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HJM-561, a Potent, Selective, and Orally Bioavailable EGFR PROTAC that Overcomes Osimertinib-Resistant EGFR Triple Mutations.

Molecular cancer therapeutics - 5 Jul 2022

Du Yong, Chen Yongfeng, Wang Yuxia, Chen Jinju, Lu Xiaorong, Zhang Li, Li Yan, Wang Zhaofu, Ye Guozhong, Zhang George

Abstract excerpt

The EGFR C797S mutation is the most common on-target resistance mechanism to osimertinib in patients with advanced non-small cell lung cancer (NSCLC). Currently there are no effective treatment options for patients with NSCLC harboring EGFR C797S triple mutants (Del19/T790M/C797S and L858R/T790M/C797S). Herein, we report an orally bioavailable EGFR PROTAC, HJM-561, which selectively degrades the EGFR...

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PMID: 35499406
DOI: 10.1158/1535-7163.MCT-21-0835

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