Details of the Drug Combination

General Information of Drug Combination (ID: DCHG9QR)

Drug Combination Name
Docetaxel Lapatinib
Indication
Disease Entry Status REF
High grade ovarian serous adenocarcinoma Investigative [1]
Component Drugs Docetaxel   DMDI269 Lapatinib   DM3BH1Y
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: OVCAR-8
Zero Interaction Potency (ZIP) Score: 7.75
Bliss Independence Score: 9.69
Loewe Additivity Score: 7.78
LHighest Single Agent (HSA) Score: 7.51

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Docetaxel
Disease Entry ICD 11 Status REF
Advanced cancer 2A00-2F9Z Approved [2]
Breast carcinoma N.A. Approved [2]
Head and neck cancer 2D42 Approved [2]
Leiomyosarcoma 2B58 Approved [2]
Lung cancer 2C25.0 Approved [2]
Non-small-cell lung cancer 2C25.Y Approved [2]
Prostate adenocarcinoma N.A. Approved [2]
Prostate cancer 2C82.0 Approved [2]
Solid tumour/cancer 2A00-2F9Z Approved [3]
Urinary system neoplasm N.A. Approved [2]
Gastric cancer 2B72 Investigative [2]
Docetaxel Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Tubulin (TUB) TTML2WA NOUNIPROTAC Inhibitor [9]
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Docetaxel Interacts with 8 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
Multidrug resistance-associated protein 1 (ABCC1) DTSYQGK MRP1_HUMAN Substrate [10]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [11]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [12]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [13]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [14]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [15]
TAP-like protein (ABCB9) DT68UV2 ABCB9_HUMAN Substrate [16]
Multidrug resistance-associated protein 7 (ABCC10) DTPS120 MRP7_HUMAN Substrate [17]
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⏷ Show the Full List of 8 DTP(s)
Docetaxel Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [18]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [19]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Metabolism [19]
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Docetaxel Interacts with 83 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Increases Response To Substance [20]
ATP-binding cassette sub-family C member 2 (ABCC2) OTJSIGV5 MRP2_HUMAN Increases ADR [21]
Multidrug resistance-associated protein 1 (ABCC1) OTGUN89S MRP1_HUMAN Increases Expression [22]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Increases Response To Substance [20]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Decreases Expression [23]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Increases Activity [24]
Tumor necrosis factor (TNF) OT4IE164 TNFA_HUMAN Decreases Expression [25]
Interleukin-6 (IL6) OTUOSCCU IL6_HUMAN Increases Expression [25]
Progesterone receptor (PGR) OT0FZ3QE PRGR_HUMAN Decreases Expression [25]
Aromatase (CYP19A1) OTZ6XF74 CP19A_HUMAN Decreases Expression [25]
Prostaglandin G/H synthase 2 (PTGS2) OT75U9M4 PGH2_HUMAN Increases Expression [25]
Dihydropyrimidine dehydrogenase (DPYD) OTWRF2NR DPYD_HUMAN Decreases Activity [6]
Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A) OTBPCU2O TR10A_HUMAN Increases Expression [26]
Tumor necrosis factor receptor superfamily member 10B (TNFRSF10B) OTA1CPBV TR10B_HUMAN Increases Expression [26]
Bcl-2-like protein 11 (BCL2L11) OTNQQWFJ B2L11_HUMAN Increases Degradation [27]
Nuclear receptor subfamily 1 group I member 2 (NR1I2) OTC5U0N5 NR1I2_HUMAN Increases Activity [28]
PC4 and SFRS1-interacting protein (PSIP1) OT4YAFUS PSIP1_HUMAN Increases Cleavage [29]
RAF proto-oncogene serine/threonine-protein kinase (RAF1) OT51LSFO RAF1_HUMAN Increases Expression [30]
Granulocyte-macrophage colony-stimulating factor (CSF2) OT1M7D28 CSF2_HUMAN Increases Secretion [31]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Increases Expression [7]
Transcription factor Jun (JUN) OTCYBO6X JUN_HUMAN Increases Phosphorylation [32]
Protein kinase C beta type (PRKCB) OTYQ0656 KPCB_HUMAN Increases Phosphorylation [33]
