General Information of Drug Combination (ID: DC6IWKC)

Drug Combination Name
Napabucasin Imatinib
Indication
Disease Entry Status REF
Hematologic Malignancy Phase 1 [1]
Component Drugs Napabucasin   DMDZ6Q3 Imatinib   DM7RJXL
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 Napabucasin
Disease Entry ICD 11 Status REF
Colorectal cancer 2B91.Z Phase 3 [2]
Pancreatic cancer 2C10 Phase 3 [2]
Solid tumour/cancer 2A00-2F9Z Phase 3 [3]
Advanced malignancy 2A00-2F9Z Phase 1/2 [2]
Gastrointestinal cancer 2C11 Phase 1/2 [2]
Hepatocellular carcinoma 2C12.02 Phase 1/2 [2]
Recurrent glioblastoma 2A00.00 Phase 1/2 [4]
Recurring respiratory infection CA07-CA45 Phase 1/2 [2]
Haematological malignancy 2B33.Y Phase 1 [2]
Napabucasin Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Signal transducer and activator of transcription 3 (STAT3) TTH8FZW STAT3_HUMAN Inhibitor [2]
------------------------------------------------------------------------------------
Napabucasin Interacts with 59 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Serine/threonine-protein kinase Chk1 (CHEK1) OTTTI622 CHK1_HUMAN Decreases Expression [12]
Inhibitor of nuclear factor kappa-B kinase subunit beta (IKBKB) OT9RDS3H IKKB_HUMAN Decreases Expression [12]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Expression [13]
Krueppel-like factor 4 (KLF4) OT4O9RQW KLF4_HUMAN Decreases Expression [13]
Tyrosine-protein kinase JAK2 (JAK2) OTBIDOOR JAK2_HUMAN Decreases Expression [12]
Serine/threonine-protein kinase LATS1 (LATS1) OTOOCG4R LATS1_HUMAN Decreases Expression [12]
Aldehyde dehydrogenase 1A1 (ALDH1A1) OTCUWZKB AL1A1_HUMAN Decreases Expression [12]
Hypoxanthine-guanine phosphoribosyltransferase (HPRT1) OTOEEEXG HPRT_HUMAN Decreases Expression [12]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [12]
Pro-epidermal growth factor (EGF) OTANRJ0L EGF_HUMAN Decreases Expression [12]
Receptor tyrosine-protein kinase erbB-2 (ERBB2) OTOAUNCK ERBB2_HUMAN Decreases Expression [12]
Large ribosomal subunit protein uL10 (RPLP0) OT3XKD6Y RLA0_HUMAN Decreases Expression [12]
Integrin beta-1 (ITGB1) OT6G1IAR ITB1_HUMAN Decreases Expression [12]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Decreases Expression [12]
Integrin alpha-4 (ITGA4) OTSCAL0V ITA4_HUMAN Decreases Expression [12]
Electron transfer flavoprotein subunit alpha, mitochondrial (ETFA) OTXX61VZ ETFA_HUMAN Decreases Expression [12]
Mucin-1 (MUC1) OTHQI7IY MUC1_HUMAN Decreases Expression [12]
CD44 antigen (CD44) OT9TTJ41 CD44_HUMAN Decreases Expression [12]
Platelet endothelial cell adhesion molecule (PECAM1) OTXOM4D9 PECA1_HUMAN Decreases Expression [12]
Epithelial cell adhesion molecule (EPCAM) OTHBZK5X EPCAM_HUMAN Decreases Expression [12]
Integrin alpha-2 (ITGA2) OTPFL017 ITA2_HUMAN Decreases Expression [12]
Endoglin (ENG) OTL2LSMI EGLN_HUMAN Decreases Expression [12]
Nuclear factor NF-kappa-B p105 subunit (NFKB1) OTNRRD8I NFKB1_HUMAN Decreases Expression [12]
Kit ligand (KITLG) OTB9AVQ4 SCF_HUMAN Decreases Expression [12]
Fibroblast growth factor receptor 2 (FGFR2) OTLOPACK FGFR2_HUMAN Decreases Expression [12]
Integrin alpha-6 (ITGA6) OT3FA39C ITA6_HUMAN Decreases Expression [12]
Signal transducer CD24 (CD24) OT7CODJ4 CD24_HUMAN Decreases Expression [12]
DNA cytosine-5)-methyltransferase 1 (DNMT1) OTM2DGTK DNMT1_HUMAN Decreases Expression [12]
