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Nelfinavir (Viracept)
 
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General Reports
Formulations
 Pharmacokinetics
 Viral Dynamics
 Drug/Drug Interactions
 Adverse Events
 Resistance
 Efficacy


 
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Last Update:  May 02, 2008
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General/Miscellaneous Reports
 
 
FULL TEXT ARTICLE
 Rate limiting steps in hepatic drug clearance: comparison of hepatocellular uptake and
metabolism with microsomal metabolism of saquinavir, nelfinavir and ritonavir.
 Parker A, Houston JB.
Drug Metab Dispos. 2008 Apr 21
Paper
 
HIV-1 Protease Inhibitors Nelfinavir and Atazanavir Induce Malignant Glioma Death
by Triggering Endoplasmic Reticulum Stress.
Pyrko P, Kardosh A, Wang W, et al 
Cancer Res. 2007 Nov 15;67(22):10920-10928
Abstract
 
Nelfinavir monotherapy increases naive T-cell numbers in HIV-negative healthy young adults.
Vlahakis SR, Tangalos EG, McClees MD, et al 
Front Biosci. 2008 Jan 1;13:1605-9.
 Abstract
 
Nelfinavir, A Lead HIV Protease Inhibitor, Is a Broad-Spectrum, Anticancer Agent that Induces
Endoplasmic Reticulum Stress, Autophagy, and Apoptosis In vitro and In vivo.
Gills JJ, Lopiccolo J, Tsurutani J, et al
Clin Cancer Res. 2007 Sep 1;13(17):5183-94
 Abstract
 
The HIV protease inhibitor nelfinavir downregulates Akt phosphorylation by inhibiting
proteasomal activity and inducing the unfolded protein response.
Gupta AK, Li B, Cerniglia GJ, Ahmed MS, et al
Neoplasia. 2007 Apr;9(4):271-8.
Abstract
 
HIV Protease Inhibitor Nelfinavir Inhibits Growth of Human Melanoma Cells by Induction of
Cell Cycle Arrest.
Jiang W, Mikochik PJ, Ra JH, et al  
Cancer Res. 2007 Feb 1;67(3):1221-7
 Abstract
 
Nelfinavir induces liposarcoma apoptosis and cell cycle arrest by upregulating sterol regulatory
element binding protein-1.
Chow WA, Guo S, Valdes-Albini F.   
Anticancer Drugs. 2006 Sep;17(8):891-903.
 Abstract
 
A review of nelfinavir for the treatment of HIV infection.
Olmo M, Podzamczer D.
Expert Opin Drug Metab Toxicol. 2006 Apr;2(2):285-300.
 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
Formulations
           
 
Assessment of the bioequivalence of two nelfinavir tablet formulations under fed and fasted
conditions in healthy subjects.
Kaeser B, Charoin JE, Gerber M, et al    
Int J Clin Pharmacol Ther. 2005 Mar;43(3):154-62.
 Abstract

Comparison of gastrointestinal tolerability and patient preference for treatment with the
625 mg and 250 mg nelfinavir tablet formulations.
Johnson M, Nieto-Cisneros L, Horban A, et al 
HIV Med. 2005 Mar;6(2):107-13.
 Abstract
Pharmacokinetics  
           
 
A WEEK-IN-REVIEW FEATURED REPORT
Pharmacokinetics of nelfinavir in subjects with hepatic impairment.
Damle B, Hewlett D Jr, Hsyu PH, et al
J Clin Pharmacol. 2006 Nov;46(11):1241-9.
 Abstract
 
Pharmacokinetics of nelfinavir in HIV-1-infected pregnant and nonpregnant women.
Villani P, Floridia M, Pirillo MF, et al 
Br J Clin Pharmacol. 2006 Sep;62(3):309-15
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Population pharmacokinetic analysis for nelfinavir and its metabolite M8 in virologically controlled
HIV-infected patients on HAART.
Panhard X, Goujard C, Legrand M, et al
Br J Clin Pharmacol. 2005 Oct;60(4):390-403.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
 The long-term pharmacokinetics and safety of adding low-dose ritonavir to a nelfinavir 1250 mg
twice-daily regimen in HIV-infected patient
ts.Justesen US, Hansen IM, Andersen AB, et al
HIV Med. 2005 Sep;6(5):334-40
 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
 