Keratin, type I cytoskeletal 18 (KRT18) OTVLQFIP K1C18_HUMAN Increases Expression [34]
Cyclin-dependent kinase 1 (CDK1) OTW1SC2N CDK1_HUMAN Increases Activity [35]
Prostate-specific antigen (KLK3) OTFGSBFJ KLK3_HUMAN Decreases Expression [36]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [32]
Androgen receptor (AR) OTUBKAZZ ANDR_HUMAN Decreases Expression [37]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [38]
Natriuretic peptides B (NPPB) OTSN2IPY ANFB_HUMAN Increases Expression [39]
Cyclic AMP-dependent transcription factor ATF-3 (ATF3) OTC1UOHP ATF3_HUMAN Decreases Expression [40]
Growth arrest and DNA damage-inducible protein GADD45 alpha (GADD45A) OTDRV63V GA45A_HUMAN Decreases Expression [40]
Cyclin-dependent kinase 2 (CDK2) OTB5DYYZ CDK2_HUMAN Increases Activity [35]
Tumor necrosis factor receptor superfamily member 6 (FAS) OTP9XG86 TNR6_HUMAN Increases Expression [41]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Increases Phosphorylation [30]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Increases Phosphorylation [30]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Decreases Phosphorylation [8]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Decreases Expression [40]
Signal transducer and activator of transcription 3 (STAT3) OTAAGKYZ STAT3_HUMAN Decreases Phosphorylation [42]
Caspase-2 (CASP2) OTUDYSPP CASP2_HUMAN Increases Activity [29]
Cyclin-dependent kinase inhibitor 2A (CDKN2A) OTN0ZWAE CDN2A_HUMAN Decreases Expression [43]
Proliferation marker protein Ki-67 (MKI67) OTA8N1QI KI67_HUMAN Decreases Expression [23]
Caspase-7 (CASP7) OTAPJ040 CASP7_HUMAN Increases Activity [44]
Caspase-9 (CASP9) OTD4RFFG CASP9_HUMAN Increases Activity [45]
E3 ubiquitin-protein ligase Mdm2 (MDM2) OTOVXARF MDM2_HUMAN Increases Expression [7]
Focal adhesion kinase 1 (PTK2) OT3Q1JDY FAK1_HUMAN Increases Cleavage [46]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [47]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) OT2YYI1A MCL1_HUMAN Increases Expression [27]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Increases Activity [46]
Bcl-2 homologous antagonist/killer (BAK1) OTDP6ILW BAK_HUMAN Increases Activity [27]
Bcl2-associated agonist of cell death (BAD) OT63ERYM BAD_HUMAN Decreases Phosphorylation [27]
ELL-associated factor 2 (EAF2) OTSOET5L EAF2_HUMAN Decreases Expression [40]
Small integral membrane protein 14 (SMIM14) OT47IF19 SIM14_HUMAN Decreases Expression [40]
Protein FAM117A (FAM117A) OT2FBGGV F117A_HUMAN Decreases Expression [40]
Delta-like protein 4 (DLL4) OTRA4K2V DLL4_HUMAN Increases Expression [44]
Tumor necrosis factor receptor superfamily member 19 (TNFRSF19) OTTVT4MB TNR19_HUMAN Decreases Expression [40]
Tropomodulin-2 (TMOD2) OTTTUH2W TMOD2_HUMAN Decreases Expression [40]
Flavin-containing monooxygenase 3 (FMO3) OT1G2EV3 FMO3_HUMAN Affects Response To Substance [48]
Kinesin heavy chain isoform 5A (KIF5A) OT3ETTI6 KIF5A_HUMAN Decreases Response To Substance [49]
Proteinase-activated receptor 1 (F2R) OT4WVWBO PAR1_HUMAN Decreases Response To Substance [50]
ATP-binding cassette sub-family G member 1 (ABCG1) OT5BG6MK ABCG1_HUMAN Affects Response To Substance [48]
Regulator of G-protein signaling 17 (RGS17) OT5RVUDS RGS17_HUMAN Increases Response To Substance [51]
Mitotic checkpoint serine/threonine-protein kinase BUB1 beta (BUB1B) OT8KME51 BUB1B_HUMAN Affects Response To Substance [52]
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Decreases Response To Substance [53]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Response To Substance [54]
Superoxide dismutase , mitochondrial (SOD2) OTIWXGZ9 SODM_HUMAN Decreases Response To Substance [55]
Cytochrome P450 1A2 (CYP1A2) OTLLBX48 CP1A2_HUMAN Affects Response To Substance [48]
Glutathione S-transferase P (GSTP1) OTLP0A0Y GSTP1_HUMAN Increases Response To Substance [20]
Receptor tyrosine-protein kinase erbB-2 (ERBB2) OTOAUNCK ERBB2_HUMAN Increases Response To Substance [56]
Kinesin-like protein KIFC3 (KIFC3) OTOPD4QO KIFC3_HUMAN Decreases Response To Substance [49]
