Page last updated: 2024-09-05

lapatinib and gefitinib

lapatinib has been researched along with gefitinib in 130 studies

Compound Research Comparison

Studies
(lapatinib)
Trials
(lapatinib)
Recent Studies (post-2010)
(lapatinib)
Studies
(gefitinib)
Trials
(gefitinib)
Recent Studies (post-2010) (gefitinib)
1,9193051,4425,2315662,919

Protein Interaction Comparison

ProteinTaxonomylapatinib (IC50)gefitinib (IC50)
epidermal growth factor receptor isoform a precursorHomo sapiens (human)0.004
Cyclin-G-associated kinaseHomo sapiens (human)0.42
Multidrug resistance-associated protein 4Homo sapiens (human)4.6
Tyrosine-protein kinase ABL1Homo sapiens (human)1.2
Epidermal growth factor receptorHomo sapiens (human)0.3676
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)0.5699
Cytochrome P450 1A2Homo sapiens (human)0.151
Cytochrome P450 2E1Homo sapiens (human)0.46
Proto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)1.7
Tyrosine-protein kinase HCKHomo sapiens (human)0.11
Quinolone resistance protein NorAStaphylococcus aureus9.7
Cytochrome P450 2C8Homo sapiens (human)0.151
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)1.1
Serine/threonine-protein kinase B-rafHomo sapiens (human)2
Receptor tyrosine-protein kinase erbB-3Homo sapiens (human)0.008
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)0.281
Cytochrome P450 2C19Homo sapiens (human)0.151
Type-1 angiotensin II receptorOryctolagus cuniculus (rabbit)0.0073
Vascular endothelial growth factor receptor 2Homo sapiens (human)0.9742
Ephrin type-B receptor 4Homo sapiens (human)1
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)0.001
Transcription factor p65Homo sapiens (human)0.055
Receptor tyrosine-protein kinase erbB-4Homo sapiens (human)0.086
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)1.29

Research

Studies (130)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's29 (22.31)29.6817
2010's87 (66.92)24.3611
2020's14 (10.77)2.80

