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齐泊腾坦

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齐泊腾坦
IUPAC名
N-(3-Methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide
别名 ZD4054
赛博特坦
识别
CAS号 186497-07-4  checkY
PubChem 9910224
ChemSpider 8085875
SMILES
 
  • O=S(=O)(Nc1ncc(nc1OC)C)c4cccnc4c3ccc(c2nnco2)cc3
InChI
 
  • 1/C19H16N6O4S/c1-12-10-21-17(19(23-12)28-2)25-30(26,27)15-4-3-9-20-16(15)13-5-7-14(8-6-13)18-24-22-11-29-18/h3-11H,1-2H3,(H,21,25)
InChIKey FJHHZXWJVIEFGJ-UHFFFAOYAL
IUPHAR配体 3539
性质
化学式 C19H16N6O4S
摩尔质量 424.43 g·mol−1
若非注明,所有数据均出自标准状态(25 ℃,100 kPa)下。

齐泊腾坦INN:Zibotentan,开发代号:ZD4054)是阿斯利康正在开发的一种实验性抗癌候选药物。[1]它是一种内皮素受体拮抗剂[2]

齐泊腾坦被FDA授予治疗前列腺癌的快速通道地位。

它未能通过针对前列腺癌的III期临床试验,[3]但计划进行其他试验。[4]齐泊腾坦加欧洲紫杉醇的耐受性已经过评估。[5]

齐泊腾坦还在临床试验中进行了研究,用于治疗乳腺癌结直肠癌非小细胞肺癌卵巢癌、硬皮病相关肾病、[6]骨转移和心力衰竭[7]

参考资料

  1. ^ James and Growcott. Drugs of the Future. 2009. 
  2. ^ Tomkinson H, Kemp J, Oliver S, Swaisland H, Taboada M, Morris T. Pharmacokinetics and tolerability of zibotentan (ZD4054) in subjects with hepatic or renal impairment: two open-label comparative studies. BMC Clin Pharmacol. 2011, 11: 3. PMC 3070638可免费查阅. PMID 21414193. doi:10.1186/1472-6904-11-3. 
  3. ^ AZ's zibotentan flunks late-stage prostate cancer trial - FierceBiotech. www.fiercebiotech.com. [16 April 2018]. (原始内容存档于2016-03-03). 
  4. ^ Pfizer, AstraZeneca, and Actelion Separately Report Phase III Trial Failures - GEN. GEN. [16 April 2018]. (原始内容存档于2018-04-17). 
  5. ^ Trump DL, Payne H, Miller K, et al. Preliminary study of the specific endothelin a receptor antagonist zibotentan in combination with docetaxel in patients with metastatic castration-resistant prostate cancer. Prostate. September 2011, 71 (12): 1264–75. PMID 21271613. doi:10.1002/pros.21342. 
  6. ^ A Phase II, Single Centre, Randomised, Placebo-controlled, 3-part Trial to Assess the Safety, Tolerability and Efficacy of Zibotentan in Patients With Renal Disease Secondary to Scleroderma - AdisInsight. adisinsight.springer.com. [16 April 2018]. (原始内容存档于2023-06-22). 
  7. ^ Zibotentan - AdisInsight. adisinsight.springer.com. [16 April 2018]. (原始内容存档于2023-06-25). 

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