Regulator of G-protein signaling 10 (RGS10) OTQ8N1QH RGS10_HUMAN Increases Response To Substance [51]
E3 ubiquitin-protein ligase CHFR (CHFR) OTRAD2TT CHFR_HUMAN Decreases Response To Substance [57]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Response To Substance [58]
Cell surface glycoprotein MUC18 (MCAM) OTT8XKGE MUC18_HUMAN Decreases Response To Substance [59]
Kinesin-like protein KIF12 (KIF12) OTTALNDD KIF12_HUMAN Decreases Response To Substance [49]
Nucleophosmin (NPM1) OTTBYYT0 NPM_HUMAN Decreases Response To Substance [60]
Flavin-containing monooxygenase 2 (FMO2) OTUJUL9S FMO2_HUMAN Affects Response To Substance [48]
NADPH--cytochrome P450 reductase (POR) OTVIDOCH NCPR_HUMAN Increases Response To Substance [20]
Kinesin-like protein KIF14 (KIF14) OTXHT4JM KIF14_HUMAN Decreases Response To Substance [61]
Mitotic spindle assembly checkpoint protein MAD2A (MAD2L1) OTXNGZCG MD2L1_HUMAN Affects Response To Substance [52]
Cellular retinoic acid-binding protein 2 (CRABP2) OTY01V9G RABP2_HUMAN Affects Response To Substance [62]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Affects Response To Substance [63]
Cytochrome P450 2D6 (CYP2D6) OTZJC802 CP2D6_HUMAN Affects Response To Substance [48]
ATP-binding cassette sub-family C member 6 (ABCC6) OTZT0LKT MRP6_HUMAN Affects Response To Substance [48]
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⏷ Show the Full List of 83 DOT(s)
Indication(s) of Lapatinib
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Approved [4]
Gastroesophageal junction adenocarcinoma 2B71 Approved [5]
Melanoma 2C30 Approved [5]
Lapatinib Interacts with 3 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Erbb2 tyrosine kinase receptor (HER2) TT6EO5L ERBB2_HUMAN Inhibitor [65]
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Inhibitor [65]
Eukaryotic elongation factor 2 kinase (eEF-2K) TT1QFLA EF2K_HUMAN Inhibitor [66]
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Lapatinib Interacts with 2 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [67]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [68]
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Lapatinib Interacts with 4 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [69]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [70]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [69]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Metabolism [70]
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Lapatinib Interacts with 36 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Decreases Activity [71]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [72]
Superoxide dismutase , mitochondrial (SOD2) OTIWXGZ9 SODM_HUMAN Increases Expression [73]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Increases Expression [73]
NAD(P)H dehydrogenase 1 (NQO1) OTZGGIVK NQO1_HUMAN Increases Expression [73]
Nuclear factor erythroid 2-related factor 2 (NFE2L2) OT0HENJ5 NF2L2_HUMAN Increases Activity [73]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Expression [74]
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Decreases Activity [71]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [75]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Decreases Expression [76]
DNA topoisomerase 1 (TOP1) OT51O0CF TOP1_HUMAN Decreases Expression [77]
DNA topoisomerase 2-alpha (TOP2A) OT6LPS08 TOP2A_HUMAN Decreases Expression [77]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [77]
Cyclin-A2 (CCNA2) OTPHHYZJ CCNA2_HUMAN Decreases Expression [75]
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_HUMAN Decreases Activity [78]
Receptor tyrosine-protein kinase erbB-3 (ERBB3) OTRSST0A ERBB3_HUMAN Decreases Activity [79]
Alanine aminotransferase 1 (GPT) OTOXOA0Q ALAT1_HUMAN Increases Secretion [80]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Decreases Expression [71]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Activity [75]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Activity [75]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Decreases Activity [71]