Authors

AuthorsStudies
Cockerill, S; Guntrip, SB; Lackey, K; Rusnak, D; Smith, K; Vanderwall, D; Wood, E; Zhang, YM1
Atteridge, CE; Azimioara, MD; Benedetti, MG; Biggs, WH; Carter, TA; Ciceri, P; Edeen, PT; Fabian, MA; Floyd, M; Ford, JM; Galvin, M; Gerlach, JL; Grotzfeld, RM; Herrgard, S; Insko, DE; Insko, MA; Lai, AG; Lélias, JM; Lockhart, DJ; Mehta, SA; Milanov, ZV; Patel, HK; Treiber, DK; Velasco, AM; Wodicka, LM; Zarrinkar, PP1
Atteridge, CE; Campbell, BT; Chan, KW; Ciceri, P; Davis, MI; Edeen, PT; Faraoni, R; Floyd, M; Gallant, P; Herrgard, S; Hunt, JP; Karaman, MW; Lockhart, DJ; Milanov, ZV; Morrison, MJ; Pallares, G; Patel, HK; Pritchard, S; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Da Settimo, F; La Motta, C; Martinelli, A; Nerini, E; Sartini, S; Tuccinardi, T1
Morphy, R1
Afshari, CA; Eschenberg, M; Hamadeh, HK; Lee, PH; Lightfoot-Dunn, R; Morgan, RE; Qualls, CW; Ramachandran, B; Trauner, M; van Staden, CJ1
Ekins, S; Williams, AJ; Xu, JJ1
Hajduk, PJ; Johnson, EF; Kifle, L; Merta, PJ; Metz, JT; Soni, NB1
Russu, WA; Shallal, HM1
Ciceri, P; Davis, MI; Herrgard, S; Hocker, M; Hunt, JP; Pallares, G; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Dohi, K; Haga, N; Iguchi, M; Inoue, M; Matsuo, K; Murashi, T; Ohara, T; Omori, N; Sentou, J; Shiota, T; Suzuki, N; Wada, T; Watanabe, F; Yari, H1
Al-Mazaideh, GM; Erdmann, F; Göllner, C; Rohe, A; Schmidt, M; Sippl, W; Wichapong, K1
Buckley, DB; Funk, RS; Hensley, T; Kazmi, F; Loewen, GJ; Parkinson, A; Pope, C1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Aleo, MD; Bonin, PD; Luo, Y; Potter, DM; Swiss, R; Will, Y1
Bullock, AN; Canning, P; Choi, S; Cuny, GD; Mohedas, AH; Sanvitale, CE; Wang, Y; Xing, X; Yu, PB1
Bugge, S; Hoff, BH; Moen, IU; Sundby, E; Sylte, KO1
Abou El Ella, DA; Aly, RM; El-Motwally, AM; Ibrahim, DA1
Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K1
Abouzid, KA; Doctor, ZM; Farag, NA; Galanis, A; Jänne, PA; Lasheen, DS; Mowafy, S; Paranal, RM1
Chen, S; Chen, YZ; Ding, C; Hu, G; Jiang, Y; Li, L; Tan, C; Zhang, C; Zhang, W1
Chen, L; Li, B; Liu, J; Wang, W; Zhang, Y; Zhao, L1
Abouzid, KAM; Lasheen, DS; Milik, SN; Serya, RAT1
Chen, L; Gao, H; Li, B; Li, X; Liu, J; Liu, R; Wang, W; Zhang, Y; Zhao, L1
Aiche, S; Bassermann, F; Becker, W; Canevari, G; Casale, E; Depaolini, SR; Ehrlich, HC; Felder, ER; Feuchtinger, A; Garz, AK; Gohlke, BO; Götze, K; Greif, PA; Hahne, H; Heinzlmeir, S; Helm, D; Huenges, J; Jeremias, I; Kayser, G; Klaeger, S; Koch, H; Koenig, PA; Kramer, K; Kuster, B; Médard, G; Meng, C; Petzoldt, S; Polzer, H; Preissner, R; Qiao, H; Reinecke, M; Reiter, K; Rueckert, L; Ruland, J; Ruprecht, B; Schlegl, J; Schmidt, T; Schneider, S; Schoof, M; Spiekermann, K; Tõnisson, N; Vick, B; Vooder, T; Walch, A; Wilhelm, M; Wu, Z; Zecha, J; Zolg, DP1
Abouzid, KAM; Esmat, A; Hossam, M; Ismail, NSM; Lasheen, DS; Mansour, AM; Singab, ANB1
Chen, L; Li, B; Li, X; Wang, W; Xu, H; Zhang, X; Zhang, Y; Zhao, L1
Abbas, SY; Ammar, YA; Belal, A; Mehany, ABM; Mohamed, YA; Ragab, A; Sh El-Sharief, AM1
Ju, Y; Li, C; Qiao, R; Wu, J; Yuan, X; Zhang, G; Zhao, L1
Guo, Y; He, J; Li, Y; Liu, M; Liu, Y; Xiao, J; Yu, W; Zhang, Q1
Das, D; Hong, J1
Asquith, CRM; Drewry, DH; East, MP; Havener, TM; Johnson, GL; Laitinen, T; Morris, DC; Naegeli, KM; Wells, CI; Zuercher, WJ1
Basetti, V; Keesara, M; Maiti, P; Mansour, TS; Moghudula, AG; Pallepati, RR; Potluri, V1
Asquith, CRM; Crona, DJ; Fleck, N; Grundner, C; Torrice, CD; Zuercher, WJ1
Jia, J; Sun, H; Sun, M; Wang, F1
Abd El-Karim, SS; Ahmed, NS; Anwar, MM; El-Hallouty, SM; Srour, AM1
Bauer, S; Baumann, M; Becker, C; Grabe, T; Hardick, J; Hodson, L; Jeyakumar, K; Ketzer, J; Keul, M; Kirschner, T; Klövekorn, P; Lategahn, J; Müller, MP; Niggenaber, J; Rauh, D; Terheyden, S; Tumbrink, HL; Unger, A; van Otterlo, WAL; Weisner, J1
Bansal, R; Malhotra, A1
Chen, XB; Wang, S; Wang, SQ; Yu, B; Yuan, XH; Zhao, W1
Cai, Z; Ghaleb, H; Huang, W; Jiang, Y; Liu, Y; Qian, H; Qiu, Q; Shi, W; Yin, Z; Zhang, P; Zhou, J; Zou, F1
Delabio, LC; Dutra, JP; Hembecker, M; Kita, DH; Moure, VR; Pereira, GDS; Scheiffer, G; Valdameri, G; Zattoni, IF1
Berlin, JD; Lockhart, AC; Lockhart, C1
Earp, HS; Gregory, CW; Liu, Y; Majumder, S; McCall, W; Mohler, JL; Sartor, CI; Whang, YE1
Aglietta, M; Montemurro, F; Valabrega, G1
Marais, R; Niculescu-Duvaz, D; Springer, C; Whittaker, S1
Boggon, TJ; Eck, MJ; Greulich, H; Li, Y; Meyerson, M; Woo, MS; Yun, CH1
Andersson, M; Nielsen, DL1
Campone, M; Coudert, B; Favier, L; Ferrant, E; Fumoleau, P; Mayer, F1
Alligood, K; Cable, L; Carter, HL; Gallagher, KT; Gilmer, TM; Rusnak, D; Shewchuk, L; Spehar, G; Truesdale, AT; Woldu, E; Wood, ER1
Giordano, S; Petrelli, A1
Bang, YJ; Han, SW; Im, SA; Kim, HP; Kim, SH; Kim, TY; Oh, DY1
Caldara, A; Graiff, C; Mandarà, M; Pedersini, R; Sava, T; Vattemi, E1
Conaway, M; Gioeli, D; Theodorescu, D; Weber, MJ; Wu, Z1
Becker, M; Börgermann, C; Rose, A; Rübben, H; Vom Dorp, F1
Agulnik, M; Wang, LX1
Antonacopoulou, A; Floratou, K; Giannopoulou, E; Kalofonos, HP; Papavassiliou, AG1
Loeffler-Ragg, J; Schwentner, I; Sprinzl, GM; Zwierzina, H1
Abidoye, O; Salgia, R; Sattler, M1
Casalini, P; Croce, CM; Di Leva, G; Iorio, MV; Ménard, S; Merlo, A; Piovan, C; Tagliabue, E; Triulzi, T1
Cohen, EE; Cooper, JB1
Arteaga, CL; Boimel, PJ; Coniglio, SJ; Hynes, NE; Kedrin, D; Segall, JE; Wyckoff, J1
Clynes, M; Collins, DM; Crown, J; Devery, A; O'Connor, R; O'Donovan, N; O'Driscoll, L; O'Sullivan, F1
Bang, YJ; Han, SW; Hur, HS; Im, SA; Kim, HP; Kim, JW; Kim, TY; Lee, JH; Oh, DY; Park, J; Yoon, YK1
Cohen, EE; Halpern, AB; Kasza, K; Kocherginsky, M; Vokes, EE; Williams, R1
Gelderblom, H; Guchelaar, HJ; van Erp, NP1
Banat, GA; Cornitescu, T; Dahal, BK; Dumitrascu, R; Ghofrani, HA; Grimminger, F; Kosanovic, D; Pullamsetti, SS; Schermuly, RT; Seeger, W; Tretyn, A; Voswinckel, R; Weissmann, N1
Carter, CA; Giaccone, G; Kelly, RJ1
D'Alessio, A; De Luca, A; Gallo, M; Lamura, L; Maiello, MR; Napolitano, M; Normanno, N; Rachiglio, AM1
Gutteridge, E; Robertson, JF1
Anderton, J; Barlaam, B; Beck, S; Callis, R; Davenport, S; Grosios, K; Hickinson, DM; Klinowska, T; Marshall, G; Mills, E; Ogilvie, D; Smith, P; Speake, G; Trigwell, C; Vincent, J; Wilkinson, RW1
Byrne, AT; Crown, J; Gallagher, WM; McGee, S; O'Connor, AE; O'Donovan, N1
Cheng, Y; Hait, WN; Li, H; Niu, T; Ren, X; Yang, J1
Amadori, D; Brigliadori, G; Carloni, S; Fabbri, F; Silvestrini, R; Ulivi, P; Zoli, W1
Cufí, S; Del Barco, S; Martin-Castillo, B; Menendez, JA; Oliveras-Ferraros, C; Vazquez-Martin, A1
Brunner, C; Hubalek, M; Marth, C; Matthä, K1
Bannykh, S; Cooper, O; Fukuoka, H; Melmed, S; Mizutani, J; Ren, SG; Tong, Y1
Angelo, A; Azzariti, A; Colucci, G; Porcelli, L; Quatrale, AE; Silvestris, N1
Baselga, J; Chandarlapaty, S; Grbovic-Huezo, O; Majumder, PK; Rodrik-Outmezguine, V; Rosen, N; Sawai, A; Scaltriti, M; Serra, V1
Beck, JF; Kurtze, I; Sonnemann, J1
Durbin, JE; Koromilas, AE; Muller, WJ; Raven, JF; Tremblay, ML; Wang, S; Williams, V1
Anadkat, MJ; Balagula, Y; Lacouture, ME; Wu, PA1
Di Gion, P; Doroshyenko, O; Fuhr, U; Scheffler, M; Wolf, J1
Pandiella, A; Sánchez-Martín, M1
Conzelmann, H; Kleiman, LB; Lauffenburger, DA; Maiwald, T; Sorger, PK1
Liebmann, C; Weisheit, S1
Bignon, YJ; Cayre, A; El Guerrab, A; Nemlin, CC; Penault-Llorca, F; Rossignol, F; Vigier, F; Zegrour, R1
Hasegawa, T; Hirakawa, K; Matsuzaki, T; Qiu, H; Yashiro, M; Zhang, X1
A'Hern, R; Anderson, H; Bliss, J; Dowsett, M; Dunbier, A; Evans, A; Ghazoui, Z; Iskender, A; Johnson, L; Pinhel, I; Robertson, J; Robison, L; Salter, J; Skene, T; Smith, I; Wilcox, M1
Lee, SH1
He, XM; Li, Y; Zhang, LY1
Arkhipov, A; Dror, RO; Eastwood, MP; Jumper, J; Kim, ET; Kuriyan, J; Shan, Y; Shaw, DE; Zhang, X1
Buechner, SA; Erne, P; Joshi, MB; Kyriakakis, E; Maslova, K; Pfaff, D; Philippova, M; Resink, TJ1
Chen, Y; Han, B; Jia, J; Jiang, Y; Ma, X; Tan, C; Wei, X; Zhang, J; Zhu, F1
Bissell, MJ; Furuta, S; Kenny, PA; Lee, SY; Lenburg, ME; Meier, R; Xu, R1
Choowongkomon, K; Gleeson, MP; Songtawee, N1
Fujii, H; Jimmy So, A; Kono, K; Mimura, K; Shabbir, A; Yong, WP1
Casanovas, O; Castillo-Ávila, W; Condom, E; Garcia Del Muro, X; Germà, JR; Graupera, M; Hernández-Losa, J; Juliachs, M; Pandiella, A; Piulats, JM; Teixidó, C; Vidal, A; Villanueva, A; Viñals, F1
Corominas-Faja, B; Cufí, S; Martin-Castillo, B; Menendez, JA; Oliveras-Ferraros, C; Urruticoechea, A; Vazquez-Martin, A1
Contini, A; Erne, P; Ferri, N; Frachet, A; Kyriakakis, E; Maslova, K; Pfaff, D; Philippova, M; Resink, TJ1
Baradia, D; Misra, A; Patil, S; Vhora, I; Yewale, C1
Fu, Y; He, Q; Lin, G; Lou, J; Ma, J; Wu, Y; Yang, B; Zheng, L; Zhu, H1
Cho, SY; Choi, J; Hwang, JJ; Jang, SJ; Kim, CS; Lee, G; Lee, JH; Lee, SW; Lim, C; Seo, J; Song, JY1
Bhosle, J; Hartley, JA; Hochhauser, D; Kiakos, K; Makris, A; Porter, AC; Wu, J1
Mehta, A; Tripathy, D1
Chen, CH; Chen, JY; Chen, WS; Chen, YJ; Chien, PH; Hsia, TC; Huang, WC; Liu, SH; Shih, CY; Tu, CY; Wei, YL; Yeh, MH; Yu, MC; Yu, YL1
Fu, X; Giuliano, M; Klinowska, T; Morrison, G; Nanda, S; Osborne, CK; Rimawi, MF; Schiff, R; Shea, M; Wang, T1
Axel, U; Baska, F; Greff, Z; Gyulavári, P; Ibolya, K; Kéri, G; Orfi, L; Peták, I; Szántai, KC; Szokol, B; Vantus, T; Zoltán, O1
He, Z; Li, J; Li, X; Lin, B; Tang, X; Zhou, K1
Chang, JC; Colon-Otero, G; Dave, B; Patel, TA; Perez, EA; Rodriguez, AA1
Chang, YH; Hong, SE; Hong, SI; Hong, YJ; Jin, HO; Kim, B; Kim, CS; Kim, JH; Kim, JY; Lee, JK; Park, IC; Park, JA1
Aderhold, C; Erben, P; Faber, A; Hoermann, K; Hofheinz, RD; Schultz, JD; Umbreit, C; Weiss, C; Wenzel, A1
Cosmai, L; Gallieni, M; Porta, C1
Ding, X; Li, Y; Mao, W; Meng, X; Tang, H; Wang, X; Xie, S; Yang, H1
Jiang, M; Liu, TT; Shen, GF; Shi, JH; Wang, Q1
Chan, KK; Furness, S; Glenny, AM; Wakeford, H; Weldon, JC; Worthington, HV1
Byrn, S; Chen, X; Fang, K; Lubach, JW; Nie, H; Smith, D; Song, Y; Su, Z; Yang, X; Zemlyanov, D1
Broutin, S; Gil, S; Jovelet, C; Mir, O; Paci, A1
Chang, TY; Chen, PS; Hsu, HP; Huang, MT; Kuo, KT; Lai, HH; Li, JN; Lyu, YJ; Su, CM; Su, JL1
Kannan, N; Katiyar, S; Ruan, Z1
Jensen, RT; Mantey, SA; Moody, TW; Moreno, P; Ramos-Alvarez, I; Ridnour, L; Wink, D1
Ben-Shlomo, A; Cooper, O1
Bode, A; Grubbs, CJ; Juliana, MM; Lubet, RA; Moeinpour, F; Steele, VE1
Kim, HS; Kim, JY; Yoon, S1
Freeman, MR; Hemler, ME; Sharma, C; Steen, H; Yang, W1
Borrero-García, LD; Del Mar Maldonado, M; Dharmawardhane, S; Grafals-Ruiz, N; Medina-Velázquez, J; Troche-Torres, AL; Velazquez, L1
Al-Zubaidi, Y; Bourget, K; Murray, M; Rahman, MK; Tam, S; Zhou, F1
Lucia, F; Nicolas, E1
Guo, R; Guo, X; Guo, Z; Kang, J; Zhang, H; Zhu, X1
Acconcia, F1
Tan, J; Xu, M; Zhong, Z1

Reviews

33 review(s) available for lapatinib and gefitinib

ArticleYear
Selectively nonselective kinase inhibition: striking the right balance.
    Journal of medicinal chemistry, 2010, Feb-25, Volume: 53, Issue:4

    Topics: Animals; Antineoplastic Agents; Drug Design; Drug Discovery; Humans; Protein Binding; Protein Kinase Inhibitors; Structure-Activity Relationship

2010
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
    Drug discovery today, 2016, Volume: 21, Issue:4

    Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk

2016
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.
    European journal of medicinal chemistry, 2017, Dec-15, Volume: 142

    Topics: Animals; Antineoplastic Agents; Drug Design; Drug Resistance, Neoplasm; ErbB Receptors; Gene Amplification; Humans; Models, Molecular; Neoplasms; Point Mutation; Protein Domains; Protein Kinase Inhibitors; Receptor, ErbB-2

2017
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.
    Bioorganic & medicinal chemistry, 2019, 02-01, Volume: 27, Issue:3

    Topics: Animals; Antineoplastic Agents; Cell Proliferation; Humans; Neoplasms; Protein Kinase Inhibitors; Protein Kinases; Quinazolines

2019
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.
    European journal of medicinal chemistry, 2019, May-15, Volume: 170

    Topics: Animals; Antineoplastic Agents; Chemistry Techniques, Synthetic; Humans; Neoplasms; Protein Kinase Inhibitors; Quinazolines

