Details of the Drug Combination

General Information of Drug Combination (ID: DC3RA6K)

Drug Combination Name
Gefitinib Imatinib
Indication
Disease Entry Status REF
Lung adenocarcinoma Investigative [1]
Component Drugs Gefitinib   DM15F0X Imatinib   DM7RJXL
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: MDA-MB-231
Zero Interaction Potency (ZIP) Score: 0.58
Bliss Independence Score: 1.97
Loewe Additivity Score: 2.41
LHighest Single Agent (HSA) Score: 3.03

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Gefitinib
Disease Entry ICD 11 Status REF
Colon adenocarcinoma N.A. Approved [2]
Glioblastoma 2A00 Approved [2]
Lung cancer 2C25.0 Approved [2]
Non-small-cell lung cancer 2C25.Y Approved [2]
Rectal adenocarcinoma 2B92 Approved [2]
Rectum mucinous adenocarcinoma N.A. Approved [2]
Solid tumour/cancer 2A00-2F9Z Approved [3]
Head and neck cancer 2D42 Phase 3 [3]
Urethral cancer 2C93 Phase 2 [3]
Colon cancer 2B90.Z Investigative [2]
Colon mucinous adenocarcinoma N.A. Investigative [2]
Gefitinib Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Inhibitor [16]
------------------------------------------------------------------------------------
Gefitinib Interacts with 4 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [17]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [18]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [19]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [19]
------------------------------------------------------------------------------------
Gefitinib Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [20]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Metabolism [21]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [20]
------------------------------------------------------------------------------------
Gefitinib Interacts with 103 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 ADR [22]
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Decreases Response To Substance [23]
Sulfhydryl oxidase 1 (QSOX1) OT4ZPK4P QSOX1_HUMAN Increases Expression [24]
Growth arrest and DNA damage-inducible protein GADD45 gamma (GADD45G) OT8V1J4M GA45G_HUMAN Decreases Expression [24]
Interferon alpha-inducible protein 6 (IFI6) OTWOOAM4 IFI6_HUMAN Decreases Expression [24]
Fibroblast growth factor 6 (FGF6) OTRJ679P FGF6_HUMAN Increases Expression [24]
Ski oncogene (SKI) OT4KJ8F6 SKI_HUMAN Increases Expression [24]
Erythropoietin receptor (EPOR) OTUIOEU3 EPOR_HUMAN Increases Expression [24]
Nuclear factor NF-kappa-B p105 subunit (NFKB1) OTNRRD8I NFKB1_HUMAN Decreases Expression [24]
Tumor necrosis factor receptor superfamily member 1B (TNFRSF1B) OTDS2EAR TNR1B_HUMAN Decreases Expression [24]
Growth arrest and DNA damage-inducible protein GADD45 alpha (GADD45A) OTDRV63V GA45A_HUMAN Increases Expression [24]
Cytochrome P450 2F1 (CYP2F1) OTY3HJH1 CP2F1_HUMAN Decreases Expression [24]
Replication protein A 70 kDa DNA-binding subunit (RPA1) OT76POLP RFA1_HUMAN Increases Expression [24]
Adenosine receptor A1 (ADORA1) OTI7X39E AA1R_HUMAN Decreases Expression [24]
14-3-3 protein sigma (SFN) OTLJCZ1U 1433S_HUMAN Decreases Expression [24]
DNA mismatch repair protein Mlh1 (MLH1) OTG5XDD8 MLH1_HUMAN Decreases Expression [24]
Glycine--tRNA ligase (GARS1) OT5B6R9Y GARS_HUMAN Increases Expression [24]
Epidermal growth factor receptor substrate 15 (EPS15) OT7NPP8U EPS15_HUMAN Increases Expression [24]
Neuronal pentraxin-2 (NPTX2) OT3SSJDP NPTX2_HUMAN Decreases Expression [24]
Leptin receptor (LEPR) OT9H7G0C LEPR_HUMAN Decreases Expression [24]
Neural retina-specific leucine zipper protein (NRL) OT65MFKQ NRL_HUMAN Decreases Expression [24]
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-2 (GNB2) OT3JPRCQ GBB2_HUMAN Decreases Expression [24]
Retinal guanylyl cyclase 1 (GUCY2D) OT81UJI0 GUC2D_HUMAN Decreases Expression [24]
Cell growth regulator with RING finger domain protein 1 (CGRRF1) OTLMNRCL CGRF1_HUMAN Increases Expression [24]
