1. Anti-infection
    Autophagy
  2. Reverse Transcriptase
    HIV
    Autophagy

Efavirenz (Synonyms: DMP 266; EFV; L-743726)

Cat. No.: HY-10572 Purity: 99.69%
Data Sheet SDS Handling Instructions

Efavirenz is a potent inhibitor of the wild-type HIV-1 RT (Ki=2.93 nM) and exhibits IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.

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Efavirenz Chemical Structure

Efavirenz Chemical Structure

CAS No. : 154598-52-4

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Description

Efavirenz is a potent inhibitor of the wild-type HIV-1 RT (Ki=2.93 nM) and exhibits IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.

IC50 & Target

Ki: 2.93 nM (HIV-1 RT)[1]

In Vitro

Efavirenz (L-743726) is found to be capable of inhibiting, with 95% inhibitory concentrations of ≤ 1.5μM, a panel of nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs)-resistant mutant viruses, each of which expresses a single RT amino acid substitution. Efavirenz is also tested for its activity against a variety of polymerase enzymes and is found to be inactive (IC50>300μM). Efavirenz effectively inhibits several wild-type T-lymphoid cell line-adapted variants. Identical activity (IC95, 1.5 to 3.0 nM) is seen with wild-type primary isolates of the virus in both primary lymphoid and monocytoid cell cultures. Efavirenz also effectively inhibits HIV-1 variants that expressed RT amino acid substitutions which confer the loss of susceptibility to other NNRTIs. For purposes of comparison[1]. Efavirenz is a non-nucleoside analog reverse transcriptase inhibitor (NNRTI) with IC50 of 60 nM[2]. Efavirenz inhibits synthesis using an RNA PPT-primed substrate with an IC50 of 17 nM[3].

