Yuki Katsuya1,2, Kentaro Miyake1,2, Takashi Higuchi1,2, Hiromichi Oshiro1,2, Norihiko Sugisawa1,2, Shree Ram Singh3, Yasushi Goto4, Ming Zhao1, Robert M Hoffman5,2. 1. AntiCancer, Inc., San Diego, CA, U.S.A. 2. Department of Surgery, University of California, San Diego, CA, U.S.A. 3. Basic Research Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD, U.S.A. all@anticancer.com singhshr@mail.nih.gov. 4. Department of Thoracic Oncology, National Cancer Center, Tokyo, Japan. 5. AntiCancer, Inc., San Diego, CA, U.S.A. all@anticancer.com singhshr@mail.nih.gov.
Abstract
BACKGROUND/AIM: Brain metastases are found in approximately 30% of patients with epidermal-growth-factor receptor (EGFR) mutant non-small cell lung cancer (NSCLC). We compared the efficacy of two EGFR-tyrosine kinase inhibitors (TKIs), erlotinib and osimertinib on a PC-9-GFP EGFR mutant NSCLC growing in the brain of nude mice. MATERIALS AND METHODS: The brain metastasis models were randomized into five groups and treated for 15 days: Control; 5 mg/kg erlotinib; 50 mg/kg erlotinib; 0.5 mg/kg osimertinib; 5 mg/kg osimertinib. Tumor volume was evaluated by non-invasive fluorescence imaging. RESULTS: Only 5 mg/kg osimertinib, a low-dose compared to the clinically-equivalent dose, showed significant tumor regression compared to the control. CONCLUSION: This study strongly supports the high activity of osimertinib for intracranial lesions of EGFR-mutant NSCLC. Copyright
BACKGROUND/AIM: Brain metastases are found in approximately 30% of patients with epidermal-growth-factor receptor (EGFR) mutant non-small cell lung cancer (NSCLC). We compared the efficacy of two EGFR-tyrosine kinase inhibitors (TKIs), erlotinib and osimertinib on a PC-9-GFP EGFR mutant NSCLC growing in the brain of nude mice. MATERIALS AND METHODS: The brain metastasis models were randomized into five groups and treated for 15 days: Control; 5 mg/kg erlotinib; 50 mg/kg erlotinib; 0.5 mg/kg osimertinib; 5 mg/kg osimertinib. Tumor volume was evaluated by non-invasive fluorescence imaging. RESULTS: Only 5 mg/kg osimertinib, a low-dose compared to the clinically-equivalent dose, showed significant tumor regression compared to the control. CONCLUSION: This study strongly supports the high activity of osimertinib for intracranial lesions of EGFR-mutant NSCLC. Copyright
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