Tenofovir

"目录号: HY-13910

Anti-infection-

Tenofovir 是一种用于治疗艾滋病毒和慢性乙型肝炎的核苷酸逆转录酶抑制剂。

HIVReverse Transcriptase

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

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

NCT01300234

GlaxoSmithKline

Hepatitis B

March 2011

Phase 3

NCT01480622

GlaxoSmithKline

Hepatitis B, Chronic

December 5, 2011

Phase 1

NCT00448669

Centers for Disease Control and Prevention-Botswana Ministry of Health-Gilead Sciences

HIV Infections

March 2007

Phase 2-Phase 3

NCT02006264

Albert Einstein College of Medicine, Inc.

HIV

November 2013

Phase 1

NCT02762617

Albert Einstein College of Medicine, Inc.

Healthy-HIV

January 2017

Phase 1

NCT01320943

Gilead Sciences

Chronic Hepatitis B

April 2011

Phase 4

NCT01277601

Gilead Sciences

Chronic Hepatitis B

April 2011

Phase 4

NCT00984152

Rush University Medical Center-Merck Sharp & Dohme Corp.

HIV-1 Infections

June 2011

Phase 3

NCT01751555

National Center for AIDS/STD Control and Prevention, China CDC-Gilead Sciences

Hiv

February 2011

Phase 4

NCT01488526

New Discovery LLC-Gilead Sciences

Hepatitis B Infection-Chronic Infection-Viremia

March 1, 2012

Phase 4

NCT02862548

Gilead Sciences

Chronic Hepatitis B

September 15, 2016

Phase 2

NCT01815255

The HIV Netherlands Australia Thailand Research Collaboration-Chulalongkorn University-Bamrasnaradura Infectious Diseases Institute

HIV-infected Thai Children

December 2010

NCT02081469

Chang Gung Memorial Hospital-Gilead Sciences

Hepatitis B, Chronic-Tumor

March 2014

Phase 4

NCT02174276

Gilead Sciences

Chronic Hepatitis B

August 21, 2014

Phase 2

NCT02836249

Gilead Sciences

HBV-Chronic HBV Infections

June 19, 2015

Phase 3

NCT02836236

Gilead Sciences

HBV-Chronic HBV Infections

June 19, 2015

Phase 3

NCT00643968

Gilead Sciences

HIV Infections

March 2003

Phase 4

NCT01160120

The HIV Netherlands Australia Thailand Research Collaboration-Mylan Laboratories

HIV

June 2010

Phase 2

NCT01286740

Gilead Sciences

HIV-1 Infection

January 2011

Phase 2

NCT02979613

Gilead Sciences

Chronic Hepatitis B

December 29, 2016

Phase 3

NCT03164564

National Institute of Allergy and Infectious Diseases (NIAID)

HIV Infections

October 2017

Phase 3

NCT01940471

Gilead Sciences

HBV-Chronic HBV Infection

August 2013

Phase 3

NCT01940341

Gilead Sciences

HBV-Chronic HIV Infection

September 2013

Phase 3

NCT00335192

Germans Trias i Pujol Hospital-Fundacio Lluita Contra la SIDA

HIV

January 2005

Phase 4

NCT01651403

Gilead Sciences

Chronic Hepatitis B Infection

December 2012

Phase 3

NCT01829802

Pedro Cahn-Merck Sharp & Dohme Corp.-The Huesped Foundation

Chronic Infection With HIV

May 2014

Phase 4

NCT00734162

Gilead Sciences

Hepatitis B Virus (HBV)

December 2008

Phase 3

NCT02345252

Gilead Sciences

HIV-1 Infection

January 26, 2015

Phase 3

NCT00737568

Gilead Sciences

Hepatitis B

September 2008

Phase 3

NCT01721109

Gilead Sciences

Acquired Immunodeficiency Syndrome-HIV Infections

December 6, 2012

Phase 2-Phase 3

NCT02345226

Gilead Sciences

HIV-1 Infection

January 27, 2015

Phase 3

NCT00298363

Gilead Sciences

Chronic Hepatitis B

April 2006

Phase 2

NCT02776748

University of Washington-Bill and Melinda Gates Foundation

HIV Pre-exposure Prophylaxis During Breastfeeding

January 2015

Phase 2-Phase 3

NCT02579382

Gilead Sciences

Chronic Hepatitis B

November 10, 2015

Phase 2

NCT01780506

Gilead Sciences

HIV-HIV Infections

December 26, 2012

Phase 3

NCT01797445

Gilead Sciences

HIV-HIV Infections

March 12, 2013

Phase 3

NCT01448616

University of Washington-CONRAD-Gilead Sciences

Herpes Simplex Type II

February 2012

Phase 4

NCT01769469

Westat

HIV Infection

November 2012

NCT02269917

Janssen R&D Ireland

Human Immunodeficiency Virus Type 1

March 30, 2015

Phase 3

NCT02404259

The HIV Netherlands Australia Thailand Research Collaboration-Chulalongkorn University-Khon Kaen University

HIV

June 2010

NCT01074645

Govind Ballabh Pant Hospital

Acute on Chronic Liver Failure-Hepatitis B

November 2007

Phase 4

NCT02121795

Gilead Sciences

HIV-1 Infection

May 8, 2014

Phase 3

NCT00116805

Gilead Sciences

Chronic Hepatitis B

June 2005

Phase 3

NCT00117676

Gilead Sciences

Chronic Hepatitis B

February 2005

Phase 3

NCT01495702

Gilead Sciences

Acquired Immunodeficiency Syndrome-HIV Infections

December 2011

Phase 3

NCT01497899

Gilead Sciences

Acquired Immunodeficiency Syndrome-HIV Infections

December 2011

Phase 2

NCT01705574

Gilead Sciences

Acquired Immunodeficiency Syndrome-HIV Infections

October 24, 2012

Phase 3

NCT01309243

Gilead Sciences

HIV-1 Infection

February 2011

Phase 3

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