2019
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
    European journal of medicinal chemistry, 2021, Feb-05, Volume: 211

    Topics: Animals; Antineoplastic Agents; Cell Proliferation; Enzyme Inhibitors; Humans; Molecular Structure; Neoplasms; Quinazolines

2021
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.
    European journal of medicinal chemistry, 2021, Mar-15, Volume: 214

    Topics: Antineoplastic Agents; Bridged Bicyclo Compounds, Heterocyclic; Humans; Molecular Structure; Neoplasms; Pyrimidines; United States; United States Food and Drug Administration

2021
Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
    European journal of medicinal chemistry, 2022, Jul-05, Volume: 237

    Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; Breast Neoplasms; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Female; Humans; Neoplasm Proteins; Neoplastic Stem Cells

2022
The epidermal growth factor receptor as a target for colorectal cancer therapy.
    Seminars in oncology, 2005, Volume: 32, Issue:1

    Topics: Aminoquinolines; Aniline Compounds; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Cell Transformation, Neoplastic; Cetuximab; Colorectal Neoplasms; Disease Progression; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Organic Chemicals; Panitumumab; Prognosis; Pyrimidines; Pyrroles; Quinazolines; Signal Transduction

2005
Trastuzumab: mechanism of action, resistance and future perspectives in HER2-overexpressing breast cancer.
    Annals of oncology : official journal of the European Society for Medical Oncology, 2007, Volume: 18, Issue:6

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Breast Neoplasms; Drug Resistance, Neoplasm; Female; Gefitinib; Gene Expression Regulation, Neoplastic; Genes, erbB-2; Humans; Lapatinib; Neovascularization, Pathologic; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Quinazolines; Receptor, ErbB-2; Trastuzumab

2007
[Molecular targeted therapies for metastatic breast cancer. Monoclonal antibodies and tyrosine kinase inhibitors].
    Ugeskrift for laeger, 2007, Sep-10, Volume: 169, Issue:37

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Humans; Lapatinib; Protein Kinase Inhibitors; Quinazolines; Receptors, Vascular Endothelial Growth Factor; Trastuzumab

2007
[Targeting ErbB receptors in breast cancer].
    Bulletin du cancer, 2007, Volume: 94, Issue:7 Suppl

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Cetuximab; Chemotherapy, Adjuvant; Clinical Trials as Topic; Erlotinib Hydrochloride; Female; Gefitinib; Humans; Lapatinib; Quinazolines; Receptor Protein-Tyrosine Kinases; Receptor, ErbB-2; Signal Transduction; Trastuzumab

2007
From single- to multi-target drugs in cancer therapy: when aspecificity becomes an advantage.
    Current medicinal chemistry, 2008, Volume: 15, Issue:5

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Benzamides; Benzenesulfonates; Bevacizumab; Cetuximab; Clinical Trials as Topic; Enzyme Inhibitors; Erlotinib Hydrochloride; Gefitinib; Humans; Imatinib Mesylate; Indoles; Lapatinib; Neoplasms; Neovascularization, Pathologic; Niacinamide; Phenylurea Compounds; Piperazines; Piperidines; Protein-Tyrosine Kinases; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Receptor Protein-Tyrosine Kinases; Sorafenib; Sunitinib; Trastuzumab

2008
Systemic therapies for recurrent and/or metastatic salivary gland cancers.
    Expert review of anticancer therapy, 2008, Volume: 8, Issue:3

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Antineoplastic Agents, Hormonal; Benzamides; Boronic Acids; Bortezomib; Cetuximab; Gefitinib; Humans; Imatinib Mesylate; Lapatinib; Neoplasm Metastasis; Neoplasm Recurrence, Local; Palliative Care; Piperazines; Pyrazines; Pyrimidines; Quinazolines; Salivary Gland Neoplasms; Trastuzumab

2008
EGFR inhibition as a therapy for head and neck squamous cell carcinoma.
    Expert opinion on investigational drugs, 2008, Volume: 17, Issue:10

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Carcinoma, Squamous Cell; Cetuximab; Clinical Trials as Topic; Combined Modality Therapy; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Gene Dosage; Head and Neck Neoplasms; Humans; Lapatinib; Protein Kinase Inhibitors; Quinazolines; Signal Transduction

2008
EGFR-targeted therapeutics: focus on SCCHN and NSCLC.
    TheScientificWorldJournal, 2008, Sep-21, Volume: 8

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Bevacizumab; Carcinoma, Non-Small-Cell Lung; Carcinoma, Squamous Cell; Cetuximab; Clinical Trials as Topic; Combined Modality Therapy; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Head and Neck Neoplasms; Humans; Lapatinib; Lung Neoplasms; Panitumumab; Protein Kinase Inhibitors; Quinazolines

2008
Mechanisms of resistance to EGFR inhibitors in head and neck cancer.
    Head & neck, 2009, Volume: 31, Issue:8

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Carcinoma, Squamous Cell; Cetuximab; Drug Resistance, Neoplasm; ErbB Receptors; Female; Gefitinib; Head and Neck Neoplasms; Humans; Lapatinib; Male; Prognosis; Protein Kinase Inhibitors; Quinazolines; Risk Assessment; Signal Transduction; Treatment Outcome

2009
Clinical pharmacokinetics of tyrosine kinase inhibitors.
    Cancer treatment reviews, 2009, Volume: 35, Issue:8

    Topics: Administration, Oral; Antineoplastic Agents; Benzamides; Benzenesulfonates; Biological Availability; Cytochrome P-450 Enzyme System; Dasatinib; Drug Interactions; Erlotinib Hydrochloride; Gefitinib; Humans; Imatinib Mesylate; Indoles; Intestinal Absorption; Lapatinib; Niacinamide; Phenylurea Compounds; Piperazines; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Thiazoles; Tissue Distribution

2009
Small-molecule inhibitors of the human epidermal receptor family.
    Expert opinion on investigational drugs, 2009, Volume: 18, Issue:12

    Topics: Antineoplastic Agents; Clinical Trials as Topic; Drug Delivery Systems; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Models, Biological; Molecular Structure; Neoplasms; Protein Kinase Inhibitors; Quinazolines

2009
Resistance to HER2-targeted therapy: mechanisms of trastuzumab resistance and possible strategies to overcome unresponsiveness to treatment.
    Wiener medizinische Wochenschrift (1946), 2010, Volume: 160, Issue:19-20

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Apoptosis; Breast Neoplasms; Cell Division; Drug Delivery Systems; Drug Resistance, Neoplasm; Female; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Phosphatidylinositol 3-Kinase; Prognosis; PTEN Phosphohydrolase; Quinazolines; Receptor, ErbB-2; Signal Transduction; Trastuzumab

2010
EGFR tyrosine kinases inhibitors in cancer treatment: in vitro and in vivo evidence.
    Frontiers in bioscience (Landmark edition), 2011, 01-01, Volume: 16, Issue:5

    Topics: Antineoplastic Agents; Apoptosis; Cell Division; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Neoplasm Invasiveness; Neoplasm Metastasis; Neoplasms; Neovascularization, Pathologic; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Signal Transduction

2011
Prophylaxis and treatment of dermatologic adverse events from epidermal growth factor receptor inhibitors.
    Current opinion in oncology, 2011, Volume: 23, Issue:4

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Cetuximab; Drug Eruptions; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Molecular Targeted Therapy; Panitumumab; Protein Kinase Inhibitors; Quinazolines

2011
Clinical pharmacokinetics of tyrosine kinase inhibitors: focus on 4-anilinoquinazolines.
    Clinical pharmacokinetics, 2011, Volume: 50, Issue:6

    Topics: Animals; Antineoplastic Agents; Drug Interactions; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Pharmacogenetics; Protein Kinase Inhibitors; Quinazolines; Tissue Distribution

2011
Role of chemotherapy on brain metastasis.
    Progress in neurological surgery, 2012, Volume: 25

    Topics: Brain Neoplasms; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Protein Kinase Inhibitors; Quinazolines

2012
Potential therapeutic significance of HER-family in esophageal squamous cell carcinoma.
    Annals of thoracic and cardiovascular surgery : official journal of the Association of Thoracic and Cardiovascular Surgeons of Asia, 2012, Volume: 18, Issue:6

    Topics: Antibodies, Monoclonal, Humanized; Antibody-Dependent Cell Cytotoxicity; Antineoplastic Agents; Carcinoma, Squamous Cell; Cetuximab; Drug Delivery Systems; Erlotinib Hydrochloride; Esophageal Neoplasms; Gefitinib; Genes, erbB-1; Genes, erbB-2; Humans; Lapatinib; Quinazolines; Trastuzumab

2012
Epidermal growth factor receptor targeting in cancer: a review of trends and strategies.
    Biomaterials, 2013, Volume: 34, Issue:34

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Cell Proliferation; Cetuximab; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Molecular Targeted Therapy; Neoplasms; Panitumumab; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines

2013
Co-targeting estrogen receptor and HER2 pathways in breast cancer.
    Breast (Edinburgh, Scotland), 2014, Volume: 23, Issue:1

    Topics: Anastrozole; Androstadienes; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Aromatase Inhibitors; Breast Neoplasms; Estradiol; Everolimus; Female; Fulvestrant; Gefitinib; Humans; Lapatinib; Letrozole; Molecular Targeted Therapy; Nitriles; Quinazolines; Receptor, ErbB-2; Receptors, Estrogen; Signal Transduction; Sirolimus; Tamoxifen; Trastuzumab; Triazoles

2014
Dual HER2 blockade: preclinical and clinical data.
    Breast cancer research : BCR, 2014, Aug-01, Volume: 16, Issue:4

    Topics: Animals; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Female; Gefitinib; Humans; Lapatinib; Molecular Targeted Therapy; Quinazolines; Randomized Controlled Trials as Topic; Receptor, ErbB-2; Trastuzumab; Xenograft Model Antitumor Assays

2014
Renal toxicity of anticancer agents targeting HER2 and EGFR.
    Journal of nephrology, 2015, Volume: 28, Issue:6

    Topics: Acute Kidney Injury; Ado-Trastuzumab Emtansine; Afatinib; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Cetuximab; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Maytansine; Neoplasms; Protein Kinase Inhibitors; Quinazolines; Receptor, ErbB-2; Renal Dialysis; Renal Insufficiency, Chronic; Trastuzumab

