General Information of Drug Combination (ID: DC9B3HT)

Drug Combination Name
CORT-125134 Enzalutamide
Indication
Disease Entry Status REF
Prostate Cancer Phase 2 [1]
Component Drugs CORT-125134   DMBS3UG Enzalutamide   DMGL19D
N.A. Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of CORT-125134
Disease Entry ICD 11 Status REF
Cushing disease 5A70 Phase 3 [2]
Solid tumour/cancer 2A00-2F9Z Phase 1/2 [3]
Alcohol dependence 6C40.2 Clinical trial [4]
CORT-125134 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Glucocorticoid receptor (NR3C1) TTYRL6O GCR_HUMAN Antagonist [3]
------------------------------------------------------------------------------------
Indication(s) of Enzalutamide
Disease Entry ICD 11 Status REF
Prostate cancer 2C82.0 Approved [5]
Enzalutamide Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Androgen receptor (AR) TTS64P2 ANDR_HUMAN Modulator [8]
------------------------------------------------------------------------------------
Enzalutamide Interacts with 117 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Androgen receptor (AR) OTUBKAZZ ANDR_HUMAN Decreases Response To Substance [9]
Very long chain fatty acid elongase 7 (ELOVL7) OT89NYVC ELOV7_HUMAN Decreases Expression [6]
Bone morphogenetic protein receptor type-1B (BMPR1B) OTGFN0OD BMR1B_HUMAN Decreases Expression [6]
Procollagen-lysine,2-oxoglutarate 5-dioxygenase 2 (PLOD2) OTKOZRZP PLOD2_HUMAN Decreases Expression [6]
RNA polymerase II elongation factor ELL2 (ELL2) OTZJRTFM ELL2_HUMAN Decreases Expression [6]
Suppressor of cytokine signaling 2 (SOCS2) OTBPNKJQ SOCS2_HUMAN Decreases Expression [6]
Transmembrane protease serine 2 (TMPRSS2) OTN44YQ5 TMPS2_HUMAN Decreases Expression [6]
ATP-binding cassette sub-family C member 4 (ABCC4) OTO27PAL MRP4_HUMAN Decreases Expression [6]
Unconventional myosin-Ib (MYO1B) OTGZUJ0I MYO1B_HUMAN Decreases Expression [6]
Kinesin heavy chain isoform 5C (KIF5C) OT35570Y KIF5C_HUMAN Decreases Expression [6]
Transcription factor Maf (MAF) OT1GR3IZ MAF_HUMAN Decreases Expression [6]
Solute carrier family 22 member 3 (SLC22A3) OTQYGVXX S22A3_HUMAN Decreases Expression [6]
Insulin-like growth factor I (IGF1) OTIIZR61 IGF1_HUMAN Decreases Expression [6]
Tyrosine-protein kinase Lck (LCK) OT883FG9 LCK_HUMAN Decreases Expression [6]
Insulin-like growth factor 1 receptor (IGF1R) OTXJIF13 IGF1R_HUMAN Decreases Expression [6]
Microtubule-associated protein 2 (MAP2) OT6UYT3X MTAP2_HUMAN Decreases Expression [6]
Plastin-2 (LCP1) OTK61F2A PLSL_HUMAN Decreases Expression [6]
Kallikrein-2 (KLK2) OT9RE37R KLK2_HUMAN Decreases Expression [6]
Zinc-alpha-2-glycoprotein (AZGP1) OTPD9TDR ZA2G_HUMAN Decreases Expression [6]
Dipeptidyl peptidase 4 (DPP4) OT16MVL9 DPP4_HUMAN Decreases Expression [6]
Prostaglandin E2 receptor EP4 subtype (PTGER4) OT2GBV06 PE2R4_HUMAN Decreases Expression [6]
Phospholipase A2 group V (PLA2G5) OTQRSKCZ PA2G5_HUMAN Decreases Expression [6]
Regulator of G-protein signaling 2 (RGS2) OT0FSRW7 RGS2_HUMAN Decreases Expression [6]
Retinaldehyde dehydrogenase 3 (ALDH1A3) OT1C9NKQ AL1A3_HUMAN Decreases Expression [6]
Selenoprotein P (SELENOP) OT02B8IR SEPP1_HUMAN Decreases Expression [6]
AF4/FMR2 family member 3 (AFF3) OTR0705Z AFF3_HUMAN Decreases Expression [6]
Cysteine-rich secretory protein 3 (CRISP3) OTBSWMPL CRIS3_HUMAN Decreases Expression [6]
