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Penetration of the blood–brain barrier by avitinib and its control of intra/extra-cranial disease in non-small cell lung cancer harboring the T790M mutation

Lung Cancer May 25, 2018

Wang H, et al. - In non-small cell lung cancer (NSCLC) patients with the epidermal growth factor receptor (EGFR) T790 M mutation, researchers assessed the safety, intra-/extracranial efficacy, and the blood–brain barrier (BBB) penetration rate of avitinib, an oral, potent, irreversible EGFR tyrosine kinase inhibitor selective for the EGFR T790 M mutation. Oral administration of avitinib (150–300 mg) twice daily for cycles of 28 continuous days was followed by a collection of blood and cerebrospinal fluid samples (2 ml each) on day 29 in available patients with brain metastases, and the tumor response was assessed. Findings demonstrated good tolerability and efficacy of avitinib in T790M-positive patients. The observed penetrability of avitinib to the BBB was weak but it demonstrated good control of asymptomatic brain metastases.
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