DNA replication licensing factor MCM7 (MCM7) OT6FXC6K MCM7_HUMAN Decreases Expression [75]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Increases Activity [77]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Increases Expression [71]
Caspase-7 (CASP7) OTAPJ040 CASP7_HUMAN Increases Activity [77]
Caspase-9 (CASP9) OTD4RFFG CASP9_HUMAN Increases Activity [77]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [76]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Decreases Activity [81]
GTPase KRas (KRAS) OT78QCN8 RASK_HUMAN Decreases Response To Substance [82]
HLA class II histocompatibility antigen, DQ alpha 1 chain (HLA-DQA1) OTC6GISG DQA1_HUMAN Increases ADR [83]
Zinc finger protein SNAI1 (SNAI1) OTDPYAMC SNAI1_HUMAN Decreases Response To Substance [84]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Increases Metabolism [77]
Cytochrome P450 3A7 (CYP3A7) OTTCDHHM CP3A7_HUMAN Increases Metabolism [77]
Transforming growth factor beta-1 proprotein (TGFB1) OTV5XHVH TGFB1_HUMAN Decreases Response To Substance [84]
Tenascin-X (TNXB) OTVBWAV5 TENX_HUMAN Increases ADR [83]
HLA class II histocompatibility antigen, DQ beta 1 chain (HLA-DQB1) OTVVI3UI DQB1_HUMAN Increases ADR [83]
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⏷ Show the Full List of 36 DOT(s)

Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Adenocarcinoma DC4VBJV DU-145 Investigative [1]
Adenocarcinoma DCHM8YK OVCAR3 Investigative [1]
Adenocarcinoma DCQFXNS NCIH23 Investigative [1]
Adenocarcinoma DC0OOEX A549 Investigative [1]
Adenocarcinoma DCQ82XX HT29 Investigative [1]
Adenocarcinoma DCU75ES SW-620 Investigative [1]
Adenocarcinoma DCVZJK5 HCC-2998 Investigative [1]
Adult acute myeloid leukemia DCJYPDC HL-60(TB) Investigative [1]
Anaplastic large cell lymphoma DCJ2DRU SR Investigative [1]
Astrocytoma DCG0H0W U251 Investigative [1]
Astrocytoma DC3SG1L SNB-19 Investigative [1]
Chronic myelogenous leukemia DCD71JE K-562 Investigative [1]
Clear cell renal cell carcinoma DCIDU6D A498 Investigative [1]
Clear cell renal cell carcinoma DCLGGE5 786-0 Investigative [1]
Clear cell renal cell carcinoma DCVRS9R CAKI-1 Investigative [1]
Cutaneous melanoma DCVYS4Y SK-MEL-28 Investigative [1]
Glioblastoma DCJUS37 SNB-75 Investigative [1]
Glioma DCUNV1Y SF-539 Investigative [1]
Glioma DC39VSH SF-295 Investigative [1]
Glioma DCCJ31K SF-268 Investigative [1]
High grade ovarian serous adenocarcinoma DCZR14Y OVCAR-4 Investigative [1]
High grade ovarian serous adenocarcinoma DCVSL3V OVCAR-5 Investigative [1]
High grade ovarian serous adenocarcinoma DCTN7WO NCI\\/ADR-RES Investigative [1]
Large cell lung carcinoma DCQMRVP NCI-H460 Investigative [1]
Lung adenocarcinoma DC99A6Q HOP-62 Investigative [1]
Lung adenocarcinoma DC7LUF1 EKVX Investigative [1]
Lung adenocarcinoma DCUQLAC MDA-MB-231 Investigative [1]
Malignant melanoma DCQORSE UACC62 Investigative [1]
Malignant melanoma DCKQFFA LOX IMVI Investigative [1]
Melanoma DCN5A0C MALME-3M Investigative [1]
Melanoma DC9LZY9 UACC-257 Investigative [1]
Minimally invasive lung adenocarcinoma DCS5KHY NCI-H322M Investigative [1]
Mixed endometrioid and clear cell carcinoma DCEKZ3B IGROV1 Investigative [1]
Papillary renal cell carcinoma DC2T3LE ACHN Investigative [1]
Plasma cell myeloma DC4E33P RPMI-8226 Investigative [1]
Prostate carcinoma DCDWB06 PC-3 Investigative [1]
Breast adenocarcinoma DC4DNP0 MDA-MB-468 Investigative [85]
Carcinoma DCRWPMI RXF 393 Investigative [85]
Carcinoma DC9IQZD MCF7 Investigative [85]
Colon adenocarcinoma DCOD7JZ COLO 205 Investigative [85]
Colon carcinoma DCX0WP7 KM12 Investigative [85]
Invasive ductal carcinoma DCI9H2I HS 578T Investigative [85]
Invasive ductal carcinoma DCUJ54V BT-549 Investigative [85]
Invasive ductal carcinoma DCSIW26 T-47D Investigative [85]
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⏷ Show the Full List of 44 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 Docetaxel 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: 6809).