Role of P-Glycoprotein in Distribution of Nelfinavir across the Blood-Mammary Tissue
Barrier and Blood-Brain Barrier.
Edwards JE, Alcorn J, Savolainen J,et al
J.Antimicrob Agents Chemother. 2005 Apr;49(4):1626-
 Abstract
 
Nelfinavir Induces Necrosis of 3T3F44-2A Adipocytes by Oxidative Stress.
Vincent S, Tourniaire F, El Yazidi CM, et al
 2004 Dec 15;37(5):1556-1562.
 Abstract
 
Effect of efavirenz treatment on the pharmacokinetics of nelfinavir boosted by
ritonavir in healthy volunteers.
la Porte CJ, de Graaff-Teulen MJ, et al 
Br J Clin Pharmacol. 2004 Dec;58(6):632-640.
 Abstract
 
Conversion of the HIV protease inhibitor nelfinavir to a bioactive metabolite by
humanliver CYP2C19.
Hirani VN, Raucy JL, Lasker JM. 
Drug Metab Dispos. 2004 Sep 24
 Abstract

Ritonavir-Enhanced Pharmacokinetics of Nelfinavir/M8 During Rifampin Use.
 Bergshoeff AS, Wolfs TF, Geelen SP, Burger DM.
Ann Pharmacother 2003 Apr;37(4):521-525
 Abstract

Pharmacokinetics, food intake requirements and tolerability of once-daily combinations
of nelfinavir and low-dose ritonavir in healthy volunteers.
Aarnoutse RE, Droste JA, Van Oosterhout JJ, et al
Br J Clin Pharmacol 2003 Feb;55(2):115-125
 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

Model-based Analysis of the Pharmacokinetic Interactions Between Ritonavir,
Nelfinavir, and Saquinavir after Simultaneous and Staggered
Oral Administration.
Lu JF, Blaschke TF, Flexner C, et al
Drug Metab Dispos 2002 Dec;30(12):1455-61
 Abstract
 
The effects of cannabinoids on the pharmacokinetics of indinavir and nelfinavir.
 Kosel BW, Aweeka FT,Benowitz NL, et al.
AIDS 2002 Mar 8;16(4):543-50
 Abstract
 
Pharmacokinetic Interactions between Nelfinavir and 3-Hydroxy-3-Methylglutaryl
Coenzyme A Reductase Inhibitors Atorvastatin and Simvastatin.
Hsyu PH, Schultz-Smith MD, Lillibridge JH, et al.
Antimicrob Agents Chemother 2001 Dec;45(12):3445-50
Abstract
 
Nelfinavir suspension obtained from nelfinavir tablets has equivalent pharmacokinetic
profile.
 Regazzi MB, Seminari E, Villani P , et al 
J Chemother 2001 Oct;13(5):569-74
Abstract
 
FULL-TEXT ARTICLE
 A population pharmacokinetic analysis of nelfinavir mesylate in human
immunodeficiency virus-infected patients enrolled in a phase III clinical trial.
Jackson KA, Rosenbaum SE, Kerr BM, et al..
Antimicrob Agents Chemother 2000 Jul;44(7):1832-1837
 Paper

 
Viral Dynamics
 
 
Baseline HIV-1 RNA Level and CD4 Cell Count Predict Time to Loss of Virologic
Response to Nelfinavir, but Not Lopinavir/Ritonavir, in Antiretroviral Therapy-Naive
Patients.
King MS, Bernstein BM, Walmsley SL, et al 
J Infect Dis. 2004 Jul 15;190(2):280-
 Abstract

FULL-TEXT PDF ARTICLE
 Differences in the detection of three HIV-1 protease inhibitors in  non-blood
compartments:clinical correlations.
 Lafeuillade A, Solas C, Halfon P, et al.
 HIV Clin Trials 2002 Jan-Feb;3(1):27-35
 PDF Paper
Drug/Drug Interactions
 
