Emtricitabine: A review of its use in the management of HIV infection

Drugs

Volumn 65, Issue 10, 2005, Pages 1427-1448

  Frampton, James E ^a   Perry, Caroline M ^a  

^a ADIS INTERNATIONAL LIMITED   (New Zealand)

Author keywords

[No Author keywords available]

Indexed keywords

ABACAVIR; ALANINE AMINOTRANSFERASE; ASPARTATE AMINOTRANSFERASE; ATAZANAVIR; CREATININE; DIDANOSINE; EFAVIRENZ; EMTRICITABINE; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; FAMCICLOVIR; INDINAVIR; LAMIVUDINE; LAMIVUDINE PLUS ZIDOVUDINE; LOPINAVIR PLUS RITONAVIR; NELFINAVIR; NEVIRAPINE; PROTEINASE INHIBITOR; RITONAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR; SAQUINAVIR; STAVUDINE; TENOFOVIR; TENOFOVIR DISOPROXIL; ZIDOVUDINE;

ABNORMALLY HIGH SUBSTRATE CONCENTRATION IN BLOOD; ALGORITHM; ANEMIA; ANTIVIRAL ACTIVITY; ASTHENIA; CLINICAL TRIAL; COUGHING; DELIRIUM; DIARRHEA; DOSE RESPONSE; DREAM; DRUG CONTRAINDICATION; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG MECHANISM; DRUG TOLERABILITY; ENZYME INHIBITION; FATIGUE; FOOD AND DRUG ADMINISTRATION; HEADACHE; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; HYPERGLYCEMIA; HYPERLACTATEMIA; IC 50; IN VITRO STUDY; LACTIC ACIDOSIS; LIPOATROPHY; LIPODYSTROPHY; LIVER TOXICITY; NAUSEA; NEUROPATHY; NONHUMAN; PANCREATITIS; PARESTHESIA; PRACTICE GUIDELINE; PREGNANCY; RASH; REVIEW; RHINITIS; SIDE EFFECT; SINGLE DRUG DOSE; SKIN DISCOLORATION; VIRUS GENOME; VIRUS LOAD; VIRUS RESISTANCE; VOMITING; WEIGHT REDUCTION;

ADULT; DEOXYCYTIDINE; HIV INFECTIONS; HUMANS; RANDOMIZED CONTROLLED TRIALS; REVERSE TRANSCRIPTASE INHIBITORS; TREATMENT OUTCOME;

HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 22944463317     PISSN: 00126667     EISSN: 00126667     Source Type: Journal    
DOI: 10.2165/00003495-200565100-00008     Document Type: Review

References (59)

