ミゾリビン
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/07/13 10:25:29」(JST)
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Mizoribine
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Systematic (IUPAC) name |
5-hydroxy-1-β-D-ribofuranosyl-1H-imidazole-4-carboxamide |
Clinical data |
AHFS/Drugs.com |
International Drug Names |
Pregnancy cat. |
? |
Legal status |
℞ Prescription only |
Routes |
Oral |
Identifiers |
CAS number |
50924-49-7 Y |
ATC code |
None |
PubChem |
CID 104762 |
UNII |
4JR41A10VP Y |
KEGG |
D01392 Y |
Synonyms |
1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-hydroxyimidazole-4-carboxamide |
Chemical data |
Formula |
C9H13N3O6 |
Mol. mass |
259.21 g/mol |
SMILES
- C1=NC(=C(N1C2C(C(C(O2)CO)O)O)O)C(=O)N
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Y (what is this?) (verify)
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Mizoribine (INN, trade name Bredinin) is an immunosuppressive drug. The compound was first observed in Tokyo, Japan, in 1971.[1] 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.
References[edit]
- ^ Hiroaki Ishikawa (1999). "Mizoribine and Mycophenolate Mofetil". Current Medicinal Chemistry (Bentham Science) 6 (7): 575–597. PMID 10390602.
Immunomodulators: Immunosuppressive drugs / Immunosuppressants (L04)
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Intracellular
(initiation) |
Antimetabolites
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- purine synthesis inhibitors: Azathioprine
- Mycophenolic acid
- pyrimidine synthesis inhibitors: Leflunomide
- Teriflunomide
antifolate: Methotrexate
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Macrolides/
other IL-2 inhibitors
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- FKBP/Cyclophilin/Calcineurin: Tacrolimus
- Ciclosporin
- Pimecrolimus
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Other
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|
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Intracellular
(reception) |
IL-1 receptor antagonists
|
|
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mTOR
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- Sirolimus
- Everolimus
- Ridaforolimus
- Temsirolimus
- Umirolimus
- Zotarolimus
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Extracellular |
Antibodies
|
Monoclonal
|
Serum target
(noncellular)
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- Complement component 5 (Eculizumab)
- TNF (Adalimumab
- Afelimomab
- Certolizumab pegol
- Golimumab
- Infliximab
- Nerelimomab)
- Interleukin 5 (Mepolizumab)
- Immunoglobulin E (Omalizumab)
- IL-12 and IL-23 (Lebrikizumab
- Ustekinumab)
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|
Cellular target
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- CD3 (Muromonab-CD3
- Otelixizumab
- Teplizumab
- Visilizumab)
- CD4 (Clenoliximab
- Keliximab
- Zanolimumab)
- CD11a (Efalizumab)
- CD18 (Erlizumab)
- CD20 (Afutuzumab
- Rituximab
- Ocrelizumab
- Pascolizumab)
- CD23 (Gomiliximab
- Lumiliximab)
- CD40 (Teneliximab
- Toralizumab)
- CD62L/L-selectin (Aselizumab)
- CD80 (Galiximab)
- CD147/Basigin (Gavilimomab)
- CD154 (Ruplizumab)
- BLyS (Belimumab)
- CTLA-4 (Ipilimumab
- Tremelimumab)
- CAT (Bertilimumab
- Lerdelimumab
- Metelimumab)
- Integrin (Natalizumab)
- Interleukin-6 receptor (Tocilizumab)
- LFA-1 (Odulimomab)
- IL-2 receptor/CD25 (Basiliximab
- Daclizumab
- Inolimomab)
- T-lymphocyte (Zolimomab aritox)
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Unsorted
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- Atorolimumab
- Cedelizumab
- Fontolizumab
- Maslimomab
- Morolimumab
- Pexelizumab
- Reslizumab
- Rovelizumab
- Siplizumab
- Talizumab
- Telimomab aritox
- Vapaliximab
- Vepalimomab
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Polyclonal
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- Anti-thymocyte globulin
- Anti-lymphocyte globulin
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-cept (Fusion)
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- CTLA-4 (Abatacept
- Belatacept)
- TNF inhibitor (Etanercept
- Pegsunercept)
- Aflibercept
- Alefacept
- Rilonacept
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cell/phys/auag/auab/comp, igrc
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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.
