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  1. 1 lip 2019 · The current study examines the efficacy, safety, and tolerability of ASP8273 versus erlotinib or gefitinib in patients with non-small-cell lung cancer (NSCLC) with activating EGFR mutations not previously treated with an EGFR inhibitor.

  2. Background: ASP8273 is a small molecule, irreversible tyrosine kinase inhibitor (TKI) that inhibits the kinase activity of both EGFR activating mutations and T790M resistance mutation, with higher potency than wild type EGFR.

  3. 15 gru 2017 · ASP8273 is a third-generation EGFR TKI with antitumor activity in preclinical models of EGFR-mutant lung cancer that targets mutant EGFR, including EGFR T790M.

  4. 14 gru 2017 · ASP8273 demonstrated antitumor activity in patients with EGFR-mutant lung cancers after prior treatment with EGFR TKIs. This study identified the ASP8273 RP2D to be 300 mg daily based on pharmacokinetics, pharmacodynamics, safety, and antitumor activity; the MTD was not established.

  5. 20 maj 2016 · Described here are the preliminary antitumor effects of the RP2D in EGFR mutation-positive non-small cell lung cancer (NSCLC) previously treated with an EGFR TKI (most patients received ≥ 1 prior treatment) in 2 study populations: all subjects and subjects with T790M.

  6. 9 maj 2019 · ASP8273, a novel, small molecule, irreversible tyrosine kinase inhibitor (TKI) specifically inhibits the epidermal growth factor receptor (EGFR) in patients with activating mutations or EGFR T790M resistance mutations.

  7. 12 gru 2017 · In this multi-cohort, phase 1 study (NCT02113813), escalating doses of ASP8273 (25–500mg) were administered once daily to non-small cell lung cancer (NSCLC) patients with disease progression after prior treatment with an EGFR TKI.

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