Hematopoietic progenitor cell antigen CD34 (CD34) OT1MOFLZ CD34_HUMAN Decreases Expression [12]
Tyrosine-protein kinase receptor UFO (AXL) OTKA2SUX UFO_HUMAN Decreases Expression [12]
Catenin beta-1 (CTNNB1) OTZ932A3 CTNB1_HUMAN Decreases Expression [12]
Polycomb complex protein BMI-1 (BMI1) OTROVLJ0 BMI1_HUMAN Decreases Expression [12]
TGF-beta receptor type-1 (TGFBR1) OT40S1SJ TGFR1_HUMAN Decreases Expression [12]
DNA-binding protein inhibitor ID-1 (ID1) OTKGNZN5 ID1_HUMAN Decreases Expression [12]
Neurogenic locus notch homolog protein 1 (NOTCH1) OTI1WADQ NOTC1_HUMAN Decreases Expression [12]
Transcription factor SOX-2 (SOX2) OTFAWCAU SOX2_HUMAN Decreases Expression [12]
Glycogen synthase kinase-3 beta (GSK3B) OTL3L14B GSK3B_HUMAN Decreases Expression [12]
Ataxin-1 (ATXN1) OTQF0HNR ATX1_HUMAN Decreases Expression [12]
Actin, cytoplasmic 1 (ACTB) OT1MCP2F ACTB_HUMAN Decreases Expression [12]
Beta-2-microglobulin (B2M) OTDWN6NX B2MG_HUMAN Decreases Expression [12]
Protein jagged-1 (JAG1) OT3LGT6K JAG1_HUMAN Decreases Expression [12]
POU domain, class 5, transcription factor 1 (POU5F1) OTDHHN7O PO5F1_HUMAN Decreases Expression [12]
Urokinase plasminogen activator surface receptor (PLAUR) OTIRKKEQ UPAR_HUMAN Decreases Expression [12]
Neurogenic locus notch homolog protein 2 (NOTCH2) OTQ3Y9PA NOTC2_HUMAN Decreases Expression [12]
Epithelial discoidin domain-containing receptor 1 (DDR1) OTYW1SH8 DDR1_HUMAN Decreases Expression [12]
Tyrosine-protein kinase Mer (MERTK) OTWBRAJ6 MERTK_HUMAN Decreases Expression [12]
Serine-protein kinase ATM (ATM) OTQVOHLT ATM_HUMAN Decreases Expression [12]
Histone deacetylase 1 (HDAC1) OTQDNOXZ HDAC1_HUMAN Decreases Expression [12]
CD166 antigen (ALCAM) OTCO4LP7 CD166_HUMAN Decreases Expression [12]
Flotillin-2 (FLOT2) OTZ0QR5L FLOT2_HUMAN Decreases Expression [12]
Tafazzin (TAFAZZIN) OTDR57KI TAZ_HUMAN Decreases Expression [12]
Krueppel-like factor 17 (KLF17) OT5NWVP7 KLF17_HUMAN Decreases Expression [12]
Mastermind-like protein 1 (MAML1) OTQA4DDN MAML1_HUMAN Decreases Expression [12]
NAD-dependent protein deacetylase sirtuin-1 (SIRT1) OTAYZMOY SIR1_HUMAN Decreases Expression [12]
Protein smoothened (SMO) OTXXE208 SMO_HUMAN Decreases Expression [12]
Forkhead box protein P1 (FOXP1) OTSG6XGF FOXP1_HUMAN Decreases Expression [12]
Homeobox protein NANOG (NANOG) OTUEY1FM NANOG_HUMAN Decreases Expression [12]
Protein lin-28 homolog A (LIN28A) OTJJBRCQ LN28A_HUMAN Decreases Expression [12]
Dachshund homolog 1 (DACH1) OTMKNAGG DACH1_HUMAN Decreases Expression [12]
------------------------------------------------------------------------------------
⏷ Show the Full List of 59 DOT(s)
Indication(s) of Imatinib
Disease Entry ICD 11 Status REF
Acute lymphoblastic leukaemia 2A85 Approved [5]
Blast phase chronic myelogenous leukemia, BCR-ABL1 positive N.A. Approved [6]
Choroidal neovascularization 9B76 Approved [6]
Chronic eosinophilic leukemia N.A. Approved [6]
Chronic myelogenous leukaemia 2A20.0 Approved [7]
Chronic myeloid leukaemia 2A20 Approved [8]
Dermatofibrosarcoma protuberans N.A. Approved [6]
Gastrointestinal stromal tumour 2B5B Approved [6]
Leukemia N.A. Approved [6]
Malignant peripheral nerve sheath tumor N.A. Approved [6]
Myeloproliferative neoplasm 2A20 Approved [6]
Pulmonary hypertension BB01 Approved [6]
Coronavirus Disease 2019 (COVID-19) 1D6Y Phase 3 [9]
