General Information of Drug Combination (ID: DCHWZY8)

Drug Combination Name
Omeprazole Regorafenib
Indication
Disease Entry Status REF
Neoplasms Phase 1 [1]
Component Drugs Omeprazole   DM471KJ Regorafenib   DMHSY1I
Small molecular drug 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 Omeprazole
Disease Entry ICD 11 Status REF
Cystic fibrosis CA25 Approved [2]
Gastric ulcer DA60 Approved [2]
Gastrinoma 2C10.1 Approved [2]
Gastroesophageal reflux disease DA22.Z Approved [3]
Laryngeal disorder N.A. Approved [2]
Nausea MD90 Approved [2]
Peptic esophagitis N.A. Approved [2]
Peptic ulcer DA61 Approved [2]
Congenital laryngomalacia N.A. Investigative [2]
Omeprazole Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Gastric H(+)/K(+) ATPase (Proton pump) TTLOKXP ATP4A_HUMAN; ATP4B_HUMAN Modulator [7]
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Omeprazole Interacts with 1 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [8]
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Omeprazole Interacts with 6 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [9]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [10]
Cytochrome P450 2C18 (CYP2C18) DEZMWRE CP2CI_HUMAN Metabolism [11]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [11]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Metabolism [12]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Metabolism [9]
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⏷ Show the Full List of 6 DME(s)
Omeprazole Interacts with 34 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Increases Expression [13]
Cytochrome P450 3A5 (CYP3A5) OTSXFBXB CP3A5_HUMAN Increases Expression [6]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Increases Expression [14]
Alcohol dehydrogenase 1C (ADH1C) OTO1DV7F ADH1G_HUMAN Decreases Expression [15]
Cytochrome P450 1A2 (CYP1A2) OTLLBX48 CP1A2_HUMAN Increases Expression [15]
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_HUMAN Decreases Expression [15]
Aldehyde dehydrogenase, dimeric NADP-preferring (ALDH3A1) OTAYZZE6 AL3A1_HUMAN Increases Expression [15]
Retinaldehyde dehydrogenase 3 (ALDH1A3) OT1C9NKQ AL1A3_HUMAN Increases Expression [15]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Increases Expression [15]
Cytochrome P450 2B6 (CYP2B6) OTOYO4S7 CP2B6_HUMAN Increases Expression [16]
Cytochrome P450 3A7 (CYP3A7) OTTCDHHM CP3A7_HUMAN Increases Expression [6]
Solute carrier organic anion transporter family member 1A2 (SLCO1A2) OTO70C5O SO1A2_HUMAN Increases Expression [6]
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) OTW8V2V1 ABCG2_HUMAN Increases Expression [17]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [18]
Aryl hydrocarbon receptor nuclear translocator (ARNT) OTMSIEZY ARNT_HUMAN Affects Localization [19]
Aryl hydrocarbon receptor (AHR) OTFE4EYE AHR_HUMAN Decreases Expression [19]
C-X-C chemokine receptor type 4 (CXCR4) OTUFSBX2 CXCR4_HUMAN Decreases Expression [19]
Transmembrane protease serine 2 (TMPRSS2) OTN44YQ5 TMPS2_HUMAN Increases Expression [20]
Nuclear receptor subfamily 1 group I member 2 (NR1I2) OTC5U0N5 NR1I2_HUMAN Increases Activity [21]
Phospholipid-transporting ATPase ABCA1 (ABCA1) OT94G6BQ ABCA1_HUMAN Increases Expression [22]
Prolactin (PRL) OTWFQGX7 PRL_HUMAN Increases Expression [23]
HLA class I histocompatibility antigen, B alpha chain (HLA-B) OTNXFWY2 HLAB_HUMAN Affects Expression [24]
Cathepsin B (CTSB) OTP9G5QB CATB_HUMAN Decreases Activity [25]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Increases Expression [26]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [27]
HLA class I histocompatibility antigen, alpha chain G (HLA-G) OTMLK1KN HLAG_HUMAN Affects Expression [24]
DNA damage-inducible transcript 3 protein (DDIT3) OTI8YKKE DDIT3_HUMAN Increases Expression [28]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Increases Expression [28]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Increases Activity [29]
Cytosolic phospholipase A2 (PLA2G4A) OTE70SOT PA24A_HUMAN Increases Phosphorylation [30]
Hepcidin (HAMP) OT607RBL HEPC_HUMAN Increases Expression [31]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Increases Cleavage [29]
Angiotensin-converting enzyme 2 (ACE2) OTTRZGU7 ACE2_HUMAN Decreases Expression [20]
Potassium-transporting ATPase alpha chain 2 (ATP12A) OTSQSKEK AT12A_HUMAN Increases ADR [32]
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⏷ Show the Full List of 34 DOT(s)
Indication(s) of Regorafenib
Disease Entry ICD 11 Status REF
Gastrointestinal stromal tumour 2B5B Approved [4]
Metastasis from malignant tumor of colon N.A. Approved [4]
Metastatic colorectal cancer 2B91 Approved [5]
Regorafenib Interacts with 3 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Tyrosine-protein kinase Kit (KIT) TTX41N9 KIT_HUMAN Modulator [34]
Proto-oncogene c-Ret (RET) TT4DXQT RET_HUMAN Modulator [34]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Modulator [34]
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Regorafenib Interacts with 4 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [35]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [36]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [37]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [35]
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Regorafenib Interacts with 2 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [38]
UDP-glucuronosyltransferase 1A9 (UGT1A9) DE85D2P UD19_HUMAN Metabolism [38]
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Regorafenib Interacts with 11 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [33]
Matrix metalloproteinase-9 (MMP9) OTB2QDAV MMP9_HUMAN Decreases Expression [33]
Alanine aminotransferase 1 (GPT) OTOXOA0Q ALAT1_HUMAN Increases Secretion [39]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Decreases Expression [33]
Tumor necrosis factor receptor superfamily member 6 (FAS) OTP9XG86 TNR6_HUMAN Increases Activity [33]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Phosphorylation [33]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Phosphorylation [33]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Increases Activity [33]
Tumor necrosis factor ligand superfamily member 6 (FASLG) OTZARCHH TNFL6_HUMAN Increases Activity [33]
Transcription factor p65 (RELA) OTUJP9CN TF65_HUMAN Decreases Expression [33]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Increases Activity [33]
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⏷ Show the Full List of 11 DOT(s)

References

1 ClinicalTrials.gov (NCT01287598) BAY73-4506 Probe Substrate Study
2 Omeprazole FDA Label
3 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4279).
4 Regorafenib FDA Label
5 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5891).
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25 Proton pump inhibitors interfere with the anti-tumor potency of RC48ADC. Toxicol In Vitro. 2022 Mar;79:105292. doi: 10.1016/j.tiv.2021.105292. Epub 2021 Dec 3.
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33 Regorefenib induces extrinsic/intrinsic apoptosis and inhibits MAPK/NF-B-modulated tumor progression in bladder cancer in vitro and in vivo. Environ Toxicol. 2019 Jun;34(6):679-688. doi: 10.1002/tox.22734. Epub 2019 Feb 25.
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