1. Anti-infection
  2. HIV
    Reverse Transcriptase

Emtricitabine (Synonyms: BW1592)

Cat. No.: HY-17427 Purity: 99.60%
Data Sheet SDS Handling Instructions

Emtricitabine is an inhibitor of the nucleoside reverse transcriptase (NRTI) and human immunodeficiency virus type 1 (HIV-1); inhibits NRTI with an EC50 of 0.01 µM in PBMC cell.

For research use only. We do not sell to patients.
Emtricitabine Chemical Structure

Emtricitabine Chemical Structure

CAS No. : 143491-57-0

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    Emtricitabine purchased from MCE. Usage Cited in: Open Virol J. 2014 Mar 7;8:1-8.

    The PKR activation block is not unique to CypI, DAAs also prevent the IFN-induced PKR activation in HCV-infected cells. JFH-1-infected Huh7.5.1 cells are treated with or without CypI (cyclosporine A and alisporivir), DAAs (the HCV NS5A inhibitor daclatasvir and the HCV protease inhibitor telaprevir) and an HIV-1 inhibitor (reverse transcriptase inhibitor emtricitabine). Results are representative of 4 independent experiments.

    Emtricitabine purchased from MCE. Usage Cited in: J Neuroimmune Pharmacol. 2017 Jul 22.

    TDF/FTC/RAL combined medication induces mouse NPC apoptosis in vitro. Mouse NPCs are treated with either DMSO or TDF/FTC/RAL for 8 h. Cleaved Caspase-3 levels are determined by Western blotting.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Emtricitabine is an inhibitor of the nucleoside reverse transcriptase (NRTI) and human immunodeficiency virus type 1 (HIV-1); inhibits NRTI with an EC50 of 0.01 µM in PBMC cell.

    IC50 & Target

    EC50: 0.01 µM (NRTI, PBMC), 0.026 µM (NRTI, HeLa cell)[1]

    In Vitro

    Emtricitabine has in vitro activity against both laboratory strains of HIV-1 and HIV-2 and clinical isolates of HIV-1. The 50% effective concentration (EC50) ranges from 0.002 to 1.5 µ mol/L, depending on the viral isolate and cell line used. Emtricitabine demonstrates in vitro synergy with zidovudine and stavudine and additive in vitro activity when combines with zalcitabine or didanosine[1].

