Balcinrenone

Summary

Balcinrenone (CHEMBL3916929) is a phase-3 clinical-stage small molecule targeting NR3C2; indicated across 6 conditions including chronic kidney disease and heart failure.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (NR3C2)
• Indications: 6 conditions
• Clinical trials: 12
• Chemistry: 399.4 Da · C20H18FN3O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3916929
Name	Balcinrenone
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	118599727
Molecular formula	C20H18FN3O5
Molecular weight	399.4
InChIKey	MBKYLPOPYYLTNW-ZDUSSCGKSA-N

SMILES: CNC(=O)C[C@H]1COC2=C(N1C(=O)C3=CC4=C(C=C3)OCC(=O)N4)C=CC(=C2)F

IUPAC name: 2-[(3S)-7-fluoro-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]-N-methylacetamide

Also known as: Azd 9977, Azd-9977, AZD-9977, Azd9977, AZD9977, Balcinrenona, Balcinrenone, US9394291, 4a, BALCINRENONE

Patent coverage: 35 distinct patent families (132 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 100 (76%) 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
NR3C2	Mineralocorticoid receptor	Antagonist	6.4	0%	P08235

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Mineralocorticoid receptor, Glucocorticoid receptor, Mineralocorticoid receptor.

Bioactivity

ChEMBL activities: 8 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
NR3C2	7.9	EC50	12.59	nM	CHEMBL_ACT_19363581
NR3C2	7.4	Ki	39.81	nM	CHEMBL_ACT_19363275
P22199	7.1	IC50	79.43	nM	CHEMBL_ACT_19363557
NR3C2	6.89	IC50	130	nM	CHEMBL_ACT_17778940
NR3C2	6.62	IC50	240	nM	CHEMBL_ACT_17778953
NR3C2	6.5	IC50	316.2	nM	CHEMBL_ACT_19363544
NR3C2	6.4	IC50	398.1	nM	CHEMBL_ACT_19363313
NR3C1	5.6	Ki	2512	nM	CHEMBL_ACT_19363294

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

6 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).

Indication	Trial phase	MONDO	EFO
chronic kidney disease	2	MONDO:0005300	EFO:0003884
heart failure	1	MONDO:0005252	EFO:0003144
cardiovascular disorder	1	MONDO:0004995	EFO:0000319
kidney disorder	1	MONDO:0005240	EFO:0003086
liver disorder	1	MONDO:0005154	EFO:0001421

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

Clinical trials

Total trials: 12.

Phase distribution

Phase	Trials
PHASE1	11
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04595370	PHASE2	COMPLETED	Efficacy, Safety and Tolerability of AZD9977 and Dapagliflozin in Participants With Heart Failure and Chronic Kidney Disease
NCT02484729	PHASE1	COMPLETED	A Study to Assess the Safety, Tolerability and Pharmacokinetics of AZD9977 After Single Ascending Doses to Healthy Males
NCT02532998	PHASE1	COMPLETED	A Study to Assess the Pharmacodynamic Effect of Single Doses of AZD9977 in Healthy Male Subjects
NCT03435276	PHASE1	COMPLETED	Multiple-ascending Dose Study to Assess the Safety, Tolerability and Pharmacokinetics of AZD9977 in Healthy Male Subjects
NCT03450759	PHASE1	COMPLETED	A Single Oral Dose Study to Evaluate Four Different Formulations of AZD9977 and the Effect of Food in Healthy Male Subjects
NCT03682497	PHASE1	TERMINATED	Study in HFpEF Patients to Compare the Effect of AZD9977 and Spironolactone on Serum Potassium
NCT03801967	PHASE1	COMPLETED	A Study to Assess the Safety, Tolerability and Pharmacokinetics of AZD9977 in Japanese Healthy Participants With Single and Multiple Ascending Dose Administration
NCT03843060	PHASE1	COMPLETED	A Phase 1 Study to Assess the Pharmacokinetics of AZD9977 Administered Alone and in Combination With Itraconazole in Healthy Volunteers
NCT04469907	PHASE1	COMPLETED	Study to Assess the Pharmacokinetics and Safety of AZD9977 in Participants With Renal Impairment
NCT06388616	PHASE1	COMPLETED	Study to Investigate the Effect of Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of Balcinrenone
NCT06651021	PHASE1	COMPLETED	A Phase I PK Study of Balcinrenone/Dapagliflozin in Healthy Chinese Participants
NCT06979388	PHASE1	COMPLETED	A Study to Investigate the Effect of Food on Balcinrenone/Dapagliflozin Pharmacokinetics in Fed and Fasted State and Pharmacokinetics of Balcinrenone When Dosed With a P-gp Inhibitor in Healthy Participants.

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.

25 molecules share ≥1 primary target. Top 25 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
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