Dual specificity protein phosphatase 9 (DUSP9) OTZZWEQL DUS9_HUMAN Decreases Expression [24]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [25]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Decreases Expression [26]
Glycogen synthase kinase-3 beta (GSK3B) OTL3L14B GSK3B_HUMAN Decreases Expression [26]
Cyclin-dependent kinase 6 (CDK6) OTR95N0X CDK6_HUMAN Decreases Expression [26]
Telomerase reverse transcriptase (TERT) OT085VVA TERT_HUMAN Decreases Expression [27]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Expression [28]
Ubiquitin-like modifier-activating enzyme ATG7 (ATG7) OTVT4YA1 ATG7_HUMAN Increases Expression [29]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [30]
Tumor necrosis factor (TNF) OT4IE164 TNFA_HUMAN Decreases Expression [12]
Interleukin-1 beta (IL1B) OT0DWXXB IL1B_HUMAN Increases Expression [31]
HLA class II histocompatibility antigen, DRB1 beta chain (HLA-DRB1) OTRGGIFP DRB1_HUMAN Affects Expression [32]
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Decreases Phosphorylation [33]
Receptor tyrosine-protein kinase erbB-2 (ERBB2) OTOAUNCK ERBB2_HUMAN Decreases Phosphorylation [34]
HLA class II histocompatibility antigen, DO alpha chain (HLA-DOA) OTZE5Q7R DOA_HUMAN Affects Expression [32]
Heat shock protein HSP 90-alpha (HSP90AA1) OTLG1WPK HS90A_HUMAN Increases Secretion [31]
Insulin-like growth factor 1 receptor (IGF1R) OTXJIF13 IGF1R_HUMAN Increases Phosphorylation [35]
High mobility group protein B1 (HMGB1) OT4B7CPF HMGB1_HUMAN Increases Secretion [31]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [36]
Heat shock 70 kDa protein 1A (HSPA1A) OTKGIE76 HS71A_HUMAN Increases Secretion [31]
C-C motif chemokine 2 (CCL2) OTAD2HEL CCL2_HUMAN Increases Secretion [37]
Matrix metalloproteinase-9 (MMP9) OTB2QDAV MMP9_HUMAN Decreases Expression [12]
Platelet endothelial cell adhesion molecule (PECAM1) OTXOM4D9 PECA1_HUMAN Decreases Expression [12]
Ribosomal protein S6 kinase beta-1 (RPS6KB1) OTAELNGX KS6B1_HUMAN Decreases Phosphorylation [29]
Alanine aminotransferase 1 (GPT) OTOXOA0Q ALAT1_HUMAN Increases Secretion [38]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Decreases Expression [23]
DnaJ homolog subfamily B member 1 (DNAJB1) OTCOSEVH DNJB1_HUMAN Increases Secretion [31]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Expression [39]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Expression [39]
Caspase-1 (CASP1) OTZ3YQFU CASP1_HUMAN Increases Activity [31]
G1/S-specific cyclin-D3 (CCND3) OTNKPQ22 CCND3_HUMAN Decreases Expression [23]
HLA class I histocompatibility antigen, alpha chain F (HLA-F) OT76CM19 HLAF_HUMAN Affects Expression [32]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Decreases Phosphorylation [40]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Decreases Expression [28]
Serine/threonine-protein kinase mTOR (MTOR) OTHH8KU7 MTOR_HUMAN Decreases Phosphorylation [29]
Cyclin-dependent kinase 4 inhibitor B (CDKN2B) OTAG24N1 CDN2B_HUMAN Increases Expression [30]
Mitogen-activated protein kinase 8 (MAPK8) OTEREYS5 MK08_HUMAN Decreases Phosphorylation [12]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Increases Expression [23]
Tumor necrosis factor ligand superfamily member 6 (FASLG) OTZARCHH TNFL6_HUMAN Increases Response To Substance [41]
Cytochrome c (CYCS) OTBFALJD CYC_HUMAN Affects Localization [36]
Transcription factor E2F1 (E2F1) OTLKYBBC E2F1_HUMAN Decreases Expression [27]
Caveolin-1 (CAV1) OTEZUR1L CAV1_HUMAN Increases Expression [39]
Sequestosome-1 (SQSTM1) OTGY5D5J SQSTM_HUMAN Decreases Expression [42]
Kelch-like ECH-associated protein 1 (KEAP1) OTFHOD0C KEAP1_HUMAN Increases Expression [43]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Increases Cleavage [41]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Decreases Activity [44]
MHC class I polypeptide-related sequence B (MICB) OTS2DVDW MICB_HUMAN Increases Expression [45]
MHC class I polypeptide-related sequence A (MICA) OTPEIEAR MICA_HUMAN Increases Expression [45]
