Details of the Drug Combination

General Information of Drug Combination (ID: DCGP215)

Drug Combination Name
Lapatinib PD-0325901
Indication
Disease Entry Status REF
Carcinoma Investigative [1]
Component Drugs Lapatinib   DM3BH1Y PD-0325901   DM27D4J
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: OV90
Zero Interaction Potency (ZIP) Score: 3.44
Bliss Independence Score: 4.94
Loewe Additivity Score: 0.08
LHighest Single Agent (HSA) Score: 8.75

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Lapatinib
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Approved [2]
Gastroesophageal junction adenocarcinoma 2B71 Approved [3]
Melanoma 2C30 Approved [3]
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 [6]
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Inhibitor [6]
Eukaryotic elongation factor 2 kinase (eEF-2K) TT1QFLA EF2K_HUMAN Inhibitor [7]
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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 [8]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [9]
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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 [10]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [11]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [10]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Metabolism [11]
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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 [12]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [13]
Superoxide dismutase , mitochondrial (SOD2) OTIWXGZ9 SODM_HUMAN Increases Expression [14]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Increases Expression [14]
NAD(P)H dehydrogenase 1 (NQO1) OTZGGIVK NQO1_HUMAN Increases Expression [14]
Nuclear factor erythroid 2-related factor 2 (NFE2L2) OT0HENJ5 NF2L2_HUMAN Increases Activity [14]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Expression [15]
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Decreases Activity [12]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [16]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Decreases Expression [17]
DNA topoisomerase 1 (TOP1) OT51O0CF TOP1_HUMAN Decreases Expression [18]
DNA topoisomerase 2-alpha (TOP2A) OT6LPS08 TOP2A_HUMAN Decreases Expression [18]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [18]
Cyclin-A2 (CCNA2) OTPHHYZJ CCNA2_HUMAN Decreases Expression [16]
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_HUMAN Decreases Activity [19]
Receptor tyrosine-protein kinase erbB-3 (ERBB3) OTRSST0A ERBB3_HUMAN Decreases Activity [20]
Alanine aminotransferase 1 (GPT) OTOXOA0Q ALAT1_HUMAN Increases Secretion [21]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Decreases Expression [12]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Activity [16]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Activity [16]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Decreases Activity [12]
DNA replication licensing factor MCM7 (MCM7) OT6FXC6K MCM7_HUMAN Decreases Expression [16]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Increases Activity [18]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Increases Expression [12]
Caspase-7 (CASP7) OTAPJ040 CASP7_HUMAN Increases Activity [18]
Caspase-9 (CASP9) OTD4RFFG CASP9_HUMAN Increases Activity [18]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [17]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Decreases Activity [22]
GTPase KRas (KRAS) OT78QCN8 RASK_HUMAN Decreases Response To Substance [23]