In Vivo

After i.v. administration, Efavirenz (L-743726) is cleared rapidly from rats, but it is cleared considerably more slowly from monkeys. The large volume of distribution (two to four times the amount of body water) in both species indicates extensive tissue binding. The oral bioavailability in rats is 16%. In monkeys, the half-life of Efavirenz after administration of a 1 mg/kg i.v. dose exceeded 2.5 h. Efavirenz is well absorbed orally. Administration to monkeys of oral doses as fine suspensions in 0.5% aqueous methylcellulose yields consistently high levels in plasma. A 2.0 mg/kg dose produces peak levels of 0.5μM at approximately 3.0 h. The absolute bioavailability is estimated to be 42%. A 10 mg/kg dose yields a peak level in plasma of 3.22 μM. A 10 mg/kg oral dose given to a single chimpanzee gave concentrations in plasma of 4.12, 2.95, and 2.69 μM at 2, 8, and 24 h after dosing, respectively[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01980342 Johns Hopkins University|American College of Obstetricians and Gynecologists|The Campbell Foundation Drug Interaction October 2014 Phase 4
NCT01087814 University of Minnesota - Clinical and Translational Science Institute HIV|HIV Infections February 2010 Phase 4
NCT00668395 Indiana University HIV May 2007
NCT01704898 Center for Clinical Pharmacology Research Bdbeq S.A.|University of the Republic, Uruguay Healthy April 2013 Phase 4
NCT00299091 Dr . BONAVENTURA CLOTET|Germans Trias i Pujol Hospital HIV September 2006 Phase 4
NCT00533390 Oswaldo Cruz Foundation|Ministry of Health, Brazil Tuberculosis|HIV Infections January 2007 Phase 4
NCT00476424 The HIV Netherlands Australia Thailand Research Collaboration|Ministry of Education, Thailand HIV Infections June 2007 Phase 2
NCT01695954 New York University School of Medicine|Bellevue/NYU AIDS Clinical Trials Unit|Kowa Pharmaceuticals America, Inc.|University at Buffalo Hyperlipidemia|HIV May 2012 Phase 1
NCT00960570 Mutual Pharmaceutical Company, Inc. Healthy February 2008 Phase 1
NCT01878890 Institut Bergonié Solid Tumors|Non-Hodgkin's Lymphoma June 2011 Phase 1
NCT02285374 St Stephens Aids Trust|ViiV Healthcare HIV November 2014 Phase 4
NCT01886404 University of Nebraska HIV Infection December 2013
NCT01098526 GlaxoSmithKline|Shionogi Infections, Human Immunodeficiency Virus and Herpesviridae|Healthy March 2010 Phase 1
NCT02164812 Bristol-Myers Squibb HIV/AIDS July 2014 Phase 1
NCT01989910 Taipei Veterans General Hospital, Taiwan HIV-1 Infection September 2013 Phase 4
NCT00314626 Germans Trias i Pujol Hospital|Fundacio Lluita Contra la SIDA HIV Infections November 2004 Phase 3
NCT01472380 Mutual Pharmaceutical Company, Inc. Healthy November 2011 Phase 1
NCT01147107 University of Hawaii|Hospital for Tropical Diseases, Ho Chi Minh City, Vietnam|Viet Tiep General Hospital, Hai Phong, Vietnam|Oxford University Clinical Research Unit, Vietnam Hepatitis C, Chronic|HIV Infection February 2014 Phase 4
NCT03227653 Radboud University|Kilimanjaro Christian Medical Centre, Tanzania|Kilimanjaro Clinical Research Institute Efavirenz|Child Behavior|Cognitive Symptom|Medication Adherence|Drug-Related Side Effects and Adverse Reactions June 19, 2017
NCT01585038 Indiana University|Janssen Services, LLC Cardiovascular Disease July 2012 Phase 4
NCT00280969 International Medical Center of Japan|Ministry of Health, Labour and Welfare, Japan HIV Infection September 2005 Phase 3
NCT00483054 Bamrasnaradura Infectious Diseases Institute|Mahidol University|Chulalongkorn University HIV Infections|Tuberculosis January 2007 Phase 3
NCT02832778 St Stephens Aids Trust|Mylan Inc.|United States Agency for International Development (USAID) HIV November 21, 2016 Phase 1
NCT00924898 University of North Carolina, Chapel Hill|Bristol-Myers Squibb|Gilead Sciences Acute HIV Infection|HIV Infections January 2005 Phase 4
NCT01541085 Janssen-Cilag S.p.A. Human Immunodeficiency Virus; HIV December 2011 Phase 4
NCT02722421 University of Nebraska|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|Infectious Diseases Institute, Uganda|University of Liverpool|Feinberg School of Medicine, Northwestern University HIV|Contraception April 6, 2017 Phase 2
NCT00364793 Bristol-Myers Squibb HIV Infections February 2007 Phase 1|Phase 2
NCT00620438 Makerere University|Health Research Board, Ireland HIV Infections|Tuberculosis February 2008 Phase 4
NCT01270802 Indiana University|Merck Sharp & Dohme Corp. HIV April 2011 Phase 4
NCT00482963 University of Colorado, Denver|The Miriam Hospital|University of Washington|Bristol-Myers Squibb HIV Infections|Contraception|Pharmacokinetics May 2007 Phase 1
NCT02489461 Viriom HIV-infection August 2014 Phase 2|Phase 3
NCT00162227 Bristol-Myers Squibb HIV Infection September 2000
NCT00162188 Bristol-Myers Squibb HIV Infection May 2001
NCT00792584 University Hospital, Geneva|University of Bern|University of Lausanne Hospitals|Hospital Lugano|University Hospital, Basel, Switzerland|Hospital of Neuchâtel Sleep Disorders November 2008
NCT00556634 Sociedad Andaluza de Enfermedades Infecciosas|Consejeria de Salud. Junta de Andalucia. Spain HIV-1 Infection|HIV Infection April 2006 Phase 4
NCT00023413 Centers for Disease Control and Prevention|VA Office of Research and Development HIV Infections|Tuberculosis November 1999 Phase 2
NCT02499874 St Stephens Aids Trust|Mylan Inc. HIV August 2015 Phase 1
