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Diltiazem

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Also known as Diltiazem extended releaseDitiazSurazem(+)-cis-DiltiazemSID11113366SID26751609SID90341257SID26751610SID50104266SID50104267SID50104268SID50104269SID144204449SID170464699Dilitazem

Summary

Diltiazem (CHEMBL23) is an approved small-molecule calcium channel blocker (ATC C05AE03) targeting CACNA1S, CACNA1C, and CACNA1D; indicated across 24 conditions including cardiovascular disorder and hemorrhoid.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C05AE03 (+1 more)
  • Targets: 9 (CACNA1S, CACNA1C, CACNA1D…)
  • Indications: 24 conditions
  • Clinical trials: 63
  • Chemistry: 414.5 Da · C22H26N2O4S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL23
NameDiltiazem
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID39186
ChEBICHEBI:101278
ATCC05AE03, C08DB01
Molecular formulaC22H26N2O4S
Molecular weight414.5
InChIKeyHSUGRBWQSSZJOP-RTWAWAEBSA-N

SMILES: CC(=O)O[C@@H]1[C@@H](SC2=CC=CC=C2N(C1=O)CCN(C)C)C3=CC=C(C=C3)OC

IUPAC name: [(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate

ChEBI definition: A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension.

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

Also known as: Diltiazem, Diltiazem extended release, Ditiaz, Surazem, diltiazem, (+)-cis-Diltiazem, SID11113366, SID26751609, SID90341257, SID26751610, SID50104266, SID50104267

Parent form; salt/anhydrous children: CHEMBL1697, CHEMBL1200805

Patent coverage: 14,488 distinct patent families (54,676 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 54,450 (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
5-HT3A4.68
CACNA1SCav1.1Antagonist4.20.2%Q13698
CACNA1CCav1.2Antagonist6.30.1%Q13936
CACNA1DCav1.33.50.3%Q01668
CACNA1FCav1.440%O60840
KCNA1Kv1.13.80%Q09470
KCNA2Kv1.2Pore blocker3.70.7%P16389
KCNA5Kv1.5Pore blocker3.90.2%P22460
KCNA7Kv1.74.20.5%Q96RP8
KCNC1Kv3.141.7%P48547

Broader ChEMBL bioactivity targets: 22 (assay-derived). Sample: Prelamin-A/C, Voltage-dependent L-type calcium channel subunit alpha-1C, Histamine H2 receptor, Thyrotropin receptor, Voltage-gated L-type calcium channel, Voltage-gated L-type calcium channel, Sodium channel alpha subunits; brain (Types I, II, III), Alpha-1A adrenergic receptor, Sodium channel alpha subunit, Voltage-dependent L-type calcium channel subunit alpha-1C.

Bioactivity

ChEMBL activities: 36 potent at pChembl ≥ 5 of 68 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P220027.8Ki16nMCHEMBL_ACT_1216781
P220027.8Ki16nMCHEMBL_ACT_612495
P220027.68Ki21nMCHEMBL_ACT_463439
P220027.68Ki21nMCHEMBL_ACT_521600
P220027.5Ki32nMCHEMBL_ACT_13340330
P220027.44IC5036nMCHEMBL_ACT_13340395
P220027.38IC5042nMCHEMBL_ACT_1216780
P220027.38IC5042nMCHEMBL_ACT_612494
P220027.34IC5046nMCHEMBL_ACT_463438
P220027.34IC5046nMCHEMBL_ACT_521599
P277327.34IC5045.71nMCHEMBL_ACT_747102
P220027.28IC5052nMCHEMBL_ACT_5165988
P220027.27IC5054nMCHEMBL_ACT_463440
P220027.07Ki85nMCHEMBL_ACT_2419632
CYP3A47Ki100nMCHEMBL_ACT_12163666
CYP3A47IC50100nMCHEMBL_ACT_15467242
CYP3A47IC50100nMCHEMBL_ACT_15467244
P220027IC50100nMCHEMBL_ACT_794611
P220026.55Ki280nMCHEMBL_ACT_521601
CACNA1S6.42Ki380nMCHEMBL_ACT_619119
CACNA1F6.35IC50450nMCHEMBL_ACT_15257926
CYP3A46.3Ki500nMCHEMBL_ACT_6075180
O355056.2IC50630nMCHEMBL_ACT_15373226
CACNA1F6.12IC50760nMCHEMBL_ACT_15373323
CYP3A45.74IC501837nMCHEMBL_ACT_7702771
CYP3A45.66Ki2200nMCHEMBL_ACT_6075145
KCNH25.59AC502565nMCHEMBL_ACT_25118512
P220025.58IC502600nMCHEMBL_ACT_2419601
CACNA1C5.57AC502700nMCHEMBL_ACT_25159135
CYP3A45.4Potency3981nMCHEMBL_ACT_5006305

