Page last updated: 2024-08-21

pyrazines and defactinib

pyrazines has been researched along with defactinib in 26 studies

Research

Studies (26)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's16 (61.54)24.3611
2020's10 (38.46)2.80

Authors

AuthorsStudies
Dalton, HJ; Hu, W; Huang, J; Ivan, C; Jennings, NB; Kang, Y; Liu, J; Liu, T; Lu, C; Miyake, T; Pecot, CV; Pradeep, S; Rupaimoole, R; Sood, AK; Taylor, M; Wen, Y; Wu, SY; Zand, B1
Annunziata, CM; Kohn, EC1
François, RA; Hochwald, SN; Kaye, FJ; Maeng, K; Nawab, A; Zajac-Kaye, M1
Bedard, PL; Bendell, JC; Cleary, JM; Houk, B; Infante, JR; Jones, SF; Pandya, SS; Pierce, KJ; Razak, AR; Roberts, WG; Shapiro, GI; Shreeve, SM; Siu, LL1
Chavan, A; Fukuoka, K; Horobin, J; Iwasa, T; Keegan, M; Nakagawa, K; Padval, M; Shimizu, T; Takeda, M; Vaickus, L; Yoshida, T1
Hallur, G; Mullangi, R; Saini, NK; Sulochana, SP; Tamizharasan, N; Zainuddin, M1
Batra, SK; Dhanasingh, I; Kanteti, R; Kaushik, G; Kindler, HL; Kulkarni, P; Mambetsariev, B; Mirzapoiazova, T; Nasser, MW; Ponnusamy, MP; Riehm, JJ; Salgia, R; Seshacharyulu, P; Wang, J1
Butler, LM; Castillo, L; Centenera, MM; Daly, RJ; Grogan, J; Haynes, AM; Horvath, LG; Kench, JG; Lee, BY; Lin, HM; Shreeve, SM; Spielman, C; Stricker, PD; Yeung, NK1
Fu, X; Guo, H; Li, CL; Lu, J; Nan, KJ; Tian, T; Wang, SH; Yang, YJ; Yao, Y1
Alcoser, SY; Aziz, A; Borgel, S; Bottaro, DP; Colantonio, S; Dieckman, L; Doroshow, JH; Hiltke, T; Hollingshead, MG; Kaczmarczyk, J; Kinders, RJ; Lee, YH; Navas, T; Parchment, RE; Pfister, TD; Saul, RG; Takebe, N; Tomaszewski, JE; Whiteley, G1
Crews, CM; Cromm, PM; Hines, J; Samarasinghe, KTG1
De Koning, L; De Wolf, J; Jaurand, MC; Jean, D; Le Pimpec-Barthes, F; Meiller, C; Montagne, F; Quetel, L; Tranchant, R; Zucman-Rossi, J1
Azab, AK; Azab, F; Buggio, M; de la Puente, P; Fiala, M; Muz, B; Pachter, JA; Padval, MV; Vij, R; Weaver, DT1
Aerts, JGJV; Baas, P; Cedrés, S; Fennell, DA; Gilligan, D; Kindler, H; Nakano, T; Nolan, L; Nowak, AK; Pachter, JA; Pavlakis, N; Scherpereel, A; Taylor, P; van Meerbeeck, JP; Weaver, DT1
Aerts, JGJV; Baas, P; Fennell, DA; Gilligan, D; Kindler, H; Nakano, T; Nowak, AK; Pavlakis, N; Scherpereel, A; Taylor, P; van Meerbeeck, JP1
Ishiki, H; Kiuchi, D; Masuda, K; Oyamada, S; Satomi, E; Shimizu, M1
Burns, TF; Camidge, DR; Cetnar, J; Gerber, DE; Horobin, JC; Jeong, W; Keegan, M; Kelly, RJ; Li, M; Morgensztern, D; Ramalingam, SS; Scaglioni, PP; Spigel, DR; Vaikus, L; Weaver, DT; Zhang, S1
Brekken, RA; Hosein, AN; Maitra, A1
Chen, L; Craven, R; Hamad, N; He, S; Huang, JA; Li, J; Liu, C; Liu, Z; Lu, X; Napier, D; Pan, Y; Qian, H; Shi, J; Thibault, O; Wang, C; Wei, D; Wei, X; Wu, Y; Xu, B; Xu, L; Yang, H; Yang, XH; Zhang, Y; Zheng, X; Zhou, BP1
Chen, J; Fan, J; Wang, Y; Zhan, Q; Zhang, J; Zhang, L; Zhang, W; Zhao, D1
Cai, T; Du, W; Fu, Y; Huang, JA; Lei, Z; Liu, T; Liu, Z; Wang, A; Zeng, Y; Zhang, Y; Zhu, J1
Sakai, M; Yoshimura, R1
Geng, X; He, J; Huang, H; Jenny Lu, HA; Jia, Y; Jin, W; Li, M; Li, X; Meng, J; Qiu, Z; Shao, G; Wang, L; Wang, S; Xu, Y; Yang, B; Zhang, S; Zhou, H1
Ai, Z; Almuttaqi, H; Berthold, DL; Bonham, S; Bullers, S; Corbin, AL; Eames, HL; Fischer, R; Jostins-Dean, L; Kessler, BM; Khoyratty, T; Pearson, C; Ryzhakov, G; Travis, SPL; Udalova, IA; Zec, K1
Bironzo, P; Bungaro, M; Capelletto, E; Denis, L; Koustenis, A; Novello, S1
Allert, C; Bauer, M; Besenbeck, B; Blank, MF; Bruckmann, M; Göllner, S; Heid, D; Janssen, M; Krijgsveld, J; Müller-Tidow, C; Pauli, C; Renders, S; Rohde, C; Trumpp, A; Waclawiczek, A; Wickenhauser, C; Zimmermann, SMN; Zinz, R1

