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Efavirenz
(Sustiva/Strocrin)
 
Pediatric Data

General Reports
Pharmacokinetics
Viral Dynamics
Resistance
Adverse Events
Efficacy
Treatment Strategies
 

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Last Update:  November 29, 2017
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General Reports
 

Journal Papers, Abstracts, and Commentaries

 
CYP2B6 Genotype-directed dosing is required for optimal efavirenz exposure in children 3 to 36 months with HIV infection.
Moore CB, Capparelli EV, Samson P, et al
AIDS
. 2017 Mar 18
Abstract

FULL-TEXT ARTICLE
Weekends-off efavirenz-based antiretroviral therapy in HIV-infected children, adolescents, and young adults (BREATHER): a randomised, open-label, non-inferiority, phase 2/3 trial.
BREATHER (PENTA 16) Trial Group.
Lancet HIV. 2016 Sep;3(9):e421-30
Paper

FULL-TEXT ARTICLE
Antiretroviral treatment in HIV-1 infected pediatric patients: focus on efavirenz.
Larru B, Eby J, Lowenthal ED.
Pediatric Health Med Ther. 2014 May 29;5:29-42
Paper

Are lopinavir and efavirenz serum concentrations in HIV-infected children in the therapeutic range in clinical practice?
von Bibra M, Rosenkranz B, Pretorius E,  et al
Paediatr Int Child Health
. 2013 Sep 2
Abstract

Middosing interval efavirenz plasma concentrations in HIV-1 infected children in Rwanda: treatment efficacy, tolerability, adherence and the influence of CYP2B6 polymorphisms.
Mutwa PR, Fillekes Q, Malgaz M, et al
J Acquir Immune Defic Syndr. 2012 Apr 4.
Abstract

Plasma Efavirenz in HIV Infected Children Treated with Generic Antiretroviral Drugs in India.
Ramachandran G, Kumar AH, Vasantha M,  et al
Indian Pediatr
. 2010 Oct 7;47(10):890-1.
Abstract

Efavirenz Plasma Concentrations at 1, 3, and 6 Months Post-Antiretroviral Therapy Initiation in HIV Type 1-Infected South African Children.
Viljoen M, Gous H, Kruger HS, et al
AIDS Res Hum Retroviruses
. 2010 May 27.
Abstract

Efavirenz-loaded polymeric micelles for pediatric anti-HIV pharmacotherapy with significantly higher oral bioavailaibility.
Chiappetta DA, Hocht C, Taira C, Sosnik A.
Nanomed
. 2010 Jan;5(1):11-23
Abstract


Are recommended dose of efavirenz optimal in young West African HIV-infected children?
(ANRS 12103).

Hirt D, Urien S, Olivier M, Peyrière H, et al
Antimicrob Agents Chemother. 2009 Jul 27
Abstract

High Prevalence of Subtherapeutic Plasma Concentrations of Efavirenz in Children.
Ren Y, Nuttall JJ, Egbers C, et al  
J Acquir Immune Defic Syndr.
2007 Apr 5;

Abstract
 

Conference Reports, Abstracts, and Posters
 
 
Equivalence of boosted atazanavir based regimens and currently effective HAART regimens with other PI's/NNRTI's in HIV+ children and adolescents with elevated lipid levels
J. Piatt, J. Foti, K. Bickes, et al
(XX International AIDS Conference)
Abstract

The predictability of NONMEM generated clearance values of efavirenz in South African children using CYP2B6 516 G>T polymorphism versus haplotype combinations (CYP2B6 515 G>T; 785 A>G and 983T>C) as covariates
M. Rheeders, R. Reay, M. Viljoen, C. Dandara
(XX International AIDS Conference)
Abstract

Plasma efavirenz concentrations in HIV-infected children in Thailand: comparison between FDA and WHO 2010 dosing guidelines
N. Homkham S. Urien, T.R. Cressey, et al
7th IAS Conference on HIV Pathogenesis, Treatment and Prevention)
Abstract

Using WHO 2010 dosing guidelines, efavirenz levels remain slightly lower and highly variable in Ugandan/Zambian children weighing 10-< 20kg
Q. Fillekes, E. Kaudha, V. Korutaro, et al
(XIX International AIDS Conference)
Abstract