    In Vivo

    Reproductive and developmental toxicology studies are conducted with emtricitabine. Oral doses up to 1000 mg/kg/day provided daily area under the curve (AUC0→24) exposure to pregnant animals approximately 60- (mice) to 120-fold (rabbits) higher than that in humans at the recommended dose of 200 mg given once per day. In a mouse fertility study, emtricitabine had no effect on fertility, sperm count, or early embryonic development. There is no increased incidence of malformations in mouse and rabbit embryofetal toxicology studies. The development and fertility of F1 progeny are unaffected by emtricitabine in a mouse pre- and post-natal study. These data demonstrate a favorable pre-clinical reproductive safety profile for emtricitabine[2].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT00743340 Gilead Sciences HIV-1 Infection November 22, 2005 Phase 2
    NCT02327689 Asian-Pacific Alliance of Liver Disease, Beijing|Beijing Ditan Hospital|Hebei Medical University Pharmaceutical Factory|National Health and Family Planning Commission, P.R.China Hepatitis B, Chronic|Fibrosis January 2015 Phase 4
    NCT02327702 Asian-Pacific Alliance of Liver Disease, Beijing|Beijing Ditan Hospital|Hebei Medical University Pharmaceutical Factory|National Health and Family Planning Commission, P.R.China Hepatitis B, Chronic|Pregnancy January 2015 Phase 4
    NCT00642291 Gilead Sciences HIV Infections November 2002 Phase 2
    NCT02327676 Asian-Pacific Alliance of Liver Disease, Beijing|Beijing Ditan Hospital|Hebei Medical University Pharmaceutical Factory|National Health and Family Planning Commission, P.R.China Hepatitis B, Chronic January 2015 Phase 4
    NCT02327715 Asian-Pacific Alliance of Liver Disease, Beijing|Beijing Ditan Hospital|Hebei Medical University Pharmaceutical Factory|National Health and Family Planning Commission, P.R.China Hepatitis B, Chronic|Pregnancy January 2015 Phase 4
    NCT02327663 Asian-Pacific Alliance of Liver Disease, Beijing|Beijing Ditan Hospital|Hebei Medical University Pharmaceutical Factory|National Health and Family Planning Commission, P.R.China Hepatitis B, Chronic December 2014 Phase 4
    NCT02530060 Janssen Pharmaceutical K.K. Healthy August 2015 Phase 4
    NCT00924898 University of North Carolina, Chapel Hill|Bristol-Myers Squibb|Gilead Sciences Acute HIV Infection|HIV Infections January 2005 Phase 4
    NCT00474435 African Poverty Related Infection Oriented Research Initiative|Radboud University|Kilimanjaro Christian Medical Centre, Tanzania Tuberculosis|HIV Infections November 2008 Phase 2
    NCT02583464 Laboratorio Elea S.A.C.I.F. y A. Acquired Immunodeficiency Syndrome September 2014 Phase 1
    NCT02104700 Philip Grant|Rwanda Biomedical Center|Gilead Sciences|Stanford University HIV April 2014 Phase 2|Phase 3
    NCT00076791 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|International Maternal Pediatric Adolescent AIDS Clinical Trials Group HIV Infections March 2004 Phase 1
    NCT02211690 Andrew Carr|ViiV Healthcare Australia Pty. Ltd|St Vincent's Hospital, Sydney Human Immunodeficiency Virus August 2014 Phase 4
    NCT02578550 Janssen Sciences Ireland UC Healthy November 2015 Phase 1
    NCT01345630 ViiV Healthcare|Pfizer HIV-1 September 2011 Phase 3
    NCT03060785 Johns Hopkins University HIV Prevention March 8, 2016 Phase 1
    NCT01715636 Andrew Carr|St Vincent's Hospital, Sydney HIV Nonoccupational Post-exposure Prophylaxis in Men Who Have Sex With Men December 2012 Phase 4
    NCT00524173 National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) Hepatitis B August 29, 2007 Phase 2
    NCT01066962 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|NEAT - European AIDS Treatment Network HIV Infections August 2010 Phase 3
    NCT01605890 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Gilead Sciences|Merck Sharp & Dohme Corp. HIV-2 Infection July 2012 Phase 2
    NCT01576731 Hospital Clinic of Barcelona HIV Infection July 2012 Phase 4
    NCT00391638 French National Agency for Research on AIDS and Viral Hepatitis|Gilead Sciences|Roche Pharma AG|French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) Hepatitis B|HIV Infections January 2007 Phase 2|Phase 3
    NCT00476463 The HIV Netherlands Australia Thailand Research Collaboration|Gilead Sciences|Ministry of Health, Thailand Hepatitis B Virus|HIV Infections April 2005 Phase 2
