恩司特韋

恩司特韋
臨床資料
其他名稱	S-217622
識別資訊
	IUPAC命名法 1-(2,4,5-trifluorobenzyl)-3-[(1-methyl-1H-1,2,4-triazol-3-yl)methyl]-(6E)-6-[(6-chloro-2-methyl-2H-indazol-5-yl)imino]-1,3,5-triazinane-2,4-dione; ;
CAS號	2647530-73-0; 2757470-18-9
PubChem CID	162533924;
UNII	PX665RAA3H;
化學資訊
化學式	C22H17ClF3N9O2
摩爾質量	531.88 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES Cn1cnc(CN2C(=O)N(Cc3cc(F)c(F)cc3F)C(=N\c3cc4cn(C)nc4cc3Cl)\NC2=O)n1;
	InChI InChI=1S/C22H17ClF3N9O2/c1-32-7-12-4-18(13(23)5-17(12)30-32)28-20-29-21(36)35(9-19-27-10-33(2)31-19)22(37)34(20)8-11-3-15(25)16(26)6-14(11)24/h3-7,10H,8-9H2,1-2H3,(H,28,29,36); Key:QMPBBNUOBOFBFS-UHFFFAOYSA-N;

恩司特韋^[1]（代號：S-217622，商品名：Xocova）^[2]是鹽野義製藥公司與北海道大學合作開發的一種抗病毒藥物，可作為口服活性3C樣蛋白酶抑制劑，用於治療COVID-19感染。^[3]^[4]它是口服的，並且已經成功地針對最近出現的奧米克戎變體進行了測試。^[5]^[6]

歷史

它已進入III期臨床試驗。^[7]據報道，日本政府正在考慮允許鹽野木在最後的試驗步驟完成之前申請醫療用途的批准，這可能會加快上市銷售。這種有條件的早期批准系統此前已在日本用於加速其他針對 COVID-19的抗病毒藥物的上市進程，包括瑞德西韋和莫努匹韋。^[8]在一項針對428名患者的研究中，病毒載量降低，但症狀並未顯著減輕。^[9]

如果獲得批准，它將成為第一個治療COVID-19的日本國產藥丸，也是第三個在日本獲得批准的藥丸。2022年2月，該公司向日本監管機構尋求緊急批准。^[9]

鹽野義製藥公司宣布，他們已達成初步協議，一旦該藥物獲得批准，將向日本政府供應100萬劑。這位執行長表示，他們有能力每年生產1000萬劑。^[10]

參見

參考文獻

^ World Health Organization. International Nonproprietary Names for Pharmaceutical Substances. Proposed INN: List 126 (PDF). WHO Drug Information. 2021, 35 (4): 1135 [2022-10-10]. （原始內容存檔 (PDF)於2022-02-04）.
^ Xocova: Powerful New Japanese Pill for Coronavirus Treatment.. BioPharma Media. February 2022 [2022-10-10]. （原始內容存檔於2022-10-13）.
^ Unoh Y, Uehara S, Nakahara K, Nobori H, Yamatsu Y, Yamamoto S, et al. Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19. Journal of Medicinal Chemistry. May 2022, 65 (9): 6499–6512. PMC 8982737  . PMID 35352927. doi:10.1021/acs.jmedchem.2c00117.
^ Shionogi presents positive Ph II/III results for COVID-19 antiviral S-217622. thepharmaletter.com. 31 January 2022 [2022-10-10]. （原始內容存檔於2022-02-08）.
^ Shionogi's new COVID pill appears to ease omicron symptoms.. Nikkei Asia. 21 December 2021 [2022-10-10]. （原始內容存檔於2022-02-09）.
^ Uraki R, Kiso M, Iida S, Imai M, Takashita E, Kuroda M, et al. Characterization and antiviral susceptibility of SARS-CoV-2 Omicron/BA.2. Nature. May 2022, 607: 119–127. PMID 35576972. doi:10.1038/s41586-022-04856-1. 已忽略未知參數|collaboration= (幫助)
^ Tyndall JD. S-217622, a 3CL Protease Inhibitor and Clinical Candidate for SARS-CoV-2. Journal of Medicinal Chemistry. May 2022, 65 (9): 6496–6498. PMID 35507419. doi:10.1021/acs.jmedchem.2c00624.
^ Japan to consider early approval for Shionogi COVID-19 pill.. Japan Times. 8 February 2022 [2022-10-10]. （原始內容存檔於2022-02-10）.
^ ^9.0 ^9.1 Japan's Shionogi seeks approval for COVID-19 pill. Reuters. 25 February 2022 [2022-10-10]. （原始內容存檔於2022-10-12）.
^ Japan's Shionogi signs government supply pact for pill to fight COVID. Reuters. 25 March 2022 [2022-10-10]. （原始內容存檔於2022-10-16）.

[1] World Health Organization. International Nonproprietary Names for Pharmaceutical Substances. Proposed INN: List 126 (PDF). WHO Drug Information. 2021, 35 (4): 1135 [2022-10-10]. （原始內容存檔 (PDF)於2022-02-04）.

[2] Xocova: Powerful New Japanese Pill for Coronavirus Treatment.. BioPharma Media. February 2022 [2022-10-10]. （原始內容存檔於2022-10-13）.

[pmid35352927-3] Unoh Y, Uehara S, Nakahara K, Nobori H, Yamatsu Y, Yamamoto S, et al. Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19. Journal of Medicinal Chemistry. May 2022, 65 (9): 6499–6512. PMC 8982737  . PMID 35352927. doi:10.1021/acs.jmedchem.2c00117.

[4] Shionogi presents positive Ph II/III results for COVID-19 antiviral S-217622. thepharmaletter.com. 31 January 2022 [2022-10-10]. （原始內容存檔於2022-02-08）.

[5] Shionogi's new COVID pill appears to ease omicron symptoms.. Nikkei Asia. 21 December 2021 [2022-10-10]. （原始內容存檔於2022-02-09）.

[pmid35576972-6] Uraki R, Kiso M, Iida S, Imai M, Takashita E, Kuroda M, et al. Characterization and antiviral susceptibility of SARS-CoV-2 Omicron/BA.2. Nature. May 2022, 607: 119–127. PMID 35576972. doi:10.1038/s41586-022-04856-1. 已忽略未知參數|collaboration= (幫助)

[pmid35507419-7] Tyndall JD. S-217622, a 3CL Protease Inhibitor and Clinical Candidate for SARS-CoV-2. Journal of Medicinal Chemistry. May 2022, 65 (9): 6496–6498. PMID 35507419. doi:10.1021/acs.jmedchem.2c00624.

[8] Japan to consider early approval for Shionogi COVID-19 pill.. Japan Times. 8 February 2022 [2022-10-10]. （原始內容存檔於2022-02-10）.

[Reuters_20220225-9] 9.0 ^9.1 Japan's Shionogi seeks approval for COVID-19 pill. Reuters. 25 February 2022 [2022-10-10]. （原始內容存檔於2022-10-12）.

[10] Japan's Shionogi signs government supply pact for pill to fight COVID. Reuters. 25 March 2022 [2022-10-10]. （原始內容存檔於2022-10-16）.

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