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Isradipine

drug
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Also known as DynacircDynacirc crIsradipinoIsrodipineNSC-759892PrescalSID11114262ISRAPIDINESID144204241SID170465070MMV001493(S)-ISRADIPINEC0164848C0237141

Summary

Isradipine (CHEMBL1648) is an approved small molecule (ATC C08CA03) targeting CACNA1C, CACNA1D, and CACNA1F; indicated across 8 conditions including cardiovascular disorder and hypertensive disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C08CA03
  • Targets: 3 (CACNA1C, CACNA1D, CACNA1F)
  • Indications: 8 conditions
  • Clinical trials: 8
  • Chemistry: 371.4 Da · C19H21N3O5

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1648
NameIsradipine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3784
ATCC08CA03
Molecular formulaC19H21N3O5
Molecular weight371.4
InChIKeyHMJIYCCIJYRONP-UHFFFAOYSA-N

SMILES: CC1=C(C(C(=C(N1)C)C(=O)OC(C)C)C2=CC=CC3=NON=C32)C(=O)OC

IUPAC name: 3-O-methyl 5-O-propan-2-yl 4-(2,1,3-benzoxadiazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

Also known as: Dynacirc, Dynacirc cr, Isradipine, Isradipino, Isrodipine, NSC-759892, Prescal, SID11114262, ISRADIPINE, isradipine, ISRAPIDINE, SID144204241

Patent coverage: 4,951 distinct patent families (20,026 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).

GeneTargetActionpAffinityCancer dependencyUniProt
CACNA1CCav1.2Antagonist8.50.1%Q13936
CACNA1DCav1.39.30.3%Q01668
CACNA1FCav1.4Antagonist0%O60840

Broader ChEMBL bioactivity targets: 27 (assay-derived). Sample: Voltage-dependent L-type calcium channel subunit alpha-1C, Sodium channel protein type 5 subunit alpha, Glucocorticoid receptor, Thromboxane A2 receptor, Menin/Histone-lysine N-methyltransferase MLL, Motilin receptor, Delta-type opioid receptor, Kappa-type opioid receptor, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 14 potent at pChembl ≥ 5 of 34 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
CACNA1C8.66IC502.2nMCHEMBL_ACT_15373248
P220028.35AC504.5nMCHEMBL_ACT_25119642
CACNA1C7.02AC5095nMCHEMBL_ACT_25159103
P153816.97IC50107nMCHEMBL_ACT_13362877
P277326.66IC50221nMCHEMBL_ACT_13362871
SCN5A5.53AC502985nMCHEMBL_ACT_25158931
CYP2C95.44IC503660nMCHEMBL_ACT_15445897
CYP2D65.32IC504790nMCHEMBL_ACT_15445896
CYP2C85.3IC505000nMCHEMBL_ACT_15447375
NR1I25.28AC505300nMCHEMBL_ACT_25188219
PDE4D5.05AC509000nMCHEMBL_ACT_25185393
CYP3A45Potency10000nMCHEMBL_ACT_4957420
CYP3A45Potency10000nMCHEMBL_ACT_5026777
CYP3A45AC5010000nMCHEMBL_ACT_6049119

Target pathways

Aggregated over 3 target gene(s): CACNA1C, CACNA1D, CACNA1F.

Top Reactome pathways

16 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
Muscle contraction1CACNA1C
Cardiac conduction1CACNA1C
Phase 0 - rapid depolarisation1CACNA1C
Phase 2 - plateau phase1CACNA1C
Sensory processing of sound1CACNA1D
Sensory processing of sound by inner hair cells of the cochlea1CACNA1D
Sensory Perception1CACNA1D

Dominant GO biological processes

GO termTargets
calcium ion transmembrane transport3
calcium ion import across plasma membrane3
monoatomic ion transport3
calcium ion transport3
monoatomic ion transmembrane transport3
transmembrane transport3
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
muscle contraction2
cell communication2
signaling2
immune system development1
positive regulation of cytosolic calcium ion concentration1

Indications & clinical

Indications

8 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).

