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Efavirenz (Sustiva/Strocrin)
 
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General/Miscellaneous Reports
 
 
A Study of the Binding Energies of Efavirenz to Wild-Type and K103N/Y181C HIV-1 Reverse
Transcriptase Based on the ONIOM Method.
 Srivab P, Hannongbua S. 
ChemMedChem. 2008 Mar 12
Abstract
 
Energetic effects for observed and unobserved HIV-1 reverse transcriptase mutations of
residues L100, V106, and Y181 in the presence of nevirapine and efavirenz.
 Kroeger Smith MB, Rader LH, et al   
Bioorg Med Chem Lett. 2007 Dec 23
Abstract
 
Intracellular Efavirenz Levels in Peripheral Blood Mononuclear Cells from HIV-Infected
Individuals.
 Tanaka R, Hanabusa H, Kinai E, et al 
Antimicrob Agents Chemother. 2007 Dec 10
Abstract
 
Efavirenz Accelerates HIV-1 Reverse Transcriptase Ribonuclease H Cleavage Leading to Diminished
Zidovudine Excision.
 Radzio J, Sluis-Cremer N
 Mol Pharmacol. 2007 Nov 16;
Abstract
 
Bioequivalence of Efavirenz/Emtricitabine/Tenofovir Disoproxil Fumarate Single-Tablet Regimen.
 Mathias AA, Hinkle J, Menning M, et al 
J Acquir Immune Defic Syndr. 2007 Jul 19;
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Efavirenz: a review.
 Vrouenraets SM, Wit FW, van Tongeren J, Lange JM.
Expert Opin Pharmacother. 2007 Apr;8(6):851-71.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Multilocus genetic interactions and response to efavirenz-containing regimens: an Adult AIDS Clinical
Trials Group study.
 Motsinger AA, Ritchie MD, Shafer RW, et al  
Pharmacogenet Genomics. 2006 Nov;16(11):837-845.
 Abstract
 
The use of the non-nucleoside reverse transcriptase inhibitors nevirapine and efavirenz
in the treatment of patients with a chronic HIV-I infection
 van Leth F, Lange JM. 
Ned Tijdschr Geneeskd. 2006 Aug 5;150(31):1719-22
 Abstract
 
Metabolism of efavirenz and 8-hydroxyefavirenz by P450 2B6 leads to inactivation by two distinct
mechanisms.
 Bumpus NN, Kent UM, Hollenberg PF
 J Pharmacol Exp Ther. 2006 Apr 12;
Abstract
 
Effects of Efavirenz Binding on the Subunit Equilibria of HIV-1 Reverse Transcriptase.
 Venezia CF, Howard KJ, Ignatov ME, et al 
Biochemistry. 2006 Mar 7;45(9):2779-89.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Pharmacogenetics of Long-Term Responses to Antiretroviral Regimens Containing Efavirenz
and/or Nelfinavir: An Adult AIDS Clinical Trials Group Study.
 Haas DW, Smeaton LM, Shafer RW,
Infect Dis. 2005 Dec 1;192(11):1931-42.
 Abstract
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Pharmacokinetics
       
 
High prevalence of the CYP2B6 516G-->T(*6) variant and effect on the population pharmacokinetics
of efavirenz in HIV/AIDS outpatients in Zimbabwe.
 Nyakutira C, Röshammar D, Chigutsa E, et al 
Eur J Clin Pharmacol. 2007 Dec 5
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Multiple-Dose Pharmacokinetics of Efavirenz with and without the Use of Rifampicin in
HIV-Positive Patients.
 Matteelli A, Regazzi M, Villani P, et al
Curr HIV Res. 2007 May;5(3):349-53.
 Abstract
 
Predictive Value of Known and Novel Alleles of CYP2B6 for Efavirenz Plasma Concentrations
in HIV-infected Individuals.
 Rotger M, Tegude H, Colombo S, et al 
Clin Pharmacol Ther. 2007 Jan 18;
Abstract
 
Efavirenz in Plasma from HIV-Infected Patients Does Not Directly Block Reverse Transcriptase
Activity in Cell-Free Assays But Inhibits HIV Replication in Cellular Assays.
 Burrer R, Spiridon G, Einius-Haessig S, et al 
AIDS Res Hum Retroviruses. 2006 Sep;22(9):865-9.
 Abstract
 