Reviews

2 review(s) available for pyrazines and defactinib

ArticleYear
Pancreatic cancer stroma: an update on therapeutic targeting strategies.
    Nature reviews. Gastroenterology & hepatology, 2020, Volume: 17, Issue:8

    Topics: 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; Angiogenesis Inhibitors; Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Benzamides; Cancer-Associated Fibroblasts; Carcinoma, Pancreatic Ductal; Extracellular Fluid; Extracellular Matrix; Focal Adhesion Protein-Tyrosine Kinases; Humans; Hyaluronic Acid; Hyaluronoglucosaminidase; Mice; Molecular Targeted Therapy; Pancreatic Neoplasms; Permeability; Pressure; Protein Kinase Inhibitors; Pyrazines; rho-Associated Kinases; Sulfonamides; Tumor Microenvironment

2020
Single agent VS-6766 or VS-6766 plus defactinib in
    Future oncology (London, England), 2022, Volume: 18, Issue:16

    Topics: Benzamides; Carcinoma, Non-Small-Cell Lung; Clinical Trials, Phase II as Topic; Humans; Lung Neoplasms; Mutation; Proto-Oncogene Proteins p21(ras); Pyrazines; Sulfonamides

2022

Trials

4 trial(s) available for pyrazines and defactinib

ArticleYear
A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors.
    Investigational new drugs, 2015, Volume: 33, Issue:5

    Topics: Adult; Aged; Antineoplastic Agents; Area Under Curve; Benzamides; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Food-Drug Interactions; Half-Life; Humans; Male; Maximum Tolerated Dose; Middle Aged; Neoplasms; Organic Chemicals; Pyrazines; Sulfonamides

2015
A first-in-Asian phase 1 study to evaluate safety, pharmacokinetics and clinical activity of VS-6063, a focal adhesion kinase (FAK) inhibitor in Japanese patients with advanced solid tumors.
    Cancer chemotherapy and pharmacology, 2016, Volume: 77, Issue:5

    Topics: Administration, Oral; Adult; Aged; Antineoplastic Agents; Area Under Curve; Asian People; Benzamides; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Focal Adhesion Kinase 1; Focal Adhesion Kinase 2; Half-Life; Humans; Male; Middle Aged; Neoplasms; Pyrazines; Response Evaluation Criteria in Solid Tumors; Sulfonamides

2016
Maintenance Defactinib Versus Placebo After First-Line Chemotherapy in Patients With Merlin-Stratified Pleural Mesothelioma: COMMAND-A Double-Blind, Randomized, Phase II Study.
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2019, 04-01, Volume: 37, Issue:10

    Topics: Adult; Aged; Aged, 80 and over; Benzamides; Diarrhea; Double-Blind Method; Fatigue; Female; Humans; Kaplan-Meier Estimate; Lung Neoplasms; Male; Mesothelioma; Mesothelioma, Malignant; Middle Aged; Nausea; Neurofibromin 2; Pleural Neoplasms; Pyrazines; Sulfonamides; Treatment Outcome