IndicationTrial phaseMONDOEFO
cardiovascular disorder4MONDO:0004995EFO:0000319
hypertensive disorder4MONDO:0005044EFO:0000537
Parkinson disease3MONDO:0005180MONDO:0005180
bipolar disorder2MONDO:0004985MONDO:0004985
opiate dependence1MONDO:0005530EFO:0005611
drug dependence1MONDO:0005303EFO:0003890
nicotine dependence0MONDO:0008575EFO:0003768

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

Clinical trials

Total trials: 8.

Phase distribution

PhaseTrials
Not specified2
PHASE2/PHASE31
PHASE31
PHASE21
PHASE1/PHASE21
PHASE11
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT01007994PHASE2/PHASE3COMPLETEDReduction of Night-time Blood Pressure in Pediatric Renal Transplant Recipients
NCT02168842PHASE3COMPLETEDEfficacy of Isradipine in Early Parkinson Disease
NCT01784666PHASE2TERMINATEDAdjunctive Isradipine for the Treatment of Bipolar Depression
NCT01895270PHASE1/PHASE2COMPLETEDImproving Buprenorphine Detoxification Outcomes With Isradipine
NCT00593463PHASE1COMPLETEDDrug Discrimination in Methadone-Maintained Humans Study 1
NCT03083353EARLY_PHASE1COMPLETEDIsradipine Enhancement of Virtual Reality Cue Exposure for Smoking Cessation
NCT01658150Not specifiedCOMPLETEDEvaluating Isradipine for Cognitive Enhancement in Schizophrenia and Schizoaffective Disorder
NCT02136823Not specifiedUNKNOWNImpact of Persistent Conductances on Motor Unit Firing in SCI

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

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

MoleculeSourceStatusShared targets
AMIODARONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
AMITRIPTYLINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
CHLORPROMAZINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
CILOSTAZOLChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
CLOZAPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
DIAZEPAMChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
DILTIAZEMChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
DOFETILIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
DONEPEZILChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
DROPERIDOLChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
DULOXETINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
FLECAINIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
HALOPERIDOLChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
IBUTILIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
IMIPRAMINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
LAMIVUDINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
LORATADINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
METHADONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
MEXILETINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
MITOXANTRONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
NIFEDIPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
NILOTINIBChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
NIMODIPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
NISOLDIPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
PAROXETINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
PHENYTOINChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
PIMOZIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
QUINIDINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
RISPERIDONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
SAQUINAVIRChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
SOLIFENACINChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
SUNITINIBChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
THIORIDAZINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
VERAPAMILChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
ASTEMIZOLEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
BEPRIDILChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
CISAPRIDEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
DASATINIBChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
HALOFANTRINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
MIBEFRADILChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
SERTINDOLEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
SPARFLOXACINChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
TACRINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
TERFENADINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
TERODILINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F
AJMALINEChEMBLPhase 3CACNA1C, CACNA1D, CACNA1F
NITRENDIPINEChEMBLPhase 3CACNA1C, CACNA1D, CACNA1F
CIFENLINEChEMBLPhase 2CACNA1C, CACNA1D, CACNA1F
GALLOPAMILChEMBLPhase 2CACNA1C, CACNA1D, CACNA1F
BelzutifanPubChemApprovedCACNA1C, CACNA1D, CACNA1F
MoxifloxacinPubChemApprovedCACNA1C, CACNA1D, CACNA1F
PaliperidonePubChemApprovedCACNA1C, CACNA1D, CACNA1F
AMLODIPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D
CeftriaxonePubChemApprovedCACNA1D, CACNA1F
DisopyramidePubChemApprovedCACNA1D, CACNA1F
LinezolidPubChemApprovedCACNA1D, CACNA1F
MelatoninPubChemApprovedCACNA1D, CACNA1F
MetronidazolePubChemApprovedCACNA1D, CACNA1F
PemigatinibPubChemApprovedCACNA1D, CACNA1F
PentobarbitalPubChemApprovedCACNA1D, CACNA1F

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