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Atlas / Drug / Captopril

Captopril

drug
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Also known as AceprilApoprilC09AA01CapotenCaptomaxCaptomexCaptoprilumEcopaceFarcoprilGarranilHypopressHyteneze 12.5Hyteneze 25Hyteneze 50KaplonLoprilMephaNoyadaNSC-757419

Summary

Captopril (CHEMBL1560) is an approved small-molecule EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor (ATC C09AA01) targeting ACE; indicated across 20 conditions including congestive heart failure and hypertensive disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C09AA01
  • Targets: 1 (ACE)
  • Indications: 20 conditions
  • Clinical trials: 37
  • Chemistry: 217.29 Da · C9H15NO3S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1560
NameCaptopril
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID44093
ChEBICHEBI:3380
ATCC09AA01
Molecular formulaC9H15NO3S
Molecular weight217.29
InChIKeyFAKRSMQSSFJEIM-RQJHMYQMSA-N

SMILES: C[C@H](CS)C(=O)N1CCC[C@H]1C(=O)O

IUPAC name: (2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid

ChEBI definition: A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.

Pharmacological roles (ChEBI): EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor, antihypertensive agent.

Also known as: Acepril, Apopril, C09AA01, Capoten, Captomax, Captomex, Captopril, Captoprilum, Ecopace, Farcopril, Garranil, Hypopress

Patent coverage: 18,303 distinct patent families (66,415 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
ACEAngiotensin-converting enzymeInhibition8.40.7%P12821

Broader ChEMBL bioactivity targets: 23 (assay-derived). Sample: Succinyl-diaminopimelate desuccinylase, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, Thrombopoietin, Peripheral myelin protein 22, Metallo-beta-lactamase type 2, Angiotensin-converting enzyme, Prothrombin.

Bioactivity

ChEMBL activities: 81 potent at pChembl ≥ 5 of 106 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
ACE9.92IC500.12nMCHEMBL_ACT_2722713
ACE9.2IC500.63nMCHEMBL_ACT_2573366
ACE8.79IC501.61nMCHEMBL_ACT_15619819
P128228.77Ki1.7nMCHEMBL_ACT_673025
REN8.77Ki1.7nMCHEMBL_ACT_748542
ACE8.7Ki2nMCHEMBL_ACT_13830431
P478208.7Ki2nMCHEMBL_ACT_830786
P128228.64IC502.3nMCHEMBL_ACT_871862
P478208.52IC503nMCHEMBL_ACT_1181536
P478208.49IC503.23nMCHEMBL_ACT_18313507
P128228.44IC503.6nMCHEMBL_ACT_871861
ACE8.3IC505nMCHEMBL_ACT_2175818
ACE8.2IC506.3nMCHEMBL_ACT_18652535
ACE8.2IC506.3nMCHEMBL_ACT_24989632
ACE8.2IC506.3nMCHEMBL_ACT_29294968
ACE8.05IC509nMCHEMBL_ACT_1162706
ACE8.05IC509nMCHEMBL_ACT_298206
P128228IC5010nMCHEMBL_ACT_679962
ACE8IC5010nMCHEMBL_ACT_876619
ACE7.96IC5011nMCHEMBL_ACT_14567912
P478207.96IC5011nMCHEMBL_ACT_599966
ACE7.92IC5012nMCHEMBL_ACT_114010
ACE7.92IC5012nMCHEMBL_ACT_25090606
P478207.92IC5012nMCHEMBL_ACT_293218
P128227.89IC5013nMCHEMBL_ACT_315152
ACE7.89IC5012.9nMCHEMBL_ACT_333748
ACE7.89IC5013nMCHEMBL_ACT_375311
P128227.82IC5015nMCHEMBL_ACT_1087213
P128227.82IC5015nMCHEMBL_ACT_1168024
P478207.82IC5015nMCHEMBL_ACT_1302082

Target pathways

Aggregated over 1 target gene(s): ACE.

Top Reactome pathways

3 total, by targets touching each:

PathwayTargetsGenes
Metabolism of Angiotensinogen to Angiotensins1ACE
Peptide hormone metabolism1ACE
Metabolism of proteins1ACE

Dominant GO biological processes

GO termTargets
kidney development1
blood vessel remodeling1
angiotensin maturation1
regulation of renal output by angiotensin1
neutrophil mediated immunity1
antigen processing and presentation of peptide antigen via MHC class I1
regulation of systemic arterial blood pressure by renin-angiotensin1
positive regulation of systemic arterial blood pressure1
proteolysis1
spermatogenesis1
regulation of blood pressure1
male gonad development1
post-transcriptional regulation of gene expression1
negative regulation of gene expression1
substance P catabolic process1

