替尼達普

**替尼達普**
臨床資料
ATC碼	M01AX23 (WHO) ;
法律規範狀態
法律規範	未上市;
識別資訊
	IUPAC命名法 5-chloro-2-hydroxy-3-(2-thienylcarbonyl)-1H-indole-1-carboxamide; ;
CAS號	120210-48-2
PubChem CID	60712;
ChemSpider	54717 ;
UNII	9K7CJ74ONH;
KEGG	D06072 ;
ChEMBL	ChEMBL1097558 ;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID9046104 ;
化學資訊
化學式	C14H9ClN2O3S
摩爾質量	320.75 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES c1cc(sc1)C(=O)c2c3cc(ccc3n(c2O)C(=O)N)Cl;
	InChI InChI=1S/C14H9ClN2O3S/c15-7-3-4-9-8(6-7)11(13(19)17(9)14(16)20)12(18)10-2-1-5-21-10/h1-6,19H,(H2,16,20) ; Key:IZSFDUMVCVVWKW-UHFFFAOYSA-N ;

替尼達普（INN：tenidap）^[1]是一種環氧合酶/5-脂氧合酶(COX/5-LOX)雙效抑制劑和細胞因子調節消炎藥候選藥物^[2]。由輝瑞公司開發的具有治療類風濕性關節炎前景的潛在藥物^[3]。但因其肝腎毒性原因，1996年上市批准遭到美國FDA拒絕，輝瑞因此停止了對其開發^[4]。造成其肝腎毒性的原因是藥物結構中含有噻吩基團的部分在體內代謝過程中會造成氧化損傷^[5]。

參考文獻[編輯]

^ 劉治軍,韓紅蕾 (編). 华法林+替尼达普(warfarin+tenidap). 药物相互作用基础与临床第三版. 北京: 人民衛生出版社. 2019.
^ Wylie G, Appelboom T, Bolten W, Breedveld FC, Feely J, Leeming MR, et al. A comparative study of tenidap, a cytokine-modulating anti-rheumatic drug, and diclofenac in rheumatoid arthritis: a 24-week analysis of a 1-year clinical trial. British Journal of Rheumatology. June 1995, 34 (6): 554–63. PMID 7543348. doi:10.1093/rheumatology/34.6.554.
^ Staff, American Journal of Nursing. Drug Watch: Tenidap Offers Arthritis Therapy Minus Toxicity AJN 1996 96(1):58
^ Pfizer. Sept 27, 1996 Press release: Pfizer To Halt Plans For Commercialization Of Tenidap For Rheumatoid Arthritis 互聯網檔案館的存檔，存檔日期2016-03-05.
^ Hwang SH, Wecksler AT, Wagner K, Hammock BD. Rationally designed multitarget agents against inflammation and pain. Current Medicinal Chemistry. 2013, 20 (13): 1783–99. PMC 4113248 . PMID 23410172. doi:10.2174/0929867311320130013.

[1] 劉治軍,韓紅蕾 (編). 华法林+替尼达普(warfarin+tenidap). 药物相互作用基础与临床第三版. 北京: 人民衛生出版社. 2019.

[2] Wylie G, Appelboom T, Bolten W, Breedveld FC, Feely J, Leeming MR, et al. A comparative study of tenidap, a cytokine-modulating anti-rheumatic drug, and diclofenac in rheumatoid arthritis: a 24-week analysis of a 1-year clinical trial. British Journal of Rheumatology. June 1995, 34 (6): 554–63. PMID 7543348. doi:10.1093/rheumatology/34.6.554.

[3] Staff, American Journal of Nursing. Drug Watch: Tenidap Offers Arthritis Therapy Minus Toxicity AJN 1996 96(1):58

[4] Pfizer. Sept 27, 1996 Press release: Pfizer To Halt Plans For Commercialization Of Tenidap For Rheumatoid Arthritis 互聯網檔案館的存檔，存檔日期2016-03-05.

[pmid23410172-5] Hwang SH, Wecksler AT, Wagner K, Hammock BD. Rationally designed multitarget agents against inflammation and pain. Current Medicinal Chemistry. 2013, 20 (13): 1783–99. PMC 4113248 . PMID 23410172. doi:10.2174/0929867311320130013.

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