Relacorilant

Summary

Relacorilant (CHEMBL4068611) is a phase-3 clinical-stage small molecule targeting NR3C1; indicated across 10 conditions including cushing syndrome and adrenal gland hyperfunction.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (NR3C1)
• Indications: 10 conditions
• Clinical trials: 17
• Chemistry: 586.6 Da · C27H22F4N6O3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4068611
Name	Relacorilant
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	73051463
Molecular formula	C27H22F4N6O3S
Molecular weight	586.6
InChIKey	WANIDIGFXJFFEL-SANMLTNESA-N

SMILES: CN1C=C(C=N1)S(=O)(=O)N2CCC3=CC4=C(C[C@@]3(C2)C(=O)C5=NC=CC(=C5)C(F)(F)F)C=NN4C6=CC=C(C=C6)F

IUPAC name: [(4aR)-1-(4-fluorophenyl)-6-(1-methylpyrazol-4-yl)sulfonyl-4,5,7,8-tetrahydropyrazolo[5,4-g]isoquinolin-4a-yl]-[4-(trifluoromethyl)-2-pyridinyl]methanone

Also known as: Cort 125134, Cort-125134, CORT125134, Relacorilant, RELACORILANT

Patent coverage: 146 distinct patent families (530 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 466 (88%) 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
NR3C1	Glucocorticoid receptor	Antagonist	8.14	0.9%	P04150

Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Glucocorticoid receptor, Cytochrome P450 2D6, Cytochrome P450 3A5, Glucocorticoid receptor, Cytochrome P450 2C9, Cytochrome P450 3A4, Cytochrome P450 2C19, Cytochrome P450 2C8.

Bioactivity

ChEMBL activities: 9 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
NR3C1	8.14	Ki	7.2	nM	CHEMBL_ACT_18235806
P06536	7.92	Ki	12	nM	CHEMBL_ACT_18235948
NR3C1	7.09	Ki	81.2	nM	CHEMBL_ACT_18235955
CYP2C8	6.68	IC50	210	nM	CHEMBL_ACT_18235930
CYP3A4	5.89	IC50	1300	nM	CHEMBL_ACT_18235934
CYP2C9	5.7	IC50	2000	nM	CHEMBL_ACT_18235931
CYP3A5	5.31	IC50	4900	nM	CHEMBL_ACT_18235935
CYP2C19	5.1	IC50	8000	nM	CHEMBL_ACT_18235932
CYP2D6	5.05	IC50	9000	nM	CHEMBL_ACT_18235933

Target pathways

Aggregated over 1 target gene(s): NR3C1.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand	1	NR3C1
Nuclear Receptor transcription pathway	1	NR3C1
SUMOylation of intracellular receptors	1	NR3C1
PTK6 Expression	1	NR3C1
Regulation of RUNX2 expression and activity	1	NR3C1
FOXO-mediated transcription of oxidative stress, metabolic and neuronal genes	1	NR3C1
Potential therapeutics for SARS	1	NR3C1
Regulation of NPAS4 gene transcription	1	NR3C1

Dominant GO biological processes

GO term	Targets
negative regulation of transcription by RNA polymerase II	1
regulation of gluconeogenesis	1
chromatin organization	1
regulation of DNA-templated transcription	1
regulation of transcription by RNA polymerase II	1
apoptotic process	1
chromosome segregation	1
signal transduction	1
glucocorticoid metabolic process	1
response to wounding	1
gene expression	1
microglia differentiation	1
adrenal gland development	1
nuclear receptor-mediated steroid hormone signaling pathway	1
regulation of glucocorticoid biosynthetic process	1

Indications & clinical

Indications

10 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
Cushing syndrome	3	MONDO:0018912	EFO:0003099
adrenal gland hyperfunction	3	MONDO:0006640	EFO:1000797
pancreatic ductal adenocarcinoma	3	MONDO:0005184	MONDO:0005184
fallopian tube carcinoma	2	MONDO:0006206	EFO:1000251
ovarian cancer	2	MONDO:0008170	MONDO:0008170
prostate adenocarcinoma	2	MONDO:0005082	EFO:0000673
neoplasm	1	MONDO:0005070	EFO:0000616
adrenal cortex carcinoma	1	MONDO:0006639	EFO:1000796
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: 17.