Target pathways

Aggregated over 9 target gene(s): CACNA1S, CACNA1C, CACNA1D, CACNA1F, KCNA1, KCNA2, KCNA5, KCNA7, KCNC1.

Top Reactome pathways

20 total, by targets touching each:

PathwayTargetsGenes
Neuronal System5KCNA1, KCNA2, KCNA5, KCNA7, KCNC1
Potassium Channels5KCNA1, KCNA2, KCNA5, KCNA7, KCNC1
Voltage gated Potassium channels5KCNA1, KCNA2, KCNA5, KCNA7, KCNC1
Developmental Biology3CACNA1C, CACNA1D, CACNA1S
NCAM signaling for neurite out-growth3CACNA1C, CACNA1D, CACNA1S
NCAM1 interactions3CACNA1C, CACNA1D, CACNA1S
Axon guidance3CACNA1C, CACNA1D, CACNA1S
Nervous system development3CACNA1C, CACNA1D, CACNA1S
Metabolism2CACNA1C, CACNA1D
Integration of energy metabolism2CACNA1C, CACNA1D
Muscle contraction2CACNA1C, KCNA5
Adrenaline,noradrenaline inhibits insulin secretion2CACNA1C, CACNA1D
Regulation of insulin secretion2CACNA1C, CACNA1D
Cardiac conduction2CACNA1C, KCNA5
Phase 3 - rapid repolarisation1KCNA5
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
monoatomic ion transport9
monoatomic ion transmembrane transport9
transmembrane transport9
action potential5
protein homooligomerization5
potassium ion transmembrane transport5
potassium ion transport5
calcium ion transport4
calcium ion transmembrane transport4
calcium ion import across plasma membrane4
muscle contraction3
regulation of heart rate by cardiac conduction3
regulation of membrane potential3
positive regulation of muscle contraction2
system process2

Indications & clinical

Indications

24 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
hemorrhoid4MONDO:0004872EFO:0009552
atrial fibrillation3MONDO:0004981EFO:0000275
hypertensive disorder3MONDO:0005044EFO:0000537
ischemia reperfusion injury3MONDO:0005203EFO:0002687
heart failure3MONDO:0005252EFO:0003144
atherosclerosis3MONDO:0005311EFO:0003914
myocardial ischemia3MONDO:0024644EFO:1001375
coronary artery disorder3MONDO:0005010EFO:0001645
severe acute respiratory syndrome3MONDO:0005091MONDO:0100096
type 2 diabetes mellitus3MONDO:0005148MONDO:0005148
hypertrophic cardiomyopathy2MONDO:0005045EFO:0000538
influenza2MONDO:0005812EFO:0007328
anus disorder2MONDO:0002519EFO:0009660
metabolic syndrome X1MONDO:0011565EFO:0000195
drug dependence1MONDO:0005303EFO:0003890
constipation disorder1MONDO:0002203HP:0002019
thrombotic disease1MONDO:0000831MONDO:0000831
neoplasm1MONDO:0005070MONDO:0004992
hypotensive disorder0MONDO:0005468EFO:0005251

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

Clinical trials

Total trials: 63.

