Small molecule epidermal growth factor receptor tyrosine kinase inhibitors: an overview.
The epidermal growth factor receptor (EGFR) has been identified as a relevant target for treatment of solid tumors, as it is involved in regulating cellular functions important in the proliferation and survival of cancer cells, is commonly expressed in a range of tumors, and high expression is often related to poor prognosis. Some of the most advanced target based agents in clinical development are the EGFR tyrosine kinase inhibitors (EGFR-TKIs). This brief review summarizes the results of phase II monotherapy trials of EGFR TKIs in cancer patients. The molecular mechanisms involved in regulating the sensitivity/resistance of tumor cells to EGFR-TKIs are also discussed.
Normanno
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N
Department of Experimental Oncology, Istituto Nazionale Tumori-Fondazione Pascale, Naples, Italy. nicnorm@yahoo.com
Maiello
M R
MR
Mancino
M
M
De Luca
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A
D001682:Biological Availability; D017321:Clinical Trials, Phase I as Topic; D017326:Clinical Trials, Phase III as Topic; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D005260:Female; D006801:Humans; D008297:Male; D008970:Molecular Weight; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D011379:Prognosis; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000627:therapeutic use; D016896:Treatment Outcome
D004791:Enzyme Inhibitors; D066246:ErbB Receptors; D011505:Protein-Tyrosine Kinases