    NCT02844634 British Columbia Centre for Disease Control HIV|Syphilis September 2016 Phase 4
    NCT01902186 Giovanni Di Perri|University of Turin, Italy|University of Milan HIV Infection|Osteopenia September 2014 Phase 4
    NCT00808002 Germans Trias i Pujol Hospital HIV Infections February 2009 Phase 3
    NCT01701882 St Stephens Aids Trust HIV Phase 3
    NCT00654147 Margaret A. Fischl, M.D.|University of Miami HIV Infections April 2008 Phase 2
    NCT00660972 National Institute of Allergy and Infectious Diseases (NIAID)|Adult AIDS Clinical Trials Group HIV Infections May 2008 Phase 1
    NCT02198443 Fundacion Clinic per a la Recerca Biomédica HIV June 6, 2015 Phase 4
    NCT03218085 University of Minnesota - Clinical and Translational Science Institute|American College of Clinical Pharmacy HIV/AIDS|Menopause|Inflammation Vagina July 14, 2017
    NCT02475135 Janssen Sciences Ireland UC Healthy June 2015 Phase 1
    NCT02159599 Fundacion SEIMC-GESIDA|Janssen, LP HIV Infection July 2014 Phase 4
    NCT00192634 Kirby Institute HIV Infections December 2005 Phase 4
    NCT00862823 University of Alabama at Birmingham|Bristol-Myers Squibb Healthy February 2009 Phase 4
    NCT01040091 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections December 2009 Phase 1
    NCT00334256 French National Agency for Research on AIDS and Viral Hepatitis|European and Developing Countries Clinical Trials Partnership (EDCTP)|Gilead Sciences HIV Infection|Pregnancy October 2006 Phase 2
    NCT02431247 Janssen Sciences Ireland UC Immunodeficiency Virus Type 1, Human July 6, 2015 Phase 3
    NCT00958100 Catholic University of the Sacred Heart HIV/AIDS|Antiretroviral Therapy|HIV Infections August 2009 Phase 2
    NCT02556333 National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) HIV|HBV September 16, 2015 Phase 2
    NCT00204308 University of North Carolina, Chapel Hill|Elizabeth Glaser Pediatric AIDS Foundation HIV|Pregnancy March 2005 Phase 2
    NCT01327651 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections August 2011 Phase 2
    NCT02770508 The Huesped Foundation|Ministry of Science and Technology,Argentine|National AIDS and STD programme,Argentine|Richmond Laboratories HIV-1 Infection November 2015 Phase 4
    NCT00106379 Gilead Sciences HIV Infections October 2004 Phase 4
    NCT00458393 National Institute of Allergy and Infectious Diseases (NIAID)|Bill and Melinda Gates Foundation HIV Infections June 2007 Phase 3
    NCT00017992 Triangle Pharmaceuticals|NIH AIDS Clinical Trials Information Service HIV Infections Phase 2
    NCT02656511 University of California, San Francisco|ViiV Healthcare|Gilead Sciences HIV December 2015 Phase 4
    NCT00244712 GlaxoSmithKline HIV Infection July 2005 Phase 4
    NCT02968576 University of Colorado, Denver Healthy Volunteers|Pharmacokinetics December 2016
    NCT01533272 Hospital Clinic of Barcelona HIV Infection February 2012 Phase 4
    NCT02831673 ViiV Healthcare|PPD|GlaxoSmithKline Infection, Human Immunodeficiency Virus July 21, 2016 Phase 3
    NCT01694407 CONRAD HIV February 2013 Phase 1
    NCT01276600 HIV Prevention Trials Network HIV January 2011 Phase 1
    NCT02831764 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus July 18, 2016 Phase 3
    NCT00528060 French National Agency for Research on AIDS and Viral Hepatitis|Bristol-Myers Squibb|Gilead Sciences HIV Infections January 2008 Phase 2
    NCT01989611 Oswaldo Cruz Foundation|University of Sao Paulo|Centro de Referência e Treinamento DST AIDS HIV June 2014
    NCT00016718 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections August 2001 Phase 1|Phase 2
    NCT02984852 Janssen Scientific Affairs, LLC Healthy December 2016 Phase 1
    NCT00127959 International Antiviral Therapy Evaluation Center|Gilead Sciences HIV Infections|Hepatitis B March 2004 Phase 4
    NCT00112047 Gilead Sciences HIV Infections July 2003 Phase 3
    NCT03220152 Oswaldo Cruz Foundation HIV, Prophylaxis July 2017 Phase 4
    NCT00115609 French National Agency for Research on AIDS and Viral Hepatitis HIV Infections|Tuberculosis January 2006 Phase 3
    NCT00711009 Abbott|Merck Sharp & Dohme Corp. Human Immunodeficiency Virus Infection July 2008 Phase 3
    NCT01270802 Indiana University|Merck Sharp & Dohme Corp. HIV April 2011 Phase 4