2015
Interventions for the treatment of oral and oropharyngeal cancers: targeted therapy and immunotherapy.
    The Cochrane database of systematic reviews, 2015, Dec-01, Issue:12

    Topics: Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Carcinoma, Squamous Cell; Cetuximab; Cisplatin; Docetaxel; ErbB Receptors; Gefitinib; Humans; Immunotherapy; Lapatinib; Molecular Targeted Therapy; Mouth Neoplasms; Oropharyngeal Neoplasms; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Randomized Controlled Trials as Topic; Taxoids

2015
[Tyrosine kinase inhibitors and pregnancy: A risk to the fetus?].
    Bulletin du cancer, 2016, Volume: 103, Issue:5

    Topics: Abnormalities, Drug-Induced; Adult; Antineoplastic Agents; Dasatinib; Erlotinib Hydrochloride; Female; Fetus; Gefitinib; Humans; Imatinib Mesylate; Lapatinib; Maternal Age; Placenta; Pregnancy; Pregnancy Complications, Neoplastic; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrimidines; Quinazolines; Risk

2016
Role of tyrosine kinase inhibitors in the treatment of pituitary tumours: from bench to bedside.
    Current opinion in endocrinology, diabetes, and obesity, 2017, Volume: 24, Issue:4

    Topics: Animals; Cell Line, Tumor; ErbB Receptors; Gefitinib; Humans; Lapatinib; Mice; Mice, Transgenic; Pituitary Neoplasms; Prolactinoma; Protein Kinase Inhibitors; Quinazolines; Translational Research, Biomedical

2017
[Radiation therapy and targeted therapies: Risks and opportunities].
    Cancer radiotherapie : journal de la Societe francaise de radiotherapie oncologique, 2022, Volume: 26, Issue:6-7

    Topics: Ado-Trastuzumab Emtansine; Antineoplastic Agents; Cetuximab; Crizotinib; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Mitogen-Activated Protein Kinase Kinases; Molecular Targeted Therapy; Panitumumab; Protein Kinase Inhibitors; Proto-Oncogene Proteins B-raf; Radiotherapy; Receptor Protein-Tyrosine Kinases; Trastuzumab

2022

Trials

1 trial(s) available for lapatinib and gefitinib

ArticleYear
Factors associated with clinical benefit from epidermal growth factor receptor inhibitors in recurrent and metastatic squamous cell carcinoma of the head and neck.
    Oral oncology, 2009, Volume: 45, Issue:10

    Topics: Age Factors; Aged; Antineoplastic Agents; Carcinoma, Squamous Cell; Disease-Free Survival; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Head and Neck Neoplasms; Humans; Lapatinib; Male; Middle Aged; Neoplasm Recurrence, Local; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Retrospective Studies; Treatment Outcome

2009

Other Studies

96 other study(ies) available for lapatinib and gefitinib

ArticleYear
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.
    Bioorganic & medicinal chemistry letters, 2004, Jan-05, Volume: 14, Issue:1

    Topics: Binding Sites; Cell Line, Tumor; Enzyme Inhibitors; ErbB Receptors; Glycoproteins; Humans; Receptor, ErbB-2; Structure-Activity Relationship

2004
A small molecule-kinase interaction map for clinical kinase inhibitors.
    Nature biotechnology, 2005, Volume: 23, Issue:3

    Topics: Benzamides; Drug Design; Escherichia coli; Escherichia coli Proteins; Imatinib Mesylate; Microchemistry; Pharmaceutical Preparations; Piperazines; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Pyrimidines

2005
A quantitative analysis of kinase inhibitor selectivity.
    Nature biotechnology, 2008, Volume: 26, Issue:1

    Topics: Binding Sites; Enzyme Activation; Humans; Phosphotransferases; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Proteome; Quantitative Structure-Activity Relationship

2008
Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies.
    Journal of medicinal chemistry, 2009, Feb-26, Volume: 52, Issue:4

    Topics: Computational Biology; Computer Simulation; Databases, Protein; Drug Evaluation, Preclinical; ErbB Receptors; Humans; Protein Binding; Quantitative Structure-Activity Relationship

2009
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
    Toxicological sciences : an official journal of the Society of Toxicology, 2010, Volume: 118, Issue:2

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Assay; Biological Transport; Cell Line; Cell Membrane; Chemical and Drug Induced Liver Injury; Cytoplasmic Vesicles; Drug Evaluation, Preclinical; Humans; Liver; Rats; Reproducibility of Results; Spodoptera; Transfection; Xenobiotics

2010
A predictive ligand-based Bayesian model for human drug-induced liver injury.
    Drug metabolism and disposition: the biological fate of chemicals, 2010, Volume: 38, Issue:12

    Topics: Bayes Theorem; Chemical and Drug Induced Liver Injury; Humans; Ligands

2010
Navigating the kinome.
    Nature chemical biology, 2011, Volume: 7, Issue:4

    Topics: Drug Design; Pharmacogenetics; Protein Kinases; Proteome; Systems Biology

2011
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
    European journal of medicinal chemistry, 2011, Volume: 46, Issue:6

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Molecular Structure; Piperazines; Protein Kinase Inhibitors; Protein Kinases; Pyrimidines; Stereoisomerism; Structure-Activity Relationship

2011
Comprehensive analysis of kinase inhibitor selectivity.
    Nature biotechnology, 2011, Oct-30, Volume: 29, Issue:11

    Topics: Catalysis; Drug Design; Enzyme Stability; High-Throughput Screening Assays; Humans; Protein Binding; Protein Kinase Inhibitors; Protein Kinases; Proteomics; Signal Transduction; Substrate Specificity

2011
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
    Bioorganic & medicinal chemistry letters, 2012, Jan-01, Volume: 22, Issue:1

    Topics: Administration, Oral; Animals; Chemistry, Pharmaceutical; Drug Design; Drug Screening Assays, Antitumor; Enzyme Inhibitors; ErbB Receptors; Humans; Hydrogen-Ion Concentration; Inhibitory Concentration 50; Mice; Microsomes, Liver; Models, Chemical; Neoplasm Transplantation; Pyrimidines; Rats; Receptor, ErbB-2; Structure-Activity Relationship

2012
Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay.
    European journal of medicinal chemistry, 2013, Volume: 61

    Topics: Dose-Response Relationship, Drug; Fluorescence Resonance Energy Transfer; Glycolipids; Humans; Membrane Proteins; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases; Structure-Activity Relationship

2013
Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
    Drug metabolism and disposition: the biological fate of chemicals, 2013, Volume: 41, Issue:4

    Topics: Adrenergic beta-Antagonists; Amines; Ammonium Chloride; Antidepressive Agents, Tricyclic; Atorvastatin; Cell Line, Transformed; Diuretics; Hepatocytes; Heptanoic Acids; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; Imipramine; Lysosomes; Monensin; Nigericin; Propranolol; Pyrroles

2013
Identification of potent Yes1 kinase inhibitors using a library screening approach.
    Bioorganic & medicinal chemistry letters, 2013, Aug-01, Volume: 23, Issue:15

    Topics: Binding Sites; Cell Line; Cell Survival; Drug Design; Humans; Hydrogen Bonding; Molecular Docking Simulation; Protein Kinase Inhibitors; Protein Structure, Tertiary; Proto-Oncogene Proteins c-yes; Small Molecule Libraries; Structure-Activity Relationship

2013
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
    Hepatology (Baltimore, Md.), 2014, Volume: 60, Issue:3

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Chemical and Drug Induced Liver Injury; Humans; Male; Mitochondria, Liver; Rats; Rats, Sprague-Dawley; Severity of Illness Index

2014
Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
    Journal of medicinal chemistry, 2014, Oct-09, Volume: 57, Issue:19

    Topics: Activin Receptors, Type I; Aminopyridines; Humans; Mutation; Myositis Ossificans; Phenols; Protein Kinase Inhibitors; Structure-Activity Relationship

2014
Truncated structures used in search for new lead compounds and in a retrospective analysis of thienopyrimidine-based EGFR inhibitors.
    European journal of medicinal chemistry, 2015, Apr-13, Volume: 94

    Topics: ErbB Receptors; Models, Molecular; Protein Kinase Inhibitors; Pyrimidines; Retrospective Studies; Stereoisomerism; Structure-Activity Relationship

2015
Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.
    European journal of medicinal chemistry, 2015, Sep-18, Volume: 102

    Topics: Antineoplastic Agents; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; MCF-7 Cells; Molecular Structure; Protein Kinase Inhibitors; Quinolines; Structure-Activity Relationship

2015
Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.
    Bioorganic & medicinal chemistry, 2016, 08-15, Volume: 24, Issue:16

    Topics: Cell Line; Drug Design; ErbB Receptors; Humans; In Vitro Techniques; Inhibitory Concentration 50; Mutation; Quinazolines

2016
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
    Bioorganic & medicinal chemistry, 2017, 01-01, Volume: 25, Issue:1

    Topics: Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Drug Design; Drug Screening Assays, Antitumor; Green Fluorescent Proteins; Histone Deacetylase Inhibitors; Humans; Hydroxamic Acids; Molecular Docking Simulation; Quinazolines; Receptor, ErbB-2; Structure-Activity Relationship; Triazoles

2017
Synthesis and in vitro biological evaluation of novel quinazoline derivatives.
    Bioorganic & medicinal chemistry letters, 2017, 04-01, Volume: 27, Issue:7

    Topics: Aniline Compounds; Antineoplastic Agents; Cell Line, Tumor; Drug Screening Assays, Antitumor; ErbB Receptors; Gefitinib; Humans; Lapatinib; Molecular Docking Simulation; Mutation; Protein Kinase Inhibitors; Quinazolines; Signal Transduction

2017
Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR and α-glucosidase.
    Bioorganic & medicinal chemistry letters, 2017, 09-15, Volume: 27, Issue:18

    Topics: 1-Deoxynojirimycin; alpha-Glucosidases; Dose-Response Relationship, Drug; ErbB Receptors; Glycoside Hydrolase Inhibitors; Humans; Molecular Structure; Protein Kinase Inhibitors; Quinazolines; Structure-Activity Relationship

2017
The target landscape of clinical kinase drugs.
    Science (New York, N.Y.), 2017, 12-01, Volume: 358, Issue:6367

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cytokines; Drug Discovery; fms-Like Tyrosine Kinase 3; Humans; Leukemia, Myeloid, Acute; Lung Neoplasms; Mice; Molecular Targeted Therapy; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proteomics; Xenograft Model Antitumor Assays

