Chronicles of EGFR TKIs

조회수 : 493 등록일 : 2019.03.20 09:34

일시 : 2019.03.20 17:00
소속 : 한국화학연구원
발표자 : 이광호
장소 : R404

Erlotinib (Tarceva) & Gefitinib (Iressa) are the first class of drugs as epidermal growth factor receptor (EGFR) kinase inhibitors for non-small cell lung cancer (NSCLC) treatment. However, their clinical use is ultimately limited due to the mechanism-based toxicity and development of drug-resistance EGFR T790M mutation. Osimeritinib (Tagrisso), an irreversible inhibitor, has recently approved as for the next generation treatment option to overcome the short-comings of the first class drug use. Latest Osimeritinib clinical trial report reveals new acquired-resistant mechanism: EGFR C797S mutation limits the irreversible inhibitor.

In this presentation, new medicinal chemistry strategy is discussed to address the currently unmet-medical needs for EGFR-related NSCLC patients. Reversible pyrimidine-based inhibitors and allosteric inhibitros are explored to overcome EGFR L858R/T790M/C797S and EGFR ex19del/T790M/C797S triple mutants for effective clinical treatment for NSCLC patients.

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