NCT02426866 Bristol-Myers Squibb|Truven health HIV/AIDS December 2014
NCT00944957 University Hospital, Geneva|University of Bern|University of Lausanne Hospitals|Hospital Lugano|University Hospital, Basel, Switzerland|Hospital of Neuchâtel|University Hospital, Zürich Sleep Disorders|HIV Infections November 2009
NCT01011413 Kirby Institute HIV Infections August 2011 Phase 3
NCT01668147 Washington University School of Medicine Drug Effects August 2012
NCT01104376 Indiana University|National Institutes of Health (NIH)|National Institute of General Medical Sciences (NIGMS) Efavirenz, Metabolism and Pharmacokinetics Changes March 2010
NCT00984152 Rush University Medical Center|Merck Sharp & Dohme Corp. HIV-1 Infections June 2011 Phase 3
NCT00474435 African Poverty Related Infection Oriented Research Initiative|Radboud University|Kilimanjaro Christian Medical Centre, Tanzania Tuberculosis|HIV Infections November 2008 Phase 2
NCT01451333 Kirby Institute|Imperial College London HIV Infection September 2011 Phase 3
NCT00775606 Rush University Medical Center|University of Chicago|University of Illinois at Chicago|Ruth M. Rothstein CORE Center|Abbott|Gilead Sciences Acquired Immune Deficiency Syndrome October 2008 Phase 4
NCT02273765 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Merck Sharp & Dohme Corp.|Ministry of Health, Brazil HIV-1 Infection|Tuberculosis September 2015 Phase 3
NCT00357188 Bristol-Myers Squibb HIV Infections|Protease Inhibitor July 2006 Phase 1
NCT00992069 National Institute of Allergy and Infectious Diseases (NIAID) Tuberculosis|HIV December 2009 Phase 1
NCT02421289 Mahidol University Cytochrome P-450 CYP2B6|Efavirenz|HIV April 2013 Phase 1
NCT01194856 The Cleveland Clinic|National Institute of Allergy and Infectious Diseases (NIAID)|Case Western Reserve University|Bristol-Myers Squibb HIV Infection|Mitochondrial Dysfunction October 2010 Phase 4
NCT01268839 Tibotec, Inc|Tibotec Therapeutics, a Division of Ortho Biotech Products, L.P., USA HIV January 2010 Phase 1
NCT00903682 Janssen-Cilag International NV HIV Infection|HIV|Acquired Immunodeficiency Syndrome June 2009 Phase 2
NCT00135343 Bristol-Myers Squibb HIV Infections April 2004 Phase 3
NCT01588002 Hoffmann-La Roche Healthy Volunteer April 2012 Phase 1
NCT00369941 Merck Sharp & Dohme Corp. HIV Infections August 2006 Phase 3
NCT03178084 Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal HIV/AIDS October 15, 2014 Phase 3
NCT00964002 Institut Bergonié|National Cancer Institute (NCI) Prostate Cancer May 2008 Phase 2
NCT00540449 Tibotec Pharmaceuticals, Ireland HIV Infections|HIV-1|Human Immunodeficiency Virus Type 1 May 2008 Phase 3
NCT01044810 Bamrasnaradura Infectious Diseases Institute|Thai Red Cross AIDS Research Centre|Clinical Research Collaborative Network Treatment Failure, HIV or AIDS|CD4 Cell Counts January 2010
NCT00350272 Achillion Pharmaceuticals HIV Infections May 2006 Phase 2
NCT00100568 National Institute of Allergy and Infectious Diseases (NIAID)|Initiative Senegalaise d'Acces aux Antiretroviraux (ISAARV) HIV Infections July 2006
NCT01632345 Merck Sharp & Dohme Corp. HIV Infections October 2012 Phase 2
NCT01241773 Tibotec Pharmaceuticals, Ireland Hepatitis C Virus October 2010 Phase 1
NCT00002225 Dupont Merck|NIH AIDS Clinical Trials Information Service HIV Infections Phase 2
NCT00002227 Dupont Merck|NIH AIDS Clinical Trials Information Service HIV Infections Phase 2
NCT00098293 ViiV Healthcare|Pfizer HIV-1 November 2004 Phase 3
NCT00162097 Bristol-Myers Squibb HIV Infections|Hepatic Impairment November 2004 Phase 1
NCT00802802 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections|Tuberculosis October 2009 Phase 1
NCT00964171 Institut Bergonié|National Cancer Institute (NCI) Pancreatic Cancer August 2008 Phase 2
NCT01935830 Washington University School of Medicine Healthy Volunteers August 2013 Early Phase 1
NCT00495326 French National Agency for Research on AIDS and Viral Hepatitis|Medecins Sans Frontieres, Netherlands Tuberculosis|Aids|Hiv Infections December 2007 Phase 2|Phase 3
NCT00158821 Gilead Sciences HIV Infections March 2000 Phase 3
NCT00828789 Tibotec BVBA Hepatitis C|HCV|HIV|AIDS February 2009 Phase 1
NCT00543725 Tibotec Pharmaceuticals, Ireland HIV Infections|HIV-1 June 2008 Phase 3
NCT02226991 Boehringer Ingelheim Healthy April 2006 Phase 1
NCT01271894 Kirby Institute|Chelsea and Westminster NHS Foundation Trust HIV Infection September 2011 Phase 3
NCT00810303 University Medicine Greifswald Pharmacokinetics|Drug Interactions|Pharmacodynamics|Intestinal Transporter Expression March 2009 Phase 1
NCT00224458 Gilead Sciences HIV Infections September 2004 Phase 4
NCT00399685 Bristol-Myers Squibb HIV Infections December 2006 Phase 1
NCT00000893 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections October 1997 Phase 1
NCT00266058 University of California, San Francisco HIV Infections|Malaria December 2005 Phase 1
NCT00730223 Vanderbilt University HIV Infections March 2004 Phase 1
NCT00004582 ViRx|NIH AIDS Clinical Trials Information Service HIV Infections Phase 2
NCT00862823 University of Alabama at Birmingham|Bristol-Myers Squibb Healthy February 2009 Phase 4
NCT00100594 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections May 2005
NCT00744809 Tibotec Pharmaceuticals, Ireland Human Volunteers August 2008 Phase 1
NCT01900015 Juan Macías|Andaluz Health Service HCV Coinfection|HIV Infection February 3, 2014 Phase 4
NCT01805258 All India Institute of Medical Sciences, New Delhi|National AIDS Control Organisation HIV/TB Co-infection June 2007 Phase 3
NCT00256828 Clinical Trial Agency of HIV Study Group HIV Infections June 2004 Phase 4
NCT00011895 GlaxoSmithKline|NIH AIDS Clinical Trials Information Service HIV Infections February 2001 Phase 4
NCT01837277 Fundação Bahiana de Infectologia Severely Immunocompromised HIV Patients March 2015 Phase 2|Phase 3
NCT00414635 Community Research Initiative of New England|The Campbell Foundation HIV Infections August 2006 Phase 4
NCT00001758 National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) HIV Infection November 1997 Phase 2
NCT00002393 Dupont Merck|NIH AIDS Clinical Trials Information Service HIV Infections Phase 3
NCT00013897 Bristol-Myers Squibb HIV Infections February 2001 Phase 3
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
NCT01516060 Kirby Institute|The HIV Netherlands Australia Thailand Research Collaboration HIV January 2012 Phase 3
NCT02269462 Adeniyi Olagunju|University of Liverpool|Obafemi Awolowo University Teaching Hospital|Obafemi Awolowo University HIV|Pregnancy|Breastfeeding December 2012
NCT00386659 Hospital Clinic of Barcelona HIV Infection Phase 4
NCT00734344 University of Alabama at Birmingham|Merck Sharp & Dohme Corp. Acute HIV Infection September 2008
NCT00002387 Merck Sharp & Dohme Corp.|NIH AIDS Clinical Trials Information Service HIV Infections
NCT02631473 St Stephens Aids Trust|University of Liverpool HIV November 2015 Phase 1
NCT00006208 Triangle Pharmaceuticals|NIH AIDS Clinical Trials Information Service HIV Infections August 2000 Phase 3
NCT00002235 Merck Sharp & Dohme Corp.|Agouron Pharmaceuticals|NIH AIDS Clinical Trials Information Service HIV Infections Phase 2
NCT00053638 GlaxoSmithKline HIV Infection February 2003 Phase 3
NCT00002220 Merck Sharp & Dohme Corp.|NIH AIDS Clinical Trials Information Service HIV Infections Phase 3
NCT01978743 Massachusetts General Hospital|Merck Sharp & Dohme Corp. HIV|HIV-associated Neurocognitive Disorder|Neurotoxicity January 2014 Phase 3
NCT00115609 French National Agency for Research on AIDS and Viral Hepatitis HIV Infections|Tuberculosis January 2006 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
NCT00549198 GlaxoSmithKline Infection, Human Immunodeficiency Virus I|HIV Infection June 2007 Phase 4
NCT00038532 Abbott HIV Infections April 2001 Phase 2
NCT00000903 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 3
NCT00727597 Georgetown University|GlaxoSmithKline Human Immunodeficiency Virus Infections July 2008 Phase 3
NCT00002230 Northwestern University|NIH AIDS Clinical Trials Information Service HIV Infections Phase 3
NCT00017758 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|HIV Seronegativity|Lipodystrophy Phase 1
NCT00002239 Hoffmann-La Roche|Trimeris HIV Infections May 1999 Phase 2
NCT02945163 Shanghai Public Health Clinical Center HIV Infections January 2017 Phase 4
NCT00002419 Gilead Sciences|Glaxo Wellcome|Dupont Applied Biosciences|NIH AIDS Clinical Trials Information Service HIV Infections Phase 2
NCT01180075 University of North Carolina, Chapel Hill|National Institute of Allergy and Infectious Diseases (NIAID) Human Immunodeficiency Virus May 2010
NCT01571414 National Institute of Allergy and Infectious Diseases (NIAID) Tuberculosis May 2012 Phase 1
NCT02777229 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Institut de Recherche pour le Developpement HIV-1 Infection July 2016 Phase 3
NCT00005000 Agouron Pharmaceuticals|NIH AIDS Clinical Trials Information Service HIV Infections December 1999 Phase 4
NCT00822315 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 Infections|Tuberculosis July 2009 Phase 2
NCT00697892 Fran Aweeka|University of California, San Francisco HIV Infections|Malaria July 2005 Phase 1
NCT00112047 Gilead Sciences HIV Infections July 2003 Phase 3
NCT00005762 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections March 2001
NCT00001086 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 2
NCT01709084 Janssen-Cilag International NV Human Immunodeficiency Virus-type 1 Infection October 2, 2013 Phase 3
NCT00001087 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 2
NCT00118898 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections September 2005 Phase 3
NCT00523458 Stanford University HIV Infections|Tuberculosis July 2007 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
NCT00116415 Bristol-Myers Squibb HIV Infections|AIDS March 2002
NCT00116298 Bristol-Myers Squibb HIV Infections|AIDS January 2001 Phase 3
NCT00116116 Bristol-Myers Squibb HIV Infections|AIDS March 2002 Phase 4
NCT02401256 Indiana University|National Institute of General Medical Sciences (NIGMS) Healthy July 2013 Phase 4
NCT00365612 Gilead Sciences|Bristol-Myers Squibb HIV Infections July 2006 Phase 4
NCT03048422 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections July 2017 Phase 3
NCT02632474 Shanghai Public Health Clinical Center HIV Infections April 2015 Phase 4
NCT01387022 Centre for the AIDS Programme of Research in South Africa Antiretroviral Treatment Outcomes June 2011
NCT00001766 National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) HIV Infection August 1998 Phase 1
NCT00002213 Glaxo Wellcome|NIH AIDS Clinical Trials Information Service HIV Infections Phase 2
NCT00075231 Abbott HIV Infections December 2003 Phase 2
NCT01014481 Bamrasnaradura Infectious Diseases Institute|Mahidol University|Thai Red Cross AIDS Research Centre HIV Infections|Tuberculosis October 2009 Phase 4
NCT00038220 Abbott HIV Infections July 2000 Phase 2
NCT00002234 Gilead Sciences|Bristol-Myers Squibb|Glaxo Wellcome|Dupont Applied Biosciences HIV Infections Phase 2
NCT01318096 Yunnan AIDS Care Center HBV Coinfection|HIV Infections March 2011
NCT01293123 University of California, San Diego|Merck Sharp & Dohme Corp. HIV December 2011
NCT00005017 Glaxo Wellcome|NIH AIDS Clinical Trials Information Service HIV Infections Phase 4
NCT02547844 Hospital Universitari Vall d'Hebron Research Institute|Gilead Sciences HIV-1 September 2015 Phase 4
NCT01192035 University of Aarhus|Aarhus University Hospital Skejby|Bandim Health Project|Ministry of Health, Guinea-Bissau|Abbott HIV-1 May 2011 Phase 4
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
NCT01789879 University of Nebraska|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|Makerere University|University of Liverpool HIV|Contraception June 2013 Phase 2
NCT00946595 French National Agency for Research on AIDS and Viral Hepatitis|Abbott|Gilead Sciences|French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) HIV Infections November 2009 Phase 2|Phase 3
NCT00433719 University of Oxford|Wellcome Trust HIV Infections|Tuberculous Meningitis September 2005
NCT00121017 Abbott HIV Infection|Hepatitis C Phase 2
NCT00335322 Kirby Institute|The University of New South Wales Human Immunodeficiency Virus (HIV) February 2007 Phase 4
NCT01641016 PENTA Foundation|Medical Research Council|French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) HIV April 2011 Phase 2|Phase 3
NCT00005018 Glaxo Wellcome|NIH AIDS Clinical Trials Information Service HIV Infections July 1999 Phase 4
NCT01075152 University of Minnesota - Clinical and Translational Science Institute|Mbarara University of Science and Technology|Makerere University|National Institute of Allergy and Infectious Diseases (NIAID)|University of Cape Town Cryptococcal Meningitis|HIV Infections|AIDS November 2010 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
NCT00004585 Glaxo Wellcome|NIH AIDS Clinical Trials Information Service HIV Infections October 1999 Phase 4
NCT00023218 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|Hepatitis C
NCT00792324 St Stephens Aids Trust HIV June 2008 Phase 3
NCT01340950 University of California, San Diego|National Institute of Mental Health (NIMH)|National Center for AIDS/STD Control and Prevention, China CDC|Beijing YouAn Hospital|Beijing Ditan Hospital|Peking University HIV Infections|Central Nervous System Diseases|Dementia July 2010 Phase 4
NCT00966160 University of Cologne Acquired Immunodeficiency Syndrome|HIV Infections January 1999 Phase 3
NCT00870363 University of California, Davis HIV Infections April 2009 Phase 4
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
NCT01187862 University Hospital, Basel, Switzerland Cytochrome|Pharmacokinetics July 2010 Phase 1
NCT00661960 University of California, Davis HIV Infections|AIDS March 2008
NCT00002448 Hoffmann-La Roche|NIH AIDS Clinical Trials Information Service HIV Infections October 1999 Phase 3
NCT00002447 Hoffmann-La Roche|NIH AIDS Clinical Trials Information Service HIV Infections October 1999 Phase 3
NCT02935075 Shanghai Public Health Clinical Center HIV Infections January 2017 Phase 4
NCT00004852 Glaxo Wellcome|NIH AIDS Clinical Trials Information Service HIV Infections September 1999 Phase 2
NCT00525239 National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) HIV Infections March 2004
NCT01445223 Göteborg University HIV April 2004 Phase 4
NCT00344760 University of Maryland HIV Infections January 2005 Phase 4
NCT01489046 Bristol-Myers Squibb HIV-1 Infection February 2011 Phase 2
NCT00127972 International Antiviral Therapy Evaluation Center|Boehringer Ingelheim HIV Infections February 2004 Phase 4
NCT00640887 French National Agency for Research on AIDS and Viral Hepatitis HIV Infections|Tuberculosis February 2009 Phase 2
NCT00532168 Juan A. Arnaiz|Hospital Clinic of Barcelona HIV Infections September 2007 Phase 4
NCT01231555 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus November 2010 Phase 2
NCT01352117 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection|Kaposi's Sarcoma October 2011 Phase 3
NCT00332306 Tuberculosis Research Centre, India|National AIDS Control Organisation|Indian Council of Medical Research Tuberculosis|Human Immunodeficiency Virus Infections June 2006 Phase 3
NCT00120510 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|Tuberculosis July 2007
NCT01618305 Westat|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections July 2013 Phase 4
NCT00951015 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus July 30, 2009 Phase 2
NCT00442962 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections May 2007 Phase 4
NCT01277627 Valme University Hospital|Boehringer Ingelheim HCV Infection.|HCV Viral Load. January 2011
NCT00100048 Merck Sharp & Dohme Corp. HIV Infections|Acquired Immunodeficiency Syndrome January 2005 Phase 2
NCT01146873 Columbia University|University of Witwatersrand, South Africa|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV/AIDS|HIV Infections July 2010 Phase 3
NCT00545558 University of Cincinnati|National Institute of Allergy and Infectious Diseases (NIAID) Hepatitis C|HIV Infections April 2006 Phase 1
NCT00018083 National Center for Research Resources (NCRR)|Centers for Disease Control and Prevention Tuberculosis|HIV Infections
NCT01583439 Harvard School of Public Health|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections September 2012
NCT00002362 Triangle Pharmaceuticals|NIH AIDS Clinical Trials Information Service HIV Infections August 1999 Phase 3
NCT00000912 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections 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
NCT01903031 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection November 2014 Phase 2
NCT00050895 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 3
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
NCT00192595 Kirby Institute|The University of New South Wales|Gilead Sciences HIV Infection|Hepatitis B Coinfection January 2004 Phase 4
NCT01641809 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus August 1, 2012 Phase 2
NCT00836212 University Hospital, Geneva|Swiss HIV Cohort Study Human Immunodeficiency Virus|HIV Infections March 2008 Phase 4
NCT00878306 University of California, San Francisco|National Institute on Drug Abuse (NIDA) HIV Infections|Drug Abuse November 2008 Phase 1
NCT00135369 Bristol-Myers Squibb HIV Infections September 2002 Phase 3
NCT02404259 The HIV Netherlands Australia Thailand Research Collaboration|Chulalongkorn University|Khon Kaen University HIV June 2010
NCT00000939 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 2
NCT00342355 National Institutes of Health Clinical Center (CC) HIV January 2004 Phase 4
NCT00110305 Tibotec Pharmaceuticals, Ireland Human Immunodeficiency Virus Type 1 June 2005 Phase 2
NCT00863668 University of Minnesota - Clinical and Translational Science Institute|Merck Sharp & Dohme Corp. HIV Infection|HIV Infections March 2009
NCT00000914 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections
NCT00005918 Bristol-Myers Squibb HIV Infections June 2000 Phase 3
NCT00016601 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections June 2001
NCT00006190 National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) HIV Infections|Lipodystrophy November 2000 Phase 4
NCT01515813 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection November 2011 Phase 2
NCT00162643 Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran|National Council of Science and Technology, Mexico|Instituto Mexicano del Seguro Social Acquired Immunodeficiency Syndrome December 2004 Phase 4
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
NCT02057796 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) HIV-1 Infection September 2014 Phase 4
NCT00158470 French National Agency for Research on AIDS and Viral Hepatitis HIV Infection September 2003 Phase 3
NCT02447016 Sheba Medical Center HIV May 2015 Phase 4
NCT01516970 Janssen-Cilag G.m.b.H Human Immunodeficiency Virus (HIV) November 25, 2011 Phase 3
NCT00260078 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections February 2006 Phase 1|Phase 2
NCT00122538 French National Agency for Research on AIDS and Viral Hepatitis HIV Infections|AIDS February 2006 Phase 2
NCT00000919 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections
NCT00000918 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 2
NCT00075907 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections July 2004 Phase 3
NCT00001122 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 2
NCT00000885 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 2
NCT00091936 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|Tuberculosis August 2009
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
NCT00084136 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections May 2005 Phase 4
NCT00021463 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|Lipodystrophy Phase 2
NCT00476606 The HIV Netherlands Australia Thailand Research Collaboration|Khon Kaen University HIV Infections March 2003
NCT01254656 Pfizer|ViiV Healthcare HIV-1 February 2011 Phase 2
NCT00127959 International Antiviral Therapy Evaluation Center|Gilead Sciences HIV Infections|Hepatitis B March 2004 Phase 4
NCT01040091 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections December 2009 Phase 1
NCT00028327 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 3
NCT00042289 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
NCT00993031 University of California, San Francisco|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) Malaria|HIV Infections December 2009 Phase 3
NCT00307502 Germans Trias i Pujol Hospital|Fundacio Lluita Contra la SIDA HIV Infections January 2005 Phase 1
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
NCT00234091 National Institute of Allergy and Infectious Diseases (NIAID)|Comprehensive International Program of Research on AIDS HIV Infections April 2006 Phase 3
NCT00031070 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 2
NCT01380080 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infection October 2011 Phase 4
NCT00051090 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|Hepatitis B
NCT00014937 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections
NCT00013520 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 3
