作者: Kong, Yun Jeong ; Cho, Jeongin ; Lee, Chae Won ; Kim, Jae-Sun ; Lee, Sunho ; Im, Kyungtaek ; Lee, Hyeonjeong ; Lee, Jae Cheol ; Kim, Sung-Eun ; Woo, Dong-Cheol ; Kim, Dong Ha ; Rho, Jin Kyung ; Kim, Da-Som ; Choi, Chang-Min ; Min, Joongkee ; Rengasamy, Rajesh ; Choi, Yun Jung ; Sung, Young Hoon ; Ryu, Hyung Chul ; Ji, Wonjun

Cancer Research

Retraction: The Reversible Fourth-Generation EGFR Tyrosine Kinase Inhibitor OBX02-011 Overcomes C797S-Mediated Resistance in Lung Cancer

作者: Kong, Yun Jeong ; Cho, Jeongin ; Lee, Chae Won ; Kim, Jae-Sun ; Lee, Sunho ; Im, Kyungtaek ; Lee, Hyeonjeong ; Woo, Dong-Cheol ; Lee, Jae Cheol ; Kim, Sung-Eun ; Kim, Dong Ha ; Rho, Jin Kyung ; Kim, Da-Som ; Choi, Chang-Min ; Min, Joongkee ; Rengasamy, Rajesh ; Choi, Yun Jung ; Sung, Young Hoon ; Ryu, Hyung Chul ; Ji, Wonjun

Cancer Research

The Reversible Fourth-Generation EGFR Tyrosine Kinase Inhibitor OBX02–011 Overcomes C797S-Mediated Resistance in Lung Cancer

Article

作者: Min, Joongkee ; Ryu, Hyung Chul ; Ji, Wonjun ; Kim, Dong Ha ; Rengasamy, Rajesh ; Woo, Dong-Cheol ; Cho, Jeongin ; Choi, Chang-Min ; Choi, Yun Jung ; Sung, Young Hoon ; Kim, Jae-Sun ; Rho, Jin Kyung ; Lee, Sunho ; Kim, Sung-Eun ; Kong, Yun Jeong ; Lee, Jae Cheol ; Lee, Hyeonjeong ; Kim, Da-Som ; Lee, Chae Won ; Im, Kyungtaek

AbstractOsimertinib is an irreversible third-generation EGFR tyrosine kinase inhibitor (TKI) that was initially developed to overcome the EGFR T790M mutation and is used as a standard therapy in patients with advanced non–small cell lung cancer (NSCLC) with EGFR-activating mutations. Despite the remarkable initial efficacy, osimertinib, like other EGFR-TKIs, is limited by the emergence of acquired resistance. As the EGFR mutation C797S has been identified as a key driver of acquired resistance to osimertinib, development of a drug that targets this clinically relevant mutation could help improve patient outcomes. Here, we report the discovery and preclinical efficacy of OBX02–011, a reversible fourth-generation EGFR-TKI that overcomes the EGFR C797S mutation. Compared with approved EGFR-TKIs, OBX02–011 showed potent anticancer effects and inhibited EGFR-related signaling in various models, including those harboring the EGFR C797S mutation. In addition, in transgenic mouse models (EGFRL858R/T790M/C797S), OBX02–011 treatment effectively inhibited tumor growth and EGFR activity, leading to enhanced survival. Collectively, these results suggest that OBX02–011 may be a promising new EGFR-TKI to overcome C797S-mediated resistance in NSCLC.Significance:OBX02–011 is designed to target EGFR C797S and can overcome EGFR double and triple mutations to effectively treat lung cancer.

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适应症	最高研发状态	国家/地区	公司	日期
ALK阳性非小细胞肺癌	临床1期	韩国	Oncobix Co., Ltd.	-
EGFR阳性非小细胞肺癌	临床1期	韩国	Oncobix Co., Ltd.	-
胶质母细胞瘤	药物发现	韩国	Oncobix Co., Ltd.	2023-04-26
特发性肺纤维化	药物发现	韩国	Oncobix Co., Ltd.	2023-04-26