rociletinib and Neoplasms

rociletinib has been researched along with Neoplasms* in 1 studies

Reviews

1 review(s) available for rociletinib and Neoplasms

ArticleYear
Recent progress on third generation covalent EGFR inhibitors.
    Bioorganic & medicinal chemistry letters, 2016, Apr-15, Volume: 26, Issue:8

    First generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (gefitinib and erlotinib) demonstrate excellent clinical efficacy for NSCLC patients carrying EGFR oncogenic mutations (L858R, del exon 19 deletions between amino acids 746 and 750). Invariable, drug resistance occurs with around 60% of it driven by the EGFR-T790M gatekeeper mutation. To counter the T790M-dependent resistance, third generation covalent EGFR inhibitors have been developed with high potency toward T790M containing mutants and selectivity over WT EGFR. This review provides an overview of the third generation drugs currently in clinical trials and also encompasses novel methodologies developed to discover third generation covalent EGFR drugs.

    Topics: Animals; Antineoplastic Agents; Drug Resistance, Neoplasm; ErbB Receptors; Humans; Neoplasms; Protein Kinase Inhibitors

2016