Ritonavir, Saquinavir and Efavirenz, but not Nevirapine, Inhibit Bile Acid Transport in Human
and Rat Hepatocytes.
 McRae MP, Lowe CM, Tian X  ,et al
J Pharmacol Exp Ther. 2006 May 23;
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
 Interpatient variability in the pharmacokinetics of the HIV non-nucleoside reverse transcriptase inhibitor |
efavirenz: the effect of gender, race, and CYP2B6 polymorphism.
 Burger D, van der Heiden I, la Porte C, et al
Br J Clin Pharmacol. 2006 Feb;61(2):148-54
 Abstract

ntracellular and plasma pharmacokinetics of efavirenz in HIV-infected individuals.
 Almond LM, Hoggard PG, Edirisinghe D, et al  
J Antimicrob Chemother. 2005 Sep 1;
 Abstract
 
Pharmacokinetics of nelfinavir and efavirenz in antiretroviral-naive, human immunodeficiency
virus-infected subjects when administered alone or in combination with nucleoside analog
reverse transcriptase inhibitors.
 Smith PF, Robbins GK, Shafer RW, et al
Antimicrob Agents Chemother. 2005 Aug;49(8):3558-61.
 Abstract
 
Amprenavir and Efavirenz Pharmacokinetics before and after the Addition of Nelfinavir,
Indinavir, Ritonavir, or Saquinavir in Seronegative Individuals.
 Morse GD, Rosenkranz S, Para MF 
Antimicrob Agents Chemother. 2005 Aug;49(8):3373-8
 Abstract
.
Population Pharmacokinetics of Efavirenz in an Unselected Cohort of HIV-1-Infected
Individuals.
 Kappelhoff BS, Huitema AD, Yalvac Z,   
Clin Pharmacokinet. 2005;44(8):849-61.
 Abstract
 
Quantum study of mutational effect in binding of efavirenz to HIV-1 RT.
 Mei Y, He X, Xiang Y, Zhang DW, Zhang JZ.
Proteins. 2005 Mar 23;
 Abstract
 
Efavirenz enhances the proteolytic processing of an HIV-1 pol polyprotein precursor
and reverse transcriptase homodimer formation.
 Tachedjian G, Moore KL, Goff SP, Sluis-Cremer N  .
FEBS Lett. 2005 Jan 17;579(2):379-384
 Abstract
 
Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS
Clinical Trials Group study.
 Haas DW, Ribaudo HJ, Kim RB, et al
AIDS. 2004 Dec 3;18(18):2391-2400.
 Abstract
 
Homozygous CYP2B6 *6 (Q172H and K262R) correlates with high plasma efavirenz
concentrations in HIV-1 patients treated with standard efavirenz-containing regimens.
 Tsuchiya K, Gatanaga H, Tachikawa N, et al 
Biochem Biophys Res Commun. 2004 Jul 9;319(4):1322-6.
 Abstract

The cytochrome P450 2B6 is the main catalyst of efavirenz primary and secondary
metabolism:implication for HIV/AIDS therapy and utility of efavirenz as substrate marker
of CYP2B6 catalytic activity.
Ward BA, Gorski CJ, Jones DR, et al.
J Pharmacol Exp Ther 2003 Apr 3;I
 Abstract

Population pharmacokinetics and effects of efavirenz in patients with human
immunodeficiency virus infection.
Csajka C, Marzolini C, Fattinger K, et al.
 Clin Pharmacol Ther 2003 Jan;73(1):20-30
 Abstract

Population Pharmacokinetics and Pharmacodynamics of Efavirenz, Nelfinavir, and
Indinavir: Adult AIDS Clinical Trial Group Study 398.
 Pfister M, Labbe L, Hammer SM, et al.
Antimicrob Agents Chemother 2003 Jan;47(1):130-137
 Abstract

  
Drug/Drug Interactions
 
 
Pharmacokinetic interaction between efavirenz and dual protease inhibitors in healthy volunteers.
 Ma Q, Forrest A, Rosenkranz SL, et al  
Biopharm Drug Dispos. 2007 Nov 27;29(2):91-101
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Outcomes of dosage adjustments used to manage antiretroviral drug interactions.
 Park-Wyllie LY, Levine MA, Holbrook A, et al
Clin Infect Dis. 2007 Oct 1;45(7):933-6.
 Abstract
 
Drug-drug interaction between itraconazole and efavirenz in a patient with AIDS and
disseminated histoplasmosis.
 Koo HL, Hamill RJ, Andrade RA.
Clin Infect Dis. 2007 Sep 15;45(6):e77-9
 Abstract
 