 
A WEEK-IN-REVIEW FEATURED REPORT
Clinical evaluation of the nelfinavir-rifabutin interaction in patients with tuberculosis and
human immunodeficiency virus infection.
Benator DA, Weiner MH, Burman WJ, et al
Pharmacotherapy. 2007 Jun;27(6):793-800.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Clinical and pharmacokinetic interactions between methadone and nelfinavir (Nemesia study).
Marco A, Deig E, Cadafalch J, et al
Med Clin (Barc). 2006 Jun 10;127(2):47-50
 Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Carbamazepine Toxicity Induced by Lopinavir/Ritonavir and Nelfinavir (June).
Bates DE, Herman RJ. 
Ann Pharmacother. 2006 May 23;
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Pharmacokinetic interaction between nelfinavir and pravastatin in HIV-seronegative
 volunteers:ACTG Study A5108.
Aberg JA, Rosenkranz SL, Fichtenbaum CJ,et al 
AIDS. 2006 Mar 21;20(5):725-729.
Abstract
 
Lack of pharmacokinetic drug interaction between tenofovir disoproxil fumarate and
nelfinavir mesylate.
Boffito M, Pozniak A, Kearney BP, et al 
Antimicrob Agents Chemother. 2005 Oct;49(10):4386-9.
 Abstract

Sildenafil does not alter nelfinavir pharmacokinetics.
Bratt G, Stahle L.
 Ther Drug Monit 2003 Apr;25(2):240-2
 Abstract

Pharmacokinetics, food intake requirements and tolerability of once-daily
combinations of nelfinavir and low-dose ritonavir in healthy volunteers.
 Aarnoutse RE, Droste JA, Van Oosterhout JJ, et al
Br J Clin Pharmacol 2003 Feb;55(2):115-125
 Abstract

Simvastatin-nelfinavir interaction implicated in rhabdomyolysis and death.
Hare CB, Vu MP, Grunfeld C, Lampiris HW. 
Clin Infect Dis 2002 Nov 15;35(10):e111-2
 Abstract

  

Pharmacokinetic Interactions between Nelfinavir and 3-Hydroxy-3-thylglutaryl
Coenzyme A Reductase Inhibitors Atorvastatin and Simvastatin.
Hsyu PH, Schultz-Smith MD, Lillibridge JH, et al.
Antimicrob Agents Chemother 2001 Dec;45(12):3445-50
Abstract

Adverse Events
 
 
A WEEK-IN-REVIEW FEATURED REPORT
Long-Term Body Fat Outcomes in Antiretroviral-Naive Participants Randomized to Nelfinavir
or Efavirenz or Both Plus Dual Nucleosides: Dual X-Ray Absorptiometry Results From A5005s,
a Substudy of Adult Clinical Trials Group 384.
Dubé MP, Komarow L, Mulligan K, et al
 J Acquir Immune Defic Syndr. 2007 Jun 21;
 Abstract
 
Incidence of and risk factors for severe hepatotoxicity of nelfinavir-containing regimens
among HIV-infected patients with chronic hepatitis C.
Mira JA, Macias J, Giron-Gonzalez JA, et al
 J Antimicrob Chemother. 2006 May 23;
 Abstract
 
Glucose metabolism, lipid, and body fat changes in antiretroviral-naive subjects
randomized to nelfinavir or efavirenz plus dual nucleosides.
Dube MP, Parker RA, Tebas P, et al 
AIDS. 2005 Nov 4;19(16):1807-1818.
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
 Liver injury and changes in hepatitis C Virus (HCV) RNA load associated with
protease inhibitor-based antiretroviral therapy for treatment-naive HCV-HIV-coinfected
patients: lopinavir-ritonavir versus nelfinavir.
Sherman KE, Shire NJ, Cernohous P, et al  Clin Infect Dis. 2005 Oct 15;41(8):1186-95.
 Abstract
 
Differences in rates of diarrhea in patients with human immunodeficiency virus
receiving lopinavir-ritonavir or nelfinavir.
Guest JL, Ruffin C, Tschampa JM, et al 
Pharmacotherapy. 2004 Jun;24(6):727-35.
Abstract
 
Nelfinavir-induced insulin resistance is associated with impaired plasma membrane
recruitment
of the PI 3-kinase effectors Akt/PKB and PKC-zeta.
Ben-Romano R, Rudich A, Tirosh A, et al 
Diabetologia. 2004 May 28
 Abstract

