EGFR tyrosine kinase

Gefitinib (Iressa) EGFR tyrosine kinase inhibitor Third-line tumor — non-small ceU Irmg Phase II... 

Erlotinib (Tarceva) EGFR tyrosine kinase inhibitor Refractory non-smaU ceU lung cancer Randomized Phase III... 

Tortora G, Caputo R, Damiano V, et al. Specific Inhibition of EGFR Tyrosine Kinase with ZD1839 ( Iressa ) Combined with a Protein Kinase a Antisense and the Novel Taxane IDN5109 Causes Cooperative Inhibition of Tumour Growth and Angiogenesis. Proceedings of the AACR, Vol. 42, March 2001. abstract 4315. 

Kitazaki T, Oka M, Nakamura Y et al. Gefitinib, an EGFR tyrosine kinase inhibitor, directly inhibits the function of P-glycoprotein in multidrug resistant cancer cells. Lung Cancer 2005 49 337-343. 

Wang SE, Narasanna A, Perez-Torres M et al. HER2 kinase domain mutation results in constitutive phosphorylation and activation of HER2 and EGFR and resistance to EGFR tyrosine kinase inhibitors. Cancer Cell 2006 10 25-38. 

Assefa, H., Kamath, S., Buolamwini, J.K. 3D-QSAR and Docking Studies on 4-An-ilinoquinazoline and 4-Anilinoquinoline Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors. 

Non-small cell lung cancer Mutation EGFR EGFR (tyrosine-kinase activity) Erlotinib, Gefitinib... 

Li J et al (2006) CYP3A Phenotyping approach to predict systemic exposure to EGFR tyrosine kinase inhibitors. J Natl Cancer Inst 98 1714-1723... 

Traxler, R, Green, J., Mett, H., Sequin, U., and Furet, R, Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors isoflavones and 3-phenyl-4(lH)-quinolones, J. Med. Chem. 42, 1018, 1999. 

Category Epidermal growth factor receptor (EGFR) Tyrosine kinase inhibitor Half-life 24 Hours... 

Sirotnak FM, Zakowski MF, Miller YA, Scher HI, Kris MG. 2000. Efficacy of cytotoxic agents against human tumor xenografts is markedly enhanced by coadministration ofZD1839 (Iressa), an inhibitor of EGFR tyrosine kinase. Clin. Cancer Res. 6 4885-92... 

Fig. 5.6 Examples of novel small molecule and peptide radiotracers for in vivo pharmacodynamic imaging, (a) f C]ML03, an irreversible inhibitor of EGFR tyrosine kinase and potential PET marker for the receptor (b) f F]SAV03, an MMP-2 inhibi-...

Binds irreversibly to the DNA-topoisomerase 1 complex, leading to the irreversible cleavage of DNA and the destruction of cellular topoisomerase 1 by the ubiquitin-proteosome pathway. Induces apopUxsi.s in many normal and tumor cell lines. Potent antimmor agent with anti-inflammatory and antioxidant properties. Potent inhibitor of protein kinase C, EGFR tyrosine kinase, and 1KB kinase. Induces apoptosis of cancer cells. 

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