"目录号: HY-15232
GS-7340(Tenofovir alafenamide)是抗病毒药物替诺福韦（Tenofovir）的前体药物，相比TFV disoproxil fumarate，GS-7340能更好的将TFV送达淋巴细胞和组织。
相关产品
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
GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate.IC50 value:Target: NRTI; HIV reverse transcriptase inhibitorGS-7340 reduces first-pass clearance to be an effective oral prodrug, its permeability and stability were characterized in vitro and detailed pharmacokinetic studies were completed in dogs. GS-7340 showed concentration-dependent permeability through monolayers of caco-2 cells and dose-dependent oral bioavailability in dogs, increasing from 1.7% at 2 mg/kg to 24.7% at 20 mg/kg, suggesting saturable intestinal efflux transport [1]. Significant reductions in plasma HIV-1 RNA from baseline to day 11 were observed for all TAF dose groups compared with placebo (P < 0.01), with a median decrease of 1.08-1.73 log10 copies per milliliter, including a dose-response relationship for viral load decrease up to 25 mg [2].
Clinical Trial
Gilead Sciences
Chronic Hepatitis B
March 2012
Phase 1
University of North Carolina, Chapel Hill-Gilead Sciences
Healthy
March 2015
Phase 1
Asian Pacific Liver Center at St. Vincent Medical Center
Hepatitis B
December 22, 2016
Phase 4
National Institute of Allergy and Infectious Diseases (NIAID)-Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
HIV Infections
March 2003
Phase 4
Erasmus Medical Center-Gilead Sciences
Renal Insufficiency,Chronic-Hiv-Therapeutic Agent Toxicity
October 2016
Phase 4
Janssen Sciences Ireland UC
Healthy
November 2015
Phase 1
Gilead Sciences
HIV Infections
March 2002
Phase 1-Phase 2
Janssen Sciences Ireland UC
Healthy
June 2015
Phase 1
Janssen Sciences Ireland UC
Immunodeficiency Virus Type 1, Human
July 6, 2015
Phase 3
National Institute of Allergy and Infectious Diseases (NIAID)-National Institutes of Health Clinical Center (CC)
HIV-HBV
September 16, 2015
Phase 2
Janssen Scientific Affairs, LLC
Healthy
December 2016
Phase 1
University Hospital Inselspital, Berne
HIV and Hepatitis B Coinfection
May 23, 2017
Phase 2
University of Colorado, Denver
Healthy Volunteers
March 2016
Phase 1
Willem Daniel Francois Venter-University of Witwatersrand, South Africa
HIV-1 Infection
January 2017
Phase 3
AIDS Clinical Trials Group-National Institute of Allergy and Infectious Diseases (NIAID)
HIV-1 Infection
January 2017
Phase 2
University of Maryland
Hepatitis B， Chronic-Hepatitis C
December 2014
CONRAD-United States Agency for International Development (USAID)-Agility Clinical, Inc.
HIV
October 2016
Phase 1
National Institute of Allergy and Infectious Diseases (NIAID)
HIV Infections
July 2017
Phase 3
View MoreCollapse
References
