Ocedurenone

drug
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Also known as Kbp-5074KBP5074

Summary

Ocedurenone (CHEMBL5314961) is a phase-3 clinical-stage small molecule targeting NR3C2; indicated across 3 conditions including chronic kidney disease and liver disorder.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 1 (NR3C2)
  • Indications: 3 conditions
  • Clinical trials: 8
  • Chemistry: 504 Da · C28H30ClN5O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL5314961
NameOcedurenone
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID75593324
Molecular formulaC28H30ClN5O2
Molecular weight504
InChIKeyUXHQLGLGLZKHTC-CUNXSJBXSA-N

SMILES: C1CCC(C1)[C@H]2[C@H]3CCC4=C(C3=NN2C5=CC(=C(C=C5)C#N)Cl)C=CC(=N4)C(=O)N6CCC(CC6)O

IUPAC name: 4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxypiperidine-1-carbonyl)-3,3a,4,5-tetrahydropyrazolo[3,4-f]quinolin-2-yl]-2-chlorobenzonitrile

Also known as: Kbp-5074, KBP5074, Ocedurenone, OCEDURENONE

Patent coverage: 7 distinct patent families (24 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 22 (92%) 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
NR3C2Mineralocorticoid receptorAntagonist8.570%P08235

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): NR3C2.

Top Reactome pathways

9 total, by targets touching each:

PathwayTargetsGenes
Cellular responses to stress1NR3C2
SUMOylation1NR3C2
SUMO E3 ligases SUMOylate target proteins1NR3C2
HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand1NR3C2
Nuclear Receptor transcription pathway1NR3C2
Metabolism of proteins1NR3C2
SUMOylation of intracellular receptors1NR3C2
Post-translational protein modification1NR3C2
Cellular responses to stimuli1NR3C2

Dominant GO biological processes

GO termTargets
regulation of transcription by RNA polymerase II1
signal transduction1
nuclear receptor-mediated steroid hormone signaling pathway1
positive regulation of non-canonical NF-kappaB signal transduction1
regulation of DNA-templated transcription1
cellular response to hormone stimulus1
response to lipid1

Indications & clinical

Indications

3 indications (0 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
chronic kidney disease3MONDO:0005300EFO:0003884
liver disorder1MONDO:0005154EFO:0001421
kidney failure1MONDO:0001106HP:0000083

Clinical trials

Total trials: 8.

Phase distribution

PhaseTrials
PHASE17
PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04968184PHASE3TERMINATEDEfficacy and Safety of KBP-5074 in Uncontrolled Hypertension and Moderate or Severe Chronic Kidney Disease (CKD)
NCT02228733PHASE1COMPLETEDPhase 1 Single Ascending Dose Study to Evaluate Safety, Tolerability and Pharmacokinetics of KBP-5074
NCT02653014PHASE1COMPLETEDSafety, Tolerability and Pharmacokinetics of KBP-5074 in Healthy Subjects and Subjects With Renal Impairment
NCT02837237PHASE1COMPLETEDSafety, Tolerability, and Pharmacokinetics of KBP-5074 Following Oral Administration in Chronic Kidney Disease
NCT03340753PHASE1COMPLETEDBioavailability of KBP-5074 Tablet vs Capsule Formulations
NCT04534699PHASE1COMPLETEDPharmacokinetics of KBP-5074 in Patients With Moderate Hepatic Impairment
NCT04606537PHASE1COMPLETEDDrug to Drug Interaction Study of KBP-5074 in Healthy Subjects
NCT04634812PHASE1COMPLETEDMass Balance Study of KBP-5074 in Healthy Male Subjects

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

26 molecules share ≥1 primary target. Top 26 by shared-target count:

MoleculeSourceStatusShared targets
EPLERENONEChEMBL + PubChemPhase 4 (approved)NR3C2
BUDESONIDEChEMBLPhase 4 (approved)NR3C2
DEXAMETHASONEChEMBLPhase 4 (approved)NR3C2
FINERENONEChEMBLPhase 4 (approved)NR3C2
FLUTICASONE FUROATEChEMBLPhase 4 (approved)NR3C2
FLUTICASONE PROPIONATEChEMBLPhase 4 (approved)NR3C2
HYDROCORTISONEChEMBLPhase 4 (approved)NR3C2
HYDROCORTISONE BUTYRATEChEMBLPhase 4 (approved)NR3C2
MEDROXYPROGESTERONEChEMBLPhase 4 (approved)NR3C2
MIFEPRISTONEChEMBLPhase 4 (approved)NR3C2
PREDNISOLONEChEMBLPhase 4 (approved)NR3C2
PROGESTERONEChEMBLPhase 4 (approved)NR3C2
SPIRONOLACTONEChEMBLPhase 4 (approved)NR3C2
ASOPRISNILChEMBLPhase 3NR3C2
BALCINRENONEChEMBLPhase 3NR3C2
CORTICOSTERONEChEMBLPhase 3NR3C2
ALDOSTERONEChEMBLPhase 2NR3C2
LY2623091ChEMBLPhase 2NR3C2
METRIBOLONEChEMBLPhase 2NR3C2
MT-3995ChEMBLPhase 2NR3C2
ONAPRISTONEChEMBLPhase 2NR3C2
STANOLONEChEMBLPhase 2NR3C2
TUROFEXORATE ISOPROPYLChEMBLPhase 2NR3C2
EnzalutamidePubChemApprovedNR3C2
FludrocortisonePubChemApprovedNR3C2
ursodiolPubChemApprovedNR3C2