HLA class II histocompatibility antigen, DQ alpha 1 chain (HLA-DQA1) OTC6GISG DQA1_HUMAN Increases ADR [24]
Zinc finger protein SNAI1 (SNAI1) OTDPYAMC SNAI1_HUMAN Decreases Response To Substance [25]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Increases Metabolism [18]
Cytochrome P450 3A7 (CYP3A7) OTTCDHHM CP3A7_HUMAN Increases Metabolism [18]
Transforming growth factor beta-1 proprotein (TGFB1) OTV5XHVH TGFB1_HUMAN Decreases Response To Substance [25]
Tenascin-X (TNXB) OTVBWAV5 TENX_HUMAN Increases ADR [24]
HLA class II histocompatibility antigen, DQ beta 1 chain (HLA-DQB1) OTVVI3UI DQB1_HUMAN Increases ADR [24]
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⏷ Show the Full List of 36 DOT(s)
Indication(s) of PD-0325901
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Phase 2 [4]
PD-0325901 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
MAPK/ERK kinase kinase (MAP3K) TTROQ37 NOUNIPROTAC Modulator [27]
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PD-0325901 Interacts with 84 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Increases Expression [28]
Cytochrome P450 3A5 (CYP3A5) OTSXFBXB CP3A5_HUMAN Increases Expression [28]
Cytochrome P450 3A7 (CYP3A7) OTTCDHHM CP3A7_HUMAN Increases Expression [28]
Nuclear receptor subfamily 0 group B member 2 (NR0B2) OT7UVICX NR0B2_HUMAN Decreases Expression [28]
Toll-like receptor 4 (TLR4) OTP7ML3S TLR4_HUMAN Decreases Expression [26]
Neuropilin-1 (NRP1) OTCGULYV NRP1_HUMAN Decreases Expression [26]
T-box transcription factor TBX3 (TBX3) OTM64N7K TBX3_HUMAN Decreases Expression [26]
Protein sprouty homolog 2 (SPRY2) OTH0CRCZ SPY2_HUMAN Decreases Expression [26]
Leupaxin (LPXN) OTUNV3CK LPXN_HUMAN Decreases Expression [26]
PR domain zinc finger protein 1 (PRDM1) OTQLSVBS PRDM1_HUMAN Decreases Expression [26]
Slit homolog 2 protein (SLIT2) OTLS2RJ4 SLIT2_HUMAN Decreases Expression [26]
Tumor necrosis factor ligand superfamily member 15 (TNFSF15) OTNGA2BW TNF15_HUMAN Decreases Expression [26]
Integrin beta-like protein 1 (ITGBL1) OTJDHE17 ITGBL_HUMAN Decreases Expression [26]
Urokinase-type plasminogen activator (PLAU) OTX0QGKK UROK_HUMAN Decreases Expression [26]
Interleukin-1 beta (IL1B) OT0DWXXB IL1B_HUMAN Decreases Expression [26]
Interstitial collagenase (MMP1) OTI4I2V1 MMP1_HUMAN Decreases Expression [26]
Glycophorin-C (GYPC) OTOEDR7O GLPC_HUMAN Decreases Expression [26]
Growth-regulated alpha protein (CXCL1) OT3WCTZV GROA_HUMAN Decreases Expression [26]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Decreases Expression [26]
Tissue factor pathway inhibitor (TFPI) OTA0FX16 TFPI1_HUMAN Decreases Expression [26]
Mast/stem cell growth factor receptor Kit (KIT) OTHUY3VZ KIT_HUMAN Decreases Expression [26]
Aminopeptidase N (ANPEP) OTP3WYFD AMPN_HUMAN Decreases Expression [26]
Integrin alpha-2 (ITGA2) OTPFL017 ITA2_HUMAN Decreases Expression [26]
Protein-glutamine gamma-glutamyltransferase 2 (TGM2) OT6MFOWF TGM2_HUMAN Decreases Expression [26]
Pentraxin-related protein PTX3 (PTX3) OTPXHRKU PTX3_HUMAN Decreases Expression [26]
5-hydroxytryptamine receptor 7 (HTR7) OT44DEWB 5HT7R_HUMAN Decreases Expression [26]
Glutaredoxin-1 (GLRX) OT0QHTAR GLRX1_HUMAN Decreases Expression [26]
17-beta-hydroxysteroid dehydrogenase type 2 (HSD17B2) OT3K7HY5 DHB2_HUMAN Decreases Expression [26]
ETS translocation variant 5 (ETV5) OTE2OBM4 ETV5_HUMAN Decreases Expression [26]
ETS translocation variant 4 (ETV4) OT8C98UZ ETV4_HUMAN Decreases Expression [26]