Indications & clinical

Indications

20 indications (10 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
congestive heart failure4MONDO:0005009EFO:0000373
hypertensive disorder4MONDO:0005044EFO:0000537
myocardial infarction4MONDO:0005068EFO:0000612
diabetic kidney disease4MONDO:0005016EFO:0000401
cardiovascular disorder4MONDO:0004995EFO:0000319
diabetic retinopathy4MONDO:0005266EFO:0003770
heart failure4MONDO:0005252EFO:0003144
rheumatic disorder4MONDO:0005554EFO:0005755
kidney failure4MONDO:0001106EFO:1002048
severe acute respiratory syndrome3MONDO:0005091MONDO:0100096
essential hypertension3MONDO:0001134MONDO:0001134
type 1 diabetes mellitus3MONDO:0005147MONDO:0005147
heart disorder2MONDO:0005267EFO:0003777
pneumonia2MONDO:0005249EFO:0003106
glioblastoma1MONDO:0018177EFO:0000519
neoplasm1MONDO:0005070EFO:0000616
pulmonary arterial hypertension1MONDO:0015924EFO:0001361
primary myelofibrosis1MONDO:0009692EFO:0002430
type 2 diabetes mellitus1MONDO:0005148MONDO:0005148

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

Clinical trials

Total trials: 37.

Phase distribution

PhaseTrials
PHASE410
Not specified10
PHASE1/PHASE25
PHASE24
PHASE14
PHASE32
PHASE2/PHASE31
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07547878PHASE4NOT_YET_RECRUITINGRapid and Simultaneous Initiation of Four Guideline-Directed CKD Therapies (RAPID-CKD)
NCT00155064PHASE4COMPLETEDKallikrein-kinin (KKS) and Renin-angiotensin-aldosterone System (RAAS) in Primary Aldosteronism
NCT00252317PHASE4UNKNOWNAcute Haemodynamic Effects of Treatment With Angiotensin Converting Enzyme (ACE)-Inhibitors in Patients With Symptomatic Aortic Stenosis
NCT00391846PHASE4COMPLETEDEvaluation of Heart Failure Treatment Guided by N-terminal Pro B-type Natriuretic Peptide (NTproBNP) vs Clinical Symptoms and Signs Alone
NCT00660309PHASE4COMPLETEDA Clinical Study to Evaluate Renal Hemodynamic Responses to Aliskiren in Patients With Type 2 Diabetes Mellitus
NCT01545479PHASE4COMPLETEDIncreased Renal Oxygenation and Angiotensin Converting Enzyme Inhibition
NCT01761916PHASE4COMPLETEDClonidine Versus Captopril for Treatment of Postpartum Very High Blood Pressure
NCT02217852PHASE4UNKNOWNTreatment of Hypertension in Tibetan Adult Population
NCT04288700PHASE4UNKNOWNEvaluation of the Efficacy of Captopril Versus Propranolol and Timolol as a Treatment of Infantile Capillary Hemangioma
NCT04485845PHASE4UNKNOWNMetformin Versus Vildagliptin in Reducing Risk of Metabolic Syndrome Complications Progression
NCT00004230PHASE3COMPLETEDCaptopril in Treating Patients Undergoing Bone Marrow or Stem Cell Transplantation
NCT00663949PHASE2/PHASE3COMPLETEDAssessment of the Effect of Captopril Versus Combination of Captopril and Pentoxifylline on Reducing Proteinuria in Type 2 Diabetic Nephropathy
NCT01437371PHASE3COMPLETEDIs There a Benefit to Optimize Heart Failure (HF) Treatment in Aged Over 80 Year’s Old Patients?
NCT00077064PHASE2TERMINATEDCaptopril in Treating Patients With Non-Small Cell Lung Cancer or Limited-Stage Small Cell Lung Cancer That Has Been Previously Treated With Radiation Therapy With or Without Chemotherapy
NCT00086723PHASE1/PHASE2COMPLETEDIn Vivo Angiostatin Generation Using Tissue Plasminogen Activator and Captopril in Treating Patients With Progressive Metastatic Cancer
NCT00742040PHASE2UNKNOWNRapid Versus Prolonged Inpatient Up-Titration of Captopril
NCT01626469PHASE1/PHASE2UNKNOWNMeasurement of Eye Blood Flow and Renal Function in Healthy and Diabetic Patients
NCT02770378PHASE1/PHASE2COMPLETEDA Proof-of-concept Clinical Trial Assessing the Safety of the Coordinated Undermining of Survival Paths by 9 Repurposed Drugs Combined With Metronomic Temozolomide (CUSP9v3 Treatment Protocol) for Recurrent Glioblastoma
NCT03179163PHASE1/PHASE2TERMINATEDPeripheral Vascular Effects of Sulfhydryl-containing Antihypertensive Pharmacotherapy on Microvessels in Humans
NCT03613506PHASE2UNKNOWNThe Role and Intervention of TGF-β in Abdominal Radiation Injury
NCT04355429PHASE2UNKNOWNEfficacy of Captopril in Covid-19 Patients With Severe Acute Respiratory Syndrome (SARS) CoV-2 Pneumonia (CAPTOCOVID)
NCT04629651PHASE1/PHASE2WITHDRAWNCaptopril Use on the Degree of Marrow Fibrosis in Bone Marrow Fibrosis/Myeloproliferative Neoplasms
NCT00223717PHASE1COMPLETEDTreatment of Supine Hypertension in Autonomic Failure
NCT01292694PHASE1TERMINATEDContribution of Angiotensin II to Supine Hypertension in Autonomic Failure
NCT04878315PHASE1WITHDRAWNBioequivalence Study Between Capoten Versus Captopril Reference Product in Healthy Adult Participants Under Fasting Conditions
NCT06292091PHASE1COMPLETEDA Study to Investigate the Effect of Urine Acid-base Disequilibrium on the Pharmacokinetics of Captopril
NCT06485661EARLY_PHASE1RECRUITINGEffect of Captopril on GLS in Duchenne Myodystrophy
NCT05442463Not specifiedRECRUITINGHormone Therapy and Angiotensin-Dependent Arterial and Renal Vasoconstriction in Humans
NCT00292162Not specifiedCOMPLETEDCuring Atrial Fibrillation in Heart Failure
NCT00917345Not specifiedUNKNOWNDiagnosis of Primary Aldosteronism: Comparison of Post Captopril Active Renin Concentration and Plasma Renin Activity
NCT00935805Not specifiedUNKNOWNGlycemic And Blood Pressure Control In Type 2 Diabetes, In A Primary Care Unit: A Staged Management Strategy
NCT03660293Not specifiedCOMPLETEDPrediction and Prevention of Asymptomatic Cardiovascular Insult in Type 1 Diabetic Children: Comparative Effectiveness of Cardioprotective Drugs
NCT04371874Not specifiedCOMPLETEDThe Standardized Management of Hypertension in Rural Shaanxi
NCT04893629Not specifiedTERMINATEDNew Horizons for the Treatment of Cardiomyopathy in Children
NCT06037434Not specifiedUNKNOWNStudy of Innovative Drug Treatment Therapy for Pediatric Mitral Regurgitation
NCT06039540Not specifiedUNKNOWNStudy of Drug Therapy for Pediatric Heart Failure
NCT06039592Not specifiedUNKNOWNStudy of Innovative Drug Strategies in Improving Left Ventricular Function After Mitral Repair