Intestinal cancer 2C0Z Phase 3 [7]
Lung cancer 2C25.0 Phase 2 [7]
Idiopathic hypereosinophilic syndrome N.A. Investigative [6]
Middle East Respiratory Syndrome (MERS) 1D64 Investigative [10]
Scleroderma 4A42 Investigative [6]
Severe acute respiratory syndrome (SARS) 1D65 Investigative [10]
Systemic mastocytosis 2A21.0 Investigative [11]
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 . [11]
Fusion protein Bcr-Abl (Bcr-Abl) TTS7G69 BCR_HUMAN-ABL1_HUMAN Inhibitor [17]
Platelet-derived growth factor receptor (PDGFR) TTI2WET NOUNIPROTAC Inhibitor [17]
Tyrosine-protein kinase Kit (KIT) TTX41N9 KIT_HUMAN Inhibitor [17]
HUMAN fusion protein Bcr-Abl (Bcr-Abl) TTE63HY BCR_HUMAN/ABL1_HUMAN Inhibitor [10]
------------------------------------------------------------------------------------
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 [18]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [19]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [20]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [21]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [22]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [20]
------------------------------------------------------------------------------------
⏷ 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 [23]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Metabolism [24]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Metabolism [25]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [26]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Metabolism [27]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [28]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Metabolism [29]
Prostaglandin G/H synthase 1 (COX-1) DE073H6 PGH1_HUMAN Metabolism [25]
------------------------------------------------------------------------------------
⏷ Show the Full List of 8 DME(s)
Imatinib Interacts with 95 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Decreases Methylation [30]
Cytochrome P450 3A5 (CYP3A5) OTSXFBXB CP3A5_HUMAN Decreases Methylation [30]
Cytochrome P450 3A7 (CYP3A7) OTTCDHHM CP3A7_HUMAN Decreases Methylation [30]
Cytochrome P450 2C8 (CYP2C8) OTHCWT42 CP2C8_HUMAN Decreases Methylation [30]
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) OTW8V2V1 ABCG2_HUMAN Increases Expression [31]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Increases Expression [31]
Aldehyde dehydrogenase, mitochondrial (ALDH2) OTKJ9I3N ALDH2_HUMAN Decreases Expression [32]
Eukaryotic translation initiation factor 4E (EIF4E) OTDAWNLA IF4E_HUMAN Decreases Expression [32]
Fructose-bisphosphate aldolase C (ALDOC) OTEC13I5 ALDOC_HUMAN Decreases Expression [32]
Pyruvate dehydrogenase E1 component subunit beta, mitochondrial (PDHB) OT2NHE5E ODPB_HUMAN Decreases Expression [32]
Cyclin-dependent kinase 4 (CDK4) OT7EP05T CDK4_HUMAN Decreases Expression [32]
Cyclin-A2 (CCNA2) OTPHHYZJ CCNA2_HUMAN Decreases Expression [32]
Ribosomal protein S6 kinase beta-1 (RPS6KB1) OTAELNGX KS6B1_HUMAN Decreases Expression [32]
Eukaryotic translation initiation factor 4B (EIF4B) OTE8TXA8 IF4B_HUMAN Decreases Expression [32]
Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) OT5BZ1J9 P85A_HUMAN Decreases Expression [32]
G1/S-specific cyclin-D3 (CCND3) OTNKPQ22 CCND3_HUMAN Decreases Expression [32]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Decreases Expression [32]
