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| Type |
Poster Presentation |
| Area |
의약화학 |
| Room No. |
포스터발표장 |
| Time |
4월 20일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-421 |
| Subject |
Development of 4th generation EGFR Inhibitors overcoming EGFR C797S mutation for lung cancer treatment |
| Authors |
전병욱, 최현정1, 신인지2, 전문국2, 채종학3, 최길돈4, 이광호5,*
서강대학교 화학과, Korea
1KAIST 화학과, Korea
2한국화학연구원 의약화학연구센터, Korea
3한국화학연구원 신물질연구본부/신약플랫폼기술팀, Korea
4한국화학연구원 의약바이오연구본부, Korea
5한국화학연구원 신물질본부/난치성, Korea
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| Abstract |
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 showing limit of the irreversible inhibitors.
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 are explored to overcome EGFR L858R/T790M/C797S and EGFR ex19del/T790M/C797S triple mutants for effective clinical treatment for NSCLC patients. |
| E-mail |
quddnr418@naver.com |
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119th General Meeting of the KCS