Mizoribine - CAS 50924-49-7
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Not Intended for Therapeutic Use. For research use only.
Mizoribine,Mizoribine (INN, trade name Bredinin) is an immunosuppressive drug. The compound was first observed in Tokyo, Japan, in 1971. It is a natural product, first isolated from the mould Eupenicillium brefeldianum. Mizoribine (MZB) is an imidazole nucleoside that has been used in renal transplantation, and in steroid-resistant nephrotic syndrome, IgA nephropathy, lupus, as well as for adults with rheumatoid arthritis, lupus nephritis and other rheumatic diseases. MZB 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. It arrests DNA synthesis in the S phase of cellular division. Thus, MZB has less toxicity than azathioprine, another immunosuppressant used for some of the same diseases.
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Mizoribine; Bredinin; HE 69; NSC 289637; 946; 8203; Bredinin.
1.Population pharmacokinetics of mizoribine in pediatric patients with kidney disease.
Kaneda H1, Shimizu M2, Ohta K3, Ushijima K4, Gotoh Y5, Satomura K6, Nagai T7, Fujieda M8, Morooka M9, Yamada T5, Yamada M10, Wada N10, Takaai M11, Hashimoto Y11, Uemura O7. Clin Exp Nephrol. 2015 Dec 9. [Epub ahead of print]
BACKGROUND: The present study aimed to obtain information enabling optimisation of the clinical effect of mizoribine (MZR) in pediatric patients with kidney disease.
2.Treatment of membranous nephropathy with mizoribine: A control trial.
Wang X1, Song X1, Liu Y1, Zhang W1, An W1, Tu Y2. Life Sci. 2016 Apr 11. pii: S0024-3205(16)30233-8. doi: 10.1016/j.lfs.2016.04.012. [Epub ahead of print]
AIM: Membranous nephropathy remains the most common form of the nephrotic syndrome in adults. The combination therapy of steroid and cyclophosphamide has routinely been used. Although satisfactory therapeutic efficacy can be achieved, its side effect on reproductive system has been a concern. Mizoribine is an imidazole nucleoside and a novel immunosuppressant that has been used to treat other immune-related diseases. In this study we examine if the combined regimen of mizoribine and steroid would be advantageous over the use of cyclophosphamide and steroid in treating adult membranous nephropathy.
3.Steroid-resistant protein-losing gastroenteropathy complicated with Sjögren's syndrome successfully treated with mizoribine.
Izumi Y1,2, Nakaoka K1,2, Kamata M2, Iwanaga N1, Imadachi S2, Kurohama H3, Ito M3, Migita K2. Mod Rheumatol. 2016 Apr 4:1-5. [Epub ahead of print]
A 64-year-old woman with leg edema was diagnosed with protein-losing gastroenteropathy and Sjögren's syndrome. Central venous nutrition led to infection of her catheter, ascites, and deep vein thrombosis. Following successful treatment of these conditions with antibiotics and anticoagulants, she was treated unsuccessfully with prednisolone and steroid pulse therapy. Mizoribine add-on markedly reduced edema and normalized serum albumin. This is the first report of a steroid-resistant protein-losing gastroenteropathy patient with Sjögren's syndrome successfully treated with mizoribine.
4.Safety and efficacy of mizoribine treatment in nephrotic syndrome complicated with hepatitis B virus infection: a clinical study.
Liu J1, Zhang K1, Ji Y1, Zhang W1, Li W1, Yong Q1, Wang J1, Sun J1, Zhang H1. Ren Fail. 2016 Mar 16:1-5. [Epub ahead of print]
Objective The objective of this study is to explore the efficacy and safety of mizoribine (MZR) in treating nephrotic syndrome patients afflicted with hepatitis B virus (HBV). Methods The present study included 36 nephrotic syndrome patients accompanied with HBV infection. A draft of MZR (150-200 mg/d), methylprednisolone (0.6-0.8 mg/kg·d), and entecavir (0.5 mg/d) was administered to study patients over 24 weeks. The serum albumin (AlB), 24-h urine protein (24-U-TP), liver and renal functions, and HBV-DNA were quantified before and at 2, 4, 8, 12, 16, 20, and 24 weeks after the treatment. The adverse responses were recorded. Results The AlB levels of patients increased gradually after comprehensive treatment, while the 24-U-TP, serum cholesterol, and triglyceride (TG) levels declined gradually. The changes at 24 weeks post-treatment were statistically significant. Compared with the levels before treatment, the HBV-DNA, transaminase, and renal functions of the patients were not significantly altered after the treatment.
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CAS 50924-49-7 Mizoribine

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