Hexokinase-4 (GCK) OTR3Q0NN HXK4_HUMAN Decreases Expression [32]
Serine/threonine-protein kinase mTOR (MTOR) OTHH8KU7 MTOR_HUMAN Decreases Expression [32]
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform (PPP2CA) OT83PT85 PP2AA_HUMAN Increases Expression [32]
Eukaryotic translation initiation factor 4E-binding protein 1 (EIF4EBP1) OTHBQVD5 4EBP1_HUMAN Decreases Expression [32]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [33]
Prostaglandin G/H synthase 2 (PTGS2) OT75U9M4 PGH2_HUMAN Decreases Expression [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 [14]
Platelet-derived growth factor subunit B (PDGFB) OTMFMFC3 PDGFB_HUMAN Decreases Expression [36]
Interferon gamma (IFNG) OTXG9JM7 IFNG_HUMAN Increases Expression [37]
Interleukin-1 beta (IL1B) OT0DWXXB IL1B_HUMAN Increases Secretion [38]
Keratin, type I cytoskeletal 14 (KRT14) OTUVZ1DW K1C14_HUMAN Increases Expression [39]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Increases Expression [40]
Heat shock protein beta-1 (HSPB1) OTHFZ8ED HSPB1_HUMAN Increases Expression [35]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Decreases Activity [41]
Intercellular adhesion molecule 1 (ICAM1) OTTOIX77 ICAM1_HUMAN Increases Expression [35]
Tyrosine-protein kinase Lck (LCK) OT883FG9 LCK_HUMAN Decreases Phosphorylation [42]
Cyclin-dependent kinase 1 (CDK1) OTW1SC2N CDK1_HUMAN Decreases Expression [37]
Cathepsin B (CTSB) OTP9G5QB CATB_HUMAN Increases Expression [14]
Proto-oncogene tyrosine-protein kinase receptor Ret (RET) OTLU040A RET_HUMAN Decreases Phosphorylation [43]
ATP-dependent 6-phosphofructokinase, muscle type (PFKM) OT1QY9JM PFKAM_HUMAN Decreases Expression [44]
Platelet-derived growth factor receptor beta (PDGFRB) OTYSNK9Q PGFRB_HUMAN Decreases Expression [36]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [45]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Increases Expression [35]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Decreases Expression [46]
Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1) OTA675TJ GTR1_HUMAN Decreases Expression [40]
Breakpoint cluster region protein (BCR) OTCN76C1 BCR_HUMAN Decreases Activity [16]
Lysosome-associated membrane glycoprotein 1 (LAMP1) OTYE92QY LAMP1_HUMAN Increases Expression [14]
Ornithine decarboxylase (ODC1) OTNDAGRR DCOR_HUMAN Increases Expression [35]
Keratin, type II cytoskeletal 5 (KRT5) OTVGI9HT K2C5_HUMAN Increases Expression [39]
Tissue factor (F3) OT3MSU3B TF_HUMAN Increases Expression [47]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [48]
Platelet-derived growth factor receptor alpha (PDGFRA) OTDJXUCN PGFRA_HUMAN Decreases Expression [36]
CCAAT/enhancer-binding protein beta (CEBPB) OTM9MQIA CEBPB_HUMAN Increases Expression [35]
Histidine decarboxylase (HDC) OT4WA5YQ DCHS_HUMAN Decreases Expression [49]
Transcription factor EB (TFEB) OTJUJJQY TFEB_HUMAN Affects Localization [14]
Fibroblast growth factor receptor 3 (FGFR3) OTSAXDIL FGFR3_HUMAN Decreases Expression [50]
Insulin-like growth factor-binding protein 4 (IGFBP4) OT2HZRBD IBP4_HUMAN Increases Expression [35]
Alanine aminotransferase 1 (GPT) OTOXOA0Q ALAT1_HUMAN Increases Secretion [51]
Interleukin-4 receptor subunit alpha (IL4R) OTTXOTCW IL4RA_HUMAN Increases Expression [35]
Cyclin-dependent kinase 2 (CDK2) OTB5DYYZ CDK2_HUMAN Decreases Expression [37]