2017
Discovery of anilino-furo[2,3-d]pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity.
    European journal of medicinal chemistry, 2018, Jan-20, Volume: 144

    Topics: Aniline Compounds; Animals; Antineoplastic Agents; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; ErbB Receptors; Female; Humans; Mice; Molecular Structure; Neoplasms, Experimental; Protein Kinase Inhibitors; Pyrimidines; Structure-Activity Relationship; Tumor Cells, Cultured

2018
6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
    European journal of medicinal chemistry, 2018, Mar-10, Volume: 147

    Topics: Antineoplastic Agents; Apoptosis; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Models, Molecular; Molecular Structure; Quinazolines; Structure-Activity Relationship

2018
Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
    European journal of medicinal chemistry, 2018, Aug-05, Volume: 156

    Topics: Antineoplastic Agents; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Isatin; Molecular Docking Simulation; Neoplasms; Protein Kinase Inhibitors

2018
Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
    Journal of medicinal chemistry, 2018, 12-27, Volume: 61, Issue:24

    Topics: A549 Cells; Adenosine Triphosphate; Aniline Compounds; Animals; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; ErbB Receptors; Female; Humans; Lapatinib; Mice, Inbred BALB C; Molecular Docking Simulation; Polyamines; Protein Domains; Protein Kinase Inhibitors; Quinazolines; Xenograft Model Antitumor Assays

2018
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
    Journal of medicinal chemistry, 2019, 05-09, Volume: 62, Issue:9

    Topics: Aminoquinolines; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Chordoma; Drug Design; ErbB Receptors; HEK293 Cells; Humans; Intracellular Signaling Peptides and Proteins; Molecular Docking Simulation; Protein Binding; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Quinazolines

2019
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
    Bioorganic & medicinal chemistry letters, 2019, 06-15, Volume: 29, Issue:12

    Topics: Exons; Humans; Mutation; Protein Kinase Inhibitors; Thioctic Acid

2019
Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.
    Bioorganic & medicinal chemistry letters, 2019, 09-15, Volume: 29, Issue:18

    Topics: Aniline Compounds; Antitubercular Agents; Dose-Response Relationship, Drug; Microbial Sensitivity Tests; Molecular Structure; Mycobacterium tuberculosis; Quinazolines; Quinolines; Structure-Activity Relationship

2019
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
    Bioorganic & medicinal chemistry letters, 2020, 05-01, Volume: 30, Issue:9

    Topics: Antineoplastic Agents; Cell Line, Tumor; Drug Design; ErbB Receptors; Humans; Inhibitory Concentration 50; Quinazolines; Receptor, ErbB-2; Structure-Activity Relationship

2020
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.
    Bioorganic & medicinal chemistry, 2020, 09-15, Volume: 28, Issue:18

    Topics: Antineoplastic Agents; Apoptosis; Benzimidazoles; Breast Neoplasms; Cell Proliferation; Drug Screening Assays, Antitumor; ErbB Receptors; Erlotinib Hydrochloride; Female; Humans; MCF-7 Cells; Molecular Docking Simulation; Protein Kinase Inhibitors; Quantitative Structure-Activity Relationship; Thiazoles

2020
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
    Journal of medicinal chemistry, 2020, 10-22, Volume: 63, Issue:20

    Topics: Dose-Response Relationship, Drug; Drug Design; Drug Evaluation, Preclinical; Humans; Kinetics; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; Pyrimidines; Pyrroles; Receptor, ErbB-2; Structure-Activity Relationship; Tumor Cells, Cultured

2020
Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
    European journal of medicinal chemistry, 2022, Apr-05, Volume: 233

    Topics: ATP Binding Cassette Transporter, Subfamily G, Member 2; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Humans; Neoplasm Proteins; Neoplasms; Paclitaxel

2022
Inhibition of HER-2/neu kinase impairs androgen receptor recruitment to the androgen responsive enhancer.
    Cancer research, 2005, Apr-15, Volume: 65, Issue:8

    Topics: Acetylation; Androgen Receptor Antagonists; Androgens; Cell Line, Tumor; Chromatin; Chromatin Immunoprecipitation; Dihydrotestosterone; ErbB Receptors; Gefitinib; Histones; Humans; Immunoglobulin Fragments; Lapatinib; Male; Prostate-Specific Antigen; Prostatic Neoplasms; Quinazolines; Receptor, ErbB-2; Receptors, Androgen; Response Elements; Transcription, Genetic

2005
The EGF receptor Hokey-Cokey.
    Cancer cell, 2007, Volume: 11, Issue:3

    Topics: Antineoplastic Agents; Enzyme Activation; ErbB Receptors; Gefitinib; Humans; Lapatinib; Models, Molecular; Mutation; Protein Conformation; Protein Structure, Tertiary; Purines; Quinazolines; Staurosporine

2007
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.
    Cancer cell, 2007, Volume: 11, Issue:3

    Topics: Antineoplastic Agents; Binding Sites; Carcinoma, Non-Small-Cell Lung; Crystallography, X-Ray; Enzyme Activation; ErbB Receptors; Gefitinib; Humans; Lapatinib; Lung Neoplasms; Models, Molecular; Mutation; Protein Conformation; Protein Structure, Tertiary; Purines; Quinazolines; Staurosporine

2007
Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib.
    Cancer research, 2008, Jan-15, Volume: 68, Issue:2

    Topics: Animals; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; CHO Cells; Cricetinae; Cricetulus; ErbB Receptors; Gefitinib; Genes, erbB-2; Humans; Lapatinib; Lung Neoplasms; Models, Molecular; Mutant Proteins; Phosphorylation; Polymorphism, Single Nucleotide; Protein Binding; Protein Kinase Inhibitors; Quinazolines; Receptor, ErbB-2; Structure-Activity Relationship; Tumor Cells, Cultured

2008
Combined lapatinib and cetuximab enhance cytotoxicity against gefitinib-resistant lung cancer cells.
    Molecular cancer therapeutics, 2008, Volume: 7, Issue:3

    Topics: Animals; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cetuximab; Chlorocebus aethiops; COS Cells; Dimerization; Drug Resistance, Neoplasm; ErbB Receptors; Gefitinib; Genes, erbB-2; Humans; Lapatinib; Lung Neoplasms; Mutation; Quinazolines

2008
Restoration of PTEN expression alters the sensitivity of prostate cancer cells to EGFR inhibitors.
    The Prostate, 2008, Jun-15, Volume: 68, Issue:9

    Topics: Benzamides; Blotting, Western; Cell Line, Tumor; Cell Proliferation; Chromones; ErbB Receptors; Gefitinib; Humans; Lapatinib; Male; Mitogen-Activated Protein Kinases; Morpholines; Neoplasms, Hormone-Dependent; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Prostatic Neoplasms; Protein Kinase Inhibitors; PTEN Phosphohydrolase; Quinazolines

2008
[Targeted therapy for metastatic bladder cancer].
    Der Urologe. Ausg. A, 2008, Volume: 47, Issue:10

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Benzenesulfonates; Bevacizumab; Carcinoma, Transitional Cell; Disease Progression; Drug Delivery Systems; Gefitinib; Humans; Lapatinib; Niacinamide; Phenylurea Compounds; Pyridines; Quinazolines; Receptor, ErbB-2; Receptors, Growth Factor; Sorafenib; Survival Rate; Trastuzumab; Urinary Bladder Neoplasms

2008
Promising newer molecular-targeted therapies in head and neck cancer.
    Drugs, 2008, Volume: 68, Issue:12

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Benzenesulfonates; Cetuximab; Clinical Trials as Topic; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Head and Neck Neoplasms; Humans; Lapatinib; Models, Biological; Niacinamide; Panitumumab; Phenylurea Compounds; Protein Kinase Inhibitors; Pyridines; Quinazolines; Receptors, Vascular Endothelial Growth Factor; Sorafenib

2008
Dual targeting of EGFR and HER-2 in colon cancer cell lines.
    Cancer chemotherapy and pharmacology, 2009, Volume: 63, Issue:6

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Apoptosis; Caco-2 Cells; Cell Proliferation; Colonic Neoplasms; Dose-Response Relationship, Drug; Drug Synergism; ErbB Receptors; Gefitinib; Humans; Lapatinib; Quinazolines; Receptor, ErbB-2; Trastuzumab

2009
microRNA-205 regulates HER3 in human breast cancer.
    Cancer research, 2009, Mar-15, Volume: 69, Issue:6

    Topics: Breast Neoplasms; Cell Growth Processes; Cell Line, Tumor; Combined Modality Therapy; Gefitinib; Genes, Tumor Suppressor; Genetic Therapy; Humans; Lapatinib; MicroRNAs; Oncogene Protein v-akt; Phosphatidylinositol 3-Kinases; Quinazolines; Receptor, ErbB-3; Transfection

2009
ERBB1 and ERBB2 have distinct functions in tumor cell invasion and intravasation.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2009, Jun-01, Volume: 15, Issue:11

    Topics: Animals; Benzothiazoles; Cell Line, Tumor; Cell Movement; ErbB Receptors; Female; Gefitinib; Humans; Lapatinib; Mammary Neoplasms, Experimental; Mice; Mice, SCID; Neoplasm Invasiveness; Neoplasm Metastasis; Phosphorylation; Quinazolines; Receptor, ErbB-2; Tyrphostins; Xenograft Model Antitumor Assays

2009
Tyrosine kinase inhibitors potentiate the cytotoxicity of MDR-substrate anticancer agents independent of growth factor receptor status in lung cancer cell lines.
    Investigational new drugs, 2010, Volume: 28, Issue:4

    Topics: Adenosine Triphosphatases; Antineoplastic Combined Chemotherapy Protocols; ATP Binding Cassette Transporter, Subfamily B; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Proliferation; Docetaxel; Dose-Response Relationship, Drug; Drug Interactions; Drug Resistance, Multiple; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Lung Neoplasms; Protein Kinase Inhibitors; Quinazolines; Taxoids

2010
Lapatinib, a dual EGFR and HER2 tyrosine kinase inhibitor, downregulates thymidylate synthase by inhibiting the nuclear translocation of EGFR and HER2.
    PloS one, 2009, Jun-16, Volume: 4, Issue:6