Estrogen receptor beta (ESR2) OTXNR2WQ ESR2_HUMAN Increases Expression [46]
Serine protease HTRA1 (HTRA1) OTR8ACBF HTRA1_HUMAN Increases Expression [47]
Major histocompatibility complex class I-related gene protein (MR1) OTZU3XX7 HMR1_HUMAN Affects Expression [32]
Autophagy protein 5 (ATG5) OT4T5SMS ATG5_HUMAN Increases Expression [29]
Transcription factor SOX-17 (SOX17) OT9H4WWE SOX17_HUMAN Decreases Localization [48]
MARVEL domain-containing protein 1 (MARVELD1) OT5CPOJE MALD1_HUMAN Decreases Response To Substance [49]
GTPase KRas (KRAS) OT78QCN8 RASK_HUMAN Decreases Response To Substance [50]
Zinc finger protein SNAI2 (SNAI2) OT7Y8EJ2 SNAI2_HUMAN Affects Response To Substance [51]
Membrane-associated progesterone receptor component 1 (PGRMC1) OTBE6WAC PGRC1_HUMAN Decreases Response To Substance [52]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Increases Response To Substance [53]
Glutamate--cysteine ligase catalytic subunit (GCLC) OTESDI4D GSH1_HUMAN Affects Response To Substance [54]
RNA-binding protein 7 (RBM7) OTFIWTMF RBM7_HUMAN Affects Response To Substance [54]
Cell death regulator Aven (AVEN) OTGIN5YK AVEN_HUMAN Affects Response To Substance [54]
Forkhead box protein O3 (FOXO3) OTHXQG4P FOXO3_HUMAN Increases Response To Substance [55]
Phospholipase B-like 1 (PLBD1) OTHYEB4W PLBL1_HUMAN Affects Response To Substance [54]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Affects Response To Substance [56]
Securin (PTTG1) OTIMYS4W PTTG1_HUMAN Decreases Response To Substance [36]
Amphiregulin (AREG) OTJFOR67 AREG_HUMAN Decreases Response To Substance [54]
Pleckstrin homology-like domain family A member 2 (PHLDA2) OTMV9DPP PHLA2_HUMAN Affects Response To Substance [54]
Aurora kinase A (AURKA) OTMX0HYT AURKA_HUMAN Decreases Response To Substance [56]
DNA excision repair protein ERCC-1 (ERCC1) OTNPYQHI ERCC1_HUMAN Affects Response To Substance [15]
Bcl-2-like protein 11 (BCL2L11) OTNQQWFJ B2L11_HUMAN Increases Response To Substance [57]
Ceramide transfer protein (CERT1) OTNUCNHX CERT_HUMAN Affects Response To Substance [54]
DNA repair protein RAD51 homolog 1 (RAD51) OTNVWGC1 RAD51_HUMAN Affects Response To Substance [58]
Oncostatin-M-specific receptor subunit beta (OSMR) OTORWHPL OSMR_HUMAN Affects Response To Substance [54]
Protransforming growth factor alpha (TGFA) OTPD1LL9 TGFA_HUMAN Decreases Response To Substance [59]
Dual specificity protein phosphatase 3 (DUSP3) OTPJX9B4 DUS3_HUMAN Affects Response To Substance [54]
Transcription factor p65 (RELA) OTUJP9CN TF65_HUMAN Decreases Response To Substance [56]
Pericentrin (PCNT) OTW4Z65J PCNT_HUMAN Decreases Response To Substance [52]
Coronin-1C (CORO1C) OTXDF9T3 COR1C_HUMAN Affects Response To Substance [54]
Ribonucleoside-diphosphate reductase large subunit (RRM1) OTXGQOR9 RIR1_HUMAN Affects Response To Substance [15]
------------------------------------------------------------------------------------
⏷ Show the Full List of 103 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 [63]
Platelet-derived growth factor receptor (PDGFR) TTI2WET NOUNIPROTAC Inhibitor [63]
Tyrosine-protein kinase Kit (KIT) TTX41N9 KIT_HUMAN Inhibitor [63]
HUMAN fusion protein Bcr-Abl (Bcr-Abl) TTE63HY BCR_HUMAN/ABL1_HUMAN Inhibitor [9]
------------------------------------------------------------------------------------
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 [64]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [65]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [19]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [66]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [67]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [19]
------------------------------------------------------------------------------------