4 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: 5692).
5 Lapatinib FDA Label
6 Synergistic effects of docetaxel and S-1 by modulating the expression of metabolic enzymes of 5-fluorouracil in human gastric cancer cell lines. Int J Cancer. 2006 Aug 15;119(4):783-91.
7 Induction of tubulin by docetaxel is associated with p53 status in human non small cell lung cancer cell lines. Int J Cancer. 2006 Jan 15;118(2):317-25. doi: 10.1002/ijc.21372.
8 Cyclooxygenase-2 inhibitor celecoxib augments chemotherapeutic drug-induced apoptosis by enhancing activation of caspase-3 and -9 in prostate cancer cells. Int J Cancer. 2005 Jun 20;115(3):484-92. doi: 10.1002/ijc.20878.
9 Docetaxel: a review of its use in metastatic breast cancer. Drugs. 2005;65(17):2513-31.
10 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
11 Transport of diclofenac by breast cancer resistance protein (ABCG2) and stimulation of multidrug resistance protein 2 (ABCC2)-mediated drug transport by diclofenac and benzbromarone. Drug Metab Dispos. 2009 Jan;37(1):129-36.
12 Effect of ABCB1 C3435T polymorphism on docetaxel pharmacokinetics according to menopausal status in breast cancer patients. Br J Cancer. 2010 Aug 10;103(4):560-6.
13 Ixabepilone, a novel microtubule-targeting agent for breast cancer, is a substrate for P-glycoprotein (P-gp/MDR1/ABCB1) but not breast cancer resistance protein (BCRP/ABCG2). J Pharmacol Exp Ther. 2011 May;337(2):423-32.
14 FDA Drug Development and Drug Interactions
15 Rapid screening of antineoplastic candidates for the human organic anion transporter OATP1B3 substrates using fluorescent probes. Cancer Lett. 2008 Feb 18;260(1-2):163-9.
16 RNA-sequencing dissects the transcriptome of polyploid cancer cells that are resistant to combined treatments of cisplatin with paclitaxel and docetaxel. Mol Biosyst. 2017 Sep 26;13(10):2125-2134.
17 Modulation of the ATPase and transport activities of broad-acting multidrug resistance factor ABCC10 (MRP7). Cancer Res. 2012 Dec 15;72(24):6457-67.
18 Randomized pharmacokinetic and pharmacodynamic study of docetaxel: dosing based on body-surface area compared with individualized dosing based on cytochrome P450 activity estimated using a urinary metabolite of exogenous cortisol. J Clin Oncol. 2005 Feb 20;23(6):1061-9.
19 Drug Interactions Flockhart Table
20 Concise prediction models of anticancer efficacy of 8 drugs using expression data from 12 selected genes. Int J Cancer. 2004 Sep 10;111(4):617-26. doi: 10.1002/ijc.20289.
21 Association of genetic polymorphisms in SLCO1B3 and ABCC2 with docetaxel-induced leukopenia. Cancer Sci. 2008 May;99(5):967-72.
22 Enhanced in vitro invasiveness and drug resistance with altered gene expression patterns in a human lung carcinoma cell line after pulse selection with anticancer drugs. Int J Cancer. 2004 Sep 10;111(4):484-93. doi: 10.1002/ijc.20230.
23 Enhanced chemotherapeutic efficacy of docetaxel in human lung cancer cell line via GLUT1 inhibitor. J Biochem Mol Toxicol. 2023 Jun;37(6):e23348. doi: 10.1002/jbt.23348. Epub 2023 Mar 31.
24 Comparison of burst of reactive oxygen species and activation of caspase-3 in apoptosis of K562 and HL-60 cells induced by docetaxel. Cancer Lett. 2004 Oct 8;214(1):103-13. doi: 10.1016/j.canlet.2004.03.047.