Pharmacokinetics
 

Journal Papers, Abstracts, and Commentaries
 
 
Pharmacokinetics of Efavirenz in 2-3 years old children: a high dose of 25 mg/kg per day.
Pressiat C, Amorissani-Folquet M, Yonaba C,
Antimicrob Agents Chemother. 2017 May 8. p
Abstract

FULL-TEXT ARTICLE
Population Pharmacokinetics Analysis to Inform Efavirenz Dosing Recommendations in Pediatric HIV Patients Aged 3 Months to 3 Years.
Luo M, Chapel S, Sevinsky H, et al
Antimicrob Agents Chemother
. 2016 Apr 11.
Paper

The impact of genetic polymorphisms on the pharmacokinetics of efavirenz in African children.
Bienczak A, Cook A, Wiesner L, Olagunju A, et al
Br J Clin Pharmacol
. 2016 Mar 16.
Abstract

A Population Pharmacokinetic/Pharmacodynamic Model Predicts Favorable HDL Cholesterol Changes Over the First 5 Years in Children Treated with Current Efavirenz-Based Regimens.
Homkham N, Cressey TR, Ingsrisawang L,  et al
 
J Clin Pharmacol
. 2016 Jan 8.
Abstract

The Effect of Malnutrition on the Pharmacokinetics and Virologic Outcomes of Lopinavir, Efavirenz and Nevirapine in Food Insecure HIV-infected Children in Tororo, Uganda.
Bartelink IH, Savic RM, Dorsey G,  et al
Pediatr Infect Dis J. 2015 Mar;34(3):e63-e70.
Abstract

Pharmacometric Characterization of Efavirenz Developmental Pharmacokinetics and Pharmacogenetics in Human Immunodeficiency Virus Infected Children.
S
alem AH, Fletcher CV, Brundage RC.
Antimicrob Agents Chemother. 2013 Oct 21
Abstract

Pediatric under-dosing of efavirenz: a pharmacokinetic study in Uganda.
Fillekes Q, Natukunda E, Balungi J,  et al
J Acquir Immune Defic Syndr. 2011 Sep 15
Abstract

A pharmacokinetic and pharmacogenetic study of efavirenz in children: dosing guidelines can result in subtherapeutic concentrations.
ter Heine R, Scherpbier HJ, Crommentuyn KM, et al

Antivir Ther. 2008;13(6):779-8
Abstract

Pharmacokinetics and Pharmacodynamics of Efavirenz and Nelfinavir in HIV-infected Children Participating in an Area-under-the-curve Controlled Trial.
Fletcher CV, Brundage RC, Fenton T, et al 
Clin Pharmacol Ther.
2007 Jul 4;

Abstract

Conference Reports, Abstracts, and Posters

 
Population pharmacokinetics of efavirenz in HIV-1-positive Thai children
N. Homkham. Urien, T.R. Cressey, et al
(XIX International AIDS Conference)
Abstract

Viral Dynamics
 

Journal Papers, Abstracts, Letters, and Commentaries

  Plasma efavirenz exposure, sex, and age predict virological response in HIV-infected African children.
Bienczak A, Denti P, Cook A, et al
J Acquir Immune Defic Syndr
. 2016 Apr 21.
Abstract

The Effect of Malnutrition on the Pharmacokinetics and Virologic Outcomes of Lopinavir, Efavirenz and Nevirapine in Food Insecure HIV-infected Children in Tororo, Uganda.
Bartelink IH, Savic RM, Dorsey G,  et al
Pediatr Infect Dis J. 2015 Mar;34(3):e63-e70.
Abstract

Patterns of plasma human immunodeficiency virus type 1 RNA response to highly active antiretroviral therapy in infected children.
Spector SA, Yong FH, Cabral S et al.

Journal of Infectious Disease
2000; 182(6): 1769-1773.