2019
Phase 2 study of the focal adhesion kinase inhibitor defactinib (VS-6063) in previously treated advanced KRAS mutant non-small cell lung cancer.
    Lung cancer (Amsterdam, Netherlands), 2020, Volume: 139

    Topics: Adenocarcinoma of Lung; Benzamides; Carcinoma, Non-Small-Cell Lung; Drug Resistance, Neoplasm; Female; Focal Adhesion Protein-Tyrosine Kinases; Follow-Up Studies; Humans; Lung Neoplasms; Male; Middle Aged; Mutation; Prognosis; Prospective Studies; Proto-Oncogene Proteins p21(ras); Pyrazines; Salvage Therapy; Sulfonamides; Survival Rate

2020

Other Studies

20 other study(ies) available for pyrazines and defactinib

ArticleYear
Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer.
    Journal of the National Cancer Institute, 2013, Oct-02, Volume: 105, Issue:19

    Topics: Animals; Antineoplastic Agents, Phytogenic; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Benzamides; Cell Line, Tumor; Cell Proliferation; Cell Survival; Drug Resistance, Neoplasm; Female; Focal Adhesion Kinase 1; Humans; Mice; Mice, Nude; Odds Ratio; Organic Chemicals; Ovarian Neoplasms; Paclitaxel; Phosphorylation; Proto-Oncogene Proteins c-akt; Pyrazines; Sulfonamides; Xenograft Model Antitumor Assays; Y-Box-Binding Protein 1

2013
Novel facts about FAK: new connections to drug resistance?
    Journal of the National Cancer Institute, 2013, Oct-02, Volume: 105, Issue:19

    Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Benzamides; Drug Resistance, Neoplasm; Female; Focal Adhesion Kinase 1; Humans; Organic Chemicals; Ovarian Neoplasms; Paclitaxel; Pyrazines; Sulfonamides; Y-Box-Binding Protein 1

2013
Targeting Focal Adhesion Kinase and Resistance to mTOR Inhibition in Pancreatic Neuroendocrine Tumors.
    Journal of the National Cancer Institute, 2015, Volume: 107, Issue:8

    Topics: Animals; Antineoplastic Agents; Apoptosis; Benzamides; Carcinoma; Cell Line, Tumor; Cell Proliferation; Cell Survival; Drug Resistance, Neoplasm; Drug Synergism; Everolimus; Female; Focal Adhesion Kinase 1; Gene Expression Regulation, Enzymologic; Gene Expression Regulation, Neoplastic; Humans; Male; Mice; Mice, Inbred NOD; Mice, SCID; Molecular Targeted Therapy; Neuroendocrine Tumors; Organic Chemicals; Pancreatic Neoplasms; Peritoneal Neoplasms; Protein Kinase Inhibitors; Pyrazines; Signal Transduction; Sirolimus; Sulfonamides; TOR Serine-Threonine Kinases; Up-Regulation; Xenograft Model Antitumor Assays

2015
LC-ESI-MS/MS determination of defactinib, a novel FAK inhibitor in mice plasma and its application to a pharmacokinetic study in mice.
    Journal of pharmaceutical and biomedical analysis, 2018, Feb-05, Volume: 149

    Topics: Animals; Area Under Curve; Benzamides; Carbon Isotopes; Chromatography, High Pressure Liquid; Drug Stability; Focal Adhesion Kinase 1; Limit of Detection; Liquid-Liquid Extraction; Male; Mice; Mice, Inbred BALB C; Nitrogen Isotopes; Piperidines; Protein Kinase Inhibitors; Pyrazines; Pyrimidines; Pyrroles; Reference Standards; Reproducibility of Results; Spectrometry, Mass, Electrospray Ionization; Sulfonamides; Tandem Mass Spectrometry

2018
Focal adhesion kinase a potential therapeutic target for pancreatic cancer and malignant pleural mesothelioma.
    Cancer biology & therapy, 2018, 04-03, Volume: 19, Issue:4

    Topics: Animals; Benzamides; Carcinoma, Pancreatic Ductal; Cell Adhesion; Cell Culture Techniques; Cell Line, Tumor; Cell Movement; Focal Adhesion Kinase 1; Focal Adhesion Kinase 2; Humans; Lung Neoplasms; Mesothelioma; Mesothelioma, Malignant; Mice; Mice, Transgenic; Neoplasms, Experimental; Pancreatic Neoplasms; Phosphorylation; Pleural Neoplasms; Proto-Oncogene Proteins p21(ras); Pyrazines; Quinolones; Sulfonamides; Sulfones