Phase distribution

PhaseTrials
PHASE126
PHASE416
PHASE36
Not specified5
PHASE24
EARLY_PHASE13
PHASE1/PHASE22
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06993038PHASE4RECRUITINGAdenosine vs Diltiazem for Treatment of SVT in the ED
NCT07103655PHASE4NOT_YET_RECRUITINGThe Therapeutic Value of Mavacamten in Hypertrophic Cardiomyopathy With Mid-to-Apical Left Ventricular Obstruction
NCT00318201PHASE4COMPLETEDThe Effect of Concomitant Administration of Erythromycin and Diltiazem on CYP3A Activity in Healthy Volunteers
NCT00712894PHASE4COMPLETEDEffects of Different Vasodilators on Coronary No-reflow During primAry percuTaneous Coronary intErvention in Patients With Acute Myocardial Infarction
NCT00893100PHASE4COMPLETEDEvaluation of Pain Reduction After Hemorrhoidectomy With Use of Diltiazim Ointment 2%
NCT01655303PHASE4COMPLETEDRate Control in Atrial Fibrillation
NCT01914926PHASE4COMPLETEDComparison of Diltiazem and Metoprolol in the Management of Acute Atrial Fibrillation or Atrial Flutter
NCT02025465PHASE4UNKNOWNRandomized Trial Comparing Diltiazem and Metoprolol For Atrial Fibrillation Rate Control
NCT02695992PHASE4COMPLETEDRate Control in Atrial Fibrillation II
NCT03472495PHASE4COMPLETEDOral vs Intravenous Diltiazem for Rapid Atrial Fibrillation/Flutter Trial
NCT03930433PHASE4COMPLETEDThe Effect of Nebivolol in Hypertensive Patients With Coronary Arterial Spasm
NCT04141553PHASE4UNKNOWNBolus vs IVP (Intravenous Push) Diltiazem for Atrial Fibrillation or Flutter
NCT05261464PHASE4UNKNOWNHeart Rate Controller in Computed Tomography Coronary Angiography
NCT05294887PHASE4UNKNOWNRandomized Trial to Examine a Differential Therapeutic Response in Symptomatic Patients With Non-obstructive Coronary Artery Disease
NCT06534671PHASE4COMPLETEDDiltiazem in Jervell and Lange-Nielsen Syndrome
NCT07456423PHASE4COMPLETEDAdenosine vs. Diltiazem
NCT06276127PHASE3NOT_YET_RECRUITINGOral Bisoprolol Vs IV Diltiazem in Atrial Fibrillation or Flutter With Rapid Ventricular Rate.
NCT00000478PHASE3COMPLETEDAsymptomatic Cardiac Ischemia Pilot (ACIP) Study
NCT00000556PHASE3COMPLETEDAtrial Fibrillation Follow-up Investigation of Rhythm Management (AFFIRM)
NCT00313157PHASE3COMPLETEDRATe Control in Atrial Fibrillation
NCT00319982PHASE2/PHASE3COMPLETEDTreatment of Preclinical Hypertrophic Cardiomyopathy With Diltiazem
NCT01217515PHASE3COMPLETEDDiltiazem Hydrochloride Cream for Anal Fissure
NCT01771978PHASE3UNKNOWNIschaemia-réperfusion During the Coronary Surgery With Beating Heart
NCT04153032PHASE2RECRUITINGComparative Evaluation of MEBO Ointment and Topical Diltiazem Ointment in the Treatment of Acute Anal Fissure
NCT01408524PHASE1/PHASE2COMPLETEDControl of Emergence Blood Pressure During Craniotomy for Tumor Surgery Between Labetolol and Diltiazem
NCT02503865PHASE1/PHASE2COMPLETEDDevelopment of Rational Ways of Medical and Non-medical Treatment Methods for Metabolic Syndrome
NCT03212716PHASE2TERMINATEDEfficiency of Antagonist Drugs of the Cellular Transcriptomic Signature of Influenza A Virus Infection.
NCT03752931PHASE2UNKNOWNCeliprolol Versus Ditiazem for the Prevention of Postoperative Cardiac Arrythmias in Thoracic Surgery
NCT04130438PHASE2TERMINATEDEfficacy of Medical Therapy in Women and Men With Angina and Myocardial Bridging
NCT00223717PHASE1COMPLETEDTreatment of Supine Hypertension in Autonomic Failure
NCT00593463PHASE1COMPLETEDDrug Discrimination in Methadone-Maintained Humans Study 1
NCT01021176PHASE1TERMINATEDEvaluate a Medication on How Hunger and Appetite Are Influenced by Smell
NCT01124760PHASE1COMPLETEDOpen Label Study, Assessing the Effect of Diltiazem or Ketoconazole on the Pharmacokinetics of AZD9742 in Healthy Volunteers
NCT01211808PHASE1COMPLETEDEffect of Diltiazem on Pharmacokinetics of BMS-914392
NCT01549496PHASE1WITHDRAWNA Drug Interaction Study of Boceprevir in Combination With Amlodipine or Diltiazem in Healthy Volunteers
NCT01816191PHASE1UNKNOWNAn Open-Label, Single- and Multi-Dose Pharmacokinetic (PK) Study of Oral Diltiazem and Topical Diltiazem Hydrochloride
NCT01816529PHASE1UNKNOWNTopical Safety Study of Topical Diltiazem Hydrochloride
NCT01821274PHASE1UNKNOWNA 21-Day Topical Safety Study of Diltiazem Hydrochloride Using a Cumulative Irritant Patch Test Design
NCT01852565PHASE1COMPLETEDStudy to Determine the Effect of Repeated Administration of Diltiazem on the Pharmacokinetics of Darapladib (Sb-480848).
NCT02300259PHASE1COMPLETEDA Study of LY2623091 in Healthy Participants