⏷ 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 [68]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Metabolism [69]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Metabolism [70]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [71]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Metabolism [72]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [73]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Metabolism [74]
Prostaglandin G/H synthase 1 (COX-1) DE073H6 PGH1_HUMAN Metabolism [70]
------------------------------------------------------------------------------------
⏷ 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 [75]
Cytochrome P450 3A5 (CYP3A5) OTSXFBXB CP3A5_HUMAN Decreases Methylation [75]
Cytochrome P450 3A7 (CYP3A7) OTTCDHHM CP3A7_HUMAN Decreases Methylation [75]
Cytochrome P450 2C8 (CYP2C8) OTHCWT42 CP2C8_HUMAN Decreases Methylation [75]
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) OTW8V2V1 ABCG2_HUMAN Increases Expression [76]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Increases Expression [76]
Aldehyde dehydrogenase, mitochondrial (ALDH2) OTKJ9I3N ALDH2_HUMAN Decreases Expression [77]
Eukaryotic translation initiation factor 4E (EIF4E) OTDAWNLA IF4E_HUMAN Decreases Expression [77]
Fructose-bisphosphate aldolase C (ALDOC) OTEC13I5 ALDOC_HUMAN Decreases Expression [77]
Pyruvate dehydrogenase E1 component subunit beta, mitochondrial (PDHB) OT2NHE5E ODPB_HUMAN Decreases Expression [77]
Cyclin-dependent kinase 4 (CDK4) OT7EP05T CDK4_HUMAN Decreases Expression [77]
Cyclin-A2 (CCNA2) OTPHHYZJ CCNA2_HUMAN Decreases Expression [77]
Ribosomal protein S6 kinase beta-1 (RPS6KB1) OTAELNGX KS6B1_HUMAN Decreases Expression [77]
Eukaryotic translation initiation factor 4B (EIF4B) OTE8TXA8 IF4B_HUMAN Decreases Expression [77]
Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) OT5BZ1J9 P85A_HUMAN Decreases Expression [77]
G1/S-specific cyclin-D3 (CCND3) OTNKPQ22 CCND3_HUMAN Decreases Expression [77]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Decreases Expression [77]
Hexokinase-4 (GCK) OTR3Q0NN HXK4_HUMAN Decreases Expression [77]
Serine/threonine-protein kinase mTOR (MTOR) OTHH8KU7 MTOR_HUMAN Decreases Expression [77]
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform (PPP2CA) OT83PT85 PP2AA_HUMAN Increases Expression [77]
Eukaryotic translation initiation factor 4E-binding protein 1 (EIF4EBP1) OTHBQVD5 4EBP1_HUMAN Decreases Expression [77]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [25]
Prostaglandin G/H synthase 2 (PTGS2) OT75U9M4 PGH2_HUMAN Decreases Expression [78]
Tumor necrosis factor receptor superfamily member 10B (TNFRSF10B) OTA1CPBV TR10B_HUMAN Increases Expression [79]
Autophagy-related protein 13 (ATG13) OTYMHNEJ ATG13_HUMAN Increases Phosphorylation [60]
Platelet-derived growth factor subunit B (PDGFB) OTMFMFC3 PDGFB_HUMAN Decreases Expression [80]
Interferon gamma (IFNG) OTXG9JM7 IFNG_HUMAN Increases Expression [81]
Interleukin-1 beta (IL1B) OT0DWXXB IL1B_HUMAN Increases Secretion [82]
Keratin, type I cytoskeletal 14 (KRT14) OTUVZ1DW K1C14_HUMAN Increases Expression [83]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Increases Expression [84]
Heat shock protein beta-1 (HSPB1) OTHFZ8ED HSPB1_HUMAN Increases Expression [79]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Decreases Activity [44]
Intercellular adhesion molecule 1 (ICAM1) OTTOIX77 ICAM1_HUMAN Increases Expression [79]
Tyrosine-protein kinase Lck (LCK) OT883FG9 LCK_HUMAN Decreases Phosphorylation [85]
Cyclin-dependent kinase 1 (CDK1) OTW1SC2N CDK1_HUMAN Decreases Expression [81]
Cathepsin B (CTSB) OTP9G5QB CATB_HUMAN Increases Expression [60]
Proto-oncogene tyrosine-protein kinase receptor Ret (RET) OTLU040A RET_HUMAN Decreases Phosphorylation [86]
ATP-dependent 6-phosphofructokinase, muscle type (PFKM) OT1QY9JM PFKAM_HUMAN Decreases Expression [87]
Platelet-derived growth factor receptor beta (PDGFRB) OTYSNK9Q PGFRB_HUMAN Decreases Expression [80]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [88]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Increases Expression [79]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Decreases Expression [89]
Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1) OTA675TJ GTR1_HUMAN Decreases Expression [84]
Breakpoint cluster region protein (BCR) OTCN76C1 BCR_HUMAN Decreases Activity [62]
Lysosome-associated membrane glycoprotein 1 (LAMP1) OTYE92QY LAMP1_HUMAN Increases Expression [60]
Ornithine decarboxylase (ODC1) OTNDAGRR DCOR_HUMAN Increases Expression [79]
Keratin, type II cytoskeletal 5 (KRT5) OTVGI9HT K2C5_HUMAN Increases Expression [83]
Tissue factor (F3) OT3MSU3B TF_HUMAN Increases Expression [90]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [91]
Platelet-derived growth factor receptor alpha (PDGFRA) OTDJXUCN PGFRA_HUMAN Decreases Expression [80]
CCAAT/enhancer-binding protein beta (CEBPB) OTM9MQIA CEBPB_HUMAN Increases Expression [79]
Histidine decarboxylase (HDC) OT4WA5YQ DCHS_HUMAN Decreases Expression [92]
Transcription factor EB (TFEB) OTJUJJQY TFEB_HUMAN Affects Localization [60]
Fibroblast growth factor receptor 3 (FGFR3) OTSAXDIL FGFR3_HUMAN Decreases Expression [93]
Insulin-like growth factor-binding protein 4 (IGFBP4) OT2HZRBD IBP4_HUMAN Increases Expression [79]
Alanine aminotransferase 1 (GPT) OTOXOA0Q ALAT1_HUMAN Increases Secretion [38]
Interleukin-4 receptor subunit alpha (IL4R) OTTXOTCW IL4RA_HUMAN Increases Expression [79]
Cyclin-dependent kinase 2 (CDK2) OTB5DYYZ CDK2_HUMAN Decreases Expression [81]
NF-kappa-B inhibitor alpha (NFKBIA) OTFT924M IKBA_HUMAN Increases Phosphorylation [79]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Phosphorylation [85]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Phosphorylation [85]
Caspase-1 (CASP1) OTZ3YQFU CASP1_HUMAN Increases Cleavage [82]
Catenin beta-1 (CTNNB1) OTZ932A3 CTNB1_HUMAN Decreases Expression [94]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Increases Activity [95]
Crk-like protein (CRKL) OTOYSD1R CRKL_HUMAN Decreases Phosphorylation [96]
Glycogen synthase kinase-3 beta (GSK3B) OTL3L14B GSK3B_HUMAN Increases Phosphorylation [60]
Hexokinase-2 (HK2) OTC0GCQO HXK2_HUMAN Decreases Expression [87]
Small ribosomal subunit protein eS6 (RPS6) OTT4D1LN RS6_HUMAN Decreases Phosphorylation [60]
Heat shock factor protein 1 (HSF1) OTYNJ4KP HSF1_HUMAN Increases Expression [79]
Transcription factor p65 (RELA) OTUJP9CN TF65_HUMAN Decreases Expression [94]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [89]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Expression [97]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) OT2YYI1A MCL1_HUMAN Decreases Expression [88]
Forkhead box protein M1 (FOXM1) OT5887KR FOXM1_HUMAN Decreases Expression [94]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Decreases Activity [98]
Sequestosome-1 (SQSTM1) OTGY5D5J SQSTM_HUMAN Increases Expression [60]
Beclin-1 (BECN1) OT4X293M BECN1_HUMAN Increases Expression [60]
Nuclear receptor subfamily 0 group B member 2 (NR0B2) OT7UVICX NR0B2_HUMAN Increases Expression [99]
NGFI-A-binding protein 2 (NAB2) OTG4BDF3 NAB2_HUMAN Increases Expression [79]
Nuclear factor erythroid 2-related factor 2 (NFE2L2) OT0HENJ5 NF2L2_HUMAN Decreases Expression [100]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Decreases Activity [44]
TRAF family member-associated NF-kappa-B activator (TANK) OTZSGFIK TANK_HUMAN Increases Expression [79]
NACHT, LRR and PYD domains-containing protein 3 (NLRP3) OTZM6MHU NLRP3_HUMAN Increases Expression [82]
Bile acid receptor (NR1H4) OTWZLPTB NR1H4_HUMAN Increases Activity [99]
Docking protein 1 (DOK1) OTGVRLW6 DOK1_HUMAN Decreases Phosphorylation [101]
Microtubule-associated proteins 1A/1B light chain 3B (MAP1LC3B) OTUYHB84 MLP3B_HUMAN Increases Expression [60]
Transcription factor SOX-17 (SOX17) OT9H4WWE SOX17_HUMAN Decreases Localization [48]
V-type proton ATPase subunit H (ATP6V1H) OTX17GQ9 VATH_HUMAN Increases Expression [60]
Tyrosine-protein kinase ABL1 (ABL1) OT09YVXH ABL1_HUMAN Increases Response To Substance [102]
