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  • 03월 02일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제109회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Pre-clinical and Clinical Development of Radotinib (Supect?) in Leukemia ; identification of a next generation Bcr-Abl tyrosine kinase inhibitor

2012년 2월 27일 10시 03분 15초
MEDI-5 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
금 12시 : 20분
의약화학 - Drugs on the way for successful IND
저자 및
가톨릭대학교 암연구소, Korea
Imatinib mesylate (Glivec? or Gleevec?; Novartis co., Switzeland) has been preferentially used as 1st line therapy in chronic myeloid leukemia (CML) and has shown imposing responses in clinical practice. However imatinib resistance has observed in some patients and a majority of patients rapidly progressed to advanced disease resulting in fatal outcome. Based on the first successful development of imatinib and the mechanism of drug resistance, the development of more effective ATP-competitive BCR-ABL tyrosine kinase inhibitor (TKI) has been triggered and eventually second generation (2G) TKIs such as dasatinib (Sprycel?; Bristol Myers Squibb co., USA), nilotinib (Tasigna?; Novartis co., Switzeland), bosutinib (Pfizer co., USA), radotinib (Supect?; Ilyang co., Korea) have developed. In multicenter phase 2 and 3 clinical trials, 2G TKIs have been found to have superior cytogenetic and molecular responses. Radotinib was designed to be a potent, highly selective inhibitor of BCR-ABL kinase and we have identified preclinical and clinical activities. In vitro potency is 35 to 50 times more potent than imatinib in various CML cell lines and at least 20 times more potent in suppressing CML tumor growth using xenograft mouse model. Except for T315I, it has sufficiently suppressed Y253H, E255K, F317L and M351T mutant clones. In phase 1 and 2 clinical studies, radotinib showed superior efficacy and good tolerability, and it was comparable to clinical results of other 2G TKIs. Radotinib is now approved for the treatment of patients with imatinib failure and a phase 3 clinical study to compare the efficacy and the tolerability with imatinib is currently ongoing in new patients. This presentation will summarize the detailed pre-clinical and clinical data of radotinib.