Page last updated: 2024-09-03

gefitinib and rociletinib

gefitinib has been researched along with rociletinib in 12 studies

Compound Research Comparison

Studies
(gefitinib)
Trials
(gefitinib)
Recent Studies (post-2010)
(gefitinib)
Studies
(rociletinib)
Trials
(rociletinib)
Recent Studies (post-2010) (rociletinib)
5,2315662,91961560

Protein Interaction Comparison

ProteinTaxonomygefitinib (IC50)rociletinib (IC50)
Epidermal growth factor receptorHomo sapiens (human)0.1682
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)0.1176
Receptor tyrosine-protein kinase erbB-3Homo sapiens (human)0.1057
Fatty-acid amide hydrolase 1Rattus norvegicus (Norway rat)0.072
Receptor tyrosine-protein kinase erbB-4Homo sapiens (human)0.1176

Research

Studies (12)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's11 (91.67)24.3611
2020's1 (8.33)2.80

Authors

AuthorsStudies
Becker, C; Engel, J; Eppmann, S; Getlik, M; Grütter, C; Heil, J; Heuckmann, JM; Hoffgaard, F; Kast, SM; Keul, M; Kibies, P; Krüll, J; Lategahn, J; Mayer-Wrangowski, S; Menninger, S; Ortiz-Cuaran, S; Rauh, D; Richters, A; Schaumann, N; Schultz-Fademrecht, C; Sos, ML; Termathe, M; Thomas, RK; Tinnefeld, V; Tomassi, S; Uhlenbrock, N; Zahedi, RP1
Ge, Y; Jin, Y; Li, Y; Liu, K; Ma, X; Peng, J; Song, Z; Tang, Z; Wang, C; Zhang, J1
Bauer, S; Baumann, M; Engel, J; Ketzer, J; Keul, M; Lategahn, J; Mühlenberg, T; Rauh, D; Schultz-Fademrecht, C; Tomassi, S; Tumbrink, HL1
Ge, Y; Li, Y; Liu, K; Ma, X; Meng, Q; Peng, J; Song, A; Tang, Z; Wang, C; Zhang, J1
Huang, S; Jiang, Y; Li, Y; Liu, K; Ma, X; Meng, Q; Shu, X; Song, Z; Sun, H; Wang, C; Yu, H1
Baumann, M; Becker, C; Engel, J; Goebel, L; Günther, G; Hengstler, JG; Hennes, E; Keul, M; Lategahn, J; Müller, H; Rauh, D; Schultz-Fademrecht, C; Smith, S; Tumbrink, HL; Unger, A1
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
An, B; Chen, C; Fan, R; Li, J; Li, X; Song, X; Wei, S; Zhang, Q; Zou, Y1
Gilligan, D; Pacey, S; Tan, CS1
Chiba, M; Kobayashi, Y; Mitsudomi, T; Mizuuchi, H; Murakami, I; Nishio, K; Sakai, K; Sato, K; Sekido, Y; Sesumi, Y; Shimoji, M; Suda, K; Takemoto, T; Tomizawa, K1
Ballard, P; Box, M; Cantarini, M; Cross, D; Grist, M; Hickey, M; Jänne, PA; Johnström, P; Jordan, A; Kim, DW; Malmquist, J; Pickup, K; Thress, KS; Varnäs, K; Yang, JC; Yang, Z; Yates, JW1
Jiang, Y; Li, Z; Wan, S; Wu, X; Yan, R; Zhang, J1

Reviews

1 review(s) available for gefitinib and rociletinib

ArticleYear
Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer.
    The Lancet. Oncology, 2015, Volume: 16, Issue:9

    Topics: Acrylamides; Afatinib; Aniline Compounds; Carcinoma, Non-Small-Cell Lung; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Protein Kinase Inhibitors; Pyrimidines; Quinazolines

2015

Other Studies

11 other study(ies) available for gefitinib and rociletinib

ArticleYear
Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.
    Journal of medicinal chemistry, 2015, Sep-10, Volume: 58, Issue:17

    Topics: Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Membrane Permeability; Crystallography, X-Ray; Databases, Chemical; Drug Design; Drug Resistance, Neoplasm; ErbB Receptors; Humans; Kinetics; Lung Neoplasms; Models, Molecular; Molecular Conformation; Mutation; Pyrazoles; Pyrimidines; Quinazolines; Small Molecule Libraries; Solubility; src-Family Kinases; Structure-Activity Relationship

