Canrenone

Summary

Canrenone (CHEMBL1463345) is an approved small molecule (ATC C03DA03) targeting NR3C2; indicated across 1 condition including cardiovascular disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C03DA03
• Targets: 1 (NR3C2)
• Indications: 1 condition
• Clinical trials: 4
• Chemistry: 340.5 Da · C22H28O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1463345
Name	Canrenone
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	13789
ATC	C03DA03
Molecular formula	C22H28O3
Molecular weight	340.5
InChIKey	UJVLDDZCTMKXJK-WNHSNXHDSA-N

SMILES: C[C@]12CCC(=O)C=C1C=C[C@@H]3[C@@H]2CC[C@]4([C@H]3CC[C@@]45CCC(=O)O5)C

IUPAC name: (8R,9S,10R,13S,14S,17R)-10,13-dimethylspiro[2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthrene-17,5’-oxolane]-2’,3-dione

Also known as: Canrenona, Canrenone, NSC-261713, SC-9376, Spironolactone metabolite m1, Spironolactone related compound a, SID49646110, CANRENONE, SID85305151, SID144205004, SID170466206, canrenone

Patent coverage: 1,357 distinct patent families (4,677 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
NR3C2	Mineralocorticoid receptor	Antagonist		0%	P08235

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Glucocorticoid receptor, Progesterone receptor, Muscarinic acetylcholine receptor M2, Kappa-type opioid receptor, Androgen receptor.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 5 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PGR	6.7	AC50	200	nM	CHEMBL_ACT_25222666
P15207	6.34	AC50	460	nM	CHEMBL_ACT_25232635
NR3C1	5.89	AC50	1300	nM	CHEMBL_ACT_25175419

Target pathways

Aggregated over 1 target gene(s): NR3C2.

Top Reactome pathways

9 total, by targets touching each:

Pathway	Targets	Genes
Cellular responses to stress	1	NR3C2
SUMOylation	1	NR3C2
SUMO E3 ligases SUMOylate target proteins	1	NR3C2
HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand	1	NR3C2
Nuclear Receptor transcription pathway	1	NR3C2
Metabolism of proteins	1	NR3C2
SUMOylation of intracellular receptors	1	NR3C2
Post-translational protein modification	1	NR3C2
Cellular responses to stimuli	1	NR3C2

Dominant GO biological processes

GO term	Targets
regulation of transcription by RNA polymerase II	1
signal transduction	1
nuclear receptor-mediated steroid hormone signaling pathway	1
positive regulation of non-canonical NF-kappaB signal transduction	1
regulation of DNA-templated transcription	1
cellular response to hormone stimulus	1
response to lipid	1

Indications & clinical

Indications

1 indication (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).

Indication	Trial phase	MONDO	EFO
cardiovascular disorder	4	MONDO:0004995	EFO:0000319

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE4	2
PHASE3	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02687178	PHASE4	COMPLETED	Canrenone as Add-on in Patients With Essential Hypertension
NCT03536806	PHASE4	UNKNOWN	Clinical Efficacy of Potassium Canrenoate in Sinus Rhythm Restoration Among Patients With Atrial Fibrillation.
NCT00403910	PHASE3	COMPLETED	Antiremodeling Effect Of Aldosterone Receptors Blockade With Canrenone In Mild Chronic Heart Failure. AREA IN-CHF Study
NCT03263962	Not specified	COMPLETED	Canrenone Effects on Cardiovascular Mortality in Patients With Congestive Heart Failure (the Coffee-it Study)

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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:

Molecule	Source	Status	Shared targets
EPLERENONE	ChEMBL + PubChem	Phase 4 (approved)	NR3C2
BUDESONIDE	ChEMBL	Phase 4 (approved)	NR3C2
DEXAMETHASONE	ChEMBL	Phase 4 (approved)	NR3C2
FINERENONE	ChEMBL	Phase 4 (approved)	NR3C2
FLUTICASONE FUROATE	ChEMBL	Phase 4 (approved)	NR3C2
FLUTICASONE PROPIONATE	ChEMBL	Phase 4 (approved)	NR3C2
HYDROCORTISONE	ChEMBL	Phase 4 (approved)	NR3C2
HYDROCORTISONE BUTYRATE	ChEMBL	Phase 4 (approved)	NR3C2
MEDROXYPROGESTERONE	ChEMBL	Phase 4 (approved)	NR3C2
MIFEPRISTONE	ChEMBL	Phase 4 (approved)	NR3C2
PREDNISOLONE	ChEMBL	Phase 4 (approved)	NR3C2
PROGESTERONE	ChEMBL	Phase 4 (approved)	NR3C2
SPIRONOLACTONE	ChEMBL	Phase 4 (approved)	NR3C2
ASOPRISNIL	ChEMBL	Phase 3	NR3C2
BALCINRENONE	ChEMBL	Phase 3	NR3C2
CORTICOSTERONE	ChEMBL	Phase 3	NR3C2
ALDOSTERONE	ChEMBL	Phase 2	NR3C2
LY2623091	ChEMBL	Phase 2	NR3C2
METRIBOLONE	ChEMBL	Phase 2	NR3C2
MT-3995	ChEMBL	Phase 2	NR3C2
ONAPRISTONE	ChEMBL	Phase 2	NR3C2
STANOLONE	ChEMBL	Phase 2	NR3C2
TUROFEXORATE ISOPROPYL	ChEMBL	Phase 2	NR3C2
Enzalutamide	PubChem	Approved	NR3C2
Fludrocortisone	PubChem	Approved	NR3C2
ursodiol	PubChem	Approved	NR3C2