NCT00006154 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 3
NCT00074581 National Institute of Allergy and Infectious Diseases (NIAID)|HIV Prevention Trials Network HIV Infections February 2005 Phase 3
NCT00102960 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections July 2005 Phase 3
NCT00197613 Harvard School of Public Health|Princess Marina Hospital, Botswana|Botswana Ministry of Health|McGill University Health Center|Bristol-Myers Squibb AIDS|HIV Infection December 2002 Phase 3
NCT00158405 French National Agency for Research on AIDS and Viral Hepatitis|Bristol-Myers Squibb HIV Infections December 2002 Phase 3
NCT00100581 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|Hepatitis C
NCT00427297 University of Washington|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections September 2007 Phase 3
NCT00255840 CIPRA SA|National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections July 2006
NCT00000922 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections
NCT00080522 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections February 2005
NCT00001119 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections October 1999
NCT00192660 Kirby Institute|St Vincent's Hospital, Sydney|National Heart, Lung, and Blood Institute (NHLBI) HIV-Associated Lipodystrophy Syndrome|Cardiovascular Disease February 2003 Phase 4
NCT00643968 Gilead Sciences HIV Infections March 2003 Phase 4
NCT00978237 Juan A. Arnaiz|Hospital Clinic of Barcelona HIV Infections|Lipoatrophy October 2009 Phase 4
NCT02345226 Gilead Sciences HIV-1 Infection January 27, 2015 Phase 3
NCT01160120 The HIV Netherlands Australia Thailand Research Collaboration|Mylan Laboratories HIV June 2010 Phase 2
NCT01751555 National Center for AIDS/STD Control and Prevention, China CDC|Gilead Sciences Hiv February 2011 Phase 4
NCT02178592 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus January 1, 2015 Phase 3
NCT02253823 Boehringer Ingelheim Healthy December 2001 Phase 1
NCT01844297 Peking Union Medical College AIDS/HIV PROBLEM May 2013
NCT02415595 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus May 12, 2015 Phase 2
NCT01309243 Gilead Sciences HIV-1 Infection February 2011 Phase 3
NCT01127204 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|European and Developing Countries Clinical Trials Partnership (EDCTP)|Public Research Centre Health, Luxembourg|Ministry of Foreign Affairs, Luxembourg|University of Ouagadougou, Burkina Faso|Programme national,ANRS,Coopération française-Côte d'Ivoire (PAC-CI), Côte d'Ivoire|Ministry of Health, Rwanda|Institut National de la Santé Et de la Recherche Médicale, France|University of Bordeaux|Institut de Sante Publique, d'Epidémiologie et de Développement|Université Montpellier|University of Paris 5 - Rene Descartes|Queen Fabiola Children's University Hospital HIV Infections June 2011 Phase 2|Phase 3
NCT00615745 Gilead Sciences HIV Infections April 2008 Phase 4
NCT01529749 Felipe Garcia|Hospital Clinic of Barcelona HIV-1 Infection February 2012 Phase 4
NCT00978068 University of California, San Francisco|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) Malaria|HIV Infections September 2009 Phase 3
NCT02750059 South East Asia Research Collaboration with Hawaii|National Institute of Neurological Disorders and Stroke (NINDS) Acute HIV Infection|HIV CNS Involvement January 2015 Phase 2
NCT02827643 Mahidol University Bone Density June 2016
NCT01344148 Shanghai Public Health Clinical Center AIDS February 2009
NCT01403051 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection September 2011 Phase 2
NCT01509508 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Africa Centre For Health and Population Studies, South Africa|University of KwaZulu HIV Infection March 2012
NCT01565889 Gilead Sciences Hepatitis C|HIV March 2012 Phase 1|Phase 2
NCT00454337 French National Agency for Research on AIDS and Viral Hepatitis|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 May 2007 Phase 3
NCT01435018 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID)|National Cancer Institute (NCI)|National Institute of Dental and Craniofacial Research (NIDCR) HIV-1 Infection August 2013 Phase 3
NCT00039741 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|PENTA Foundation HIV Infections August 2002 Phase 2|Phase 3
NCT00385957 Hospital Clinic of Barcelona HIV Infections Phase 4
NCT01815736 Gilead Sciences HIV|HIV Infections March 27, 2013 Phase 3
NCT01714414 Michael Hoelscher|European and Developing Countries Clinical Trials Partnership (EDCTP)|German Federal Ministry of Education and Research|National Institute for Medical Research, Tanzania|Treichville Academic hospital center, Division of infectious and tropical diseases (SMIT)|French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Kumasi Centre for Collaborative Research (KCCR)|Bernhard Nocht Institute for Tropical Medicine|Pharmaceutical Company (Chiracon GmbH)|Pharmaceutical Company (STADA Vietnam Joint Venture Co. Ltd.)|Ludwig-Maximilians - University of Munich HIV-1 Infection December 2012 Phase 2
NCT00824421 Pfizer HIV-1 February 2009 Phase 2
NCT02284035 Juan A. Arnaiz|Hospital Clinic of Barcelona AIDS January 2015 Phase 3
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 3.1678 mL 15.8388 mL 31.6776 mL
5 mM 0.6336 mL 3.1678 mL 6.3355 mL
10 mM 0.3168 mL 1.5839 mL 3.1678 mL
Kinase Assay
[1]

