Details of the Drug Combination

General Information of Drug Combination (ID: DCQJHXB)

Drug Combination Name
Regorafenib Imatinib
Indication
Disease Entry Status REF
Gastrointestinal Stromal Tumour Phase 2 [1]
Component Drugs Regorafenib   DMHSY1I Imatinib   DM7RJXL
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 Regorafenib
Disease Entry ICD 11 Status REF
Gastrointestinal stromal tumour 2B5B Approved [2]
Metastasis from malignant tumor of colon N.A. Approved [2]
Metastatic colorectal cancer 2B91 Approved [3]
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 [4]
Proto-oncogene c-Ret (RET) TT4DXQT RET_HUMAN Modulator [4]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Modulator [4]
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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 [12]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [13]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [14]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [12]
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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 [15]
UDP-glucuronosyltransferase 1A9 (UGT1A9) DE85D2P UD19_HUMAN Metabolism [15]
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Regorafenib Interacts with 6 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [11]
Tumor necrosis factor receptor superfamily member 6 (FAS) OTP9XG86 TNR6_HUMAN Increases Activity [11]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Phosphorylation [11]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Phosphorylation [11]
Tumor necrosis factor ligand superfamily member 6 (FASLG) OTZARCHH TNFL6_HUMAN Increases Activity [11]
Transcription factor p65 (RELA) OTUJP9CN TF65_HUMAN Decreases Expression [11]
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⏷ Show the Full List of 6 DOT(s)
Indication(s) of Imatinib
Disease Entry ICD 11 Status REF
Acute lymphoblastic leukaemia 2A85 Approved [4]
Blast phase chronic myelogenous leukemia, BCR-ABL1 positive N.A. Approved [5]
Choroidal neovascularization 9B76 Approved [5]
Chronic eosinophilic leukemia N.A. Approved [5]
Chronic myelogenous leukaemia 2A20.0 Approved [6]
Chronic myeloid leukaemia 2A20 Approved [7]
Dermatofibrosarcoma protuberans N.A. Approved [5]
Gastrointestinal stromal tumour 2B5B Approved [5]
Leukemia N.A. Approved [5]
Malignant peripheral nerve sheath tumor N.A. Approved [5]
Myeloproliferative neoplasm 2A20 Approved [5]
Pulmonary hypertension BB01 Approved [5]
Coronavirus Disease 2019 (COVID-19) 1D6Y Phase 3 [8]
Intestinal cancer 2C0Z Phase 3 [6]
Lung cancer 2C25.0 Phase 2 [6]
Idiopathic hypereosinophilic syndrome N.A. Investigative [5]
Middle East Respiratory Syndrome (MERS) 1D64 Investigative [9]
Scleroderma 4A42 Investigative [5]
Severe acute respiratory syndrome (SARS) 1D65 Investigative [9]
Systemic mastocytosis 2A21.0 Investigative [10]
Imatinib Interacts with 5 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Mcl-1 messenger RNA (MCL-1 mRNA) TTN6ORK MCL1_HUMAN . [10]
Fusion protein Bcr-Abl (Bcr-Abl) TTS7G69 BCR_HUMAN-ABL1_HUMAN Inhibitor [19]
Platelet-derived growth factor receptor (PDGFR) TTI2WET NOUNIPROTAC Inhibitor [19]
Tyrosine-protein kinase Kit (KIT) TTX41N9 KIT_HUMAN Inhibitor [19]
HUMAN fusion protein Bcr-Abl (Bcr-Abl) TTE63HY BCR_HUMAN/ABL1_HUMAN Inhibitor [9]
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Imatinib Interacts with 6 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [20]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [21]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [22]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [23]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [24]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [22]
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⏷ Show the Full List of 6 DTP(s)
Imatinib Interacts with 8 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [25]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Metabolism [26]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Metabolism [27]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [28]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Metabolism [29]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [30]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Metabolism [31]
Prostaglandin G/H synthase 1 (COX-1) DE073H6 PGH1_HUMAN Metabolism [27]
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⏷ Show the Full List of 8 DME(s)
