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Molecular Cancer Therapeutics

Molecular Cancer Therapeutics

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

Published:2 May 2022 DOI: 10.1158/1535-7163.mct-21-0835
Yong Du,?Yongfeng Chen,?Yuxia Wang,?Jinju Chen,?Xiaorong Lu,?Li Zhang,?Yan Li,?Zhaofu Wang,?Guozhong Ye,?George Zhang

Abstract

The epidermal growth factor receptor (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 NSCLC patients 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 C797S-containing triple mutants. HJM-561 potently inhibits the proliferation of Del19/T790M/C797S and L858R/T790M/C797S Ba/F3 cells while sparing cells expressing wild type EGFR. Oral administration of HJM-561 shows robust anti-tumor activity in EGFR Del19/T790M/C797S-driven Ba/F3 CDX and PDX models that were resistant to osimertinib treatment. Taken together, our results suggest that HJM-561 is a promising therapeutic option for overcoming EGFR triple mutation-mediated drug resistance in NSCLC.

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EGFR-IN-7 (compound 34) 2267329-76-8 C32H41BrN9O2P 78 suppliers Inquiry
EGFR-IN-7 (compound 34) 2267329-76-8 C32H41BrN9O2P 78 suppliers Inquiry
EGFR-IN-7 (compound 34) 2267329-76-8 C32H41BrN9O2P 78 suppliers Inquiry
EGFR-IN-7 (compound 34) 2267329-76-8 C32H41BrN9O2P 78 suppliers Inquiry

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