Rifampicin is a semisynthetic derivative of rifamycin B and inhibits the growth of a variety of bacteria. Rifampicin causes an increase in corticosteroid clearance, and a decrease in the blood concentrations of calcineurin inhibitors by inducing Cytochrome P450 3A4 in the liver. It is generally acknowledged that a substantial increase in the dosage of calcineurin inhibitors is required to achieve the efficacious target concentrations and avoid graft rejection. We report a case of patient who received a living-related donor renal transplant with stable renal function during the rifampicin based anti-tuberculosis treatment, even the blood concentration of tacrolimus (FK506) decreased. Interestingly, acute rejection was observed at the end of anti-tuberculosis treatment, even the blood concentration of FK506 was reduced to target level.