The use of calcium carbonate in nelfinavir-associated diarrhoea in HIV-1-infected
patients.
Jensen-Fangel S, Justesen US, Black FT, et al
HIV Med 2003 Jan;4(1):48-52
 Abstract

High concentrations of nelfinavir as an independent risk factor for lipodystrophy in
human immunodeficiency virus-infected patients.
Treluyer JM, Morini JP, Dimet J, et al. 
 Antimicrob Agents Chemother 2002 Dec;46(12):4009-12
 Abstract

FULL-TEXT ARTICLE                
Suppression of preadipocyte differentiation and promotion of  adipocyte death  by HIV
protease inhibitors.
 Dowell P, Flexner C, Kwiterovich PO, Lane MD. 
J Biol Chem 2000 Dec 29;275(52):41325-32
 Paper 

 
Resistance
 
 
Co-evolution of nelfinavir-resistant HIV-1 protease and the p1-p6 substrate.
Kolli M, Lastere S, Schiffer CA. 
Virology. 2006 Jan 19;
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
FULL-TEXT ARTICLE
 HIV-1 genotypes related to failure of nelfinavir as the first protease inhibitor treatment.
Tupinambas U, Aleixo A, Greco D.
Braz J Infect Dis. 2005 Aug;9(4):324-9.
 Paper
 
Diverse pattern of protease inhibitor resistance mutations in HIV-1 infected patients failing nelfinavir.
Svedhem V, Lindkvist A, Bergroth T, et al  
J Med Virol. 2005 Jun 23;76(4):447-451
Abstract
 
Relationship between Adherence and the Development of Resistance in Antiretroviral-
Naive, HIV-1-Infected Patients Receiving Lopinavir/Ritonavir or Nelfinavir.
King MS, Brun SC, Kempf DJ.
Infect Dis. 2005 Jun 15;191(12):2046-52.
Abstract
 
HIV-1 genotype resistance pattern and evolution in patients failing nelfinavir-containing
regimens.
Quiros-Roldan E, Moretti F, et al 
J Clin Lab Anal. 2005 Jan 11;19(1):26-29
 Abstract
 

Primary nelfinavir (NFV)-associated resistance mutations during a follow-up period of
108 weeks in protease inhibitor naive patients treated with NFV-containing regimens in
an HIV clinic cohort.
Tsuchiya K, Matsuoka-Aizawa S, Yasuoka A, 
J Clin Virol. 2003 Aug;27(3):252-262.
Abstract

Drug resistance mutations and outcome of second-line treatment in patients with
first-line protease inhibitor failure on nelfinavir-containing
HAART.
Roge BT, Katzenstein TL, Nielsen HL, Gerstoft J.
HIV Med 2003 Jan;4(1):38-47
Abstract

Drug resistance mutations and outcome of second-line treatment in patients with
first-line protease inhibitor failure on nelfinavir-containing HAART.
Roge BT, Katzenstein TL, Nielsen HL, Gerstoft J.
HIV Med 2003 Jan;4(1):38-47
 Abstract

Resistance mutations in HIV-infected patients experiencing early failure with nelfinavir-
containing triple combinations.
Nunez M, Mendoza C, Valer L, et al.
Med Sci Monit 2002 Sep;8(9):CR620-3
 Abstract

 Plasma drug levels, genotypic resistance, and virological response to  a nelfinavir plus s
aquinavir-containing regimen.
Casado JL, Moreno S, Hertogs K, et al.
AIDS 2002 Jan 4;16(1):47-52
 Abstract

  
Efficacy
 
HIV
 
 
Comparison of the effectiveness of initial combined antiretroviral therapy with nelfinavir or
efavirenz at a university-based outpatient service in Brazil.
 Vanni T, Morejón KM, Santana RC, et al 
Braz J Med Biol Res. 2007 Jul;40(7):963-9.
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Efficacy of nelfinavir-based treatment in the central nervous system of HIV-1 infected patients.
Karlstrom O, Stahle L, Perrin L, et al 
Scand J Infect Dis. 2006 May;38(5):371-374
 Abstract
 
Efficacy, Tolerability and Pharmacokinetics of Two Nelfinavir-Based Regimens in Human
Immunodeficiency Virus-Infected Children and Adolescents: Pediatric AIDS Clinical Trials
Group Protocol 403.
King JR, Nachman S, Yogev R, et al 
Pediatr Infect Dis J. 2005 Oct;24(10):880-885.
 Abstract
 