LYR motif-containing protein 9 (LYRM9) OT1MILTK LYRM9_HUMAN Affects Response To Substance [103]
Leptin (LEP) OT5Q7ODW LEP_HUMAN Increases ADR [104]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Response To Substance [105]
Bcl-2-like protein 11 (BCL2L11) OTNQQWFJ B2L11_HUMAN Increases Response To Substance [106]
Tyrosine-protein kinase Lyn (LYN) OTP686K2 LYN_HUMAN Decreases Response To Substance [96]
Serine/threonine-protein kinase PLK1 (PLK1) OTRZX45T PLK1_HUMAN Increases Response To Substance [88]
------------------------------------------------------------------------------------
⏷ Show the Full List of 95 DOT(s)

Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Adult acute myeloid leukemia DCM1VGD HL-60(TB) Investigative [1]
Adult T acute lymphoblastic leukemia DC0I4BT MOLT-4 Investigative [1]
Childhood T acute lymphoblastic leukemia DCDB6PV CCRF-CEM Investigative [1]
Chronic myelogenous leukemia DC77KMM K-562 Investigative [1]
High grade ovarian serous adenocarcinoma DC9K7IM OVCAR-5 Investigative [1]
Melanoma DC66PA5 UACC-257 Investigative [1]
------------------------------------------------------------------------------------
⏷ Show the Full List of 6 DrugCom(s)

References

1 Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
2 Gefitinib 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: 4941).
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
5 Imatinib FDA Label
6 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).
7 FDA Approved Drug Products from FDA Official Website. 2019. Application Number: (ANDA) 078340.
8 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.
9 Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47.
10 Design and development of antisense drugs. Expert Opin. Drug Discov. 2008 3(10):1189-1207.
11 Synergistic antitumor effect of S-1 and the epidermal growth factor receptor inhibitor gefitinib in non-small cell lung cancer cell lines: role of gefitinib-induced down-regulation of thymidylate synthase. Mol Cancer Ther. 2008 Mar;7(3):599-606.
12 Frankincense myrrh attenuates hepatocellular carcinoma by regulating tumor blood vessel development through multiple epidermal growth factor receptor-mediated signaling pathways. World J Gastrointest Oncol. 2022 Feb 15;14(2):450-477. doi: 10.4251/wjgo.v14.i2.450.
13 EGFR inhibitors enhanced the susceptibility to NK cell-mediated lysis of lung cancer cells. J Immunother. 2011 May;34(4):372-81. doi: 10.1097/CJI.0b013e31821b724a.
14 Overcoming acquired resistance of gefitinib in lung cancer cells without T790M by AZD9291 or Twist1 knockdown in vitro and in vivo. Arch Toxicol. 2019 Jun;93(6):1555-1571. doi: 10.1007/s00204-019-02453-2. Epub 2019 Apr 16.
15 DNA repair gene polymorphisms and benefit from gefitinib in never-smokers with lung adenocarcinoma. Cancer. 2011 Jul 15;117(14):3201-8. doi: 10.1002/cncr.25863. Epub 2011 Jan 24.
16 Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
17 Gefitinib-phenytoin interaction is not correlated with the C-erythromycin breath test in healthy male volunteers. Br J Clin Pharmacol. 2009 Aug;68(2):226-37.
18 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
19 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
20 Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res. 2007 Jun 15;13(12):3731-7.
21 Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol. Clin Pharmacokinet. 2005;44(10):1067-81.
22 Pharmacogenetics of ABCG2 and adverse reactions to gefitinib. J Natl Cancer Inst. 2006 Dec 6;98(23):1739-42.
23 Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res. 2006 Jun 1;66(11):5542-8. doi: 10.1158/0008-5472.CAN-05-4620.
24 Identification of genes linked to gefitinib treatment in prostate cancer cell lines with or without resistance to androgen: a clue to application of gefitinib to hormone-resistant prostate cancer. Oncol Rep. 2006 Jun;15(6):1453-60.
25 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.
