卡莫司他

卡莫司他(英語:camostat,开发代码FOY-305),是一种丝氨酸蛋白酶抑制剂,在体内有各种功能。被用来治疗某些肿瘤,并被用来有效地抵抗病毒感染。还可抑制肝脏纤维化、肾病或胰腺炎[1][2][3][4][5]在日本被批准使用。[6] 2020年德国科学家在细胞杂志上发表论文指出甲磺酸卡莫司他(英語:camostat mesylate)积极对抗TMPRSS2,部分阻断SARS-2-S-驱动的进入Caco-2和Vero195 TMPRSS2细胞。[7]

卡莫司他
Camostat.svg
系统(IUPAC)命名名称
N,N-Dimethylcarbamoylmethyl 4-(4-guanidinobenzoyloxy)phenylacetate
临床数据
商品名Foipan
Drugs.com国际药品名称
给药途径Oral
合法狀態
合法状态
  • US: Not FDA approved
  • 处方药(-only)
识别信息
CAS注册号59721-28-7  ✓
ATC代码B02AB04
PubChemCID 2536
IUPHAR/BPS英语IUPHAR/BPS6432
ChemSpider2440 ✓
UNII0FD207WKDU ✓
ChEMBL英语ChEMBLCHEMBL590799 ✓
化学信息
化学式C20H22N4O5
摩尔质量398.42 g·mol−1

来源编辑

  1. ^ Okuno, M.; Kojima, S.; Akita, K.; Matsushima-Nishiwaki, R.; Adachi, S.; Sano, T.; Takano, Y.; Takai, K.; Obora, A.; Yasuda, I.; Shiratori, Y.; Okano, Y.; Shimada, J.; Suzuki, Y.; Muto, Y.; Moriwaki, Y. Retinoids in liver fibrosis and cancer. Frontiers in Bioscience. 2002, 7 (4): d204–18. PMID 11779708. doi:10.2741/A775. 
  2. ^ Hsieh, H. P.; Hsu, J. T. Strategies of development of antiviral agents directed against influenza virus replication. Current Pharmaceutical Design. 2007, 13 (34): 3531–42. PMID 18220789. doi:10.2174/138161207782794248. 
  3. ^ Kitamura, K.; Tomita, K. Proteolytic activation of the epithelial sodium channel and therapeutic application of a serine protease inhibitor for the treatment of salt-sensitive hypertension. Clinical and Experimental Nephrology. 2012, 16 (1): 44–8. PMID 22038264. doi:10.1007/s10157-011-0506-1. 
  4. ^ Zhou, Y.; Vedantham, P.; Lu, K.; Agudelo, J.; Carrion Jr, R.; Nunneley, J. W.; Barnard, D.; Pöhlmann, S.; McKerrow, J. H.; Renslo, A. R.; Simmons, G. Protease inhibitors targeting coronavirus and filovirus entry. Antiviral Research. 2015, 116: 76–84. PMC 4774534 . PMID 25666761. doi:10.1016/j.antiviral.2015.01.011. 
  5. ^ Ueda, M.; Uchimura, K.; Narita, Y.; Miyasato, Y.; Mizumoto, T.; Morinaga, J.; Hayata, M.; Kakizoe, Y.; Adachi, M.; Miyoshi, T.; Shiraishi, N.; Kadowaki, D.; Sakai, Y.; Mukoyama, M.; Kitamura, K. The serine protease inhibitor camostat mesilate attenuates the progression of chronic kidney disease through its antioxidant effects. Nephron. 2015, 129 (3): 223–32. PMID 25766432. doi:10.1159/000375308. 
  6. ^ Camostat. drugs.com. [2020-03-02]. (原始内容存档于2020-03-05). 
  7. ^ SARS-CoV-2 cell entry depends on ACE2 and TMPRSS2 and is blocked by a clinically-proven protease inhibitor. [2020-03-05]. (原始内容存档于2021-02-24).