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In this study, our objective was to analysis the association of CYP3A4* 1G, CYP3A5* 3 and MDR1 C3435T gene polymorphisms with the antihypertensive efficacy of amlodipine in hypertensive patients after renal transplantation.Blood samples were collected from 76 patients on amlodipine (5 mg/d) therapy. Polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) and gene sequencing were applied to detect CYP3A4* 1G, CYP3A5* 3 and MDR1 C3435T gene polymorphism and antihypertensive effects were analyzed according to genotype. At the same time, blood pressure values were detected per week and recorded.After 4- weeks treatment, the blood pressure of 79% patients were controlled to standard. And the efficacy of amlodipine in patients with CYP3A5 *3*3 genotype was significantly higher than others (P < 0.05). In addition, the reduction of DBP in patients with CYP3A5*3*3 genotype was significantly higher than others (P < 0.05), the reduction of DBP in patients with CYP3A4*1G*1G genotype was significantly lower than the othera (P < 0.05). As for a linkage disequilibrium exists between CYP3A4* 1G and CYP3A5* 3 allele, our study also observed that DBP reduction in GG GG genetypes was the highest in all genetypes.Our study demonstrates that amlodipine could control BP effectively for hypertensive patients after renal transplantation. CYP3A5* 3 polymorphisms affect antihypertensive efficacy of amlodipine in Chinese hypertensive patients after renal transplantation.