4 (approved)ADORA3
CABOZANTINIBChEMBLPhase 4 (approved)ADORA3
CAFFEINEChEMBLPhase 4 (approved)ADORA3
CALCIPOTRIENEChEMBLPhase 4 (approved)ADORA3
CALCITRIOLChEMBLPhase 4 (approved)ADORA3
CANAGLIFLOZINChEMBLPhase 4 (approved)ADORA3
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)ADORA3
CANNABIDIOLChEMBLPhase 4 (approved)ADORA3
CAPSAICINChEMBLPhase 4 (approved)ADORA3
CARVEDILOLChEMBLPhase 4 (approved)ADORA3
CASPOFUNGINChEMBLPhase 4 (approved)ADORA3
CEFACLORChEMBLPhase 4 (approved)ADORA3
CELECOXIBChEMBLPhase 4 (approved)ADORA3
CEPHRADINEChEMBLPhase 4 (approved)ADORA3
CHLORDIAZEPOXIDEChEMBLPhase 4 (approved)ADORA3
CHLORHEXIDINEChEMBLPhase 4 (approved)ADORA3
CHLORMADINONEChEMBLPhase 4 (approved)ADORA3
CHLOROTRIANISENEChEMBLPhase 4 (approved)ADORA3
CHLORPROMAZINEChEMBLPhase 4 (approved)ADORA3
CHLORPROTHIXENEChEMBLPhase 4 (approved)ADORA3
CHOLECALCIFEROLChEMBLPhase 4 (approved)ADORA3
CIANIDANOLChEMBLPhase 4 (approved)ADORA3
CICLESONIDEChEMBLPhase 4 (approved)ADORA3
CILOSTAZOLChEMBLPhase 4 (approved)ADORA3
CINACALCETChEMBLPhase 4 (approved)ADORA3
CINNARIZINEChEMBLPhase 4 (approved)ADORA3

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
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot