齐泊腾坦

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
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]

Quick Facts 齐泊腾坦, 识别 ...

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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]

[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 . 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）.

参考资料

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 ^Y
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。