    NCT00006208 Triangle Pharmaceuticals|NIH AIDS Clinical Trials Information Service HIV Infections August 2000 Phase 3
    NCT02987530 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Institut National de la Santé Et de la Recherche Médicale, France HIV-1 Infection January 2017 Phase 3
    NCT01180075 University of North Carolina, Chapel Hill|National Institute of Allergy and Infectious Diseases (NIAID) Human Immunodeficiency Virus May 2010
    NCT00002362 Triangle Pharmaceuticals|NIH AIDS Clinical Trials Information Service HIV Infections August 1999 Phase 3
    NCT03197961 Jessica Tarleton|University of Pittsburgh HIV/AIDS|Contraception July 2017 Early Phase 1
    NCT01855867 Kenneth H. Mayer, MD|Gilead Sciences|Fenway Community Health Human Immunodeficiency Virus May 2013 Phase 4
    NCT01709084 Janssen-Cilag International NV Human Immunodeficiency Virus-type 1 Infection October 2, 2013 Phase 3
    NCT00043966 Abbott HIV Infections July 2002 Phase 3
    NCT02149888 St. Michael's Hospital, Toronto|Hassle Free Clinic|Maple Leaf Medical Clinic|Ryerson University|AIDS Committee of Toronto|Canadian AIDS Treatment Information Exchange|Gilead Sciences HIV|Human Immunodeficiency Virus October 2014 Phase 4
    NCT01687218 CONRAD|National Institute of Allergy and Infectious Diseases (NIAID)|National Institute of Mental Health (NIMH)|National Institutes of Health (NIH) HIV September 25, 2013 Phase 2
    NCT00298363 Gilead Sciences Chronic Hepatitis B April 2006 Phase 2
    NCT00414635 Community Research Initiative of New England|The Campbell Foundation HIV Infections August 2006 Phase 4
    NCT00158457 French National Agency for Research on AIDS and Viral Hepatitis|Gilead Sciences|Institut de Médecine et d'Epidémiologie Appliquée - Fondation Internationale Léon M'Ba HIV Infection June 2004 Phase 3
    NCT01458977 Fundacio Lluita Contra la SIDA HIV|Dyslipidemia January 2012 Phase 4
    NCT00662545 University of California, San Francisco|Bristol-Myers Squibb HIV Infections|Hepatitis B April 2008 Phase 4
    NCT02815566 University Health Network, Toronto|University of Modena and Reggio Emilia|San Raffaele University Hospital, Italy|Gilead Sciences|CIHR Canadian HIV Trials Network Osteoporosis|HIV|Menopause June 2017 Phase 4
    NCT00307489 Gilead Sciences Chronic Hepatitis B March 2006 Phase 2
    NCT00364793 Bristol-Myers Squibb HIV Infections February 2007 Phase 1|Phase 2
    NCT02116660 Merck Sharp & Dohme Corp. HIV Infections September 3, 2014 Phase 2
    NCT00105079 Hoffmann-La Roche HIV Infections April 2005 Phase 3
    NCT00365612 Gilead Sciences|Bristol-Myers Squibb HIV Infections July 2006 Phase 4
    NCT01274780 Juan A. Arnaiz|Hospital Clinic of Barcelona HIV-1 May 2011 Phase 4
    NCT02962739 University of Colorado, Denver Healthy Volunteers March 2016 Phase 1
    NCT01777997 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection February 2013 Phase 4
    NCT02180438 University of Washington|Clinique des Maladies Infectieuses Ibrahima DIOP Mar/CRCF, Centre Hospitalier Universitaire de Fann|Gilead Sciences HIV-2 Infection September 2014 Phase 4
    NCT00759070 Juan A. Arnaiz|Fundació Institut de Recerca de l'Hospital de la Santa Creu i Sant Pau|Germans Trias i Pujol Hospital|Hospital Universitari Joan XXIII de Tarragona.|Hospitales Universitarios Virgen del Rocío|Hospital Clinic of Barcelona HIV Infections September 2008 Phase 4
    NCT01025427 University of California, San Francisco|California HIV/AIDS Research Program|Gilead Sciences|Merck Sharp & Dohme Corp. HIV|HIV Infections December 2009 Phase 4
    NCT01326221 University of North Carolina, Chapel Hill|Gilead Sciences Pharmacokinetic Study in Healthy Volunteers October 2008 Phase 4
    NCT01033760 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Gilead Sciences|Merck Sharp & Dohme Corp.|Pfizer|Janssen-Cilag Ltd. HIV-1 Infections April 2010 Phase 3
    NCT02150993 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) HIV-2 Infection January 26, 2016 Phase 2|Phase 3
    NCT00549198 GlaxoSmithKline Infection, Human Immunodeficiency Virus I|HIV Infection June 2007 Phase 4
    NCT00448669 Centers for Disease Control and Prevention|Botswana Ministry of Health|Gilead Sciences HIV Infections March 2007 Phase 2|Phase 3
    NCT00444379 University of California, San Francisco|National Institutes of Health (NIH)|Gilead Sciences|Abbott|Merck Sharp & Dohme Corp. Kaposi's Sarcoma|HIV Infections April 2007 Phase 4
