トラニラスト
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2012/09/22 10:46:33」(JST)
[Wiki en表示]
Tranilast
|
Systematic (IUPAC) name |
2-{[(2E)-3-(3,4-dimethoxyphenyl)prop-2- enoyl]amino}benzoic acid |
Clinical data |
AHFS/Drugs.com |
International Drug Names |
Pregnancy cat. |
? |
Legal status |
℞ Prescription only |
Routes |
Oral |
Identifiers |
CAS number |
53902-12-8 |
ATC code |
None |
PubChem |
CID 5282230 |
UNII |
HVF50SMY6E Y |
ChEMBL |
CHEMBL415324 |
Chemical data |
Formula |
C18H17NO5 |
Mol. mass |
327.33 g/mol |
SMILES
- COC1=C(C=C(C=C1)C=CC(=O)NC2=CC=CC=C2C(=O)O)OC
|
Tranilast (INN, brand name Rizaben) is an antiallergic drug. It was developed by Kissei Pharmaceuticals and was approved in 1982 for use in Japan and South Korea for bronchial asthma. Indications for keloid and hypertrophic scar were added in 1993.[1] It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.
In-vitro it reduces collagen synthesis in fibroblasts[2], and inhibits growth of neurofibroma cells[3].
In-vitro it inhibits the production of interleukin-6 in endothelial cells.[4]
It is relatively safe and well tolerated by most patients at doses of up to 600 mg/day for months.
After promising results in three small trial Tranilast was studied in a major clinical trial (the PRESTO trial) for prevention of restenosis after percutaneous transluminal coronary revascularization, but was not found effective for that application.[5]
It has also been investigated for use as an antiproliferative drug on drug-eluting stents.
A phase II trial is recruiting rheumatoid arthritis patients.[6]
A phase III trial is evaluating tranilast for Pterygium[7].
References
- ^ http://www.fiercebiotech.com/story/press-release-nuon-therapeutics-completes-agreement-tranilast-kissei-pharmaceutical/2007-07-23
- ^ http://jb.oxfordjournals.org/cgi/content/abstract/116/4/892
- ^ http://www.jstage.jst.go.jp/article/tjem/217/3/217_193/_article "Tranilast, an Anti-Allergic Drug, Down-Regulates the Growth of Cultured Neurofibroma Cells Derived from Neurofibromatosis Type 1" 2009
- ^ http://molpharm.aspetjournals.org/content/62/4/856.full "Tranilast Inhibits Cytokine-Induced Nuclear Factor κB Activation in Vascular Endothelial Cells" 2002
- ^ http://www.circ.ahajournals.org/cgi/content/full/106/10/1243 "Results of Prevention of REStenosis with Tranilast and its Outcomes (PRESTO) Trial" 2002
- ^ http://clinicaltrials.gov/ct2/show/NCT00882024
- ^ http://clinicaltrials.gov/ct2/show/NCT01003613
External links
- Enzo Life Sciences
- Nuon Therapeutics
UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
English Journal
- Development of novel solid dispersion of tranilast using amphiphilic block copolymer for improved oral bioavailability.
- Onoue S, Kojo Y, Suzuki H, Yuminoki K, Kou K, Kawabata Y, Yamauchi Y, Hashimoto N, Yamada S.SourceDepartment of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan. Electronic address: onoue@u-shizuoka-ken.ac.jp.
- International journal of pharmaceutics.Int J Pharm.2013 May 18. pii: S0378-5173(13)00425-0. doi: 10.1016/j.ijpharm.2013.05.022. [Epub ahead of print]
- The present study aimed to develop novel solid dispersion (SD) of tranilast (TL) using amphiphilic block copolymer, poly[MPC-co-BMA] (pMB), to improve the dissolution and pharmacokinetic behavior of TL. pMB-based SD of TL (pMB-SD/TL) with drug loading of 50% (w/w) was prepared by wet-mill technology
- PMID 23694807
- Tranilast Binds to Aβ Monomers and Promotes Aβ Fibrillation.