Recombinant RT enzymes are expressed, purified, and assessed for inhibition by Efavirenz (L-743726). Ki and Kii values are determined for each enzyme tested. The wild-type RT exhibited exclusively noncompetitive inhibition kinetics (data not shown), and, therefore, the Ki and Kii values are identical. Pure noncompetitive inhibition is not assumed for the mutant enzymes, and, hence, the values of both Ki and Kii are obtained from the linear mixed-type inhibition equation. The two- to threefold differences between the Ki and Kii values probably reflect a small contribution of competitive inhibition with the mutant RTs[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Efavirenz (L-743726) is prepared in 0.5% aqueous methylcellulose (Mice)[1].

Mice[1]
Studies are performed in rats, rhesus monkeys, and a single chimpanzee. For analyses of the drug given to rats intravenously (i.v.), a group (n=4 or 5) of fasted male Sprague-Dawley rats (weight, 250 to 450 g) receive a bolus (at a volume of 1mL/kg of body weight) of Efavirenz in DMSO via a cannula implanted in the right jugular vein. For oral studies, rats are dosed by gavage by using a suspension of Efavirenz prepared in 0.5% aqueous methylcellulose. Similarly, four monkeys receive either an i.v. bolus of the compound in DMSO via the saphenous vein at a volume of 0.1 mL/kg or are administered the compound orally in suspension by using a nasogastric tube. Monkeys are fasted for 18 h prior to dosing. One nonanesthetized, nonfasted male chimpanzee (weight, approximately 60 kg) is dosed orally by voluntary ingestion by using an aqueous suspension of the compound. In all studies, heparinized blood is obtained at appropriate times. Plasma is separated immediately by centrifugation and is stored at -20°C until analysis. Plasma samples are extracted with methylene chloride; this is followed by analysis by high-performance liquid chromatography. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
M.Wt

315.68

Formula

C₁₄H₉ClF₃NO₂

CAS No.

154598-52-4

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 38 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.69%

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Efavirenz
Cat. No.:
HY-10572
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