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 4 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.

32 molecules share ≥1 primary target. Top 32 by shared-target count:

MoleculeSourceStatusShared targets
LOSARTANChEMBL + PubChemPhase 4 (approved)ACE
PERINDOPRILChEMBL + PubChemPhase 4 (approved)ACE
SITAGLIPTINChEMBL + PubChemPhase 4 (approved)ACE
BENAZEPRILChEMBLPhase 4 (approved)ACE
ENALAPRILChEMBLPhase 4 (approved)ACE
ENALAPRILATChEMBLPhase 4 (approved)ACE
FOSINOPRILChEMBLPhase 4 (approved)ACE
IMIDAPRILChEMBLPhase 4 (approved)ACE
LISINOPRILChEMBLPhase 4 (approved)ACE
MOEXIPRILChEMBLPhase 4 (approved)ACE
QUINAPRILChEMBLPhase 4 (approved)ACE
RAMIPRILChEMBLPhase 4 (approved)ACE
TELMISARTANChEMBLPhase 4 (approved)ACE
TRANDOLAPRILChEMBLPhase 4 (approved)ACE
EDETIC ACIDChEMBLPhase 3ACE
QUINAPRILATChEMBL + PubChemPhase 2 (approved)ACE
BENAZEPRILATChEMBLPhase 2ACE
CERONAPRILChEMBLPhase 2ACE
FOSINOPRILATChEMBLPhase 2ACE
IMIDAPRILATChEMBLPhase 2ACE
LIBENZAPRILChEMBLPhase 2ACE
MOEXIPRILATChEMBLPhase 2ACE
OMAPATRILATChEMBLPhase 2ACE
PROLINEChEMBLPhase 2ACE
RENTIAPRILChEMBLPhase 2ACE
SAMPATRILATChEMBLPhase 2ACE
SPIRAPRILATChEMBLPhase 2ACE
TEPROTIDEChEMBLPhase 2ACE
ZOFENOPRILChEMBLPhase 2ACE
Gallic AcidPubChemApprovedACE
HydrochlorothiazidePubChemApprovedACE
PaclitaxelPubChemApprovedACE

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