    Topics: Active Transport, Cell Nucleus; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Cell Line, Tumor; Down-Regulation; ErbB Receptors; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Neoplasm Transplantation; Oligonucleotide Array Sequence Analysis; Promoter Regions, Genetic; Protein Kinase Inhibitors; Pyrimidines; Quinazolines; Receptor, ErbB-2; Trastuzumab

2009
Role of epidermal growth factor inhibition in experimental pulmonary hypertension.
    American journal of respiratory and critical care medicine, 2010, Jan-15, Volume: 181, Issue:2

    Topics: Animals; Antineoplastic Agents; Cell Division; Cell Survival; Disease Models, Animal; Dose-Response Relationship, Drug; Epidermal Growth Factor; Erlotinib Hydrochloride; Gefitinib; Gene Expression; Humans; Hypertension, Pulmonary; Lapatinib; Male; Mice; Muscle, Smooth, Vascular; Polymerase Chain Reaction; Protein Kinase Inhibitors; Pulmonary Wedge Pressure; Quinazolines; Rats; Rats, Sprague-Dawley; RNA, Messenger; Vascular Resistance

2010
Effects of the combined blockade of EGFR and ErbB-2 on signal transduction and regulation of cell cycle regulatory proteins in breast cancer cells.
    Breast cancer research and treatment, 2010, Volume: 123, Issue:2

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cyclin-Dependent Kinase Inhibitor p27; Drug Synergism; ErbB Receptors; Female; Forkhead Box Protein O3; Forkhead Transcription Factors; Gefitinib; Humans; Intracellular Signaling Peptides and Proteins; Lapatinib; Mitogen-Activated Protein Kinases; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Quinazolines; Receptor, ErbB-2; Retinoblastoma-Like Protein p130; RNA Interference; RNA, Messenger; Signal Transduction; Time Factors; Trastuzumab

2010
Are current drug development programmes realising the full potential of new agents? Tyrosine kinase inhibitors.
    Breast cancer research : BCR, 2009, Volume: 11 Suppl 3

    Topics: Animals; Breast Neoplasms; Drug Discovery; Drug Industry; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Humans; Lapatinib; Protein Kinase Inhibitors; Quinazolines; Receptor, ErbB-2; Technology, Pharmaceutical

2009
AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2010, Feb-15, Volume: 16, Issue:4

    Topics: Animals; Carcinoma, Squamous Cell; Cell Line, Tumor; Cell Proliferation; ErbB Receptors; Gefitinib; Head and Neck Neoplasms; Humans; Lapatinib; Mice; Mice, Nude; Mice, SCID; Quinazolines; Receptor, ErbB-2; Receptor, ErbB-3; Signal Transduction; Xenograft Model Antitumor Assays

2010
Synergistic interaction between trastuzumab and EGFR/HER-2 tyrosine kinase inhibitors in HER-2 positive breast cancer cells.
    Investigational new drugs, 2011, Volume: 29, Issue:5

    Topics: Animals; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Drug Synergism; ErbB Receptors; Female; Gefitinib; Humans; Immunoblotting; Inhibitory Concentration 50; Lapatinib; Mice; Mice, Inbred BALB C; Molecular Targeted Therapy; Protein Kinase Inhibitors; Quinazolines; Receptor, ErbB-2; Trastuzumab; Xenograft Model Antitumor Assays

2011
Cytoprotective effect of the elongation factor-2 kinase-mediated autophagy in breast cancer cells subjected to growth factor inhibition.
    PloS one, 2010, Mar-16, Volume: 5, Issue:3

    Topics: Adenylate Kinase; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Autophagy; Breast Neoplasms; Calcium; Cell Line, Tumor; Elongation Factor 2 Kinase; Female; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Intercellular Signaling Peptides and Proteins; Lapatinib; Quinazolines; Signal Transduction; Trastuzumab

2010
Tyrosine kinase inhibitors gefitinib, lapatinib and sorafenib induce rapid functional alterations in breast cancer cells.
    Current cancer drug targets, 2010, Volume: 10, Issue:4

    Topics: Antineoplastic Agents; Apoptosis; Base Sequence; Benzenesulfonates; Breast Neoplasms; Calcium; Cell Division; Cell Line, Tumor; Cytosol; DNA Primers; Endoplasmic Reticulum; Flow Cytometry; Gefitinib; Humans; Lapatinib; Membrane Potentials; Niacinamide; Phenylurea Compounds; Protein Kinase Inhibitors; Pyridines; Quinazolines; Reverse Transcriptase Polymerase Chain Reaction; Sorafenib

2010
Lapatinib, a dual HER1/HER2 tyrosine kinase inhibitor, augments basal cleavage of HER2 extracellular domain (ECD) to inhibit HER2-driven cancer cell growth.
    Journal of cellular physiology, 2011, Volume: 226, Issue:1

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; ErbB Receptors; Female; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Protein Binding; Protein Kinase Inhibitors; Protein Structure, Tertiary; Quinazolines; Receptor, ErbB-2; Trastuzumab

2011
HER2/ErbB2 receptor signaling in rat and human prolactinoma cells: strategy for targeted prolactinoma therapy.
    Molecular endocrinology (Baltimore, Md.), 2011, Volume: 25, Issue:1

    Topics: Animals; Cell Line, Tumor; Cell Proliferation; Female; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Lactotrophs; Lapatinib; Molecular Targeted Therapy; Prolactin; Prolactinoma; Quinazolines; Rats; Receptor, ErbB-2; RNA, Messenger; Signal Transduction

2011
AKT inhibition relieves feedback suppression of receptor tyrosine kinase expression and activity.
    Cancer cell, 2011, Jan-18, Volume: 19, Issue:1

    Topics: Animals; Benzylamines; Breast Neoplasms; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Drug Therapy, Combination; Feedback, Physiological; Female; Forkhead Transcription Factors; Gefitinib; Gene Expression; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Mechanistic Target of Rapamycin Complex 1; Mice; Mice, Nude; Models, Biological; Multiprotein Complexes; Neoplasms; Phosphorylation; Promoter Regions, Genetic; Protein Binding; Protein Kinase Inhibitors; Proteins; Proto-Oncogene Proteins c-akt; Quinazolines; Quinoxalines; Receptor Protein-Tyrosine Kinases; Receptor, ErbB-2; Receptor, ErbB-3; Receptor, IGF Type 1; Receptor, Insulin; RNA, Small Interfering; Signal Transduction; TOR Serine-Threonine Kinases; Up-Regulation; Xenograft Model Antitumor Assays

2011
KRAS-mutated non-small cell lung cancer cells are responsive to either co-treatment with erlotinib or gefitinib and histone deacetylase inhibitors or single treatment with lapatinib.
    Oncology reports, 2011, Volume: 25, Issue:4

    Topics: Adenocarcinoma; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Erlotinib Hydrochloride; Flow Cytometry; Gefitinib; Histone Deacetylase Inhibitors; Humans; Hydroxamic Acids; Lapatinib; Lung Neoplasms; Membrane Potential, Mitochondrial; Mutation; Proto-Oncogene Proteins; Proto-Oncogene Proteins p21(ras); Quinazolines; ras Proteins; Tumor Cells, Cultured; Vorinostat

2011
Stat1 is a suppressor of ErbB2/Neu-mediated cellular transformation and mouse mammary gland tumor formation.
    Cell cycle (Georgetown, Tex.), 2011, Mar-01, Volume: 10, Issue:5

    Topics: Animals; Antineoplastic Agents; Cell Line; Cell Transformation, Neoplastic; Chlorocebus aethiops; Disease Progression; Female; Gefitinib; Humans; Lapatinib; Mammary Glands, Animal; Mammary Neoplasms, Experimental; Mice; Mice, Transgenic; Phosphorylation; Quinazolines; Receptor, ErbB-2; Signal Transduction; STAT1 Transcription Factor; Transplantation, Heterologous

2011
Differential action of small molecule HER kinase inhibitors on receptor heterodimerization: therapeutic implications.
    International journal of cancer, 2012, Jul-01, Volume: 131, Issue:1

    Topics: Aminoquinolines; Aniline Compounds; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Humans; Lapatinib; Morpholines; Protein Kinase Inhibitors; Protein Multimerization; Quinazolines; Quinolines; Receptor, ErbB-2; Trastuzumab

2012
Rapid phospho-turnover by receptor tyrosine kinases impacts downstream signaling and drug binding.
    Molecular cell, 2011, Sep-02, Volume: 43, Issue:5

    Topics: Binding Sites; ErbB Receptors; Gefitinib; Humans; Lapatinib; Models, Biological; Pharmaceutical Preparations; Phosphorylation; Quinazolines; Receptor Protein-Tyrosine Kinases; Receptor, ErbB-2; Receptor, ErbB-3; Signal Transduction; Tumor Cells, Cultured

2011
Allosteric modulation by protein kinase Cε leads to modified responses of EGF receptor towards tyrosine kinase inhibitors.
    Cellular signalling, 2012, Volume: 24, Issue:2

    Topics: Antineoplastic Agents; Apoptosis; Blotting, Western; Carcinoma, Squamous Cell; Cell Cycle; Cell Line, Tumor; Dimerization; ErbB Receptors; Flow Cytometry; Gefitinib; Gene Expression; Head and Neck Neoplasms; Humans; Immunoprecipitation; Lapatinib; Plasmids; Protein Conformation; Protein Kinase C-epsilon; Protein Kinase Inhibitors; Quinazolines; Receptor, ErbB-2; Signal Transduction; Transfection

2012
Differential impact of EGFR-targeted therapies on hypoxia responses: implications for treatment sensitivity in triple-negative metastatic breast cancer.
    PloS one, 2011, Volume: 6, Issue:9

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Cell Movement; Cell Survival; Cetuximab; DNA; Drug Screening Assays, Antitumor; Enzyme-Linked Immunosorbent Assay; ErbB Receptors; Female; Flow Cytometry; Gefitinib; Gene Expression Regulation, Neoplastic; Genes, Reporter; Green Fluorescent Proteins; Humans; Hypoxia; Hypoxia-Inducible Factor 1; Lapatinib; Molecular Sequence Data; Neoplasm Metastasis; Quinazolines; Transcription, Genetic

2011
An EGFR inhibitor enhances the efficacy of SN38, an active metabolite of irinotecan, in SN38-refractory gastric carcinoma cells.
    British journal of cancer, 2011, Nov-08, Volume: 105, Issue:10