NF-kappa-B inhibitor alpha (NFKBIA) OTFT924M IKBA_HUMAN Increases Phosphorylation [35]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Phosphorylation [42]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Phosphorylation [42]
Caspase-1 (CASP1) OTZ3YQFU CASP1_HUMAN Increases Cleavage [38]
Catenin beta-1 (CTNNB1) OTZ932A3 CTNB1_HUMAN Decreases Expression [52]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Increases Activity [53]
Crk-like protein (CRKL) OTOYSD1R CRKL_HUMAN Decreases Phosphorylation [54]
Glycogen synthase kinase-3 beta (GSK3B) OTL3L14B GSK3B_HUMAN Increases Phosphorylation [14]
Hexokinase-2 (HK2) OTC0GCQO HXK2_HUMAN Decreases Expression [44]
Small ribosomal subunit protein eS6 (RPS6) OTT4D1LN RS6_HUMAN Decreases Phosphorylation [14]
Heat shock factor protein 1 (HSF1) OTYNJ4KP HSF1_HUMAN Increases Expression [35]
Transcription factor p65 (RELA) OTUJP9CN TF65_HUMAN Decreases Expression [52]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [46]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Expression [55]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) OT2YYI1A MCL1_HUMAN Decreases Expression [45]
Forkhead box protein M1 (FOXM1) OT5887KR FOXM1_HUMAN Decreases Expression [52]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Decreases Activity [56]
Sequestosome-1 (SQSTM1) OTGY5D5J SQSTM_HUMAN Increases Expression [14]
Beclin-1 (BECN1) OT4X293M BECN1_HUMAN Increases Expression [14]
Nuclear receptor subfamily 0 group B member 2 (NR0B2) OT7UVICX NR0B2_HUMAN Increases Expression [57]
NGFI-A-binding protein 2 (NAB2) OTG4BDF3 NAB2_HUMAN Increases Expression [35]
Nuclear factor erythroid 2-related factor 2 (NFE2L2) OT0HENJ5 NF2L2_HUMAN Decreases Expression [58]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Decreases Activity [41]
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 [38]
Bile acid receptor (NR1H4) OTWZLPTB NR1H4_HUMAN Increases Activity [57]
Docking protein 1 (DOK1) OTGVRLW6 DOK1_HUMAN Decreases Phosphorylation [59]
Microtubule-associated proteins 1A/1B light chain 3B (MAP1LC3B) OTUYHB84 MLP3B_HUMAN Increases Expression [14]
Transcription factor SOX-17 (SOX17) OT9H4WWE SOX17_HUMAN Decreases Localization [60]
V-type proton ATPase subunit H (ATP6V1H) OTX17GQ9 VATH_HUMAN Increases Expression [14]
Tyrosine-protein kinase ABL1 (ABL1) OT09YVXH ABL1_HUMAN Increases Response To Substance [61]
LYR motif-containing protein 9 (LYRM9) OT1MILTK LYRM9_HUMAN Affects Response To Substance [62]
Leptin (LEP) OT5Q7ODW LEP_HUMAN Increases ADR [63]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Response To Substance [64]
Bcl-2-like protein 11 (BCL2L11) OTNQQWFJ B2L11_HUMAN Increases Response To Substance [65]
Tyrosine-protein kinase Lyn (LYN) OTP686K2 LYN_HUMAN Decreases Response To Substance [54]
Serine/threonine-protein kinase PLK1 (PLK1) OTRZX45T PLK1_HUMAN Increases Response To Substance [45]
------------------------------------------------------------------------------------
⏷ Show the Full List of 95 DOT(s)

References

1 ClinicalTrials.gov (NCT02352558) A Study of BBI608 in Adult Patients With Advanced, Refractory Hematologic Malignancies
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 First-in-Class Cancer Stemness Inhibitor Shows Promising Results in Advanced Colorectal Cancer. 2016 ASCO GI Conference. January 26, 2016.
