Zipalertinib (TAS6417) (10-200 mg/kg) causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models. TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues[1].
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Zipalertinib (TAS6417) had no effect on EGFR-independent proliferation in NCI-H23 or NCI-H460 cells[1].
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Zipalertinib (TAS6417) administered at 20 mg/kg, which achieves complete suppression of tumor growth, induces a significant decrease in pEGFR, leading to reduction of pAKT and pERK at 1 h. The inhibitory effect is still noted at 6 h, and phosphorylation of EGFR, ATK, and ERK recovered by 24 h[1].
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Zipalertinib (TAS6417) (100 and 200 mg/kg/day) prolongs survival of animals bearing lung cancer[1].
| Animal Model: | Mice implanted with NCI-H1975 EGFR D770_N771insSVD xenografts[1]. |
| Dosage: | 50 and 100 mg/kg. |
| Administration: | Orally once daily for 14 days. |
| Result: | Showed marked tumor growth inhibition with treatment/control (T/C) ratios of 51% and 19%, respectively. |