Imatinib Interacts with 48 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) OTW8V2V1 ABCG2_HUMAN Increases Expression [32]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Increases Expression [32]
Aldehyde dehydrogenase, mitochondrial (ALDH2) OTKJ9I3N ALDH2_HUMAN Decreases Expression [33]
Eukaryotic translation initiation factor 4E (EIF4E) OTDAWNLA IF4E_HUMAN Decreases Expression [33]
Fructose-bisphosphate aldolase C (ALDOC) OTEC13I5 ALDOC_HUMAN Decreases Expression [33]
Pyruvate dehydrogenase E1 component subunit beta, mitochondrial (PDHB) OT2NHE5E ODPB_HUMAN Decreases Expression [33]
Eukaryotic translation initiation factor 4B (EIF4B) OTE8TXA8 IF4B_HUMAN Decreases Expression [33]
Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) OT5BZ1J9 P85A_HUMAN Decreases Expression [33]
G1/S-specific cyclin-D3 (CCND3) OTNKPQ22 CCND3_HUMAN Decreases Expression [33]
Hexokinase-4 (GCK) OTR3Q0NN HXK4_HUMAN Decreases Expression [33]
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform (PPP2CA) OT83PT85 PP2AA_HUMAN Increases Expression [33]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [34]
Tumor necrosis factor receptor superfamily member 10B (TNFRSF10B) OTA1CPBV TR10B_HUMAN Increases Expression [35]
Autophagy-related protein 13 (ATG13) OTYMHNEJ ATG13_HUMAN Increases Phosphorylation [16]
Keratin, type I cytoskeletal 14 (KRT14) OTUVZ1DW K1C14_HUMAN Increases Expression [36]
Heat shock protein beta-1 (HSPB1) OTHFZ8ED HSPB1_HUMAN Increases Expression [35]
Tyrosine-protein kinase Lck (LCK) OT883FG9 LCK_HUMAN Decreases Phosphorylation [37]
ATP-dependent 6-phosphofructokinase, muscle type (PFKM) OT1QY9JM PFKAM_HUMAN Decreases Expression [38]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [39]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Increases Expression [35]
Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1) OTA675TJ GTR1_HUMAN Decreases Expression [40]
Keratin, type II cytoskeletal 5 (KRT5) OTVGI9HT K2C5_HUMAN Increases Expression [36]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [41]
Transcription factor EB (TFEB) OTJUJJQY TFEB_HUMAN Affects Localization [16]
Insulin-like growth factor-binding protein 4 (IGFBP4) OT2HZRBD IBP4_HUMAN Increases Expression [35]
Interleukin-4 receptor subunit alpha (IL4R) OTTXOTCW IL4RA_HUMAN Increases Expression [35]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Phosphorylation [37]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Phosphorylation [37]
Catenin beta-1 (CTNNB1) OTZ932A3 CTNB1_HUMAN Decreases Expression [42]
Crk-like protein (CRKL) OTOYSD1R CRKL_HUMAN Decreases Phosphorylation [43]
Small ribosomal subunit protein eS6 (RPS6) OTT4D1LN RS6_HUMAN Decreases Phosphorylation [16]
Heat shock factor protein 1 (HSF1) OTYNJ4KP HSF1_HUMAN Increases Expression [35]
Transcription factor p65 (RELA) OTUJP9CN TF65_HUMAN Decreases Expression [42]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Expression [44]
Nuclear receptor subfamily 0 group B member 2 (NR0B2) OT7UVICX NR0B2_HUMAN Increases Expression [45]
NGFI-A-binding protein 2 (NAB2) OTG4BDF3 NAB2_HUMAN Increases Expression [35]
TRAF family member-associated NF-kappa-B activator (TANK) OTZSGFIK TANK_HUMAN Increases Expression [35]
NACHT, LRR and PYD domains-containing protein 3 (NLRP3) OTZM6MHU NLRP3_HUMAN Increases Expression [46]
Bile acid receptor (NR1H4) OTWZLPTB NR1H4_HUMAN Increases Activity [45]
Docking protein 1 (DOK1) OTGVRLW6 DOK1_HUMAN Decreases Phosphorylation [47]
Microtubule-associated proteins 1A/1B light chain 3B (MAP1LC3B) OTUYHB84 MLP3B_HUMAN Increases Expression [16]
Transcription factor SOX-17 (SOX17) OT9H4WWE SOX17_HUMAN Decreases Localization [48]
V-type proton ATPase subunit H (ATP6V1H) OTX17GQ9 VATH_HUMAN Increases Expression [16]
LYR motif-containing protein 9 (LYRM9) OT1MILTK LYRM9_HUMAN Affects Response To Substance [49]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Response To Substance [50]
Bcl-2-like protein 11 (BCL2L11) OTNQQWFJ B2L11_HUMAN Increases Response To Substance [51]
Tyrosine-protein kinase Lyn (LYN) OTP686K2 LYN_HUMAN Decreases Response To Substance [43]
Serine/threonine-protein kinase PLK1 (PLK1) OTRZX45T PLK1_HUMAN Increases Response To Substance [39]
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⏷ Show the Full List of 48 DOT(s)

References

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2 Regorafenib 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: 5891).
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