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 13 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.

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

MoleculeSourceStatusShared targets
FLECAINIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S, KCNA1, KCNA5, KCNA7
NIFEDIPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S, KCNA1, KCNA5
QUINIDINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S, KCNA5, KCNA7
AMIODARONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S, KCNA7
VERAPAMILChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S, KCNA7
SERTINDOLEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S, KCNA5
BelzutifanPubChemApprovedCACNA1C, CACNA1D, CACNA1F, CACNA1S, KCNA5
AMITRIPTYLINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
CHLORPROMAZINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
CILOSTAZOLChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
CLOZAPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
DIAZEPAMChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
DOFETILIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
DONEPEZILChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
DROPERIDOLChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
DULOXETINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
HALOPERIDOLChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
IBUTILIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
IMIPRAMINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
LAMIVUDINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
LORATADINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
METHADONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
MEXILETINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
MITOXANTRONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
NILOTINIBChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
NIMODIPINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
NisoldipineChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
PAROXETINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
PHENYTOINChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
PIMOZIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
RISPERIDONEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
SAQUINAVIRChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
SOLIFENACINChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
SUNITINIBChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
THIORIDAZINEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
ASTEMIZOLEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
BEPRIDILChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
CISAPRIDEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
DASATINIBChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
HALOFANTRINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
MIBEFRADILChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
SPARFLOXACINChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
TACRINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
TERFENADINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
TERODILINEChEMBLPhase 4 (approved)CACNA1C, CACNA1D, CACNA1F, CACNA1S
AJMALINEChEMBLPhase 3CACNA1C, CACNA1D, CACNA1F, CACNA1S
NITRENDIPINEChEMBLPhase 3CACNA1C, CACNA1D, CACNA1F, CACNA1S
CIFENLINEChEMBLPhase 2CACNA1C, CACNA1D, CACNA1F, CACNA1S
GALLOPAMILChEMBLPhase 2CACNA1C, CACNA1D, CACNA1F, CACNA1S
MoxifloxacinPubChemApprovedCACNA1C, CACNA1D, CACNA1F, CACNA1S
PaliperidonePubChemApprovedCACNA1C, CACNA1D, CACNA1F, CACNA1S
CeftriaxonePubChemApprovedCACNA1D, CACNA1F, CACNA1S
DisopyramidePubChemApprovedCACNA1D, CACNA1F, CACNA1S
LinezolidPubChemApprovedCACNA1D, CACNA1F, CACNA1S
MelatoninPubChemApprovedCACNA1D, CACNA1F, CACNA1S
MetronidazolePubChemApprovedCACNA1D, CACNA1F, CACNA1S
PemigatinibPubChemApprovedCACNA1D, CACNA1F, CACNA1S
PentobarbitalPubChemApprovedCACNA1D, CACNA1F, CACNA1S
ProcainamidePubChemApprovedCACNA1D, CACNA1F, CACNA1S
RaltegravirPubChemApprovedCACNA1D, CACNA1F, CACNA1S

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