Abstract: As an effective oral immunosuppressant, mizoribine is usually recommended for kidney transplantation at the dose of 1-3 mg/(kg·d)． However, as the development of kidney transplantation technology, some researches suggest that this dosage displays an inferior anti-rejection effect when compared with mycophenolate mofetil． Recently, high-dose 5-6 mg/(kg·d) of mizoribine has been used for renal transplants in Japan and it has already achieved promising outcomes with satisfied anti-rejection effect and safety, which will be illustrated in this review．