齐泊腾坦
化合物
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 | |
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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 ![]() |
PubChem | 9910224 |
ChemSpider | 8085875 |
SMILES |
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InChI |
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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。 |
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
- ^ James and Growcott. Drugs of the Future. 2009.
- ^ 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 . PMID 21414193. doi:10.1186/1472-6904-11-3.
- ^ 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).
- ^ 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).
- ^ 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.
- ^ 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).
- ^ Zibotentan - AdisInsight. adisinsight.springer.com. [16 April 2018]. (原始内容存档于2023-06-25).
外部链接
- Zibotentan (页面存档备份,存于互联网档案馆)