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
6 Imatinib FDA Label
7 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: 5687).
8 FDA Approved Drug Products from FDA Official Website. 2019. Application Number: (ANDA) 078340.
9 ClinicalTrials.gov (NCT04356495) Treatments to Decrease the Risk of Hospitalization or Death in Elderly Outpatients With Symptomatic SARS-CoV-2 Infection (COVID-19). U.S. National Institutes of Health.
10 Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47.
11 Design and development of antisense drugs. Expert Opin. Drug Discov. 2008 3(10):1189-1207.
12 Suppression of cancer relapse and metastasis by inhibiting cancer stemness. Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44. doi: 10.1073/pnas.1424171112. Epub 2015 Jan 20.
13 Suppression of prostate cancer progression by cancer cell stemness inhibitor napabucasin. Cancer Med. 2016 Jun;5(6):1251-8. doi: 10.1002/cam4.675. Epub 2016 Feb 21.
14 Imatinib disturbs lysosomal function and morphology and impairs the activity of mTORC1 in human hepatocyte cell lines. Food Chem Toxicol. 2022 Apr;162:112869. doi: 10.1016/j.fct.2022.112869. Epub 2022 Feb 16.
15 Insulin-like growth factor I receptor pathway inhibition by ADW742, alone or in combination with imatinib, doxorubicin, or vincristine, is a novel therapeutic approach in Ewing tumor. Clin Cancer Res. 2006 Jun 1;12(11 Pt 1):3532-40. doi: 10.1158/1078-0432.CCR-05-1778.
16 Sensitivity to imatinib therapy may be predicted by testing Wilms tumor gene expression and colony growth after a short in vitro incubation. Cancer. 2004 Sep 1;101(5):979-88. doi: 10.1002/cncr.20457.
17 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
18 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
19 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
20 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
21 Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia. Leuk Lymphoma. 2008 Apr;49(4):639-42.
22 Environmental and genetic factors affecting transport of imatinib by OATP1A2. Clin Pharmacol Ther. 2011 Jun;89(6):816-20.
23 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
24 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
25 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
26 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
27 Drug Interactions Flockhart Table
28 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
29 Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
30 Participation of CYP2C8 and CYP3A4 in the N-demethylation of imatinib in human hepatic microsomes. Br J Pharmacol. 2010 Nov;161(5):1059-69. doi: 10.1111/j.1476-5381.2010.00946.x.
31 Chronic imatinib mesylate exposure leads to reduced intracellular drug accumulation by induction of the ABCG2 (BCRP) and ABCB1 (MDR1) drug transport pumps. Cancer Biol Ther. 2005 Jul;4(7):747-52.
32 A systems biology understanding of the synergistic effects of arsenic sulfide and Imatinib in BCR/ABL-associated leukemia. Proc Natl Acad Sci U S A. 2009 Mar 3;106(9):3378-83.
33 Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. Toxicol Sci. 2010 Dec; 118(2):485-500.
34 Anti-leukemic effects of gallic acid on human leukemia K562 cells: downregulation of COX-2, inhibition of BCR/ABL kinase and NF-B inactivation. Toxicol In Vitro. 2012 Apr;26(3):396-405.