2015
Synthesis and biological evaluation of azole-diphenylpyrimidine derivatives (AzDPPYs) as potent T790M mutant form of epidermal growth factor receptor inhibitors.
    Bioorganic & medicinal chemistry, 2016, 11-01, Volume: 24, Issue:21

    Topics: Azoles; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; ErbB Receptors; Humans; Models, Molecular; Molecular Structure; Mutation; Protein Kinase Inhibitors; Pyrimidines; Structure-Activity Relationship

2016
Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.
    Journal of medicinal chemistry, 2017, 03-23, Volume: 60, Issue:6

    Topics: Animals; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Drug Resistance, Neoplasm; ErbB Receptors; Humans; Indazoles; Lung; Lung Neoplasms; Mice; Molecular Docking Simulation; Mutation; Protein Kinase Inhibitors

2017
C-2 (E)-4-(Styryl)aniline substituted diphenylpyrimidine derivatives (Sty-DPPYs) as specific kinase inhibitors targeting clinical resistance related EGFR
    Bioorganic & medicinal chemistry, 2017, 05-15, Volume: 25, Issue:10

    Topics: Aniline Compounds; Antineoplastic Agents; Binding Sites; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; ErbB Receptors; Humans; Molecular Docking Simulation; Mutation; Protein Kinase Inhibitors; Protein Structure, Tertiary; Pyrimidines; Stereoisomerism; Structure-Activity Relationship

2017
Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC).
    European journal of medicinal chemistry, 2017, Jun-16, Volume: 133

    Topics: Animals; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Drug Resistance, Neoplasm; ErbB Receptors; Gefitinib; Humans; Lung; Lung Neoplasms; Mice; Models, Molecular; Morpholines; Point Mutation; Protein Kinase Inhibitors; Pyrimidines; Quinazolines; Xenograft Model Antitumor Assays

2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.
    Journal of medicinal chemistry, 2017, 09-28, Volume: 60, Issue:18

    Topics: Animals; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Drug Resistance, Neoplasm; ErbB Receptors; Humans; Lung Neoplasms; Male; Mice; Molecular Docking Simulation; Point Mutation; Protein Kinase Inhibitors; Pyrazoles; Pyrimidines

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
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR
    European journal of medicinal chemistry, 2021, Feb-15, Volume: 212

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; ErbB Receptors; Humans; Male; Mice; Mice, Nude; Models, Molecular; Molecular Structure; Neoplasms, Experimental; Protein Kinase Inhibitors; Pyrimidines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship

2021
Oncogene swap as a novel mechanism of acquired resistance to epidermal growth factor receptor-tyrosine kinase inhibitor in lung cancer.
    Cancer science, 2016, Volume: 107, Issue:4

    Topics: Acrylamides; Cell Line, Tumor; Drug Resistance, Neoplasm; ErbB Receptors; Gefitinib; Humans; Lung Neoplasms; Mutation; Oncogenes; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-met; Pyrimidines; Quinazolines

2016
Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2016, Oct-15, Volume: 22, Issue:20

    Topics: Acrylamides; Afatinib; Aniline Compounds; Animals; Antineoplastic Agents; Biological Transport; Blood-Brain Barrier; Brain Neoplasms; Caco-2 Cells; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Disease Progression; Dogs; Drug Evaluation, Preclinical; Drug Resistance, Neoplasm; ErbB Receptors; Female; Gefitinib; Humans; Lung Neoplasms; Madin Darby Canine Kidney Cells; Male; Mice; Mice, SCID; Middle Aged; Piperazines; Protein Kinase Inhibitors; Pyrimidines; Quinazolines; Rats; Xenograft Model Antitumor Assays

2016
Insight into binding mechanisms of EGFR allosteric inhibitors using molecular dynamics simulations and free energy calculations.
    Journal of biomolecular structure & dynamics, 2019, Volume: 37, Issue:16

    Topics: Acrylamides; Allosteric Regulation; Aniline Compounds; Benzeneacetamides; Carcinoma, Non-Small-Cell Lung; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Molecular Dynamics Simulation; Mutation; Protein Binding; Protein Kinase Inhibitors; Pyrimidines; Thiazoles

2019