    NCT00118898 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections September 2005 Phase 3
    NCT00323544 Gilead Sciences HIV Infections October 2004 Phase 3
    NCT03043326 Asociación Civil Impacta Salud y Educación, Peru|Gilead Sciences HIV Prevention January 23, 2017
    NCT00931801 Community Research Initiative of New England|Bristol-Myers Squibb|Merck Sharp & Dohme Corp. HIV December 2009 Phase 4
    NCT00335322 Kirby Institute|The University of New South Wales Human Immunodeficiency Virus (HIV) February 2007 Phase 4
    NCT00724711 Gilead Sciences HIV Infection July 2008 Phase 4
    NCT00729573 National Institute of Allergy and Infectious Diseases (NIAID)|Microbicide Trials Network HIV Infections November 2009
    NCT00221286 University Hospital, Bonn|Hoffmann-La Roche Chronic Hepatitis B|HIV Infections September 2004 Phase 3
    NCT01505114 National Institute of Allergy and Infectious Diseases (NIAID)|HIV Prevention Trials Network|AIDS Clinical Trials Group HIV Infection June 2012 Phase 2
    NCT01910402 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus August 1, 2013 Phase 3
    NCT00768989 Bristol-Myers Squibb|Merck Sharp & Dohme Corp. HIV November 2008 Phase 2
    NCT00121017 Abbott HIV Infection|Hepatitis C Phase 2
    NCT01332227 Bristol-Myers Squibb HIV, Combination Therapy October 2011 Phase 4
    NCT00532168 Juan A. Arnaiz|Hospital Clinic of Barcelona HIV Infections September 2007 Phase 4
    NCT00544128 International Medical Center of Japan|Ministry of Health, Labour and Welfare, Japan HIV Infections October 2007 Phase 4
    NCT00272779 Bristol-Myers Squibb HIV Infections November 2005 Phase 3
    NCT00557245 University of Washington|Bill and Melinda Gates Foundation HIV-1 Infections|HIV Infections May 2008 Phase 3
    NCT01394133 University of Alabama at Birmingham|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infected July 2011
    NCT03163277 Giovanni Di Perri|University of Turin, Italy Hiv|Neurocognitive Dysfunction May 15, 2017 Phase 4
    NCT00705679 National Institute of Allergy and Infectious Diseases (NIAID)|Microbicide Trials Network HIV Infections August 2009 Phase 2
    NCT00928187 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Gilead Sciences|Janssen Pharmaceutica HIV|HIV Infections November 2009 Phase 3
    NCT01929759 Massachusetts General Hospital|Brigham and Women's Hospital|Gilead Sciences HIV Disease January 2014
    NCT03202511 Indiana University Pre-Exposure Prophylaxis June 23, 2017 Early Phase 1
    NCT02859558 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection January 2017 Phase 2
    NCT00943540 Radboud University HIV Infection|HIV Infections July 2009 Phase 2
    NCT03120936 Public Health Foundation Enterprises, Inc.|San Francisco Department of Public Health|University of California, San Francisco|API Wellness|Tri-City Health Center|California HIV/AIDS Research Program Transgender Persons|Pre-Exposure Prophylaxis May 2017 Phase 4
    NCT00869960 University of Alabama at Birmingham|National Institute of Allergy and Infectious Diseases (NIAID) Healthy March 2009 Phase 4
    NCT00087464 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections
    NCT03120494 Puerto Rico Community Network for Clinical Research on AIDS|Gilead Sciences HIV/AIDS November 2016 Phase 4
    NCT01602822 Kenneth H. Mayer, MD|Bristol-Myers Squibb|Gilead Sciences|Abbott|Fenway Community Health HIV February 2012 Phase 4
    NCT00811954 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID)|Bristol-Myers Squibb|Gilead Sciences|Merck Sharp & Dohme Corp.|Tibotec Therapeutics, a Division of Ortho Biotech Products, L.P., USA HIV Infection May 2009 Phase 3
    NCT00442962 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections May 2007 Phase 4
    NCT02206555 Kirby Institute HIV November 2014 Phase 4
    NCT00545558 University of Cincinnati|National Institute of Allergy and Infectious Diseases (NIAID) Hepatitis C|HIV Infections April 2006 Phase 1
    NCT03058835 Rutgers, The State University of New Jersey PrEP Adherence Monitoring September 2016 Phase 4
    NCT02411630 University of North Carolina, Chapel Hill|National Institute on Drug Abuse (NIDA)|National Institute of Mental Health (NIMH) HIV Infection June 2013
    NCT01772940 Centre Hospitalier Universitaire Saint Pierre|University Hospital of Liege|Ministry of Public Health, Democratic Republic of the Congo|Pierre and Marie Curie University|University Paris 7 - Denis Diderot|Gilead Sciences|Abbott HIV-1 Infection December 2008 Phase 4
    NCT00851799 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infection June 2009
    NCT01781806 University of California, Los Angeles|Los Angeles County Department of Public Health|Los Angeles LGBT Center|The OASIS Clinic|AIDS Project Los Angeles HIV Prevention May 2013 Phase 4
    NCT00641641 Kirby Institute|Merck Sharp & Dohme Corp. HIV Infection March 2008
    NCT00302822 French National Agency for Research on AIDS and Viral Hepatitis|Hoffmann-La Roche|Gilead Sciences|French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) HIV Infections|AIDS April 2006 Phase 3
    NCT01352117 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection|Kaposi's Sarcoma October 2011 Phase 3
    NCT01400412 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection December 2011 Phase 2
    NCT00414518 University of Colorado, Denver|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections January 2007
    NCT01258439 St Vincent's Hospital, Sydney|Merck Sharp & Dohme Corp. HIV|Cardiovascular Disease November 2010 Phase 4
    NCT00002335 Glaxo Wellcome|NIH AIDS Clinical Trials Information Service HIV Infections Phase 1
    NCT01003990 Bristol-Myers Squibb HIV October 2002 Phase 3
    NCT00551018 Merck Sharp & Dohme Corp. HIV Infections December 2007 Phase 2
    NCT02495779 Ronald Stall|Fenway Community Health|National Institute of Mental Health (NIMH)|University of Pittsburgh Human Immunodeficiency Virus July 2015
    NCT02065986 MRC [ycm]|Medical Research Council HIV October 2012 Phase 4
    NCT02285374 St Stephens Aids Trust|ViiV Healthcare HIV November 2014 Phase 4
    NCT02097381 University of Roma La Sapienza|Istituto Superiore di Sanità HIV Infection April 2010
    NCT01772823 Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infection November 2012 Phase 2
    NCT01769456 Westat HIV Infection March 2013 Phase 2
    NCT00949234 University of California, Los Angeles|Los Angeles County Department of Public Health|AIDS Project Los Angeles|Los Angeles LGBT Center|OASIS Clinic HIV Transmission|HIV Infections March 2010 Phase 2
    NCT02904369 CONRAD|United States Agency for International Development (USAID)|Agility Clinical, Inc. HIV October 2016 Phase 1
    NCT01869634 University of California, Davis Human Immunodeficiency Virus Infection June 2013 Phase 4
    NCT00552240 Boehringer Ingelheim HIV Infections September 2007 Phase 4
    NCT01583439 Harvard School of Public Health|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections September 2012
    NCT00757783 Tibotec, Inc|Tibotec Therapeutics, a Division of Ortho Biotech Products, L.P., USA HIV October 2008 Phase 4
    NCT00357552 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections January 2008
    NCT02367807 Philadelphia Fight HIV February 2015
    NCT00090779 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID)|Adult AIDS Clinical Trials Group HIV Infections January 2005 Phase 2
    NCT00936195 French National Agency for Research on AIDS and Viral Hepatitis|Gilead Sciences|Merck Sharp & Dohme Corp.|GlaxoSmithKline|Abbott HIV Infection|Pregnancy|Breastfeeding|HIV Infections January 2010 Phase 3
    NCT02203461 Technische Universität München|Gilead Sciences|MUC Research GmbH Insulin Resistance July 2014 Phase 1
    NCT01033942 University of North Carolina, Chapel Hill|National Institute on Drug Abuse (NIDA)|National Institute of Mental Health (NIMH) HIV August 2009 Phase 2
    NCT01234116 Henry Ford Health System|Merck Sharp & Dohme Corp. Human Immunodeficiency Virus February 2011 Phase 4
    NCT02499874 St Stephens Aids Trust|Mylan Inc. HIV August 2015 Phase 1
    NCT01620944 Bristol-Myers Squibb HIV July 2012 Phase 3
    NCT01154673 University of Toronto|St. Michael's Hospital, Toronto|Maple Leaf Medical Clinic Acute HIV Infection November 2011 Phase 2|Phase 3
    NCT02447016 Sheba Medical Center HIV May 2015 Phase 4
    NCT03048422 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections July 2017 Phase 3
    NCT00120367 French National Agency for Research on AIDS and Viral Hepatitis|Hoffmann-La Roche|Gilead Sciences Leukoencephalopathy, Progressive Multifocal|HIV Infections April 2005 Phase 2