Phase distribution

Phase	Trials
PHASE1	11
PHASE2	4
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03697109	PHASE3	COMPLETED	A Study of the Efficacy and Safety of Relacorilant in Patients With Endogenous Cushing Syndrome
NCT04308590	PHASE3	COMPLETED	A Study of the Efficacy and Safety of Relacorilant in Patients With Cortisol-Secreting Adrenal Adenomas
NCT03604198	PHASE2	ACTIVE_NOT_RECRUITING	Extension Study to Evaluate the Safety of Long-Term Use of Relacorilant in Patients With Cushing Syndrome
NCT05726292	PHASE2	RECRUITING	A Study of Enzalutamide Plus the Glucocorticoid Receptor Antagonist Relacorilant Versus Placebo for Patients With High-risk Localized Prostate Cancer
NCT02804750	PHASE2	COMPLETED	Study to Evaluate CORT125134 in Participants With Cushing’s Syndrome
NCT03776812	PHASE2	COMPLETED	Study of Relacorilant in Combination With Nab-Paclitaxel for Patients With Recurrent Platinum-Resistant Ovarian, Fallopian Tube, or Primary Peritoneal Cancer
NCT03442621	PHASE1	COMPLETED	Relacorilant Food Effect Study in Healthy Subjects
NCT03457597	PHASE1	COMPLETED	Study in Healthy Subjects to Determine the Effect of Relacorilant on Exposure to Probe Substrates for Cytochrome P450s
NCT03508635	PHASE1	COMPLETED	CORT125134 Single Ascending Dose (SAD) and Multiple Ascending Dose (MAD)
NCT03512548	PHASE1	COMPLETED	Study in Healthy Subjects to Determine the Effect of an Inhibitor on Exposure to Relacorilant and Its Metabolites
NCT03674814	PHASE1	COMPLETED	Study of Drug 1 (Enzalutamide) Plus Drug 2 (Relacorilant) for Patients With Prostate Cancer
NCT04373265	PHASE1	COMPLETED	Study of Relacorilant in Combination With Pembrolizumab for Patients With Adrenocortical Carcinoma Which Produces Too Much Stress Hormone (Cortisol)
NCT04795479	PHASE1	COMPLETED	T/QT Study to Investigate the Effect of Relacorilant on Cardiac Repolarization in Healthy Volunteers
NCT05347979	PHASE1	COMPLETED	Effect of Relacorilant on the Pharmacokinetics of the Sensitive P-glycoprotein Substrate Dabigatran Etexilate in Healthy Participants
NCT06094712	PHASE1	COMPLETED	A Study to Evaluate the Pharmacokinetics of the CORT125134 Phase 2 Formulation in Healthy Male Subjects
NCT06094725	PHASE1	COMPLETED	A Study to Evaluate the Effects of Hepatic Impairment on the Pharmacokinetics of Relacorilant
NCT06094790	PHASE1	COMPLETED	A Study to Evaluate the Pharmacokinetics of the Current Capsule Formulation of CORT125134 in Healthy Subjects

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.