- Connors CR, Rosenman DJ, Lopes DH, Mittal S, Bitan G, Sorci M, Belfort G, Garcia AE, Wang C.AbstractThe anti-allergy and potential anti-cancer drug tranilast has been patented for treating Alzheimer's Disease (AD), in which amyloid β-protein (Aβ) plays a key pathogenic role. We used solution NMR to determine that tranilast binds to Aβ40 monomers with ~300 μM affinity. Remarkably, tranilast increases Aβ40 fibrillation more than 20-fold in the thioflavin T assay at a 1:1 molar ratio, as well as significantly reducing the lag time. Tranilast likely promotes fibrillation by shifting Aβ monomer conformations to those capable of seed formation and fibril elongation. Molecular docking results qualitatively agree with NMR chemical shift perturbation, which together indicate that hydrophobic interactions are the major driving force of the Aβ-tranilast interaction. These data suggest that AD may be a potential complication for tranilast usage in elderly patients.
- Biochemistry.Biochemistry.2013 May 16. [Epub ahead of print]
- The anti-allergy and potential anti-cancer drug tranilast has been patented for treating Alzheimer's Disease (AD), in which amyloid β-protein (Aβ) plays a key pathogenic role. We used solution NMR to determine that tranilast binds to Aβ40 monomers with ~300 μM affinity. Remarkably, tranilast inc
- PMID 23679559
Japanese Journal
- 藤本 和久,川崎 裕史,稲葉 基之 [他]
- Journal of environmental dermatology and cutaneous allergology 6(5), 439-444, 2012-10-00
- NAID 40019481111
- 遷延した混合型薬物性肝障害に対して茵茵陳蒿湯を含む多剤薬物療法が有効であった2例
- 酒見 亮介,垣内 誠也,森光 洋介 [他],久保 保彦,松垣 論,宗 祐人,酒見 美幸,下河辺 正行,原田 大,佐田 通夫
- 肝臓 53(5), 291-297, 2012-05-25
- 外傷後のケロイド治療及び術後のケロイド予防目的に対してトラニラスト(リザベン)を服用した2例の男性患者が内服終了後の約3週目より黄疸が出現し来院した.臨床所見ならびに検査所見などから2例ともトラニラストの薬物性肝障害を強く疑われ,ウルソデオキシコール酸(UDCA)製剤を内服したが,減黄を認めなかった.トラニラストにより,胆汁分泌機能の役割を担うビリルビントランスポーターに障害を来たしたと考え,我々 …
- NAID 10030625556
- 肺野病変にトラニラストが有効であった皮下型サルコイドーシスの1例
- 宍倉 裕,笹森 寛,泉山 典子 [他],菊地 正,三木 祐,飯澤 理,菊池 喜博
- 日本呼吸器学会誌 = Annals of the Japanese Respiratory Society 1(2), 165-169, 2012-02-10
- NAID 10030269286
Related Links
- Sigma-Aldrich offers Sigma-T0318, Tranilast for your research needs. Find product specific information including CAS, MSDS, protocols and references. ... Application The effect of Tranilast on mast cell surface receptors was ...
- Buy Tranilast (CAS 53902-12-8), an inhibitor of angiogenesis and the release of histamine and prostaglandins, from Santa Cruz. Purity: ≥98%,MW: 327.33 ... 同義語 N-(3,4-Dimethoxycinnamoyl)anthranilic Acid; 2-[[3-(3,4 ...
Related Pictures
★リンクテーブル★
[★]
- 英
- tranilast
- 商
- アレニスト、ガレシロール、トラメラス、フスチゲン、ブレクルス、ラミセンス、リザベン、ルミオス
- 関
- 眼科用剤
薬理作用
- 肥満細胞や各種炎症細胞からのヒスタミンおよびロイコトリエンなど化学伝達物質の遊離を抑制
- サイトカインや活性酸素の産生や遊離を抑制し、ケロイドおよび肥厚性瘢痕由来線維芽細胞のコラーゲン合成を抑制
適応