Efficacy, Tolerability and Pharmacokinetics of Two Nelfinavir-Based Regimens in
Human Immunodeficiency Virus-Infected Children and Adolescents: Pediatric AIDS
Clinical Trials Group Protocol 403.
King JR, Nachman S, Yogev R, et al 
Pediatr Infect Dis J. 2005 Oct;24(10):880-885.
 Abstract
 
Therapeutic drug monitoring of nelfinavir and indinavir in treatment-naive HIV-1-
infected individuals.
 Burger D, Hugen P, Reiss P, et al.
AIDS. 2003 May 23;17(8):1157-1165.
Abstract

Coadministration of Indinavir and Nelfinavir in Human Immunodeficiency Virus Type 1-
Infected Adults: Safety, Pharmacokinetics, and Antiretroviral Activity.
 Riddler SA, Havlir D, Squires KE, et al.
Antimicrob Agents Chemother 2002 Dec;46(12):3877-3882
 Abstract

Modulation of Human Immunodeficiency Virus (HIV)-Specific Immune Response by
Using Efavirenz, Nelfinavir, and Stavudine in a Rescue T herapy Regimen for
HIV-Infected, Drug-Experienced Patients.
Trabattoni D, Lo Caputo S, Biasin M, et al.
Clin Diagn Lab Immunol 2002 Sep;9(5):1114-8
 Abstract
 
Nelfinavir plasma levels under twice-daily and three-times-daily regimens: high
interpatient and low intrapatient variability.
 Marzolini C, Buclin T, Decosterd LA, et al
Ther Drug Monit   2001 Aug;23(4):394-398
 Abstract
 
Stable or increasing bone mineral density in HIV-infected patients treated with
nelfinavir or indinavir.
Nolan D, Upton R, McKinnon E, et al.
AIDS 2001 Jul 6;15(10):1275-1280
 Abstract
 
The effect of nevirapine in combination with nelfinavir in heavily pretreated
HIV-1-infected patients: a  prospective, open-label, controlled, randomized study.
Jensen-Fangel S, Thomsen HF, Larsen L, Black FT, Obel N
J  Acquir Immune Defic Syndr 2001 Jun 1;27(2):124-129
Abstract
 
Short-term measures of relative efficacy predict longer-term reductions in human
immunodeficiency virus type 1 RNA levels following nelfinavir monotherapy.
Mittler J,  Essunger P, Yuen GJ, et al.
Antimicrob Agents Chemother 2001 May;45(5):1438-1443
 Abstract
 

    HIV Treatment Strategies
 


 		 A comparison of the effects of nevirapine and nelfinavir on metabolism and body
habitus in antiretroviral-naive human immunodeficiency virus-infected patients: a
randomized controlled study.
 Fisac C, Virgili N, Ferrer E, et al 
J Clin Endocrinol Metab. 2003 Nov;88(11):5186-92
 Abstract

     HIV Treatment Failure
 

  Treatment failure of nelfinavir-containing triple therapy can largely be explained by low
nelfinavir plasma concentrations.
Burger DM, Hugen PW, Aarnoutse RE, et al.
Ther Drug Monit 2003 Feb;25(1):73-80
 Abstract		  

HIV/HCV

 
Safety, efficacy, and tolerability of nelfinavir-containing antiretroviral therapy for patients
coinfected with HIV and hepatitis C undergoing methadone maintenance.
Brown LS Jr, Kritz S, Chu M, Madray C.  
J Subst Abuse Treat. 2006 Jun;30(4):331-5.
Abstract

Clinical Pharmacokinetics of Nelfinavir and Its Metabolite M8 in Human
Immunodeficiency Virus (HIV)-Positive and HIV-Hepatitis C Virus-Coinfected
Subjects.
Regazzi M, Maserati R, Villani P, et al
 Antimicrob Agents Chemother. 2005 Feb;49(2):643-9.
 Abstract

SARS

  HIV protease inhibitor nelfinavir inhibits replication of SARS-associated coronavirus.
Yamamoto N, Yang R, Yoshinaka Y, et al 
Biochem Biophys Res Commun. 2004 Jun 4;318(3):719-25
 Abstract

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