2018
Effect of FAK inhibitor VS-6063 (defactinib) on docetaxel efficacy in prostate cancer.
    The Prostate, 2018, Volume: 78, Issue:4

    Topics: Animals; Antineoplastic Agents; Apoptosis; Benzamides; Cell Count; Cell Line, Tumor; Cell Proliferation; Cell Survival; Docetaxel; Drug Resistance, Neoplasm; Focal Adhesion Kinase 1; Humans; Immunoblotting; Immunohistochemistry; Male; Mice; Prostate; Prostatic Neoplasms, Castration-Resistant; Pyrazines; Sulfonamides; Xenograft Model Antitumor Assays

2018
β1 integrin-mediated multicellular resistance in hepatocellular carcinoma through activation of the FAK/Akt pathway.
    The Journal of international medical research, 2018, Volume: 46, Issue:4

    Topics: Apoptosis; Benzamides; Carcinoma, Hepatocellular; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; Focal Adhesion Protein-Tyrosine Kinases; Humans; Integrin beta1; Liver Neoplasms; Proto-Oncogene Proteins c-akt; Pyrazines; Signal Transduction; Spheroids, Cellular; Sulfonamides

2018
Novel antibody reagents for characterization of drug- and tumor microenvironment-induced changes in epithelial-mesenchymal transition and cancer stem cells.
    PloS one, 2018, Volume: 13, Issue:6

    Topics: AC133 Antigen; Animals; Antibodies, Monoclonal; Antineoplastic Agents; Benzamides; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Epithelial-Mesenchymal Transition; Female; Gene Knock-In Techniques; Hepatocyte Growth Factor; Humans; Indicators and Reagents; Lung Neoplasms; Mice, Transgenic; Neoplastic Stem Cells; Phenotype; Pyrazines; Sulfonamides; Triple Negative Breast Neoplasms; Tumor Microenvironment; Xenograft Model Antitumor Assays

2018
Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation.
    Journal of the American Chemical Society, 2018, 12-12, Volume: 140, Issue:49

    Topics: Antineoplastic Agents; Benzamides; Cell Line, Tumor; Cell Movement; Drug Design; Focal Adhesion Kinase 1; Humans; Protein Kinase Inhibitors; Proteolysis; Pyrazines; Signal Transduction; Sulfonamides

2018
Assessment of signaling pathway inhibitors and identification of predictive biomarkers in malignant pleural mesothelioma.
    Lung cancer (Amsterdam, Netherlands), 2018, Volume: 126

    Topics: Antineoplastic Agents; Apoptosis; Benzamides; Biomarkers, Tumor; Cell Proliferation; Cell Survival; Gene Expression Regulation, Neoplastic; Humans; Lung Neoplasms; Mesothelioma; Phenols; Pleural Neoplasms; Pyrazines; Quinolones; RNA Interference; Signal Transduction; Sulfonamides; Tumor Cells, Cultured; Verteporfin

2018
PYK2/FAK inhibitors reverse hypoxia-induced drug resistance in multiple myeloma.
    Haematologica, 2019, Volume: 104, Issue:7

    Topics: Aminopyridines; Benzamides; Drug Resistance, Neoplasm; Focal Adhesion Kinase 1; Focal Adhesion Kinase 2; Humans; Hypoxia; Multiple Myeloma; Proteasome Inhibitors; Pyrazines; Sulfonamides; Tumor Cells, Cultured

2019
Reply to K. Masuda et al.
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2019, 09-01, Volume: 37, Issue:25

    Topics: Benzamides; Double-Blind Method; Humans; Mesothelioma; Neurofibromin 2; Pyrazines; Sulfonamides

2019
Questions Regarding the Randomized Phase II Trial of Defactinib as Maintenance Therapy in Malignant Pleural Mesothelioma.
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2019, 09-01, Volume: 37, Issue:25

    Topics: Benzamides; Double-Blind Method; Humans; Mesothelioma; Neurofibromin 2; Pleural Neoplasms; Pyrazines; Sulfonamides

2019
BRD4 modulates vulnerability of triple-negative breast cancer to targeting of integrin-dependent signaling pathways.
    Cellular oncology (Dordrecht), 2020, Volume: 43, Issue:6