26 Effects and mechanisms of betulinic acid on improving EGFR TKI-resistance of lung cancer cells. Environ Toxicol. 2018 Nov;33(11):1153-1159.
27 Antiproliferative effects of gefitinib are associated with suppression of E2F-1 expression and telomerase activity. Anticancer Res. 2006 Sep-Oct;26(5A):3387-91.
28 Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. doi: 10.1016/j.taap.2017.09.017. Epub 2017 Sep 21.
29 EGFR tyrosine kinase inhibitors activate autophagy as a cytoprotective response in human lung cancer cells. PLoS One. 2011;6(6):e18691. doi: 10.1371/journal.pone.0018691. Epub 2011 Jun 2.
30 ZD1839 induces p15INK4b and causes G1 arrest by inhibiting the mitogen-activated protein kinase/extracellular signal-regulated kinase pathway. Mol Cancer Ther. 2007 May;6(5):1579-87. doi: 10.1158/1535-7163.MCT-06-0814.
31 Reactive metabolite of gefitinib activates inflammasomes: implications for gefitinib-induced idiosyncratic reaction. J Toxicol Sci. 2020;45(11):673-680. doi: 10.2131/jts.45.673.
32 Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis. Chem Res Toxicol. 2015 May 18;28(5):927-34. doi: 10.1021/tx5005248. Epub 2015 Apr 3.
33 Bidirectional cross talk between ERalpha and EGFR signalling pathways regulates tamoxifen-resistant growth. Breast Cancer Res Treat. 2006 Mar;96(2):131-46. doi: 10.1007/s10549-005-9070-2. Epub 2005 Oct 27.
34 Epidermal growth factor receptor activity determines response of colorectal cancer cells to gefitinib alone and in combination with chemotherapy. Clin Cancer Res. 2005 Oct 15;11(20):7480-9. doi: 10.1158/1078-0432.CCR-05-0328.
35 Implication of the insulin-like growth factor-IR pathway in the resistance of non-small cell lung cancer cells to treatment with gefitinib. Clin Cancer Res. 2007 May 1;13(9):2795-803. doi: 10.1158/1078-0432.CCR-06-2077.
36 Evidence of securin-mediated resistance to gefitinib-induced apoptosis in human cancer cells. Chem Biol Interact. 2013 Apr 25;203(2):412-22. doi: 10.1016/j.cbi.2013.03.011. Epub 2013 Mar 22.
37 Crosstalk between alveolar macrophages and alveolar epithelial cells/fibroblasts contributes to the pulmonary toxicity of gefitinib. Toxicol Lett. 2021 Mar 1;338:1-9. doi: 10.1016/j.toxlet.2020.11.011. Epub 2020 Nov 25.
38 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.
39 Growth of hormone-dependent MCF-7 breast cancer cells is promoted by constitutive caveolin-1 whose expression is lost in an EGF-R-mediated manner during development of tamoxifen resistance. Breast Cancer Res Treat. 2010 Feb;119(3):575-91. doi: 10.1007/s10549-009-0355-8. Epub 2009 Mar 15.
40 Dihydromyricetin suppresses tumor growth via downregulation of the EGFR/Akt/survivin signaling pathway. J Biochem Mol Toxicol. 2023 Jun;37(6):e23328. doi: 10.1002/jbt.23328. Epub 2023 Feb 19.
41 The anti-cancer drug gefitinib accelerates Fas-mediated apoptosis by enhancing caspase-8 activation in cancer cells. J Toxicol Sci. 2019;44(6):435-440. doi: 10.2131/jts.44.435.
42 Autophagy Inhibition Overcomes the Antagonistic Effect Between Gefitinib and Cisplatin in Epidermal Growth Factor Receptor Mutant Non--Small-Cell Lung Cancer Cells. Clin Lung Cancer. 2015 Sep;16(5):e55-66. doi: 10.1016/j.cllc.2015.03.006. Epub 2015 Apr 2.
43 Nrf2 but not autophagy inhibition is associated with the survival of wild-type epidermal growth factor receptor non-small cell lung cancer cells. Toxicol Appl Pharmacol. 2016 Nov 1;310:140-149. doi: 10.1016/j.taap.2016.09.010. Epub 2016 Sep 14.
44 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.
45 Susceptibility to natural killer cell-mediated lysis of colon cancer cells is enhanced by treatment with epidermal growth factor receptor inhibitors through UL16-binding protein-1 induction. Cancer Sci. 2012 Jan;103(1):7-16. doi: 10.1111/j.1349-7006.2011.02109.x. Epub 2011 Nov 15.