Pharmacokinetic interaction between TMC114/r and efavirenz in healthy volunteers.
 Sekar VJ, De Pauw M, Mariën K,   et al
Antivir Ther. 2007;12(4):509-14
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Effect of efavirenz on the pharmacokinetics of ketoconazole in HIV-infected patients.
 Sriwiriyajan S, Mahatthanatrakul W, Ridtitid W, Jaruratanasirikul S.
Eur J Clin Pharmacol. 2007 Mar 8
 Abstract
 
Assessment of Drug-Drug Interactions Between Tenofovir Disoproxil Fumarate and the
Nonnucleoside Reverse Transcriptase Inhibitors Nevirapine and Efavirenz in HIV-Infected Patients.
 Droste JA, Kearney BP, Hekster YA, Burger DM.
 J Acquir Immune Defic Syndr. 2006 Jan 1;41(1):37-43.
 Abstract
 
Evaluation of the Drug Interaction Between Rifabutin and Efavirenz in Patients with HIV Infection
and Tuberculosis.
 Weiner M, Benator D, Peloquin CA, et al 
Clin Infect Dis. 2005 Nov 1;41(9):1343-9.
Abstract
 
Effect of Efavirenz on the Pharmacokinetics of Simvastatin, Atorvastatin, and Pravastatin:
Results of AIDS Clinical Trials Group 5108 Study.
 Gerber JG, Rosenkranz SL, Fichtenbaum CJ, et al 
J Acquir Immune Defic Syndr. 2005 Jul 1;39(3):307-312.
Abstract
 
Effects of Valproic Acid Coadministration on Plasma Efavirenz and Lopinavir
Concentrations in Human Immunodeficiency Virus-Infected Adults.
 Dicenzo R, Peterson D, Cruttenden K, et al 
Antimicrob Agents Chemother. 2004 Nov;48(11):4328-433
 Abstract
 
Safety and Antiretroviral Effectiveness of Concomitant Use of Rifampicin and
Efavirenz for Antiretroviral-Naive Patients in India Who Are Coinfected With Tuberculosis
and HIV-1.
 Patel A, Patel K, Patel J, et al   
J Acquir Immune Defic Syndr. 2004 Sep 1;37(1):1166-1169.
 Abstract

The Pharmacokinetics of Methadone in HIV Positive Patients Receiving the
Non-nucleoside Reverse Transcriptase Inhibitor Efavirenz
Susan M Clarke, Fiona M Mulcahy, John Tjia, et al.
Br J Clin Pharm 2001:51:3:213-218
 Abstract

 FULL-TEXT ARTICLE
 Selective interaction of the human immunodeficiency virus type 1 reverse transcriptase
nonnucleoside inhibitor efavirenz and its thio-substituted analog with different enzyme-
substrate complexes.
Maga G, Ubiali D, Salvetti R, et al.  
 Antimicrob Agents Chemother 2000 May;44(5):1186-1194
 Paper

 		 
Viral Dynamics
          
 
A WEEK-IN-REVIEW FEATURED REPORT
 Racial differences in virologic failure associated with adherence and quality of life on
efavirenz-containing regimens for initial HIV therapy: results of ACTG A5095.
 Schackman BR, Ribaudo HJ, Krambrink A, et al
J Acquir Immune Defic Syndr. 2007 Dec 15;46(5):547-54.
 Abstract

Predictors of Residual Viremia in HIV-Infected Patients Successfully Treated
with Efavirenz and Lamivudine plus either Tenofovir or Stavudine.
Havlir DV, Koelsch KK, Strain MC, et al 
J Infect Dis. 2005 Apr 1;191(7):1164-8.
 Abstract
 
Predictors of virologic failure and resistance in HIV-infected patients treated with
nevirapine- or efavirenz-based antiretroviral therapy.
 Parienti JJ, Massari V, Descamps D, et al
Clin Infect Dis. 2004 May 1;38(9):1311-6.
 Abstract
 
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Clinical, Virologic, and Immunologic Response to Efavirenz-or Protease
Inhibitor-Based Highly Active Antiretroviral Therapy in a Cohort of Antiretroviral-Naive
Patients With Advanced HIV Infection (EfaVIP 2 Study).
 The EfaVIP Cohort Study Group.
J Acquir Immune Defic Syndr. 2004 Apr 20;35(4):343-350.
 Abstract
 
Resistance
          
 
Preexisting Resistance to Nonnucleoside Reverse-Transcriptase Inhibitors Predicts Virologic
Failure of an Efavirenz-Based Regimen in Treatment-Naive HIV-1-Infected Subjects.
 Kuritzkes DR, Lalama CM, Ribaudo HJ, et al
 J Infect Dis. 2008 Feb 12
 Abstract
 