UpToDate Contents
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English Journal
- Ulcerative colitis associated with nephrotic syndrome after treatment with mesalazine developed into rectal carcinoma: a case study.
- Sameshima S1, Koketsu S2, Okuyama T2, Kubota Y2, Ono Y3, Noie T2, Oya M2.
- World journal of surgical oncology.World J Surg Oncol.2016 Jul 22;14(1):192. doi: 10.1186/s12957-016-0950-1.
- BACKGROUND: Previous studies reported that nephrotic syndrome is associated with ulcerative colitis (UC) patients treated with mesalazine. Dysplasia associated with UC often develops into colorectal carcinoma.CASE PRESENTATION: A 17-year-old man was referred to our hospital, complaining of diarrhea
- PMID 27450459
- Successful treatment with oral mizoribine in refractory ocular manifestation of mucosal pemphigus vulgaris: A unique response to different immunosuppressive drugs.
- Oyama N1,2, Togashi A, Nomura E2, Kaneko F2.
- Dermatologic therapy.Dermatol Ther.2016 Jul 15. doi: 10.1111/dth.12386. [Epub ahead of print]
- Pemphigus vulgaris (PV) is an acquired autoimmune disease in which the disease characteristic antibodies are directed against the desmosomal transmembrane glycoprotein, desmoglein 3 (Dsg 3), resulting in flaccid blisters and erosions of skin and mucous membrane. Among various affected sites, ocular
- PMID 27418118
- A-306989, an inhibitor of adenosine kinase, is renoprotective in rodent models of podocyte, basement membrane, and obstructive injury.
- Zhu CZ1, Gopalakrishnan S2, Doyle K2, Nikkel AL2, Olson L2, Abraham VC2, Leys L2, Widomski D2, Salte K2, Putman B2, Pratt S2, Ma J2, Su Z2, Gopalakrishnan M2, Lee CH2, McGaraughty SP2.
- European journal of pharmacology.Eur J Pharmacol.2016 Jun 8;788:1-11. doi: 10.1016/j.ejphar.2016.06.012. [Epub ahead of print]
- Adenosine (ADO) is an important regulatory purine nucleoside that accumulates at sites of inflammation and tissue injury including in diseases associated with renal pathology. Endogenous levels of ADO may be increased by inhibiting the ADO-metabolizing enzyme, ADO kinase (AK). AK inhibitors have dem
- PMID 27288879
Japanese Journal
- 症例報告 ミゾリビンパルス療法が有効であった若年女性の全身性エリテマトーデスの1例
- 野村 尚志,江上 将平,笠井 弘子 [他]
- 臨床皮膚科 = Japanese journal of clinical dermatology 69(1), 52-56, 2015-01
- NAID 40020304039
- IgA Nephropathy and Psoriatic Arthritis that Improved with Steroid Pulse Therapy and Mizoribine in Combination with Treatment for Chronic Tonsillitis and Epipharyngitis
- , , , , ,
- Internal Medicine 54(9), 1085-1090, 2015
- … As a renal biopsy showed IgA nephropathy (IgAN), bilateral tonsillectomy was performed, and one course of steroid pulse therapy with an oral steroid and mizoribine were subsequently administered. …
- NAID 130005068305
- ミゾリビンの関節リウマチにおける市販後調査の集計結果 -24週間の使用成績-
- 岩下 輝美,吉田 寿雄,岡田 研也
- 臨床リウマチ 27(1), 37-44, 2015
- ミゾリビンの関節リウマチ患者に対する使用実態の把握,使用実態下における安全性・有効性に関する情報を収集し,本剤の適正使用に資することを目的として,2008年10月~2010年10月の間に本剤が投与開始された関節リウマチ患者を対象に市販後調査を実施した.安全性解析対象症例3,325例の平均年齢は66.2±12.5歳で,65歳以上が61.1%,75歳以上が28.4%であった.合併症は59.3%に …
- NAID 130005067619
Related Links
- Mizoribine NEW 100mg 1g 15,000 100,000 *希望納入価格には消費税等が含まれておりません。 *希望納入価格は、2012年1月現在の価格です。 ページトップへ 関連商品 コードNo. 品 名 容 量 希望納入価格(円) プリン代謝 拮抗 ...
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