"目錄號(hào): HY-13910
Tenofovir 是一種用于治療艾滋病毒和慢性乙型肝炎的核苷酸逆轉(zhuǎn)錄酶抑制劑。
相關(guān)產(chǎn)品
Dolutegravir-Maraviroc-Elvitegravir-Atazanavir sulfate-Tenofovir Disoproxil Fumarate-Tipranavir-Triciribine-Emtricitabine-Efavirenz-Miltefosine-Ritonavir-Delavirdine mesylate-Lamivudine-Abacavir-BI 224436-
生物活性
Description
Tenofovir is anucleotide reverse transcriptase inhibitorto treat HIV and chronic Hepatitis B.
In Vitro
Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage[1]. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaLand X4-tropic HIV-1IIIbin activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs[2].
In Vivo
Tenofovir Disoproxil Fumarate (20, 50, 140, or 300?mg/kg) administered to BLT mice, shows dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50, 140, 300?mg/kg) significantly reduces HIV transmission in BLT mice[3]. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil Fumarate administration is safe and effective in the woodchuck model of chronic HBV infection[4].
Clinical Trial
GlaxoSmithKline
Hepatitis B
March 2011
Phase 3
GlaxoSmithKline
Hepatitis B, Chronic
December 5, 2011
Phase 1
Centers for Disease Control and Prevention-Botswana Ministry of Health-Gilead Sciences
HIV Infections
March 2007
Phase 2-Phase 3
Albert Einstein College of Medicine, Inc.
HIV
November 2013
Phase 1
Albert Einstein College of Medicine, Inc.
Healthy-HIV
January 2017
Phase 1
Gilead Sciences
Chronic Hepatitis B
April 2011
Phase 4
Gilead Sciences
Chronic Hepatitis B
April 2011
Phase 4
Rush University Medical Center-Merck Sharp & Dohme Corp.
HIV-1 Infections
June 2011
Phase 3
National Center for AIDS/STD Control and Prevention, China CDC-Gilead Sciences
Hiv
February 2011
Phase 4
New Discovery LLC-Gilead Sciences
Hepatitis B Infection-Chronic Infection-Viremia
March 1, 2012
Phase 4
Gilead Sciences
Chronic Hepatitis B
September 15, 2016
Phase 2
The HIV Netherlands Australia Thailand Research Collaboration-Chulalongkorn University-Bamrasnaradura Infectious Diseases Institute
HIV-infected Thai Children
December 2010
Chang Gung Memorial Hospital-Gilead Sciences
Hepatitis B, Chronic-Tumor
March 2014
Phase 4
Gilead Sciences
Chronic Hepatitis B
August 21, 2014
Phase 2
Gilead Sciences
HBV-Chronic HBV Infections
June 19, 2015
Phase 3
Gilead Sciences
HBV-Chronic HBV Infections
June 19, 2015
Phase 3
Gilead Sciences
HIV Infections
March 2003
Phase 4
The HIV Netherlands Australia Thailand Research Collaboration-Mylan Laboratories
HIV
June 2010
Phase 2
Gilead Sciences
HIV-1 Infection
January 2011
Phase 2
Gilead Sciences
Chronic Hepatitis B
December 29, 2016
Phase 3
National Institute of Allergy and Infectious Diseases (NIAID)
HIV Infections
October 2017
Phase 3
Gilead Sciences
HBV-Chronic HBV Infection
August 2013
Phase 3
Gilead Sciences
HBV-Chronic HIV Infection
September 2013
Phase 3
Germans Trias i Pujol Hospital-Fundacio Lluita Contra la SIDA
HIV
January 2005
Phase 4
Gilead Sciences
Chronic Hepatitis B Infection
December 2012
Phase 3
Pedro Cahn-Merck Sharp & Dohme Corp.-The Huesped Foundation
Chronic Infection With HIV
May 2014
Phase 4
Gilead Sciences
Hepatitis B Virus (HBV)
December 2008
Phase 3
Gilead Sciences
HIV-1 Infection
January 26, 2015
Phase 3
Gilead Sciences
Hepatitis B
September 2008
Phase 3
Gilead Sciences
Acquired Immunodeficiency Syndrome-HIV Infections
December 6, 2012
Phase 2-Phase 3
Gilead Sciences
HIV-1 Infection
January 27, 2015
Phase 3
Gilead Sciences
Chronic Hepatitis B
April 2006
Phase 2
University of Washington-Bill and Melinda Gates Foundation
HIV Pre-exposure Prophylaxis During Breastfeeding
January 2015
Phase 2-Phase 3
Gilead Sciences
Chronic Hepatitis B
November 10, 2015
Phase 2
Gilead Sciences
HIV-HIV Infections
December 26, 2012
Phase 3
Gilead Sciences
HIV-HIV Infections
March 12, 2013
Phase 3
University of Washington-CONRAD-Gilead Sciences
Herpes Simplex Type II
February 2012
Phase 4
Westat
HIV Infection
November 2012
Janssen R&D Ireland
Human Immunodeficiency Virus Type 1
March 30, 2015
Phase 3
The HIV Netherlands Australia Thailand Research Collaboration-Chulalongkorn University-Khon Kaen University
HIV
June 2010
Govind Ballabh Pant Hospital
Acute on Chronic Liver Failure-Hepatitis B
November 2007
Phase 4
Gilead Sciences
HIV-1 Infection
May 8, 2014
Phase 3
Gilead Sciences
Chronic Hepatitis B
June 2005
Phase 3
Gilead Sciences
Chronic Hepatitis B
February 2005
Phase 3
Gilead Sciences
Acquired Immunodeficiency Syndrome-HIV Infections
December 2011
Phase 3
Gilead Sciences
Acquired Immunodeficiency Syndrome-HIV Infections
December 2011
Phase 2
Gilead Sciences
Acquired Immunodeficiency Syndrome-HIV Infections
October 24, 2012
Phase 3
Gilead Sciences
HIV-1 Infection
February 2011
Phase 3