Abstract


Resistance
 

Journal Papers, Abstracts, Letters, and Commentaries

  Drug Resistance Profiles among HIV-1 Infected Children Experiencing Delayed Switch and 12-months Efficacy after Using Second-line Antiretroviral Therapy: An Observational Cohort Study in Rural China.
Zhao Y, Mu W, Harwell J,  et al
J Acquir Immune Defic Syndr
. 2011 Jun 30

Abstract

Adverse Events
 

Journal Papers, Abstracts, Letters, and Commentaries

  Efavirenz is associated with higher bone mass in South African children with HIV.
Arpadi SM, Shiau S, Strehlau R,  et al
AIDS
. 2016 Jul 16.
Abstract

FULL-TEXT PDF ARTICLE
Efavirenz-induced gynecomastia in a prepubertal girl with human immunodeficiency virus infection: a case report.
van Ramshorst MS, Kekana M, Struthers HE, et al
BMC Pediatr. 2013 Aug 13;13(1):120
Paper

FULL-TEXT ARTICLE
Efavirenz poisoning in a 12 year old HIV negative African boy
Nazziwa R, Sekadde M, Kanyike F, et al
Pan Afr Med J
. 2012;12:86.

Paper

Absence Seizures Associated With Efavirenz Initiation.
Strehlau R, Martens L, Coovadia A,  et al
Pediatr Infect Dis J. 2011 May 31.
Abstract

Psychosis in a 12-year-old HIV-positive girl with an increased serum concentration of efavirenz.
Lowenhaupt EA, Matson K, Qureishi B,et al  
Clin Infect Dis.
2007 Nov 15;45(10):e128-30.

Abstract
 


Efficacy
 

Journal Papers, Abstracts, Letters, and Commentaries
 
 
Virologic Response to First-line Efavirenz- or Nevirapine-based Antiretroviral Therapy in HIV-infected African Children.
Kekitiinwa A, Szubert AJ, Spyer M,  et al
Pediatr Infect Dis J. 2017 Jun;36(6):588-59
Abstract

Efavirenz-Based Antiretroviral Therapy Among Nevirapine-Exposed HIV-Infected Children in South Africa: A Randomized Clinical Trial.
Coovadia A, Abrams EJ, Strehlau R,  et aj
JAMA
. 2015 Nov 3;314(17):1808-17.
Abstract

Efavirenz Capsule Sprinkle and Liquid Formulations with Didanosine and Emtricitabine in HIV-1-Infected Infants and Children 3 Months to 6 Years of Age: Study AI266-922.
Pavia-Ruz N, Rossouw M, Sáez-Llorens X,  et al
Pediatr Infect Dis J. 2015 Sep 15.
Abstract

Association between efavirenz-based compared with nevirapine-based antiretroviral regimens and virological failure in HIV-infected children.
Lowenthal ED, Ellenberg JH, Machine E,  et al
JAMA
. 2013 May 1;309(17):1803-9.
Abstract

Efficacy and tolerability of nevirapine- versus efavirenz-containing regimens in HIV-infected Thai children.
Lapphra K, Vanprapar N, Chearskul S, et al
Int J Infect Dis. 2008 Jun 21.
Abstract
 

Antiviral efficacy, tolerability and pharmacokinetics of efavirenz in an unselected cohort of HIV-infected children.
Wintergerst U, Hoffmann F, Jansson A, et al 
J Antimicrob Chemother. 2
008 Mar 13
Abstract
 
Once-Daily Highly Active Antiretroviral Therapy for HIV-Infected Children: Safety and Efficacy of an Efavirenz-Containing Regimen.
Scherpbier HJ, Bekker V, Pajkrt D, et al 
Pediatrics. 2007 Feb 16;
Abstract
 
Effect of First Line Therapy Including Efavirenz and Two Nucleoside Reverse Transcriptase Inhibitors in HIV-infected Children.
Funk MB, Notheis G, Schuster T, et al 
Eur J Med Res. 2005 Dec 7;10(12):503-8.
Abstract
 
Safety and efficacy of a NRTI-sparing HAART regimen of efavirenz and lopinavir/ritonavir in HIV-1-infected children.
Fraaij PL, Neubert J, Bergshoeff AS
Antivir Ther.
2004 Apr;9(2):297-9
Letter

FULL-TEXT ARTICLE
Impact of Protease Inhibitor Substitution With Efavirenz in HIV-Infected Children: Results of the First Pediatric Switch Study.
McComsey G, Bhumbra N, Ma JF, et al 

