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Association details:
| Biomarker: | EGFR C797S + EGFR T790M + EGFR exon 19 deletion |
|---|---|
| Cancer: | Non Small Cell Lung Cancer |
| Drug: | HJM-561 (EGFR degrader) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
HJM-561, a Potent, Selective, and Orally Bioavailable EGFR PROTAC that Overcomes Osimertinib-Resistant EGFR Triple Mutations
Published date:
07/05/2022
Excerpt:
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 antitumor activity in EGFR Del19/T790M/C797S-driven Ba/F3 CDX and PDX models that were resistant to osimertinib treatment.
DOI:
10.1158/1535-7163.MCT-21-0835
