PURPOSE: @entity41059 is a new first-generation @entity470 ( @entity470 ) @entity4149 kinase inhibitors. A phase II study was conducted to evaluate the efficacy and safety of @entity41059 in combination with whole-brain radiotherapy (WBRT) in Chinese NSCLC @entity1 with brain metastases (BMs); the cerebrospinal fluid (CSF)/plasma concentrations of @entity41059 were also investigated. METHODS: Eligible @entity1 had BMs from NSCLC, regardless of the @entity470 status. @entity41059 was administered at 125  mg orally 3 times/day until @entity5 progression or unacceptable @entity137 , concurrently with WBRT (3.0  Gy per day, 5  days per week, to 30  Gy). CSF and plasma samples were collected simultaneously from 10 @entity1 . @entity41059 concentrations in the CSF and plasma were measured by high-performance liquid chromatography coupled with tandem mass spectrometry. RESULTS: Twenty @entity1 were enrolled. The median follow-up time was 20.0  months. The overall response rate was 80.0  %. The median progression-free survival time was 7.0  months (95  % CI 1.2-13.2  months), and the @entity1349 ( @entity1349 ) was 14.6  months (95  % CI 12.5-16.7  months). Of the 18 @entity1 with known @entity470 status, the @entity1349 was 22.0  months for those with an @entity470 mutation and was 7.5  months for those with wild-type @entity470 (P  =  0.0001). The CSF concentration and penetration rate of @entity41059 were 11.6      9.1  ng/mL and 1.4      1.1  %, respectively. No @entity1 experienced >= grade 4 @entity137 . CONCLUSIONS: @entity41059 was well tolerated in combination with WBRT and showed efficacy in @entity1 with BMs from NSCLC. This clinical benefit was related to the presence of activating @entity470 mutations.

A phase II study of @entity41059 and whole-brain radiotherapy in Chinese XXXX with brain metastases from non-small cell lung cancer.

@entity1 :: ('9606', 'Species') :: ['patients', 'patient'] @entity137 :: ('MESH:D064420', 'Disease') :: ['toxicity'] @entity470 :: ('1956', 'Gene') :: ['EGFR', 'epidermal growth factor receptor'] @entity5 :: ('MESH:D009369', 'Disease') :: ['tumor'] @entity41059 :: ('MESH:C531470', 'Chemical') :: ['icotinib', 'Icotinib'] @entity4149 :: ('D014443', 'Chemical') :: ['tyrosine'] @entity1349 :: ('MESH:D011475', 'Disease') :: ['median survival time', 'MST']
@entity1 :: (9606,Species) :: ['patients']
