Mizoribine: Mode of action and effects in clinical use

Pediatrics International - Tập 44 Số 2 - Trang 196-198 - 2002
Shumpei Yokota1
1Department of Pediatrics, YokohamaCity University School of Medicine

Tóm tắt

AbstractMizoribine is a new immunosuppressive drug and was authorized by the Japanese Government in 1984. The strong immunosuppressive activity of mizoribine was already demonstrated in various animal models, in renal transplantation and in steriod‐resistant nephrotic syndrome. Recently, the remarkable clinical advantages of an imidazole for adults with rheumatoid arthritis, lupus nephritis and other rheumatic diseases were reported. Mizoribine is an imidazole nucleoside and the metabolites, MZ‐5‐P, exerts its activity through selective inhibition of inosine monophosphate synthetase and guanosine monophosphate synthetase, resulting in the complete inhibition of guanine nucleotide synthesis without incorporation into nucleotides. Thus, mizoribine is superior to azathioprine, in that it may not cause damages to normal cells and normal nucleic acid.

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Tài liệu tham khảo

10.1097/00007890-198302000-00007

10.1097/00007890-198811000-00026

Murase J, 1978, Absorption,distribution, metabolism and excretion of bredinin in rats, Pharmacometrics, 15, 829

Dayton JS, 1992, Comparison of the effects of mizoribinewith those of azathioprine, 6‐mercaptopurine, and mycophenolic acidon T lymphocyte proliferation and purine ribonucleotide metabolism, Mol. Pharmacol., 41, 671

10.1002/cbf.290070308

LePage GA, 1971, Pharmacologyof 6‐thioguanine in man, Cancer Res., 31, 1627

O’Shea J, 1987, Alminum fluoride induces phosphatidylinoditol turn‐over, elevationof cytoplasmic free calcium, and phos­phorylation of theT cell antigen receptor in murine T cells, J. Immunol., 139, 3463, 10.4049/jimmunol.139.10.3463

Ledbetter JA, 1986, Antibody binding to CD5 (Tp67) and Tp44 T cell surfacemolecules: Effects on cyclic nucleotides, cytoplasmic free calcium,and cAMP‐mediated suppression, J. Immunol., 137, 3299, 10.4049/jimmunol.137.10.3299

10.1172/JCI115101

Uchida H, 1979, Effectivenessof a new drug, bredinin, on canine kidney allotransplantation survival, Transplant. Proc., 11, 865

Marumo F, 1988, Aclinical study of renal transplant recipients receiving triple‐drugtherapy − cyclosporine A, mizoribine, and prednisolone, Transplant. Proc., 20, 406

10.1177/095632029400500603

Shiraki K, 1992, Effectsof cyclosporine, azathioprine, mizoribine and prednisolone on replicationof human cytomegarovirus, Transplant. Proc., 22, 1682