25 Down-regulation of intratumoral aromatase messenger RNA levels by docetaxel in human breast cancers. Clin Cancer Res. 2004 Dec 15;10(24):8163-9.
26 Pretreatment with paclitaxel enhances apo-2 ligand/tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis of prostate cancer cells by inducing death receptors 4 and 5 protein levels. Cancer Res. 2001 Jan 15;61(2):759-63.
27 Docetaxel-induced apoptosis of human melanoma is mediated by activation of c-Jun NH2-terminal kinase and inhibited by the mitogen-activated protein kinase extracellular signal-regulated kinase 1/2 pathway. Clin Cancer Res. 2007 Feb 15;13(4):1308-14. doi: 10.1158/1078-0432.CCR-06-2216.
28 PXR-mediated induction of P-glycoprotein by anticancer drugs in a human colon adenocarcinoma-derived cell line. Cancer Chemother Pharmacol. 2010 Sep;66(4):765-71. doi: 10.1007/s00280-009-1221-4. Epub 2009 Dec 30.
29 Docetaxel-induced prostate cancer cell death involves concomitant activation of caspase and lysosomal pathways and is attenuated by LEDGF/p75. Mol Cancer. 2009 Aug 28;8:68. doi: 10.1186/1476-4598-8-68.
30 Docetaxel induces p53-dependent apoptosis and synergizes with farnesyl transferase inhibitor r115777 in human epithelial cancer cells. Front Biosci. 2005 Sep 1;10:2566-75. doi: 10.2741/1720.
31 Kaempferol and quercetin stimulate granulocyte-macrophage colony-stimulating factor secretion in human prostate cancer cells. Mol Cell Endocrinol. 2008 Jun 11;287(1-2):57-64. doi: 10.1016/j.mce.2008.01.015. Epub 2008 Feb 3.
32 All-trans retinoic acid potentiates Taxotere-induced cell death mediated by Jun N-terminal kinase in breast cancer cells. Oncogene. 2004 Jan 15;23(2):426-33. doi: 10.1038/sj.onc.1207040.
33 Docetaxel Facilitates Endothelial Dysfunction through Oxidative Stress via Modulation of Protein Kinase C Beta: The Protective Effects of Sotrastaurin. Toxicol Sci. 2015 May;145(1):59-67. doi: 10.1093/toxsci/kfv017. Epub 2015 Jan 28.
34 Docetaxel induces apoptosis in hormone refractory prostate carcinomas during multiple treatment cycles. Br J Cancer. 2006 Jun 5;94(11):1592-8. doi: 10.1038/sj.bjc.6603129.
35 The proteasome inhibitor bortezomib enhances the activity of docetaxel in orthotopic human pancreatic tumor xenografts. Mol Cancer Ther. 2004 Jan;3(1):59-70.
36 Tubulin-targeting chemotherapy impairs androgen receptor activity in prostate cancer. Cancer Res. 2010 Oct 15;70(20):7992-8002. doi: 10.1158/0008-5472.CAN-10-0585. Epub 2010 Aug 31.
37 Anti-cancer effects of novel flavonoid vicenin-2 as a single agent and in synergistic combination with docetaxel in prostate cancer. Biochem Pharmacol. 2011 Nov 1;82(9):1100-9. doi: 10.1016/j.bcp.2011.07.078. Epub 2011 Jul 23.
38 Replication-dependent -H2AX formation is involved in docetaxel-induced apoptosis in NSCLC A549 cells. Oncol Rep. 2010 Nov;24(5):1297-305. doi: 10.3892/or_00000986.
39 Docetaxel induced cardiotoxicity. Heart. 2001 Aug;86(2):219. doi: 10.1136/heart.86.2.219.
40 Development and validation of the TGx-HDACi transcriptomic biomarker to detect histone deacetylase inhibitors in human TK6 cells. Arch Toxicol. 2021 May;95(5):1631-1645. doi: 10.1007/s00204-021-03014-2. Epub 2021 Mar 26.
41 [The mechanism of docetaxel-induced apoptosis in human lung cancer cells]. Zhonghua Zhong Liu Za Zhi. 2000 May;22(3):208-11.