35 Effects of Imatinib Mesylate (Gleevec) on human islet NF-kappaB activation and chemokine production in vitro. PLoS One. 2011;6(9):e24831. doi: 10.1371/journal.pone.0024831. Epub 2011 Sep 14.
36 Chemosensitization by STI571 targeting the platelet-derived growth factor/platelet-derived growth factor receptor-signaling pathway in the tumor progression and angiogenesis of gastric carcinoma. Cancer. 2005 May 1;103(9):1800-9. doi: 10.1002/cncr.20973.
37 Imatinib mesylate, a new kid on the block for the treatment of anti-neutrophil cytoplasmic autoantibodies-associated vasculitis?. Clin Exp Immunol. 2008 Mar;151(3):391-8. doi: 10.1111/j.1365-2249.2007.03572.x. Epub 2008 Jan 10.
38 Imatinib-induced hepatotoxicity via oxidative stress and activation of NLRP3 inflammasome: an in vitro and in vivo study. Arch Toxicol. 2022 Apr;96(4):1075-1087. doi: 10.1007/s00204-022-03245-x. Epub 2022 Feb 22.
39 Oral lichenoid eruption secondary to imatinib (Glivec). J Dermatolog Treat. 2004 Jul;15(4):253-5. doi: 10.1080/09546630410015556.
40 AMP-activated protein kinase activation primes cytoplasmic translocation and autophagic degradation of the BCR-ABL protein in CML cells. Cancer Sci. 2021 Jan;112(1):194-204. doi: 10.1111/cas.14698. Epub 2020 Nov 16.
41 Association of CYP1A1 and CYP1B1 inhibition in in vitro assays with drug-induced liver injury. J Toxicol Sci. 2021;46(4):167-176. doi: 10.2131/jts.46.167.
42 Imatinib mesylate inhibits T-cell proliferation in vitro and delayed-type hypersensitivity in vivo. Blood. 2004 Aug 15;104(4):1094-9. doi: 10.1182/blood-2003-12-4266. Epub 2004 Apr 20.
43 Dual inhibition of RET and FGFR4 restrains medullary thyroid cancer cell growth. Clin Cancer Res. 2005 Feb 1;11(3):1336-41.
44 Combination of imatinib and clotrimazole enhances cell growth inhibition in T47D breast cancer cells. Chem Biol Interact. 2015 May 25;233:147-56. doi: 10.1016/j.cbi.2015.03.028. Epub 2015 Apr 8.
45 Efficacy of the polo-like kinase inhibitor rigosertib, alone or in combination with Abelson tyrosine kinase inhibitors, against break point cluster region-c-Abelson-positive leukemia cells. Oncotarget. 2015 Aug 21;6(24):20231-40. doi: 10.18632/oncotarget.4047.
46 Saikosaponin D disrupts platelet-derived growth factor- receptor/p38 pathway leading to mitochondrial apoptosis in human LO2 hepatocyte cells: a potential mechanism of hepatotoxicity. Chem Biol Interact. 2013 Oct 25;206(1):76-82. doi: 10.1016/j.cbi.2013.08.006. Epub 2013 Aug 28.
47 Elucidating mechanisms of toxicity using phenotypic data from primary human cell systems--a chemical biology approach for thrombosis-related side effects. Int J Mol Sci. 2015 Jan 5;16(1):1008-29. doi: 10.3390/ijms16011008.
48 Proapoptotic activity of bortezomib in gastrointestinal stromal tumor cells. Cancer Res. 2010 Jan 1;70(1):150-9. doi: 10.1158/0008-5472.CAN-09-1449. Epub 2009 Dec 22.
49 The CML-related oncoprotein BCR/ABL induces expression of histidine decarboxylase (HDC) and the synthesis of histamine in leukemic cells. Blood. 2006 Nov 15;108(10):3538-47. doi: 10.1182/blood-2005-12-028456. Epub 2006 Jul 18.
50 Increased expression of fibroblast growth factor receptor 3 in CD34+ BCR-ABL+ cells from patients with chronic myeloid leukemia. Leukemia. 2003 Dec;17(12):2418-25. doi: 10.1038/sj.leu.2403152.
