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Objective: To determine the relationship of Imatinib (IM) concentration in bone marrow and its therapeutic response in patients with chronic myelogenous leukemia in China.To explore the underlying mechanism.Method: 90 patients enrolled were all diagnosed with chronic myelogenous leukemia according to the guidelines of NCCN 2011, with 88 patients in chronic phase (CP) and 2 in accelerated phase (AC).The median age was 40 years (range from 11 to 77 years).All diagnostic patients had received IM treatment at the dosage of 400mg (range from 300 to 800mg) for 30 months (range 1 to 117 months).Bone marrow mononuclear cells were collected 0.5 hour before IM administration in order to test the expression of Bcr/abl by using FISH and RQ-PCR, the mRNA expression of hOCT1and ABCB1 by QRT-PCR and the gene polymorphism of ABCB1 on C1236T, C3435T and G2677T.IM concentration in bone marrow mononuclear cells was measured by a method of liquid chromatography in tandem with mass spectrometr.We then analyzed IM concentration, expression of hOCT1 and ABCB1 and their relationship with therapeutic response.Result: In 61 patients with CCR, the mRNA expression of ABCB1 (88.05, range from 3.3 to 1558.8) was significantly lower than that of 17 patients in resistant group (102, range from 11.3 to 1604.9, p < 0.01) and 17 in PCyR group (33.1, range from 2.2 to 108.2, p < 0.01).On the other hand, the mRNA expression of hOCT1 was significantly higher in CCR group (16.6, range 1.7 to 199.8) as compared with that in drug-resistant group (10.1, range from 0.7 to 33.5, p < 0.01) and PCyR group (5.9, range from 1.4 to 30.3, p < 0.01).IM concentration was found to be positively associated with the mRNA expression of hOCT1 (r=0.456, p=0.033) and has negatively associated with the mRNA expression of ABCB1 (r=-0.491,p=0.015).Data from the gene polymorphism of ABCB1 indicated that in 48 patients with mRNA expression of ABCB1 above the median level, and patients without CCR had a significant higher frequency of T alleles than C on C1236T (x2=4, P=0.046), while C and G higher than T on C3435T (x2=7.11, p < 0.01) and C2677T (x2=5.44, p < 0.01) respectively.Conclusion: IM concentration in bone marrow cells is regulated by hOCT1 and ABCB1 and they promisingly affect the therapeutic response.