Transcription factor SOX-9 (SOX9) OTVDJFGN SOX9_HUMAN Decreases Expression [26]
ETS translocation variant 1 (ETV1) OT6PMJIK ETV1_HUMAN Decreases Expression [26]
Stanniocalcin-1 (STC1) OTGVVXYF STC1_HUMAN Decreases Expression [26]
Paired mesoderm homeobox protein 1 (PRRX1) OTTZK5G8 PRRX1_HUMAN Decreases Expression [26]
Epithelial membrane protein 1 (EMP1) OTSZHUHQ EMP1_HUMAN Decreases Expression [26]
Forkhead box protein G1 (FOXG1) OTAW57J4 FOXG1_HUMAN Decreases Expression [26]
ADP-ribosylation factor-like protein 4C (ARL4C) OTQ3QNNU ARL4C_HUMAN Decreases Expression [26]
Reelin (RELN) OTLKMW1O RELN_HUMAN Decreases Expression [26]
C-C motif chemokine 20 (CCL20) OTUCJY4N CCL20_HUMAN Decreases Expression [26]
A-kinase anchor protein 12 (AKAP12) OTCVRDDX AKA12_HUMAN Decreases Expression [26]
Urokinase plasminogen activator surface receptor (PLAUR) OTIRKKEQ UPAR_HUMAN Decreases Expression [26]
Dual specificity protein phosphatase 4 (DUSP4) OT6WAO12 DUS4_HUMAN Decreases Expression [26]
Semaphorin-3A (SEMA3A) OTQJSV7W SEM3A_HUMAN Decreases Expression [26]
Monocyte to macrophage differentiation factor (MMD) OTB5I4OC PAQRB_HUMAN Decreases Expression [26]
Syntaxin-1A (STX1A) OTSBUZB4 STX1A_HUMAN Decreases Expression [26]
Dual specificity protein phosphatase 6 (DUSP6) OT4H6RKW DUS6_HUMAN Decreases Expression [26]
Kinesin-like protein KIF24 (KIF24) OTJTA5V3 KIF24_HUMAN Decreases Expression [26]
Anoctamin-1 (ANO1) OTSREUNI ANO1_HUMAN Decreases Expression [26]
NADH-cytochrome b5 reductase 2 (CYB5R2) OTTLM7XN NB5R2_HUMAN Decreases Expression [26]
Dynamin-binding protein (DNMBP) OTMHH14H DNMBP_HUMAN Decreases Expression [26]
Sialic acid-binding Ig-like lectin 15 (SIGLEC15) OTON4K9S SIG15_HUMAN Decreases Expression [26]
UPF0606 protein KIAA1549L (KIAA1549L) OT80HUVY K154L_HUMAN Decreases Expression [26]
Neuron navigator 3 (NAV3) OT97M1TR NAV3_HUMAN Decreases Expression [26]
Dedicator of cytokinesis protein 4 (DOCK4) OTH3XY8B DOCK4_HUMAN Decreases Expression [26]
Transmembrane protein 156 (TMEM156) OTH7YJID TM156_HUMAN Decreases Expression [26]
Tribbles homolog 2 (TRIB2) OTHSX3MX TRIB2_HUMAN Decreases Expression [26]
Hyaluronan synthase 2 (HAS2) OTTD3PAL HYAS2_HUMAN Decreases Expression [26]
Neuronal cell adhesion molecule (NRCAM) OT80HHQ2 NRCAM_HUMAN Decreases Expression [26]
Discoidin, CUB and LCCL domain-containing protein 2 (DCBLD2) OTB71I02 DCBD2_HUMAN Decreases Expression [26]
Formin-like protein 2 (FMNL2) OT9OVWCV FMNL2_HUMAN Decreases Expression [26]
Monoglyceride lipase (MGLL) OT5ES4IE MGLL_HUMAN Decreases Expression [26]
Paternally-expressed gene 3 protein (PEG3) OTHQW98S PEG3_HUMAN Decreases Expression [26]
Disintegrin and metalloproteinase domain-containing protein 19 (ADAM19) OTH88TXU ADA19_HUMAN Decreases Expression [26]
Sodium-dependent neutral amino acid transporter B(0)AT2 (SLC6A15) OTGMPVNR S6A15_HUMAN Decreases Expression [26]
Endothelial cell-specific molecule 1 (ESM1) OT331Y8V ESM1_HUMAN Decreases Expression [26]
Interleukin-1 receptor accessory protein-like 1 (IL1RAPL1) OTW3T4B2 IRPL1_HUMAN Decreases Expression [26]
Neurotrimin (NTM) OTHF0UQU NTRI_HUMAN Decreases Expression [26]
Histone deacetylase 9 (HDAC9) OTO8O0LF HDAC9_HUMAN Decreases Expression [26]
Type 2 lactosamine alpha-2,3-sialyltransferase (ST3GAL6) OTB17Q43 SIA10_HUMAN Decreases Expression [26]
Bcl-2-like protein 11 (BCL2L11) OTNQQWFJ B2L11_HUMAN Increases Expression [29]
Forkhead box protein O3 (FOXO3) OTHXQG4P FOXO3_HUMAN Increases Expression [30]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [31]