    NCT01641809 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus August 1, 2012 Phase 2
    NCT01450189 William (Bill) C. Miller, MD|University of North Carolina, Chapel Hill HIV October 2011
    NCT00002416 Triangle Pharmaceuticals|NIH AIDS Clinical Trials Information Service HIV Infections Phase 3
    NCT00099632 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections March 2006 Phase 2
    NCT02470650 Juan A. Arnaiz|Hospital Clinic of Barcelona Patient Compliance|Antiretroviral Therapy Intolerance June 2015 Phase 4
    NCT02832778 St Stephens Aids Trust|Mylan Inc.|United States Agency for International Development (USAID) HIV November 21, 2016 Phase 1
    NCT00573001 French National Agency for Research on AIDS and Viral Hepatitis|Institut de Médecine et d'Epidémiologie Appliquée - Fondation Internationale Léon M'Ba|Gilead Sciences|Merck Sharp & Dohme Corp.|French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) HIV Infections July 2008 Phase 3
    NCT01285050 Johns Hopkins University|National Institute on Drug Abuse (NIDA) HIV Infection|Hepatitis C January 2011 Phase 4
    NCT01515813 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection November 2011 Phase 2
    NCT00346567 Rigshospitalet, Denmark|University of Copenhagen HIV Infections June 2006
    NCT02475915 South East Asia Research Collaboration with Hawaii|The Thai Red Cross AIDS Research Centre|Cooper Human Systems Acute HIV Infection January 2015 Phase 1|Phase 2
    NCT00677300 Dallas VA Medical Center|Merck Sharp & Dohme Corp.|Tibotec Pharmaceutical Limited HIV Infections January 2009 Phase 4
    NCT00380159 Achillion Pharmaceuticals HIV-1 Infection September 2006 Phase 2
    NCT00608569 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections March 2009
    NCT00006144 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections October 2000 Phase 2
    NCT00196612 French National Agency for Research on AIDS and Viral Hepatitis|Triangle Pharmaceuticals|Gilead Sciences|Bristol-Myers Squibb|Dupont Applied Biosciences HIV Infections April 2001 Phase 3
    NCT00196599 French National Agency for Research on AIDS and Viral Hepatitis|Triangle Pharmaceuticals|Gilead Sciences|Bristol-Myers Squibb|Dupont Applied Biosciences HIV Infections|Antiretroviral Naive February 1999 Phase 2
    NCT00705419 Merck Sharp & Dohme Corp. HIV Infections July 2007
    NCT00084136 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections May 2005 Phase 4
    NCT00799864 Janssen Sciences Ireland UC Human Immuno Deficiency (HIV) Infection January 7, 2011 Phase 2
    NCT00036452 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 2
    NCT00863668 University of Minnesota - Clinical and Translational Science Institute|Merck Sharp & Dohme Corp. HIV Infection|HIV Infections March 2009
    NCT00055120 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|AIDS-Related Opportunistic Infections March 2003 Phase 4
    NCT01803074 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus April 2013 Phase 2
    NCT00051831 National Institute of Allergy and Infectious Diseases (NIAID)|AIDS Clinical Trials Group HIV Infections October 2003
    NCT02449733 Emory University HIV May 2015
    NCT00089505 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections November 2006 Phase 3
    NCT00537966 University of Zurich HIV Infections January 2002
    NCT01632891 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection|Pf Subclinical Parasitemia July 2013 Phase 1|Phase 2
    NCT01253538 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV April 2011
    NCT01061151 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections March 2011
    NCT00074581 National Institute of Allergy and Infectious Diseases (NIAID)|HIV Prevention Trials Network HIV Infections February 2005 Phase 3
    NCT01352715 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection January 2012 Phase 3
    NCT00102206 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections Phase 2
    NCT01641367 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection October 2012 Phase 4
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 4.0445 mL 20.2224 mL 40.4449 mL
    5 mM 0.8089 mL 4.0445 mL 8.0890 mL
    10 mM 0.4044 mL 2.0222 mL 4.0445 mL
    Cell Assay
    [3]