Tumor protein D52 (TPD52) OTPKSK43 TPD52_HUMAN Decreases Expression [6]
Testican-1 (SPOCK1) OTLTDGK7 TICN1_HUMAN Decreases Expression [6]
Acyl-coenzyme A synthetase ACSM1, mitochondrial (ACSM1) OT1TS9M9 ACSM1_HUMAN Decreases Expression [6]
Ras GTPase-activating-like protein IQGAP2 (IQGAP2) OTX2UA7P IQGA2_HUMAN Decreases Expression [6]
Glycine N-methyltransferase (GNMT) OT0O2OQO GNMT_HUMAN Decreases Expression [6]
Ketimine reductase mu-crystallin (CRYM) OTRGSR6B CRYM_HUMAN Decreases Expression [6]
Manganese-dependent ADP-ribose/CDP-alcohol diphosphatase (ADPRM) OTXE3X5J ADPRM_HUMAN Decreases Expression [6]
Protein GREB1 (GREB1) OTU6ZA26 GREB1_HUMAN Decreases Expression [6]
EF-hand calcium-binding domain-containing protein 12 (EFCAB12) OT1QZJEI EFC12_HUMAN Decreases Expression [6]
Rho-related GTP-binding protein RhoU (RHOU) OTERIAD4 RHOU_HUMAN Decreases Expression [6]
Transient receptor potential cation channel subfamily M member 8 (TRPM8) OT7ACGYK TRPM8_HUMAN Decreases Expression [6]
Alpha-protein kinase 2 (ALPK2) OTWZZDQ9 ALPK2_HUMAN Decreases Expression [6]
Kynurenine/alpha-aminoadipate aminotransferase, mitochondrial (AADAT) OTO68C3Y AADAT_HUMAN Decreases Expression [6]
Chondroitin sulfate N-acetylgalactosaminyltransferase 1 (CSGALNACT1) OTBML9D9 CGAT1_HUMAN Decreases Expression [6]
Homeobox protein Nkx-3.1 (NKX3-1) OT0DO6ZU NKX31_HUMAN Decreases Expression [6]
Specifically androgen-regulated gene protein (C1ORF116) OTPYEXDM SARG_HUMAN Decreases Expression [6]
ER degradation-enhancing alpha-mannosidase-like protein 3 (EDEM3) OT4GJX9R EDEM3_HUMAN Decreases Expression [6]
Alpha-N-acetylgalactosaminide alpha-2,6-sialyltransferase 1 (ST6GALNAC1) OT3JQD99 SIA7A_HUMAN Decreases Expression [6]
Teneurin-1 (TENM1) OTSKSU4V TEN1_HUMAN Decreases Expression [6]
Transmembrane and coiled-coil domain protein 3 (TMCC3) OTAIQ6V6 TMCC3_HUMAN Decreases Expression [6]
E3 ubiquitin-protein ligase NEURL1B (NEURL1B) OT3BZWO8 NEU1B_HUMAN Affects Expression [7]
Disintegrin and metalloproteinase domain-containing protein 10 (ADAM10) OTOKUXUH ADA10_HUMAN Affects Expression [7]
Integrin beta-1-binding protein 1 (ITGB1BP1) OTVQFNGS ITBP1_HUMAN Affects Expression [7]
Sushi domain-containing protein 5 (SUSD5) OTIMJGDH SUSD5_HUMAN Affects Expression [7]
GDP-mannose 4,6 dehydratase (GMDS) OTWV79YD GMDS_HUMAN Affects Expression [7]
Polycomb protein EED (EED) OTJFHCDF EED_HUMAN Decreases Expression [10]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [11]
Amyloid-beta precursor protein (APP) OTKFD7R4 A4_HUMAN Affects Expression [7]
Prostate-specific antigen (KLK3) OTFGSBFJ KLK3_HUMAN Decreases Expression [11]
Beta-microseminoprotein (MSMB) OTYORAJC MSMB_HUMAN Decreases Expression [12]
Keratin, type I cytoskeletal 19 (KRT19) OTDGDQ75 K1C19_HUMAN Affects Expression [7]
Annexin A4 (ANXA4) OTUCRYXL ANXA4_HUMAN Affects Expression [7]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Decreases Cleavage [11]
G2/mitotic-specific cyclin-B1 (CCNB1) OT19S7E5 CCNB1_HUMAN Decreases Expression [10]
Membrane cofactor protein (CD46) OTQ8NWJD MCP_HUMAN Increases Expression [13]
Aspartate aminotransferase, cytoplasmic (GOT1) OTZLM5UB AATC_HUMAN Affects Expression [7]
Midkine (MDK) OTF24HKC MK_HUMAN Affects Expression [7]
Hepatocyte nuclear factor 1-beta (HNF1B) OTSYIC3T HNF1B_HUMAN Affects Expression [7]