DNA excision repair protein ERCC-1 (ERCC1) OTNPYQHI ERCC1_HUMAN Decreases Expression [32]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [33]
Fos-related antigen 1 (FOSL1) OT9YTYMB FOSL1_HUMAN Decreases Expression [34]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Phosphorylation [35]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Phosphorylation [35]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Increases Phosphorylation [33]
Small ribosomal subunit protein eS6 (RPS6) OTT4D1LN RS6_HUMAN Decreases Phosphorylation [36]
Heat shock factor protein 1 (HSF1) OTYNJ4KP HSF1_HUMAN Decreases Activity [37]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) OT2YYI1A MCL1_HUMAN Decreases Expression [29]
Bcl-2 homologous antagonist/killer (BAK1) OTDP6ILW BAK_HUMAN Increases Expression [33]
DNA repair endonuclease XPF (ERCC4) OTFIOPG1 XPF_HUMAN Increases Expression [32]
Ras-related C3 botulinum toxin substrate 1 (RAC1) OTKRO61U RAC1_HUMAN Affects Response To Substance [38]
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⏷ Show the Full List of 84 DOT(s)

Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Breast and ovarian cancer syndrome DCN0E7E UWB1289 Investigative [1]
Breast and ovarian cancer syndrome DCL98IZ UWB1289+BRCA1 Investigative [1]
Breast carcinoma DCZY7TD ZR751 Investigative [1]
Breast carcinoma DC909I2 KPL1 Investigative [1]
Breast carcinoma DCBGYAK OCUBM Investigative [1]
Carcinoma DCK8EQV EFM192B Investigative [1]
Carcinoma DCMEXFB MDAMB436 Investigative [1]
Colon adenocarcinoma DCJSORG LOVO Investigative [1]
Colon carcinoma DCJ5A6D RKO Investigative [1]
Invasive ductal carcinoma DCJ3U73 T-47D Investigative [1]
Rectal adenocarcinoma DCUCGP5 SW837 Investigative [1]
Adenocarcinoma DCJLIXT CAOV3 Investigative [39]
Adenocarcinoma DCQDUXE OVCAR3 Investigative [39]
Adenocarcinoma DCI4N4J A427 Investigative [39]
Adenocarcinoma DCN9156 NCIH1650 Investigative [39]
Adenocarcinoma DC7Q9B6 NCIH2122 Investigative [39]
Adenocarcinoma DCWPX30 NCIH23 Investigative [39]
Adenocarcinoma DC078BX NCIH520 Investigative [39]
Adenocarcinoma DCQMU7N COLO320DM Investigative [39]
Adenocarcinoma DCWGBCD DLD1 Investigative [39]
Adenocarcinoma DCHBSZJ HT29 Investigative [39]
Amelanotic melanoma DC5OTT4 A2058 Investigative [39]
Ewing sarcoma-peripheral primitive neuroectodermal tumour DCO4MNH ES2 Investigative [39]
Germ cell tumour DCZ9V28 PA1 Investigative [39]
Large cell lung carcinoma DCGNIMN NCI-H460 Investigative [39]
Malignant melanoma DCGTD23 HT144 Investigative [39]
Malignant melanoma DCS4RNP RPMI7951 Investigative [39]
Malignant melanoma DCFVMNF UACC62 Investigative [39]
Ovarian endometrioid adenocarcinoma DCSAETK A2780 Investigative [39]
Ovarian serous cystadenocarcinoma DC0YFC7 SK-OV-3 Investigative [39]
Prostate carcinoma DCAII4H LNCAP Investigative [39]
Prostate carcinoma DCMOFZ7 VCAP Investigative [39]
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⏷ Show the Full List of 32 DrugCom(s)

References

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38 Genome and transcriptome sequencing of lung cancers reveal diverse mutational and splicing events. Genome Res. 2012 Dec;22(12):2315-27. doi: 10.1101/gr.140988.112. Epub 2012 Oct 2.
39 Loss of function mutations in VARS encoding cytoplasmic valyl-tRNA synthetase cause microcephaly, seizures, and progressive cerebral atrophy.Hum Genet. 2018 Apr;137(4):293-303. doi: 10.1007/s00439-018-1882-3. Epub 2018 Apr 24.