Pediatrics
2003 Mar;111(3):E275-E281

Paper

Combination therapy with efavirenz, nelfinavir, and nucleoside reverse- transcriptase inhibitors in children infected with human immunodeficiency virus type 1.
Pediatric AIDS Clinical Trials Group 382 Team. Starr SE, Fletcher CV, et al.
New England Journal of Medicine 1999; 341(25): 1874-881.
Abstract
 

 
Conference Reports, Abstracts, and Posters
 
 
Two-year treatment outcomes of efavirenz-based first line regimen among South African children genotyped for CYP2B6 516G>T polymorphism
M. Viljoen, M. Rheeders, T.M. Meye,, et al
(XIX International AIDS Conference)
Abstract

Treatment Strategies
 

General Reports
 
Journal Papers, Abstracts, Letters, and Commentaries
 
  Weekends-off efavirenz-based antiretroviral therapy in HIV-infected children, adolescents, and young adults (BREATHER): a randomised, open-label, non-inferiority, phase 2/3 trial.
BREATHER (PENTA 16) Trial Group.
Lancet HIV. 2016 Sep;3(9):e421-30.

Abstract

Switching Therapies

Journal Papers, Abstracts, Letters, and Commentaries
 
 

 

 

Discontinuation of Efavirenz in Paediatric Patients: Why do Children Switch?
Wynberg E, Williams E, Tudor-Williams G, et al
Clin Drug Investig. 2017 Nov 27.
Abstract

Switching to efavirenz versus remaining on ritonavir-boosted lopinavir in HIV-infected children exposed to nevirapine: long-term outcomes of a randomized trial.
Murnane PM, Strehlau R, Shiau S, et al
Clin Infect
Dis
. 2017 Apr 17
Abstract

Long-term body composition and metabolic changes in HIV-infected children switched from stavudine to tenofovir and from protease inhibitors to efavirenz.
Fabiano V, Giacomet V, Viganò A, et al
Eur J Pediatr
. 2013 May 1.
Abstract

Conference Reports, Abstracts, and Posters

  Substitutions to initial antiretroviral therapy in children in South Africa: the international epidemiologic databases to evaluate AIDS, Southern Africa (IeDEA-SA) Collaboration
L. Kampiire, D. Garone, J. Giddy, et al_
(XIX International AIDS Conference)
Abstract

 

HIV/TB Coinfection
 
Journal Papers, Abstracts, Letters, and Commentaries
 
 

 

Effects of rifampin-based antituberculosis therapy on plasma efavirenz concentrations in children vary by CYP2B6 genotype.
McIlleron HM, Schomaker M, Ren Y, et al
AIDS. 2013 Jul 31;27(12):1933-40.
Abstract

FULL-TEXT ARTICLE
Effectiveness of Efavirenz-Based Regimens in Young HIV-Infected Children Treated for Tuberculosis: A Treatment Option for Resource-Limited Settings.
van Dijk JH, Sutcliffe CG, Hamangaba F,  et al
PLoS One
. 2013;8(1):e55111.
Paper

Serum Nevirapine and Efavirenz Concentrations and Effect of Concomitant Use of Rifampicin in HIV Infected Children on Antiretroviral Therapy.
Shah I, Swaminathan S, Ramachandran G, et al
Indian Pediatr
. 2011 Mar 15.
Abstract

Effect of Rifampicin on Efavirenz Pharmacokinetics in HIV-Infected Children With Tuberculosis.
Ren Y, Nuttall JJ, Eley BS, et al
J Acquir Immune Defic Syndr. 2009 Feb 13.
Abstract

Conference Reports, Abstracts, and Posters
 

  Effectiveness of EFV-based ART regimens in young children requiring TB/HIV co-treatment: a possible treatment option for resource-limited settings
J.H. van Dijk, C.G. Sutcliffe, F. Hamangaba. et al
(XIX International AIDS Conference)
Abstract

Examining the effect of rfampicin and CYP2B6 genotype on efavirenz auto-induction and exposure in Tanzanian HIV patients with and without tuberculosis: a prospective comparative study
E. Ngaimisi, S. Mugusi, O.M.S. Minzi, et al
(XIX International AIDS Conference)
Abstract


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 Efavirenz Pediatric Data