42 Sensitization to docetaxel in prostate cancer cells by green tea and quercetin. J Nutr Biochem. 2015 Apr;26(4):408-15. doi: 10.1016/j.jnutbio.2014.11.017. Epub 2015 Jan 15.
43 Azidothymidine and cisplatin increase p14ARF expression in OVCAR-3 ovarian cancer cell line. Toxicol Appl Pharmacol. 2006 Oct 1;216(1):89-97. doi: 10.1016/j.taap.2006.04.015. Epub 2006 May 19.
44 Role of delta-like ligand-4 in chemoresistance against docetaxel in MCF-7 cells. Hum Exp Toxicol. 2017 Apr;36(4):328-338. doi: 10.1177/0960327116650006. Epub 2016 Jun 22.
45 Roles of CYP3A4, CYP3A5 and CYP2C8 drug-metabolizing enzymes in cellular cytostatic resistance. Chem Biol Interact. 2021 May 1;340:109448. doi: 10.1016/j.cbi.2021.109448. Epub 2021 Mar 26.
46 Focal adhesion kinase silencing augments docetaxel-mediated apoptosis in ovarian cancer cells. Clin Cancer Res. 2005 Dec 15;11(24 Pt 1):8829-36. doi: 10.1158/1078-0432.CCR-05-1728.
47 Enhanced Bax in oral SCC in relation to antitumor effects of chemotherapy. J Oral Pathol Med. 2005 Feb;34(2):93-9. doi: 10.1111/j.1600-0714.2004.00257.x.
48 Pharmacogenomics variation in drug metabolizing enzymes and transporters in relation to docetaxel toxicity in Lebanese breast cancer patients: paving the way for OMICs in low and middle income countries. OMICS. 2013 Jul;17(7):353-67. doi: 10.1089/omi.2013.0019. Epub 2013 Jun 11.
49 Specific kinesin expression profiles associated with taxane resistance in basal-like breast cancer. Breast Cancer Res Treat. 2012 Feb;131(3):849-58. doi: 10.1007/s10549-011-1500-8. Epub 2011 Apr 9.
50 PAR1-mediated NFkappaB activation promotes survival of prostate cancer cells through a Bcl-xL-dependent mechanism. J Cell Biochem. 2005 Oct 15;96(3):641-52. doi: 10.1002/jcb.20533.
51 Regulators of G-Protein signaling RGS10 and RGS17 regulate chemoresistance in ovarian cancer cells. Mol Cancer. 2010 Nov 2;9:289. doi: 10.1186/1476-4598-9-289.
52 Mitotic checkpoint genes, hsMAD2 and BubR1, in oesophageal squamous cancer cells and their association with 5-fluorouracil and cisplatin-based radiochemotherapy. Clin Oncol (R Coll Radiol). 2008 Oct;20(8):639-46. doi: 10.1016/j.clon.2008.06.010. Epub 2008 Aug 8.
53 EGFR mediates docetaxel resistance in human castration-resistant prostate cancer through the Akt-dependent expression of ABCB1 (MDR1). Arch Toxicol. 2015 Apr;89(4):591-605. doi: 10.1007/s00204-014-1275-x. Epub 2014 Jun 3.
54 [Antisense RNA targeting survivin enhances the chemosensitivity of LOVO/Adr cells to taxotere]. Zhonghua Wei Chang Wai Ke Za Zhi. 2005 Sep;8(5):455-8.
55 Manganese superoxide dismutase is a promising target for enhancing chemosensitivity of basal-like breast carcinoma. Antioxid Redox Signal. 2014 May 20;20(15):2326-46. doi: 10.1089/ars.2013.5295. Epub 2013 Nov 14.
56 HER-2/neu as a predictive marker in a population of advanced breast cancer patients randomly treated either with single-agent doxorubicin or single-agent docetaxel. Breast Cancer Res Treat. 2004 Aug;86(3):197-206. doi: 10.1023/B:BREA.0000036783.88387.47.
57 Epigenetic inactivation of the CHFR gene in cervical cancer contributes to sensitivity to taxanes. Int J Oncol. 2007 Oct;31(4):713-20.
58 Differential effect of anti-apoptotic genes Bcl-xL and c-FLIP on sensitivity of MCF-7 breast cancer cells to paclitaxel and docetaxel. Anticancer Res. 2005 May-Jun;25(3c):2367-79.
