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Association details:
| Biomarker: | EGFR C797S + EGFR T790M + EGFR L858R |
|---|---|
| Cancer: | Non Small Cell Lung Cancer |
| Drug: | H002 (EGFR inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
5461 - H002: A wide spectrum, highly selective fourth-generation EGFR inhibitor overcoming resistance harboring C797S mutation in NSCLC
Published date:
03/09/2022
Excerpt:
In vitro and in vivo anti-tumor efficacy was determined in drug-resistant mutant cell lines, CDX and PDX models. Single mutants (Del or L858R), double mutants (Del/T790M or L858R/T790M) and triple mutants (Del/T790M/C797S or L858R/T790M/C797S)...H002 was highly active against all forementioned single, double or triple EGFR mutants (IC50 < 5 nM)...H002 also exhibited potent anti-tumor effects in a dose-dependent manner in various CDX and PDX models....H002 has been demonstrated as a promising next generation EGFR inhibitor, with high selectivity, a wide spectrum and potent anti-tumor activity against various EGFR activating mutations, favorable DMPK and safety profiles.