    EA.hy926 cells were plated in a 12-, 24- or 96-well plates and grown in DMEM media supplemented with 3% FCS. Endothelial cells from PARP+/+and PARP-/- mice were isolated and cultured. Cell viability was determined by the reduction of yellow MTT into a purple formazan product by mitochondrial dehydrogenases of metabolically active cells. Following the treatment period, the experimental medium was removed and 100 μL MTT (1 mg/mL) added. After 1 h incubation, the MTT solution was carefully removed and the purple crystals were solubilized in 100 μL of DMSO. The DMSO was transferred to an ELISA plate and absorbance measured at 550 nm with a 620 nm[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice: Emtricitabine (free base) is suspended in 0.5% aqueous methylcellulose and given by gavage, with the daily dose divided into two equal installments administered approximately 6 h apart. The dose volume is 5 mL/kg/dose (10 mL/kg/day). In 1- and 6-month oral toxicity studies in mice, the maximum tolerated dose of emtricitabine is >3000 mg/kg/day. However, dose-range-finding studies are performed in pregnant CD-1 mice and in New Zealand White rabbits at top doses of 1000 mg/kg/day[2]. Rabbits: Mature artificially inseminated rabbits are given emtricitabine on gestational day 7 through 19. On gestational day 19, blood samples for toxicokinetics are taken from five satellite does in each group at 30–60 min prior to dosing, and at 1, 3, 7, and 12 h after the first daily-dose (prior to the second daily-dose). On gestational day 20, the satellite does are sacrificed at 1 h after the final dose, and maternal blood and fetal umbilical blood samples are collected for toxicokinetics[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

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