新药研究信息：Bayer公司的 Bay 41-4109

FlyMa

不知有人发过没

主要是抑制病毒衣壳形成并随之而产生的核心蛋白半衰期缩短。
体外实验中，在可以产生HBV的HepG2.2.15细胞系中，Bay 41-4109 可以阻断50%的HBV复制。

http://www.biomedcentral.com/news/20030207/03/
February 7, 2003 Previous | Next
Hepatitis B drug breakthroughA novel class of drugs inhibits hepatitis B virus capsid formation and replication. | Tudor P Toma

Chronic hepatitis B is a viral infection that can currently only be treated with interferon-α and nucleosidic inhibitors of viral polymerase — 3TC and adefovir — but these treatments are limited by serious side effects and a high failure rate. Novel therapeutic regimes are urgently required. In the February 7 Science, Karl Deres and colleagues at the Bayer Research Center, Wuppertal, Germany, describe a substance class for the treatment of HBV infection that displays a highly specific antiviral inhibition of capsid formation, concomitant with a reduced half-life of the core protein (Science 299:893-896, February 7, 2003).

Deres et al. analyzed the in vitro profile and mechanism of action for the heteroaryldihydropyrimidine Bay 41-4109 and the congeners Bay 38-7690 and Bay 39-5493.They observed that Bay 41-4109 blocked by 50% the HBV replication when incubated with HBV-producing HepG2.2.15 cells. In addition, they showed that Bay 41-4109 and Bay 38-7690 reduced HBV core protein levels in cell culture and induced depletion of newly synthesized core proteins.

"The candidate, Bay 41-4109, may become a valuable addition to future [anti-HBV] therapy (mono- or combination-therapy regimens) in light of its specific mechanism of action," conclude the authors.

Links for this article
C.T. Wai et al., "Treatment of hepatitis B," Journal of Gastroenterology, 37:771-778, 2002.
[PubMed Abstract]  

K. Deres et al. "Inhibition of Hepatitis B Virus Replication by Drug-Induced Depletion of Nucleocapsids," Science 299:893-896, February 7, 2003.
http://www.sciencemag.org

Bayer Research Center
http://www.bayerresearchcenter.com/