齊泊騰坦

齊泊騰坦
	IUPAC名; N-(3-Methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide
別名	ZD4054; 賽博特坦
識別
CAS號	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配體	3539
性質
化學式	C19H16N6O4S
摩爾質量	424.43 g·mol−1
	若非註明，所有數據均出自標準狀態（25 ℃，100 kPa）下。

齊泊騰坦（INN：Zibotentan，開發代號：ZD4054）是阿斯利康正在開發的一種實驗性抗癌候選藥物。^[1]它是一種內皮素受體拮抗劑。^[2]

齊泊騰坦被FDA授予治療前列腺癌的快速通道地位。

它未能通過針對前列腺癌的III期臨床試驗，^[3]但計劃進行其他試驗。^[4]齊泊騰坦加歐洲紫杉醇的耐受性已經過評估。^[5]

齊泊騰坦還在臨床試驗中進行了研究，用於治療乳腺癌、結直腸癌、非小細胞肺癌、卵巢癌、硬皮病相關腎病、^[6]骨轉移和心力衰竭。^[7]

參考資料[編輯]

^ 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]. （原始內容存檔於2016-03-03）.
^ Pfizer, AstraZeneca, and Actelion Separately Report Phase III Trial Failures - GEN. GEN. [16 April 2018]. （原始內容存檔於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]. （原始內容存檔於2023-06-22）.
^ Zibotentan - AdisInsight. adisinsight.springer.com. [16 April 2018]. （原始內容存檔於2023-06-25）.