Small ribosomal subunit protein eS19 (RPS19) OTBKGP48 RS19_HUMAN Affects Expression [7]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Decreases Expression [10]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Affects Expression [7]
Neurogenic locus notch homolog protein 1 (NOTCH1) OTI1WADQ NOTC1_HUMAN Affects Expression [7]
Transcription factor SOX-9 (SOX9) OTVDJFGN SOX9_HUMAN Affects Expression [7]
CCAAT/enhancer-binding protein alpha (CEBPA) OTOM9OE4 CEBPA_HUMAN Affects Expression [7]
Presenilin-1 (PSEN1) OTKL39RT PSN1_HUMAN Affects Expression [7]
Presenilin-2 (PSEN2) OTOW778B PSN2_HUMAN Affects Expression [7]
Hepatocyte nuclear factor 3-alpha (FOXA1) OTEBY0TD FOXA1_HUMAN Affects Expression [7]
Ubiquitin-ribosomal protein eS31 fusion protein (RPS27A) OTIIGGZ2 RS27A_HUMAN Affects Expression [7]
Protein jagged-1 (JAG1) OT3LGT6K JAG1_HUMAN Affects Expression [7]
Disintegrin and metalloproteinase domain-containing protein 17 (ADAM17) OTTM6KRB ADA17_HUMAN Affects Expression [7]
Neurogenic locus notch homolog protein 2 (NOTCH2) OTQ3Y9PA NOTC2_HUMAN Affects Expression [7]
Recombining binding protein suppressor of hairless (RBPJ) OTD7CUG0 SUH_HUMAN Affects Expression [7]
Histone acetyltransferase p300 (EP300) OTL8QJDX EP300_HUMAN Affects Expression [7]
Peptidyl-prolyl cis-trans isomerase FKBP5 (FKBP5) OT404F9K FKBP5_HUMAN Decreases Expression [11]
SNW domain-containing protein 1 (SNW1) OTKWG3PS SNW1_HUMAN Affects Expression [7]
Transcription factor HES-1 (HES1) OT8P19W2 HES1_HUMAN Affects Expression [7]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Decreases Expression [10]
Polycomb protein SUZ12 (SUZ12) OT655XF8 SUZ12_HUMAN Decreases Expression [10]
Histone-lysine N-methyltransferase EZH2 (EZH2) OTIEHTKW EZH2_HUMAN Decreases Expression [10]
Probable E3 ubiquitin-protein ligase DTX2 (DTX2) OT7QLDU4 DTX2_HUMAN Affects Expression [7]
E3 ubiquitin-protein ligase MIB1 (MIB1) OT5C404P MIB1_HUMAN Affects Expression [7]
NF-kappa-B-activating protein (NKAP) OT7K7I8Q NKAP_HUMAN Affects Expression [7]
Probable E3 ubiquitin-protein ligase DTX3 (DTX3) OTSUUV9N DTX3_HUMAN Affects Expression [7]
Polypeptide N-acetylgalactosaminyltransferase 11 (GALNT11) OTANT9E6 GLT11_HUMAN Affects Expression [7]
Gamma-secretase subunit APH-1B (APH1B) OTQHPTGC APH1B_HUMAN Affects Expression [7]
Nicastrin (NCSTN) OT5QBTA4 NICA_HUMAN Affects Expression [7]
Mastermind-like protein 1 (MAML1) OTQA4DDN MAML1_HUMAN Affects Expression [7]
CREB-binding protein (CREBBP) OTPA4QGM CBP_HUMAN Affects Expression [7]
Histone acetyltransferase KAT2B (KAT2B) OTWQITWK KAT2B_HUMAN Affects Expression [7]
E3 ubiquitin-protein ligase MIB2 (MIB2) OTJCC3HS MIB2_HUMAN Affects Expression [7]
Gamma-secretase subunit APH-1A (APH1A) OT97F1TU APH1A_HUMAN Affects Expression [7]
p53 apoptosis effector related to PMP-22 (PERP) OTP0YL53 PERP_HUMAN Affects Expression [7]
E3 ubiquitin-protein ligase Itchy homolog (ITCH) OTUOMKF5 ITCH_HUMAN Affects Expression [7]
Mastermind-like protein 3 (MAML3) OTZFV53Z MAML3_HUMAN Affects Expression [7]
Intraflagellar transport protein 74 homolog (IFT74) OTZBFEDD IFT74_HUMAN Affects Expression [7]
RNA-binding protein 15 (RBM15) OT8ZPGWF RBM15_HUMAN Affects Expression [7]
Msx2-interacting protein (SPEN) OT37A2MD MINT_HUMAN Affects Expression [7]
Sphingosine 1-phosphate receptor 3 (S1PR3) OTXBIYO8 S1PR3_HUMAN Affects Expression [7]
GDP-fucose protein O-fucosyltransferase 1 (POFUT1) OTOBJZIT OFUT1_HUMAN Affects Expression [7]