    Topics: Azepines; Bcl-2-Like Protein 11; Benzamides; Cell Cycle Proteins; Cell Death; Cell Line, Tumor; Cell Survival; Focal Adhesion Protein-Tyrosine Kinases; Gene Expression Regulation, Neoplastic; Genome, Human; Humans; Integrins; Proto-Oncogene Proteins c-myc; Pyrazines; RNA, Messenger; Signal Transduction; Sulfonamides; Transcription Factors; Triazoles; Triple Negative Breast Neoplasms

2020
Focal adhesion kinase (FAK) inhibitor-defactinib suppresses the malignant progression of human esophageal squamous cell carcinoma (ESCC) cells via effective blockade of PI3K/AKT axis and downstream molecular network.
    Molecular carcinogenesis, 2021, Volume: 60, Issue:2

    Topics: Animals; Benzamides; Carcinoma, Squamous Cell; Cell Line, Tumor; Disease Progression; Esophageal Neoplasms; Female; Focal Adhesion Protein-Tyrosine Kinases; Gene Expression Profiling; Gene Expression Regulation, Neoplastic; Gene Ontology; Gene Regulatory Networks; Humans; Kaplan-Meier Estimate; Mice, Inbred BALB C; Mice, Nude; Phosphatidylinositol 3-Kinase; Proto-Oncogene Proteins c-akt; Pyrazines; Signal Transduction; Sulfonamides; Xenograft Model Antitumor Assays

2021
Abnormally activated OPN/integrin αVβ3/FAK signalling is responsible for EGFR-TKI resistance in EGFR mutant non-small-cell lung cancer.
    Journal of hematology & oncology, 2020, 12-07, Volume: 13, Issue:1

    Topics: Animals; Antineoplastic Agents; Benzamides; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Drug Resistance, Neoplasm; ErbB Receptors; Focal Adhesion Kinase 1; Gefitinib; Humans; Integrin alphaVbeta3; Lung Neoplasms; Male; Mice, Inbred BALB C; Mice, Nude; Osteopontin; Protein Kinase Inhibitors; Pyrazines; Signal Transduction; Sulfonamides

2020
Mechanotransduction-Targeting Drugs Attenuate Stiffness-Induced Hepatic Stellate Cell Activation in Vitro.
    Biological & pharmaceutical bulletin, 2021, Mar-01, Volume: 44, Issue:3

    Topics: Actins; Adenosine Triphosphate; Animals; Benzamides; Cells, Cultured; Colchicine; Collagen Type I; Hepatic Stellate Cells; Imidazoles; Integrins; Male; Mechanotransduction, Cellular; Paclitaxel; Piperazines; Pyrazines; Quinoxalines; Rats, Sprague-Dawley; Roscovitine; Sulfonamides; Transforming Growth Factor beta; Tubulin Modulators

2021
Inhibiting Focal Adhesion Kinase Ameliorates Cyst Development in Polycystin-1-Deficient Polycystic Kidney Disease in Animal Model.
    Journal of the American Society of Nephrology : JASN, 2021, Volume: 32, Issue:9

    Topics: Aminopyridines; Animals; Benzamides; Cell Culture Techniques; Cell Proliferation; Disease Models, Animal; Dogs; Epithelial Cells; Focal Adhesion Protein-Tyrosine Kinases; Humans; Hydroxamic Acids; Mice; Mice, Inbred C57BL; Polycystic Kidney, Autosomal Dominant; Pyrazines; Signal Transduction; Sulfonamides

2021
Defactinib inhibits PYK2 phosphorylation of IRF5 and reduces intestinal inflammation.
    Nature communications, 2021, 11-18, Volume: 12, Issue:1

    Topics: Animals; Benzamides; Cells, Cultured; Colitis; Cytokines; Focal Adhesion Kinase 2; Gene Expression Profiling; HEK293 Cells; Humans; Inflammation; Interferon Regulatory Factors; Intestines; Macrophages; Male; Mice; Mice, Inbred C57BL; Mutation; Phosphorylation; Pyrazines; RAW 264.7 Cells; Sulfonamides

2021
Protein tyrosine kinase 2b inhibition reverts niche-associated resistance to tyrosine kinase inhibitors in AML.
    Leukemia, 2022, Volume: 36, Issue:10

    Topics: Animals; Benzamides; Cell Line, Tumor; Daunorubicin; Drug Resistance, Neoplasm; fms-Like Tyrosine Kinase 3; Focal Adhesion Kinase 2; Humans; Leukemia, Myeloid, Acute; Mice; Mutation; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proteome; Pyrazines; Sulfonamides

2022