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

Molecule	Source	Status	Shared targets
FULVESTRANT	ChEMBL + PubChem	Phase 4 (approved)	NR3C1
PODOFILOX	ChEMBL + PubChem	Phase 4 (approved)	NR3C1
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	NR3C1
ACENOCOUMAROL	ChEMBL	Phase 4 (approved)	NR3C1
ALCLOMETASONE DIPROPIONATE	ChEMBL	Phase 4 (approved)	NR3C1
AMCINONIDE	ChEMBL	Phase 4 (approved)	NR3C1
AMIODARONE	ChEMBL	Phase 4 (approved)	NR3C1
APREPITANT	ChEMBL	Phase 4 (approved)	NR3C1
AURANOFIN	ChEMBL	Phase 4 (approved)	NR3C1
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	NR3C1
BECLOMETHASONE DIPROPIONATE	ChEMBL	Phase 4 (approved)	NR3C1
BENZBROMARONE	ChEMBL	Phase 4 (approved)	NR3C1
BETAMETHASONE	ChEMBL	Phase 4 (approved)	NR3C1
BETAMETHASONE DIPROPIONATE	ChEMBL	Phase 4 (approved)	NR3C1
BETAMETHASONE PHOSPHORIC ACID	ChEMBL	Phase 4 (approved)	NR3C1
BETAMETHASONE VALERATE	ChEMBL	Phase 4 (approved)	NR3C1
BUDESONIDE	ChEMBL	Phase 4 (approved)	NR3C1
BUTOCONAZOLE	ChEMBL	Phase 4 (approved)	NR3C1
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	NR3C1
CANRENONE	ChEMBL	Phase 4 (approved)	NR3C1
CHLORMADINONE	ChEMBL	Phase 4 (approved)	NR3C1
CICLESONIDE	ChEMBL	Phase 4 (approved)	NR3C1
CLOBETASOL PROPIONATE	ChEMBL	Phase 4 (approved)	NR3C1
CLOFAZIMINE	ChEMBL	Phase 4 (approved)	NR3C1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	NR3C1
CORTISONE	ChEMBL	Phase 4 (approved)	NR3C1
DANAZOL	ChEMBL	Phase 4 (approved)	NR3C1
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	NR3C1
DEFLAZACORT	ChEMBL	Phase 4 (approved)	NR3C1
DESOGESTREL	ChEMBL	Phase 4 (approved)	NR3C1
DESONIDE	ChEMBL	Phase 4 (approved)	NR3C1
DESOXIMETASONE	ChEMBL	Phase 4 (approved)	NR3C1
DESOXYCORTICOSTERONE PIVALATE	ChEMBL	Phase 4 (approved)	NR3C1
DEXAMETHASONE	ChEMBL	Phase 4 (approved)	NR3C1
DEXTROTHYROXINE	ChEMBL	Phase 4 (approved)	NR3C1
DIENESTROL	ChEMBL	Phase 4 (approved)	NR3C1
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	NR3C1
DIFLORASONE DIACETATE	ChEMBL	Phase 4 (approved)	NR3C1
DOXORUBICIN	ChEMBL	Phase 4 (approved)	NR3C1
DROSPIRENONE	ChEMBL	Phase 4 (approved)	NR3C1
ECONAZOLE	ChEMBL	Phase 4 (approved)	NR3C1
EFAVIRENZ	ChEMBL	Phase 4 (approved)	NR3C1
ENZALUTAMIDE	ChEMBL	Phase 4 (approved)	NR3C1
EPLERENONE	ChEMBL	Phase 4 (approved)	NR3C1
ESTRADIOL	ChEMBL	Phase 4 (approved)	NR3C1
ESTRIOL	ChEMBL	Phase 4 (approved)	NR3C1
ETHINYL ESTRADIOL	ChEMBL	Phase 4 (approved)	NR3C1
EXEMESTANE	ChEMBL	Phase 4 (approved)	NR3C1
FELODIPINE	ChEMBL	Phase 4 (approved)	NR3C1
FLUDROCORTISONE	ChEMBL	Phase 4 (approved)	NR3C1
FLUNISOLIDE	ChEMBL	Phase 4 (approved)	NR3C1
FLUOCINOLONE ACETONIDE	ChEMBL	Phase 4 (approved)	NR3C1
FLUOCINONIDE	ChEMBL	Phase 4 (approved)	NR3C1
FLUOROMETHOLONE	ChEMBL	Phase 4 (approved)	NR3C1
FLUOXYMESTERONE	ChEMBL	Phase 4 (approved)	NR3C1
FLURANDRENOLIDE	ChEMBL	Phase 4 (approved)	NR3C1
FLUTICASONE FUROATE	ChEMBL	Phase 4 (approved)	NR3C1
FLUTICASONE PROPIONATE	ChEMBL	Phase 4 (approved)	NR3C1
GLUCAGON	ChEMBL	Phase 4 (approved)	NR3C1
HALCINONIDE	ChEMBL	Phase 4 (approved)	NR3C1