Notchless protein homolog 1 (NLE1) OT1BV82K NLE1_HUMAN Affects Expression [7]
Gamma-secretase subunit PEN-2 (PSENEN) OTJ7M7G9 PEN2_HUMAN Affects Expression [7]
Protein sel-1 homolog 1 (SEL1L) OTC0FB7T SE1L1_HUMAN Affects Expression [7]
Intraflagellar transport protein 172 homolog (IFT172) OT12DW08 IF172_HUMAN Affects Expression [7]
Neurogenic locus notch homolog protein 3 (NOTCH3) OTMVVA7F NOTC3_HUMAN Affects Expression [7]
Protein jagged-2 (JAG2) OTH7KRRF JAG2_HUMAN Affects Expression [7]
E3 ubiquitin-protein ligase DTX4 (DTX4) OTGX30AO DTX4_HUMAN Affects Expression [7]
Epsin-1 (EPN1) OT4Q1NIV EPN1_HUMAN Affects Expression [7]
Signal transducer and activator of transcription 3 (STAT3) OTAAGKYZ STAT3_HUMAN Decreases Response To Substance [14]
Ephrin type-B receptor 4 (EPHB4) OTKLPVXJ EPHB4_HUMAN Affects Response To Substance [11]
Interleukin-6 (IL6) OTUOSCCU IL6_HUMAN Decreases Response To Substance [14]
------------------------------------------------------------------------------------
⏷ Show the Full List of 117 DOT(s)

Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Prostate Cancer DCQKVR2 N. A. Phase 1 [15]
------------------------------------------------------------------------------------

References

1 ClinicalTrials.gov (NCT05726292) A Study of Enzalutamide Plus the Glucocorticoid Receptor Antagonist Relacorilant Versus Placebo for Patients With High-risk Localized Prostate Cancer
2 ClinicalTrials.gov (NCT03697109) A Study of the Efficacy and Safety of Relacorilant in Patients With Endogenous Cushing Syndrome (GRACE). U.S. National Institutes of Health.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
6 LSD1 activates a lethal prostate cancer gene network independently of its demethylase function. Proc Natl Acad Sci U S A. 2018 May 1;115(18):E4179-E4188.
7 NOTCH signaling is activated in and contributes to resistance in enzalutamide-resistant prostate cancer cells. J Biol Chem. 2019 May 24;294(21):8543-8554. doi: 10.1074/jbc.RA118.006983. Epub 2019 Apr 2.
8 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
9 Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies. Nucleic Acids Res. 2015 Jul 13;43(12):5880-97. doi: 10.1093/nar/gkv262. Epub 2015 Apr 23.
10 Dual targeting of EZH2 and androgen receptor as a novel therapy for castration-resistant prostate cancer. Toxicol Appl Pharmacol. 2020 Oct 1;404:115200. doi: 10.1016/j.taap.2020.115200. Epub 2020 Aug 14.
11 Inhibition of the erythropoietin-producing receptor EPHB4 antagonizes androgen receptor overexpression and reduces enzalutamide resistance. J Biol Chem. 2020 Apr 17;295(16):5470-5483. doi: 10.1074/jbc.RA119.011385. Epub 2020 Mar 17.
12 In silico and in vitro assessment of androgen receptor antagonists. Comput Biol Chem. 2021 Jun;92:107490. doi: 10.1016/j.compbiolchem.2021.107490. Epub 2021 Apr 23.
13 Targeting CD46 for both adenocarcinoma and neuroendocrine prostate cancer. JCI Insight. 2018 Sep 6;3(17):e121497. doi: 10.1172/jci.insight.121497. eCollection 2018 Sep 6.
14 Niclosamide suppresses cell migration and invasion in enzalutamide resistant prostate cancer cells via Stat3-AR axis inhibition. Prostate. 2015 Sep;75(13):1341-53. doi: 10.1002/pros.23015. Epub 2015 May 13.
15 ClinicalTrials.gov (NCT03674814) Study of Drug 1 (Enzalutamide) Plus Drug 2 (Relacorilant) for Patients With Prostate Cancer