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Objective The purpose of this study was to investigate the single nucleotide polymorphisms (SNPs) of ATP binding cassette superfamily G member 2 (ABCG2) gene and to study the correlation between ABCG2 gene polymorphisms and outcome and prognosis of tyrosine kinase inhibitions (TKIs) therapy in Chinese advanced non-small-cell lung cancer (NSCLC) patients.MethodsFour functionalSNPs(34 G/A, 421 C/A, 1143 C/T and-15622 C/T)ofABCG2 gene in 100 patients were tested using matrix-assisted laser desorption/ionization time-of-flight mass spectrometry.The clinical characteristics of 100 patients were collected.A total of 70 patients were treated with TKIs(gefitinib, erlotinib and icotinib).The association between ABCG2 polymorphisms and clinical characteristicswas evaluated.