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Title: | Targeting non-small cell lung cancer with small-molecule EGFR tyrosine kinase inhibitor |
Authors: | Jadhav, Hemant R. |
Keywords: | Pharmacy Epidermal growth factor (EGFR) Tyrosine kinase inhibitors (TKIs) NSCLC |
Issue Date: | Mar-2018 |
Publisher: | Elsevier |
Abstract: | Epidermal growth factor (EGFR) tyrosine kinase inhibitors (TKIs), such as gefitinib and erlotinib, show excellent clinical efficacy for patients with non-small cell lung cancer (NSCLC) with EGFR mutations, including Exon 19 deletion and single-point substitution, and L858R of exon 21. The reason for the reduction in effectiveness of these EGFR TKIs is the T790M gatekeeper mutation in the ATP-binding pocket of Exon 20, which increases the affinity of EGFR for ATP. Newer EGFR TKIs, such as afatinib, osimertinib, rociletinib, EGF816 and ASP8273, selectively target T790M mutants, sparing wild-type EGFR. EGFR TKIs have fewer adverse effects than chemotherapy and also improve progression-free survival. Combination therapy of EGFR TKIs with anti-EGFR antibodies is recommended for overcoming the problem of resistance to some extent. This review could help medicinal chemists to design novel EGFR TKIs against NSCLC. |
URI: | https://www.sciencedirect.com/science/article/abs/pii/S1359644617303719 http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/13264 |
Appears in Collections: | Department of Pharmacy |
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