46 Combined tamoxifen and gefitinib in non-small cell lung cancer shows antiproliferative effects. Biomed Pharmacother. 2010 Feb;64(2):88-92. doi: 10.1016/j.biopha.2009.06.010. Epub 2009 Oct 23.
47 Inorganic arsenic exposure promotes malignant progression by HDAC6-mediated down-regulation of HTRA1. J Appl Toxicol. 2023 Aug;43(8):1214-1224. doi: 10.1002/jat.4457. Epub 2023 Mar 11.
48 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.
49 Inhibition of SREBP increases gefitinib sensitivity in non-small cell lung cancer cells. Oncotarget. 2016 Aug 9;7(32):52392-52403.
50 The K-Ras effector p38 MAPK confers intrinsic resistance to tyrosine kinase inhibitors by stimulating EGFR transcription and EGFR dephosphorylation. J Biol Chem. 2017 Sep 8;292(36):15070-15079. doi: 10.1074/jbc.M117.779488. Epub 2017 Jul 24.
51 Slug confers resistance to the epidermal growth factor receptor tyrosine kinase inhibitor. Am J Respir Crit Care Med. 2011 Apr 15;183(8):1071-9. doi: 10.1164/rccm.201009-1440OC. Epub 2010 Oct 29.
52 Identification of protein expression alterations in gefitinib-resistant human lung adenocarcinoma: PCNT and mPR play key roles in the development of gefitinib-associated resistance. Toxicol Appl Pharmacol. 2015 Nov 1;288(3):359-73. doi: 10.1016/j.taap.2015.08.008. Epub 2015 Aug 20.
53 Induction of CYP1A1 increases gefitinib-induced oxidative stress and apoptosis in A549 cells. Toxicol In Vitro. 2017 Oct;44:36-43.
54 Prediction of sensitivity of advanced non-small cell lung cancers to gefitinib (Iressa, ZD1839). Hum Mol Genet. 2004 Dec 15;13(24):3029-43. doi: 10.1093/hmg/ddh331. Epub 2004 Oct 20.
55 The transcription factor FOXO3a is a crucial cellular target of gefitinib (Iressa) in breast cancer cells. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3169-79. doi: 10.1158/1535-7163.MCT-07-0507.
56 Aurora-A promotes gefitinib resistance via a NF-B signaling pathway in p53 knockdown lung cancer cells. Biochem Biophys Res Commun. 2011 Feb 11;405(2):168-72. doi: 10.1016/j.bbrc.2011.01.001. Epub 2011 Jan 7.
57 BIM induction of apoptosis triggered by EGFR-sensitive and resistance cell lines of non-small-cell lung cancer. Med Oncol. 2011 Jun;28(2):572-7. doi: 10.1007/s12032-010-9470-y. Epub 2010 Mar 17.
58 E3 ubiquitin ligase RNF180 reduces sensitivity of triple-negative breast cancer cells to Gefitinib by downregulating RAD51. Chem Biol Interact. 2022 Feb 25;354:109798. doi: 10.1016/j.cbi.2022.109798. Epub 2022 Jan 6.
59 Increases of amphiregulin and transforming growth factor-alpha in serum as predictors of poor response to gefitinib among patients with advanced non-small cell lung cancers. Cancer Res. 2005 Oct 15;65(20):9176-84. doi: 10.1158/0008-5472.CAN-05-1556.
60 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.
61 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.
62 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.
63 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.
64 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.
65 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
66 Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia. Leuk Lymphoma. 2008 Apr;49(4):639-42.
67 Environmental and genetic factors affecting transport of imatinib by OATP1A2. Clin Pharmacol Ther. 2011 Jun;89(6):816-20.
68 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.
69 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
70 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.
71 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
72 Drug Interactions Flockhart Table
73 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
74 Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
75 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.
76 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.
77 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.
78 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.
79 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.
80 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.
81 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.
82 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.
83 Oral lichenoid eruption secondary to imatinib (Glivec). J Dermatolog Treat. 2004 Jul;15(4):253-5. doi: 10.1080/09546630410015556.
84 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.
85 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.
86 Dual inhibition of RET and FGFR4 restrains medullary thyroid cancer cell growth. Clin Cancer Res. 2005 Feb 1;11(3):1336-41.
87 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.
88 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.
89 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.
90 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.
91 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.
92 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.
93 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.
94 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.
95 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.
96 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.
97 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.
98 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.
99 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.
100 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.
101 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.
102 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.
103 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.
104 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.
105 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.
106 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.