齊泊騰坦

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
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  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

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]. （原始內容存檔於2016-03-03）.
4. 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）.
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]. （原始內容存檔於2023-06-22）.
7. Zibotentan - AdisInsight. adisinsight.springer.com. [16 April 2018]. （原始內容存檔於2023-06-25）.

外部連結

• Zibotentan （頁面存檔備份，存於網際網路檔案館）