Drug intelligence / Profile preview

mizoribine + tacrolimus

Development stage
Preclinical
Lead developer
Asahi Kasei
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Mizoribine + tacrolimus is a combination of two immunosuppressive agents used primarily in the management of autoimmune diseases such as lupus nephritis and in organ transplantation, particularly kidney transplantation. Mizoribine is a nucleoside analog that selectively inhibits inosine monophosphate dehydrogenase (IMPDH), thereby blocking the de novo synthesis of guanine nucleotides essential for lymphocyte proliferation. Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by inhibiting the phosphatase activity of calcineurin, leading to reduced interleukin-2 (IL-2) production and T-cell proliferation. The combination aims to provide synergistic immunosuppression with potentially lower toxicity compared to regimens using higher doses or other agents. This regimen has been studied as an alternative induction or maintenance therapy for lupus nephritis and as part of post-transplant immunosuppression protocols[1][2][4][5].

Other names
mizoribine and tacrolimusMZR + TAC
02

Targets

CN (Calcineurin)HSP60 (60 kDa heat shock protein, mitochondrial)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)

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