Comparison of genotypic resistance profiles and virological response between patients
starting nevirapine and efavirenz in EuroSIDA.
 Bannister WP, Ruiz L, Cozzi-Lepri A, et al  
AIDS. 2008 Jan 30;22(3):367-76
 Abstract
 
Relative replication fitness of efavirenz-resistant mutants of HIV-1: Correlation with frequency
during clinical therapy and evidence of compensation for the reduced fitness of K103N + L100I
by the nucleoside resistance mutation L74V.
 Koval CE, Dykes C, Wang J, Demeter LM.   
Virology. 2006 Jun 20;
 Abstract
 
Genotypic and phenotypic resistance patterns at virological failure in a simplification trial with
nevirapine, efavirenz or abacavir.
 de Echaguen AO, Arnedo M, Xercavins M, et al
AIDS. 2005 Sep 2;19(13):1385-1391.
Abstract
 
The efavirenz-induced increase in HDL-cholesterol is influenced by the multidrug
resistance  gene 1 C3435T polymorphism.
 Alonso-Villaverde C, Coll B, Gomez F, et al 
AIDS. 2005 Feb 18;19(3):341-2.
 Abstract
 
Mutations in HIV-1 Reverse Transcriptase Potentially Associated with
Hypersusceptibility to  Nonnucleoside Reverse-Transcriptase Inhibitors: Effect on
Response to Efavirenz-Based Therapy in an Urban Observational Cohort.
 Tozzi V, Zaccarelli M, Narciso P, et al
J Infect Dis. 2004 May 1;189(9):1688-95
 Abstract

Development of drug resistance in HIV-1 patients receiving a combination of s
tavudine, lamivudine and efavirenz.
Re MC, Monari P, Bon I, et al  
Int J Antimicrob Agents 2002 Sep;20(3):223
 Abstract

Resistance profile and cross-resistance of HIV-1 among patients failing a
non-nucleoside reverse transcriptase inhibitor-containing regimen.
Delaugerre C, Rohban R, Simon A. et al.  
 J Med Virol 2001  Nov;65(3):445-8
Abstract

FULL-TEXT ARTICLE
 Human immunodeficiency virus type 1 mutations selected in patients failing efavirenz
combination therapy.
Bacheler LT, Anton ED, Kudish P, Baker D. et al
Antimicrob Agents Chemother 2000 Sep;44(9):2475-2484
 Paper

 
Diagnostics/Drug Monitoring
 
 
Determination of abacavir, amprenavir, didanosine, efavirenz, nevirapine, and stavudine concentration
in human plasma by MALDI-TOF/TOF.
 Notari S, Mancone C, Alonzi T, et al  
J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Jan 16
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Intra-Individual Variability in Efavirenz Plasma Concentrations Supports Therapeutic
Drug Monitoring Based on Quarterly Sampling in the First Year of Therapy.
 Pereira SA, Branco T, Caixas U, et al
Ther Drug Monit. 2008 Feb;30(1):60-66
 Abstract
 
A WEEK IN REVIEW FEATURED  REPORT
Efavirenz and Nevirapine in HIV-1 Infection : Is There a Role for Clinical Pharmacokinetic
Monitoring?
 Dahri K, Ensom MH. 
Clin Pharmacokinet. 2007;46(2):109-32.
 Abstract

Efavirenz and nevirapine plasma levels in HIV-infected patients with hemophilia.
 Martorell M, Lopez RM, Ribera E
Enferm Infecc Microbiol Clin. 2005 Jun;23(6):349-5
 Abstract
 
Efavirenz Plasma Concentrations in HIV-Infected Patients: Inter- and Intraindividual Variability
and Clinical Effects.
 Stahle L, Moberg L, Svensson JO, Sonnerborg A.
Ther Drug Monit. 2004 Jun;26(3):267-270.
 Abstract

Diagnostics
 
  Development of a competitive immunoassay for efavirenz: Hapten design and validation
studies.
 Roucairol C, Azoulay S, Nevers MC, et al
Anal Chim Acta. 2007 Apr 18;589(1):142-9.
 Abstract
 
Efavirenz and nevirapine plasma levels in HIV-infected patients with hemophilia.
 Martorell M, Lopez RM, Ribera E
Enferm Infecc Microbiol Clin. 2005 Jun;23(6):349-5
 Abstract
 
Recreational substance use and tolerance of efavirenz in HIV-1 infected patients.
 Faggian F, Lattuada E, Lanzafame M, et al 
AIDS Care. 2005 Oct;17(7):908-910.
 Abstract
 

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Efavirenz: Journal Papers, Abstracts, and Commentaries