    Topics: Animals; Apoptosis; Camptothecin; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Drug Screening Assays, Antitumor; Drug Synergism; ErbB Receptors; Gefitinib; Genes, erbB-2; Humans; Irinotecan; Lapatinib; Mice; Mice, Inbred BALB C; Mice, Nude; Quinazolines; Stomach Neoplasms

2011
Endocrine therapy, new biologicals, and new study designs for presurgical studies in breast cancer.
    Journal of the National Cancer Institute. Monographs, 2011, Volume: 2011, Issue:43

    Topics: Anastrozole; Antineoplastic Agents, Hormonal; Antineoplastic Combined Chemotherapy Protocols; Biomarkers, Tumor; Breast Neoplasms; Chemotherapy, Adjuvant; Clinical Trials as Topic; Erlotinib Hydrochloride; Female; Gefitinib; Humans; Ki-67 Antigen; Lapatinib; Molecular Targeted Therapy; Multicenter Studies as Topic; Neoadjuvant Therapy; Nitriles; Predictive Value of Tests; Preoperative Period; Quinazolines; Receptors, Estrogen; Receptors, Progesterone; Tamoxifen; Treatment Outcome; Triazoles

2011
[Inhibitory effect of gefitinib and lapatinib on proliferation of HEL cells].
    Zhongguo shi yan xue ye xue za zhi, 2012, Volume: 20, Issue:2

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Gefitinib; Humans; Janus Kinase 2; Lapatinib; Mutation; Myeloproliferative Disorders; Protein Kinase Inhibitors; Quinazolines

2012
Oncogenic mutations counteract intrinsic disorder in the EGFR kinase and promote receptor dimerization.
    Cell, 2012, May-11, Volume: 149, Issue:4

    Topics: Amino Acid Sequence; Crystallography, X-Ray; ErbB Receptors; Gefitinib; Humans; Lapatinib; Molecular Dynamics Simulation; Molecular Sequence Data; Neoplasms; Point Mutation; Protein Folding; Protein Kinase Inhibitors; Protein Multimerization; Protein Structure, Tertiary; Quinazolines; Sequence Alignment; Signal Transduction

2012
T-Cadherin is an auxiliary negative regulator of EGFR pathway activity in cutaneous squamous cell carcinoma: impact on cell motility.
    The Journal of investigative dermatology, 2012, Volume: 132, Issue:9

    Topics: Cadherins; Carcinoma, Squamous Cell; Cell Line, Tumor; Cell Movement; ErbB Receptors; Gefitinib; Gene Silencing; Humans; Lapatinib; Membrane Microdomains; Quinazolines; rho GTP-Binding Proteins; Signal Transduction; Skin Neoplasms

2012
Analysis of bypass signaling in EGFR pathway and profiling of bypass genes for predicting response to anticancer EGFR tyrosine kinase inhibitors.
    Molecular bioSystems, 2012, Volume: 8, Issue:10

    Topics: Antineoplastic Agents; Biomarkers, Pharmacological; Carcinoma, Non-Small-Cell Lung; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Gene Expression Profiling; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Lung Neoplasms; Mutation; Predictive Value of Tests; Protein Kinase Inhibitors; Quinazolines; Signal Transduction; Support Vector Machine

2012
FAM83A confers EGFR-TKI resistance in breast cancer cells and in mice.
    The Journal of clinical investigation, 2012, Volume: 122, Issue:9

    Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; ErbB Receptors; Female; Gefitinib; Gene Knockdown Techniques; Humans; Kaplan-Meier Estimate; Lapatinib; Mice; Mice, Inbred BALB C; Mice, Nude; Neoplasm Proteins; Phosphorylation; Protein Processing, Post-Translational; Proto-Oncogene Proteins c-raf; Quinazolines; RNA Interference; Signal Transduction; Tyrphostins; Xenograft Model Antitumor Assays

2012
Computational study of EGFR inhibition: molecular dynamics studies on the active and inactive protein conformations.
    Journal of molecular modeling, 2013, Volume: 19, Issue:2

    Topics: Adenosine Triphosphate; Binding Sites; Drug Design; ErbB Receptors; Gefitinib; Humans; Hydrophobic and Hydrophilic Interactions; Kinetics; Lapatinib; Molecular Dynamics Simulation; Protein Kinase Inhibitors; Protein Structure, Secondary; Protein Structure, Tertiary; Quinazolines; Static Electricity; Structure-Activity Relationship; Thermodynamics

2013
ErbBs inhibition by lapatinib blocks tumor growth in an orthotopic model of human testicular germ cell tumor.
    International journal of cancer, 2013, Volume: 133, Issue:1

    Topics: Animals; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Blotting, Western; Carcinoma, Embryonal; Cell Survival; Cetuximab; Choriocarcinoma; Endodermal Sinus Tumor; ErbB Receptors; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Immunoprecipitation; Lapatinib; Male; Mice; Mice, Nude; Neoplasms, Experimental; Neoplasms, Germ Cell and Embryonal; Phosphorylation; Protein Kinase Inhibitors; Quinazolines; Real-Time Polymerase Chain Reaction; Receptor, ErbB-2; Receptor, ErbB-3; Teratocarcinoma; Testicular Neoplasms; Transplantation, Heterologous

2013
Autophagy-related gene 12 (ATG12) is a novel determinant of primary resistance to HER2-targeted therapies: utility of transcriptome analysis of the autophagy interactome to guide breast cancer treatment.
    Oncotarget, 2012, Volume: 3, Issue:12

    Topics: Animals; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Autophagy; Autophagy-Related Protein 12; Breast Neoplasms; Cell Line, Tumor; Cell Survival; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Erlotinib Hydrochloride; Female; Gefitinib; Gene Expression Profiling; Gene Expression Regulation, Neoplastic; Genetic Predisposition to Disease; Humans; Lapatinib; Mice; Mice, Nude; Molecular Targeted Therapy; Oligonucleotide Array Sequence Analysis; Phenotype; Precision Medicine; Protein Kinase Inhibitors; Quinazolines; Real-Time Polymerase Chain Reaction; Receptor, ErbB-2; RNA Interference; Small Ubiquitin-Related Modifier Proteins; Time Factors; Transfection; Trastuzumab; Tumor Burden; Xenograft Model Antitumor Assays

2012
Cross-talk between EGFR and T-cadherin: EGFR activation promotes T-cadherin localization to intercellular contacts.
    Cellular signalling, 2013, Volume: 25, Issue:5

    Topics: Cadherins; Cell Communication; Cell Line, Tumor; Cytoskeleton; Epidermal Growth Factor; ErbB Receptors; Gefitinib; Humans; Lapatinib; Mitogen-Activated Protein Kinase 1; Mitogen-Activated Protein Kinase 3; p38 Mitogen-Activated Protein Kinases; Phosphorylation; Protein Kinase Inhibitors; Quinazolines; rac1 GTP-Binding Protein; Signal Transduction

2013
Nutlin-3 inhibits epithelial-mesenchymal transition by interfering with canonical transforming growth factor-β1-Smad-Snail/Slug axis.
    Cancer letters, 2014, Jan-01, Volume: 342, Issue:1

    Topics: Antigens, CD; Antineoplastic Agents; Cadherins; Cell Line, Tumor; Cell Movement; Drug Evaluation, Preclinical; Drug Synergism; Epithelial-Mesenchymal Transition; ErbB Receptors; Gefitinib; Gene Expression; Humans; Imidazoles; Lapatinib; Phosphorylation; Piperazines; Protein Kinase Inhibitors; Protein Processing, Post-Translational; Quinazolines; RNA, Messenger; Signal Transduction; Smad Proteins; Snail Family Transcription Factors; Transcription Factors; Transforming Growth Factor beta1; Up-Regulation

2014
Dual inhibition of MEK1/2 and EGFR synergistically induces caspase-3-dependent apoptosis in EGFR inhibitor-resistant lung cancer cells via BIM upregulation.
    Investigational new drugs, 2013, Volume: 31, Issue:6

    Topics: Antineoplastic Agents; Apoptosis; Apoptosis Regulatory Proteins; Bcl-2-Like Protein 11; Benzimidazoles; Carcinoma, Non-Small-Cell Lung; Caspase 3; Cell Line, Tumor; Drug Synergism; ErbB Receptors; Gefitinib; Humans; Lapatinib; Lung Neoplasms; MAP Kinase Kinase 1; MAP Kinase Kinase 2; Membrane Proteins; Mutation; Protein Kinase Inhibitors; Proto-Oncogene Proteins; Pyridones; Quinazolines; Sulfonamides

2013
Treatment with gefitinib or lapatinib induces drug resistance through downregulation of topoisomerase IIα expression.
    Molecular cancer therapeutics, 2013, Volume: 12, Issue:12

    Topics: Amsacrine; Antigens, Neoplasm; Antineoplastic Agents; Apoptosis; Cell Cycle; Cell Line, Tumor; DNA Breaks, Double-Stranded; DNA Topoisomerases, Type II; DNA-Binding Proteins; Doxorubicin; Drug Resistance, Neoplasm; Etoposide; Gefitinib; Gene Expression Regulation, Neoplastic; Histones; Humans; Lapatinib; Protein Kinase Inhibitors; Quinazolines

2013
Lapatinib-induced NF-kappaB activation sensitizes triple-negative breast cancer cells to proteasome inhibitors.
    Breast cancer research : BCR, 2013, Nov-12, Volume: 15, Issue:6

    Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Boronic Acids; Bortezomib; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Humans; I-kappa B Kinase; Lapatinib; Mice, SCID; NF-kappa B; Phosphorylation; Proteasome Inhibitors; Pyrazines; Quinazolines; Receptor, ErbB-2; Triple Negative Breast Neoplasms; Xenograft Model Antitumor Assays

2013
Therapeutic potential of the dual EGFR/HER2 inhibitor AZD8931 in circumventing endocrine resistance.
    Breast cancer research and treatment, 2014, Volume: 144, Issue:2

    Topics: Animals; Apoptosis; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; ErbB Receptors; Estradiol; Female; Fulvestrant; Gefitinib; Humans; Lapatinib; MCF-7 Cells; Mice; Mice, Nude; Quinazolines; Random Allocation; Receptor, ErbB-2; Receptors, Estrogen; Signal Transduction; Tamoxifen; Up-Regulation; Xenograft Model Antitumor Assays

2014
[Development and biochemical characterization of EGFR/c-Met dual inhibitors].
    Acta pharmaceutica Hungarica, 2013, Volume: 83, Issue:4