51 Cytotoxicity of 34 FDA approved small-molecule kinase inhibitors in primary rat and human hepatocytes. Toxicol Lett. 2018 Jul;291:138-148. doi: 10.1016/j.toxlet.2018.04.010. Epub 2018 Apr 12.
52 Anthelmintic Niclosamide Disrupts the Interplay of p65 and FOXM1/-catenin and Eradicates Leukemia Stem Cells in Chronic Myelogenous Leukemia. Clin Cancer Res. 2017 Feb 1;23(3):789-803. doi: 10.1158/1078-0432.CCR-16-0226. Epub 2016 Aug 4.
53 In vitro studies of the combination of imatinib mesylate (Gleevec) and arsenic trioxide (Trisenox) in chronic myelogenous leukemia. Exp Hematol. 2002 Jul;30(7):729-37. doi: 10.1016/s0301-472x(02)00836-6.
54 Establishment and characterization of a novel imatinib-sensitive chronic myeloid leukemia cell line MYL, and an imatinib-resistant subline MYL-R showing overexpression of Lyn. Eur J Haematol. 2007 May;78(5):417-31. doi: 10.1111/j.1600-0609.2007.00835.x.
55 The catalytic DNA topoisomerase II inhibitor dexrazoxane (ICRF-187) induces differentiation and apoptosis in human leukemia K562 cells. Mol Pharmacol. 2001 Mar;59(3):453-61. doi: 10.1124/mol.59.3.453.
56 Downregulation of hERG channel expression by tyrosine kinase inhibitors nilotinib and vandetanib predominantly contributes to arrhythmogenesis. Toxicol Lett. 2022 Jul 15;365:11-23. doi: 10.1016/j.toxlet.2022.06.001. Epub 2022 Jun 6.
57 Investigation of imatinib and other approved drugs as starting points for antidiabetic drug discovery with FXR modulating activity. Biochem Pharmacol. 2012 Jun 15;83(12):1674-81. doi: 10.1016/j.bcp.2012.02.027. Epub 2012 Mar 7.
58 A new strategy for the rapid identification and validation of direct toxicity targets of psoralen-induced hepatotoxicity. Toxicol Lett. 2022 Jun 15;363:11-26. doi: 10.1016/j.toxlet.2022.05.002. Epub 2022 May 18.
59 Sorafenib induces apoptosis specifically in cells expressing BCR/ABL by inhibiting its kinase activity to activate the intrinsic mitochondrial pathway. Cancer Res. 2009 May 1;69(9):3927-36. doi: 10.1158/0008-5472.CAN-08-2978. Epub 2009 Apr 14.
60 A high-throughput screen for teratogens using human pluripotent stem cells. Toxicol Sci. 2014 Jan;137(1):76-90. doi: 10.1093/toxsci/kft239. Epub 2013 Oct 23.
61 Denaturing-HPLC-based assay for detection of ABL mutations in chronic myeloid leukemia patients resistant to Imatinib. Clin Chem. 2004 Jul;50(7):1205-13. doi: 10.1373/clinchem.2004.031112. Epub 2004 Apr 23.
62 Identification of Genes That Modulate Susceptibility to Formaldehyde and Imatinib by Functional Genomic Screening in Human Haploid KBM7 Cells. Toxicol Sci. 2016 May;151(1):10-22. doi: 10.1093/toxsci/kfw032. Epub 2016 Mar 22.
63 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
64 Disruption of the inhibitor of apoptosis protein survivin sensitizes Bcr-abl-positive cells to STI571-induced apoptosis. Cancer Res. 2005 Sep 15;65(18):8224-32. doi: 10.1158/0008-5472.CAN-05-0303.
65 Epigenetic down-regulation of BIM expression is associated with reduced optimal responses to imatinib treatment in chronic myeloid leukaemia. Eur J Cancer. 2009 Jul;45(10):1877-89. doi: 10.1016/j.ejca.2009.04.005. Epub 2009 May 4.