59 CD146 expression in human breast cancer cell lines induces phenotypic and functional changes observed in Epithelial to Mesenchymal Transition. PLoS One. 2012;7(8):e43752. doi: 10.1371/journal.pone.0043752. Epub 2012 Aug 30.
60 Proteomic identification of differentially expressed proteins associated with the multiple drug resistance in methotrexate-resistant human breast cancer cells. Int J Oncol. 2014 Jul;45(1):448-58.
61 KIF14 promotes AKT phosphorylation and contributes to chemoresistance in triple-negative breast cancer. Neoplasia. 2014 Mar;16(3):247-56, 256.e2. doi: 10.1016/j.neo.2014.03.008.
62 The prognostic gene CRABP2 affects drug sensitivity by regulating docetaxel-induced apoptosis in breast invasive carcinoma: A pan-cancer analysis. Chem Biol Interact. 2023 Mar 1;373:110372. doi: 10.1016/j.cbi.2023.110372. Epub 2023 Feb 2.
63 Association of the CYP1B1*3 allele with survival in patients with prostate cancer receiving docetaxel. Mol Cancer Ther. 2008 Jan;7(1):19-26. doi: 10.1158/1535-7163.MCT-07-0557. Epub 2008 Jan 9.
64 UGT-dependent regioselective glucuronidation of ursodeoxycholic acid and obeticholic acid and selective transport of the consequent acyl glucuronides by OATP1B1 and 1B3. Chem Biol Interact. 2019 Sep 1;310:108745. doi: 10.1016/j.cbi.2019.108745. Epub 2019 Jul 9.
65 Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
66 Inhibition of eEF-2 kinase sensitizes human nasopharyngeal carcinoma cells to lapatinib-induced apoptosis through the Src and Erk pathways.BMC Cancer. 2016 Oct 19;16(1):813.
67 Tarascon Pocket Pharmacopoeia 2018 Classic Shirt-Pocket Edition.
68 The role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactions. Drug Metab Dispos. 2008 Apr;36(4):695-701.
69 Mechanism-based inactivation of cytochrome P450 3A4 by lapatinib. Mol Pharmacol. 2010 Oct;78(4):693-703.
70 Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706.
71 The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res. 2005 Jan 1;65(1):18-25.
72 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.
73 P450 3A-catalyzed O-dealkylation of lapatinib induces mitochondrial stress and activates Nrf2. Chem Res Toxicol. 2016 May 16;29(5):784-96.
74 Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells. Oncogene. 2005 Sep 15;24(41):6213-21. doi: 10.1038/sj.onc.1208774.
75 CDK4/6 inhibition provides a potent adjunct to Her2-targeted therapies in preclinical breast cancer models. Genes Cancer. 2014 Jul;5(7-8):261-72. doi: 10.18632/genesandcancer.24.
76 Effects of lapatinib on cell proliferation and apoptosis in NB4 cells. Oncol Lett. 2018 Jan;15(1):235-242. doi: 10.3892/ol.2017.7342. Epub 2017 Nov 3.
77 The involvement of hepatic cytochrome P450s in the cytotoxicity of lapatinib. Toxicol Sci. 2023 Dec 21;197(1):69-78. doi: 10.1093/toxsci/kfad099.
78 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
79 Suppression of HER2/HER3-mediated growth of breast cancer cells with combinations of GDC-0941 PI3K inhibitor, trastuzumab, and pertuzumab. Clin Cancer Res. 2009 Jun 15;15(12):4147-56. doi: 10.1158/1078-0432.CCR-08-2814. Epub 2009 Jun 9.
80 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.
81 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.
82 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.
83 HLA-DQA1*02:01 is a major risk factor for lapatinib-induced hepatotoxicity in women with advanced breast cancer. J Clin Oncol. 2011 Feb 20;29(6):667-73. doi: 10.1200/JCO.2010.31.3197. Epub 2011 Jan 18.
84 Niclosamide inhibits epithelial-mesenchymal transition and tumor growth in lapatinib-resistant human epidermal growth factor receptor 2-positive breast cancer. Int J Biochem Cell Biol. 2016 Feb;71:12-23. doi: 10.1016/j.biocel.2015.11.014. Epub 2015 Nov 28.
85 Biologically active neutrophil chemokine pattern in tonsillitis.Clin Exp Immunol. 2004 Mar;135(3):511-8. doi: 10.1111/j.1365-2249.2003.02390.x.