    Topics: Afatinib; Aminopyridines; Anilides; Antineoplastic Agents; Apoptosis; Blotting, Western; Carcinoma, Non-Small-Cell Lung; Cell Line; Cell Line, Tumor; Computer Simulation; Crizotinib; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Imidazoles; Lapatinib; Lung Neoplasms; Molecular Structure; Protein Kinase Inhibitors; Protein Kinases; Protein-Tyrosine Kinases; Proto-Oncogene Proteins c-met; Pyrazines; Pyrazoles; Pyridines; Pyridones; Quinazolines; Quinolines

2013
Biomarkers for predicting response to tyrosine kinase inhibitors in drug-sensitive and drug-resistant human bladder cancer cells.
    Oncology reports, 2015, Volume: 33, Issue:2

    Topics: Adenosine Triphosphate; Antineoplastic Agents; Biomarkers, Tumor; Cell Line, Tumor; Drug Resistance, Neoplasm; Gefitinib; Genes, p53; Humans; Lapatinib; Mitogen-Activated Protein Kinase 1; Mitogen-Activated Protein Kinase 3; Mutation; Phosphorylation; Protein Kinase Inhibitors; Quinazolines; Receptor, ErbB-2; Signal Transduction; Urinary Bladder Neoplasms

2015
Combined effects of EGFR tyrosine kinase inhibitors and vATPase inhibitors in NSCLC cells.
    Toxicology and applied pharmacology, 2015, Aug-15, Volume: 287, Issue:1

    Topics: Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Survival; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Hypoxia-Inducible Factor 1, alpha Subunit; Lapatinib; Lung Neoplasms; Macrolides; Membrane Proteins; Protein Kinase Inhibitors; Proto-Oncogene Proteins; Quinazolines; RNA Interference; Transfection; Vacuolar Proton-Translocating ATPases

2015
MMP9, Cyclin D1 and β-Catenin Are Useful Markers of p16-positive Squamous Cell Carcinoma in Therapeutic EGFR Inhibition In Vitro.
    Anticancer research, 2015, Volume: 35, Issue:7

    Topics: Antineoplastic Agents; beta Catenin; Biomarkers, Tumor; Cadherins; Carcinoma, Squamous Cell; Cell Line, Tumor; Cyclin D1; Epigenesis, Genetic; ErbB Receptors; Gefitinib; Human papillomavirus 16; Humans; Lapatinib; Matrix Metalloproteinase 9; Quinazolines; Vimentin

2015
Drug response to HER2 gatekeeper T798M mutation in HER2-positive breast cancer.
    Amino acids, 2016, Volume: 48, Issue:2

    Topics: Antineoplastic Agents; Breast Neoplasms; Bridged Bicyclo Compounds, Heterocyclic; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Humans; Hydroxybutyrates; Lapatinib; Molecular Dynamics Simulation; Mutation; Protein Kinase Inhibitors; Purines; Quinazolines; Receptor, ErbB-2; Staurosporine

2016
Spectroscopic and molecular docking studies of binding interaction of gefitinib, lapatinib and sunitinib with bovine serum albumin (BSA).
    Journal of photochemistry and photobiology. B, Biology, 2015, Volume: 153

    Topics: Animals; Binding Sites; Cattle; Circular Dichroism; Fluorescence Resonance Energy Transfer; Gefitinib; Indoles; Lapatinib; Molecular Docking Simulation; Protein Binding; Protein Structure, Tertiary; Pyrroles; Quinazolines; Serum Albumin, Bovine; Spectrophotometry, Ultraviolet; Spectroscopy, Fourier Transform Infrared; Sunitinib; Thermodynamics

2015
Acid-Base Interactions of Polystyrene Sulfonic Acid in Amorphous Solid Dispersions Using a Combined UV/FTIR/XPS/ssNMR Study.
    Molecular pharmaceutics, 2016, Feb-01, Volume: 13, Issue:2

    Topics: Acid-Base Equilibrium; Antineoplastic Agents; Calorimetry, Differential Scanning; Crystallization; Drug Carriers; Drug Compounding; Drug Stability; Excipients; Gefitinib; Lapatinib; Magnetic Resonance Spectroscopy; Photoelectron Spectroscopy; Polystyrenes; Quinazolines; Solubility; Spectrophotometry, Ultraviolet; Spectroscopy, Fourier Transform Infrared

2016
A novel application of E1A in combination therapy with EGFR-TKI treatment in breast cancer.
    Oncotarget, 2016, Sep-27, Volume: 7, Issue:39

    Topics: Adenovirus E1A Proteins; Animals; Apoptosis; Axl Receptor Tyrosine Kinase; Breast Neoplasms; Cell Line, Tumor; Cell Survival; Disease Progression; Down-Regulation; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Genetic Therapy; Humans; Kaplan-Meier Estimate; Lapatinib; Mice; Mice, SCID; Neoplasm Transplantation; Prognosis; Protein Kinase Inhibitors; Proto-Oncogene Proteins; Quinazolines; Receptor Protein-Tyrosine Kinases

2016
Computational and Experimental Characterization of Patient Derived Mutations Reveal an Unusual Mode of Regulatory Spine Assembly and Drug Sensitivity in EGFR Kinase.
    Biochemistry, 2017, Jan-10, Volume: 56, Issue:1

    Topics: Allosteric Regulation; Amino Acid Motifs; Animals; Catalytic Domain; CHO Cells; Cricetinae; Cricetulus; Drug Resistance; Enzyme Activation; Epidermal Growth Factor; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Hydrophobic and Hydrophilic Interactions; Immunoblotting; Lapatinib; Molecular Dynamics Simulation; Mutation; Protein Kinase Inhibitors; Protein Structure, Secondary; Quinazolines

2017
Endothelin causes transactivation of the EGFR and HER2 in non-small cell lung cancer cells.
    Peptides, 2017, Volume: 90

    Topics: Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Proliferation; Endothelins; ErbB Receptors; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Peptides, Cyclic; Protein Kinase Inhibitors; Pyrrolidines; Quinazolines; Receptor, Endothelin A; Receptor, Endothelin B; Receptor, ErbB-2; Transcriptional Activation

2017
Daily or weekly dosing with EGFR inhibitors, gefitinib and lapatinib, and AKt inhibitor MK2206 in mammary cancer models.
    Oncology reports, 2018, Volume: 40, Issue:3

    Topics: Animals; Disease Models, Animal; Drug Administration Schedule; ErbB Receptors; Female; Gefitinib; Heterocyclic Compounds, 3-Ring; Lapatinib; Male; Mammary Neoplasms, Experimental; Mice; Mice, Knockout; Protein Kinase Inhibitors; Quinazolines; Rats; Rats, Sprague-Dawley; Triazoles

2018
Tyrosine Kinase Inhibitors Imatinib and Erlotinib Increase Apoptosis of Antimitotic Drug-resistant KBV20C Cells Without Inhibiting P-gp.
    Anticancer research, 2019, Volume: 39, Issue:7

    Topics: Antimitotic Agents; Apoptosis; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cell Line, Tumor; Drug Resistance, Neoplasm; Erlotinib Hydrochloride; Gefitinib; Humans; Imatinib Mesylate; Lapatinib; Protein Kinase Inhibitors; Vincristine

2019
Antioxidant functions of DHHC3 suppress anti-cancer drug activities.
    Cellular and molecular life sciences : CMLS, 2021, Volume: 78, Issue:5

    Topics: Acyltransferases; Antineoplastic Agents; Antioxidants; Apoptosis; Breast Neoplasms; Camptothecin; Cell Line, Tumor; Female; Gefitinib; Humans; Lapatinib; Male; Prostatic Neoplasms; RNA Interference

2021
Rac inhibition as a novel therapeutic strategy for EGFR/HER2 targeted therapy resistant breast cancer.
    BMC cancer, 2021, Jun-01, Volume: 21, Issue:1

    Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Breast Neoplasms; Carbazoles; Cell Line, Tumor; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; ErbB Receptors; Female; Gain of Function Mutation; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; MAP Kinase Signaling System; Point Mutation; Protein Kinase Inhibitors; Pyrimidines; rac GTP-Binding Proteins; Receptor, ErbB-2; Spheroids, Cellular; Up-Regulation

2021
The ixabepilone and vandetanib combination shows synergistic activity in docetaxel-resistant MDA-MB-231 breast cancer cells.
    Pharmacological reports : PR, 2022, Volume: 74, Issue:5

    Topics: Annexin A5; Antineoplastic Agents; Apoptosis; Caspase 3; Cell Line, Tumor; Cell Proliferation; Cytotoxins; Docetaxel; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-bcl-2; Triple Negative Breast Neoplasms

2022
Dual Inhibition of EGFR and IGF-1R Signaling Leads to Enhanced Antitumor Efficacy against Esophageal Squamous Cancer.
    International journal of molecular sciences, 2022, Sep-08, Volume: 23, Issue:18

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; ErbB Receptors; Esophageal Neoplasms; Esophageal Squamous Cell Carcinoma; Gefitinib; Humans; Insulin-Like Growth Factor I; Lapatinib; Protein Kinase Inhibitors; Receptor, IGF Type 1

2022
Evaluation of the Sensitivity of Breast Cancer Cell Lines to Cardiac Glycosides Unveils ATP1B3 as a Possible Biomarker for the Personalized Treatment of ERα Expressing Breast Cancers.
    International journal of molecular sciences, 2022, Sep-21, Volume: 23, Issue:19

    Topics: Adenosine Triphosphatases; Anastrozole; Aromatase Inhibitors; Biomarkers; Breast Neoplasms; Cardiac Glycosides; Cell Line, Tumor; Epidermal Growth Factor; ErbB Receptors; Erlotinib Hydrochloride; Estradiol; Estrogen Receptor alpha; Female; Fulvestrant; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Letrozole; MCF-7 Cells; Ouabain; Precision Medicine; Sodium-Potassium-Exchanging ATPase; Tamoxifen

2022
Identification of an Oxidative Stress-Related LncRNA Signature for Predicting Prognosis and Chemotherapy in Patients With Hepatocellular Carcinoma.
    Pathology oncology research : POR, 2022, Volume: 28

    Topics: Biomarkers, Tumor; Carcinoma, Hepatocellular; Dasatinib; Erlotinib Hydrochloride; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Liver Neoplasms; Oxidative Stress; Prognosis; RNA, Long Noncoding; Sorafenib

2022