"目录号: HY-13623
Entecavir（SQ 34676; BMS 200475）是有选择且有效地HBV抑制剂。在HepG2细胞中的EC50值为3.75 nM。
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生物活性
Description
Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor ofHBV, with anEC50of 3.75 nM in HepG2 cell.
IC50& Target
EC50: 3.75 nM (anti-HBV, HepG2 cell)[2]
In Vitro
BMS-200475 has a EC50of 3.75 nM against HBV. It is incorporated into the protein primer of HBV and subsequently inhibits the priming step of the reverse transcriptase. The antiviral activity of BMS-200475 is significantly less against the other RNA and DNA viruses[1]. Entecavir is more readily phosphorylated to its active metabolites than other deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine. The intracellular half-life of entecavir is 15 h[2].
In Vivo
Daily oral treatment with BMS-200475 at doses ranging from 0.02 to 0.5 mg/kg of body weight for 1 to 3 months effectively reduces the level of woodchuck hepatitis virus (WHV) viremia in chronically infected woodchucks[3].
Clinical Trial
The University of Hong Kong
Hepatitis B, Chronic
June 2007
HepNet Study House, German Liverfoundation-Hannover Medical School
Liver Transplantation-Hepatitis B-Liver Disease
March 2008
Phase 3
Sun Yat-sen University
Colorectal Neoplasms
May 2015
Phase 2
Sun Yat-sen University
Stomach Neoplasms
June 2015
Phase 2
Bangabandhu Sheikh Mujib Medical University, Dhaka, Bangladesh
Chronic Hepatitis B
March 2012
Phase 1-Phase 2
Shanghai Changzheng Hospital
Hepatitis B Virus-Decompensated Cirrhosis
January 2008
Phase 4
Peking University
Hepatitis B
January 2013
Phase 4
National Taiwan University Hospital
Hepatitis-Tuberculosis-hepatitisB
December 2012
Phase 4
Bristol-Myers Squibb
Chronic Hepatitis B
December 2003
Phase 2
Chulalongkorn University
Chronic Hepatitis B
March 2011
Taichung Veterans General Hospital-GlaxoSmithKline
Chronic Hepatitis B
July 2012
Phase 4
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)-University of Pittsburgh
Hepatitis B
May 2012
Phase 3
Guangdong General Hospital
Hepatitis B Virus Associated Nephrotic Syndrome
February 1, 2017
Phase 4
Peking University
Hepatitis B
January 2013
Phase 4
Taipei Veterans General Hospital, Taiwan-Bristol-Myers Squibb
Non Hodgkin's Lymphoma-Hepatitis B
April 2009
Phase 4
Bristol-Myers Squibb
Chronic Hepatitis B Virus
May 2004
Phase 3
Fudan University
Non-Hodgkin Lymphoma-Hepatitis B Reactivation
February 2013
Phase 2
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
Hepatitis B
September 2012
Phase 3
Sun Yat-sen University
Hepatitis B
July 2012
Pacific Health Foundation-Bristol-Myers Squibb
Hepatitis B
May 2008
Asan Medical Center
Lactic Acidosis
May 2011
Phase 4
National Cheng-Kung University Hospital
Chronic Hepatitis
September 2008
Phase 4
National Taiwan University Hospital-Roche Pharma AG
Chronic Hepatitis B
January 2013
Phase 4
National Taiwan University Hospital-National Science Council, Taiwan
Hepatitis B, Chronic
February 2007
Phase 4
Yonsei University-Pusan National University Hospital
Hepatitis B, Chronic
February 2008
Phase 4
Pusan National University Hospital-Yonsei University
Hepatitis B, Chronic
February 2008
Phase 4
Asan Medical Center-Samsung Medical Center-Konkuk University Medical Center-Korea University Guro Hospital-Seoul National University Hospital
Chronic Viral Hepatitis B Without Delta-agent
September 2012
Phase 4
Taipei Veterans General Hospital, Taiwan
Rheumatoid Arthritis-Hepatitis B Reactivation-Exposure to Hepatitis B Virus
July 2013
Phase 4
Bristol-Myers Squibb
Hepatitis B, Chronic
June 30, 2007
Phase 1-Phase 2
Korea University-Gilead Sciences
Chronic Hepatitis B
April 2013
Phase 4
Bristol-Myers Squibb
Hepatitis B, Chronic
July 2008
Phase 4
Yonsei University-Pusan National University Hospital
Hepatitis B, Chronic
February 2008
Phase 4
Yonsei University-Bristol-Myers Squibb-Seoul St. Mary's Hospital-The Catholic University of Korea
Chronic Hepatitis B
August 2012
Phase 4
Asan Medical Center
Chronic Viral Hepatitis B Without Delta-agent
May 2012
Phase 3
Foundation for Liver Research
Chronic Hepatitis B
August 2009
Phase 4
Bristol-Myers Squibb
Hepatitis B, Chronic
April 2007
Phase 3
National Taiwan University Hospital-Bristol-Myers Squibb
Chronic Hepatitis B
January 2008
Phase 4
Zhejiang University
Chronic Hepatitis B-Hepatic Steatosis
June 2010
Phase 4
Bristol-Myers Squibb
Chronic Hepatitis B Virus, Pediatric
June 30, 2010
Phase 3
Guangxi Medical University
Hepatocellular Carcinoma
July 2015
Phase 2-Phase 3
Beijing Ditan Hospital
Chronic Hepatitis B
January 2013
Phase 4
Sun Yat-sen University
Liver Failure
August 2007
Phase 2
Foundation for Liver Research
Entecavir for Chronic Hepatitis B Patients
November 2010
Asan Medical Center
Hepatitis B, Chronic
November 2009
Phase 4
ShuGuang Hospital-Shanghai Zhongshan Hospital-Guangxi Ruikang Hospital-Hubei Hospital of Traditional Chinese Medicine-The First Affiliated Hospital of Hunan University of Traditional Chinese Medicine-Huai'an No. 4 People's Hospital-Ruijin Hospital-Shenzhen Third People's Hospital-Beijing Ditan Hospital-Beijing YouAn Hospital-China-Japan Friendship Hospital-Tongji Hospital-Wenzhou Central Hospital-Jingmen No.1 People’s Hospital-Affiliated Hospital of Shandong Univercity of TCM-Guang'anmen Hospital of China Academy of Chinese Medical Sciences-The Ninth Hospital of Nanchang-The People's Hospital of Ningxia-Fifth Hospital of Shijiazhuang City-The Fifth People's Hospital of Suzhou-The Fifth People’s Hospital of Anyang
Hepatitis B Virus Related Cirrhosis
September 2014
Phase 4
Chongqing Jiachen Biotechnology Ltd.-Third Military Medical University
Chronic Hepatitis B
June 2010
Phase 2
Korea University-GlaxoSmithKline
Chronic Hepatitis B
April 2007
Phase 4
