恩司特韦

恩司特韦
临床资料
其他名称	S-217622
识别信息
	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号	2647530-73-0; 2757470-18-9
PubChem CID	162533924;
UNII	PX665RAA3H;
化学信息
化学式	C22H17ClF3N9O2
摩尔质量	531.88 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	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;

恩司特韦^[1]（代号：S-217622，商品名：Xocova）^[2]是盐野义制药公司与北海道大学合作开发的一种抗病毒药物，可作为口服活性3C样蛋白酶抑制剂，用于治疗COVID-19感染。^[3]^[4]它是口服的，并且已经成功地针对最近出现的奥米克戎变体进行了测试。^[5]^[6]

历史

它已进入III期临床试验。^[7]据报道，日本政府正在考虑允许盐野木在最后的试验步骤完成之前申请医疗用途的批准，这可能会加快上市销售。这种有条件的早期批准系统此前已在日本用于加速其他针对 COVID-19的抗病毒药物的上市进程，包括瑞德西韦和莫努匹韦。^[8]在一项针对428名患者的研究中，病毒载量降低，但症状并未显着减轻。^[9]

如果获得批准，它将成为第一个治疗COVID-19的日本国产药丸，也是第三个在日本获得批准的药丸。2022年2月，该公司向日本监管机构寻求紧急批准。^[9]

盐野义制药公司宣布，他们已达成初步协议，一旦该药物获得批准，将向日本政府供应100万剂。这位首席执行官表示，他们有能力每年生产1000万剂。^[10]

参见

参考文献

^ World Health Organization. International Nonproprietary Names for Pharmaceutical Substances. Proposed INN: List 126 (PDF). WHO Drug Information. 2021, 35 (4): 1135 [2022-10-10]. （原始内容存档 (PDF)于2022-02-04）.
^ Xocova: Powerful New Japanese Pill for Coronavirus Treatment.. BioPharma Media. February 2022 [2022-10-10]. （原始内容存档于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]. （原始内容存档于2022-02-08）.
^ Shionogi's new COVID pill appears to ease omicron symptoms.. Nikkei Asia. 21 December 2021 [2022-10-10]. （原始内容存档于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. 已忽略未知参数|collaboration= (帮助)
^ 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]. （原始内容存档于2022-02-10）.
^ ^9.0 ^9.1 Japan's Shionogi seeks approval for COVID-19 pill. Reuters. 25 February 2022 [2022-10-10]. （原始内容存档于2022-10-12）.
^ Japan's Shionogi signs government supply pact for pill to fight COVID. Reuters. 25 March 2022 [2022-10-10]. （原始内容存档于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]. （原始内容存档 (PDF)于2022-02-04）.

[2] Xocova: Powerful New Japanese Pill for Coronavirus Treatment.. BioPharma Media. February 2022 [2022-10-10]. （原始内容存档于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]. （原始内容存档于2022-02-08）.

[5] Shionogi's new COVID pill appears to ease omicron symptoms.. Nikkei Asia. 21 December 2021 [2022-10-10]. （原始内容存档于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. 已忽略未知参数|collaboration= (帮助)

[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]. （原始内容存档于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]. （原始内容存档于2022-10-12）.

[10] Japan's Shionogi signs government supply pact for pill to fight COVID. Reuters. 25 March 2022 [2022-10-10]. （原始内容存档于2022-10-16）.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]

[10]