1. Palella FJ, Delaney KM, Moorman MC, et al. Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. N Engl J Med 1998; 338: 853-60
2. Department of Health and Human Services (US). Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (April 7, 2005) [online]. Available from URL: http://aidsinfo.nih.gov/guidelines/adult/ AA_040705.pdf [Accessed 2005 Apr 14]
3. Cahn P. Emtricitabine: a new nucleoside analogue for once-daily antiretroviral therapy. Expert Opin Investig Drugs 2004 Jan; 13 (1): 55-68
4. Modrzejewski KA, Herman RA. Emtricitabine: a once-daily nucleoside reverse transcriptase inhibitor. Ann Pharmacother 2004 Jun; 38: 1006-14
5. Anderson PL. Pharmacologic perspectives for once-daily antiretroviral therapy. Ann Pharmacother 2004 Nov; 38 (11): 1924-34
6. Gathe JJr. Adherence and potency with antiretroviral therapy: a combination for success. J Acquir Immune Defic Syndr 2003 Oct 1; 34 Suppl. 2: S118-22
7. Bartlett JA, DeMasi R, Quinn J, et al. Overview of the effectiveness of triple combination therapy in antiretroviral-naive HIV-1 infected adults. AIDS 2001 Jul 27; 15 (11): 1369-77
8. Bang LM, Scott LJ. Emtricitabine: an antiretroviral agent for HIV infection. Drugs 2003; 63 (22): 2413-24; discussion 2425-6
9. Gilead Sciences. Emtriva (emtricitabine) capusles prescribing information [online]. Available from URL: http://www.gilead.com/pdf/emtriva.pdf [Accessed 2003 Jul 7]
10. Gilead Sciences International Limited. Emtriva 200mg hard capsules: summary of product characteristics [online]. Available from URL: http://emc.medicines.org.uk/emc/assets/c/html/ displayDocPrinterFriendly.asp? documentid=13635 [Accessed 2005 May 19]
11. Wiznia A, Violari A, Ndiweni D, et al. Once daily (QD) emtricitabine (FTC) with other antiretroviral agents (ART) in HIV-infected pediatric patients at 48 weeks [abstract no. TuPeB4431 plus poster]. 15th International AIDS Conference; 2004 Jul 11-16; Bangkok
12. McKinney R, Rodman J, Rathore M, et al. PACTG 1021: Extended follow-up and pharmacokinetics for once daily emtricitabine, didanosine, and efavirenz for antiretroviral naive children and adolescents [abstract no. 936 plus poster]. 11th Conference on Retroviruses and Opportunistic Infections; 2004 Feb 8-11; San Francisco
13. Gilead Sciences, Inc.. Emtriva (emtricitabine). Product monograph. Foster City (CA): Gilead Sciences, Inc., 2003 Jul
14. Schinazi R. Assessment of the relative potency of emtricitabine and lamivudine. J Acquir Immune Defic Syndr 2003; 34 (2): 243-5
15. Rousseau FS, Wakeford C, Mommeja-Marin H, et al. Prospective randomized trial of emtricitabine versus lamivudine short-term monotherapy in human immunodeficiency virus-infected patients. J Infect Dis 2003 Dec 1; 188 (11): 1652-8
16. Schinazi RF, Lloyd RM, Nguyen M-H, et al. Characterization of human immunodeficiency viruses resistant to oxathiolane-cytosine nucleosides. Antimicrob Agents Chemother 1993; 37 (4): 875-81
17. Saag MS, Cahn P, Raffi F, et al. Efficacy and safety of emtricitabine vs stavudine in combination therapy in antiretroviral-naive patients: a randomized trial. JAMA 2004 Jul 14; 292 (2): 180-9
18. Gazzard B, Dejesus E, Campo R, et al. The combination of tenofovir DF (TDF), emtricitabine (FTC) and efavirenz (EFV) has significantly greater response vs fixed dose zidovudine/ lamivudine (CBV) and EFV in antiretroviral naive patients: a 24 week preliminary analysis [abstract no. H-1137c oral presentation plus poster]. 44th Interscience Conference on Antimithe crobial Agents and Chemotherapy: Late Breakers; 2004 Oct 30-Nov 2; Washington, DC
19. Arribas JR, Pozniak AL, Gallant JE. Superior outcome for tenofovir DF (TDF), emtricitabine (FTC) and efavirenz (EFV) compared to fixed dose zidovudine/lamivudine (CBV) and EFV in antiretroviral naive patients. 18th International Conference on Antiviral Research; 2005 April 10-14; Barcelona
20. Benson CA, van der Horst C, LaMarca A, et al. A randomized study of emtricitabine and lamivudine in stably suppressed patients with HIV. AIDS 2004; 18: 2269-7 6
21. Lyseng-Williamson KA, Reynolds NA, Plosker G. Tenofovir disproxil fumarate: a review of its use in the management of HIV infection. Drugs 2005; 65 (3): 413-32
22. Tisdale M, Kemp SD, Parry NR, et al. Rapid in vitro selection of human immunodeficiency virus type 1 resistant to 3′-thiacytidine inhibitors due to a mutation in the YMDD region of reverse transcriptase. Proc Natl Acad Sci U S A 1993; 90: 5653-6
23. Molina JM, Journot V, Morand-Joubert L, et al. Simplification therapy with once-daily emtricitabine, didanosine, and efavirenz in HIV-1-infected adults with viral suppression receiving a protease inhibitor-based regimen: a randomized trial. J Infect Dis 2005 Mar 15; 191: 830-9
24. Powderly W, Cahn P, Raffi F, et al. Lipid abnormalities and body habitus in a double-blind, randomized, controlled trial comparing emtricitabine to stavudine in HIV(+) ART-naive patients [abstract no. 717 plus poster]. 11th Conference on Retroviruses and Opportunistic Infections; 2004 Feb 8-11; San Francisco
25. Molina JM, Journot V, Rozenbaum W, et al. Simplification therapy with once-daily efavirenz, emtricitabine, and didanosine in patients virologically suppressed with a protease inhibitor-based regimen: 3-year follow-up of the Alize-ANRS 099 trial [abstract no. 573 plus poster]. 12th Conference on Retroviruses and Opportunistic Infections; 2005 Feb 22-25; Boston
26. Wang LH, Gardner P, Frick LW, et al. Pharmacokinetics and safety of 524W91 following single oral administration of escalating doses in HIV-infected volunteers [abstract no. A129]. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1995 Sep 17-20; San Francisco
27. Saez-Llorens X, Violari A, Ndiweni D, et al. Once daily emtricitabine (FTC) in HIV-infected paediatric patients with other antiretroviral agents [abstract no. 872 plus poster]. 10th Conference on Retroviral and Opportunistic Infections; 2003 Feb 10-14; Boston
28. Wang LH, Delehanty J, Blum MR, et al. FTC: a potent and selective anti-HIV and anti-HBV agent demonstrating desirable pharmacokinetic characteristics [abstract no. 415]. Clin Infect Dis 1998; 27: 999
29. Zong J, Blum MR, Chittick G, et al. Steady-state evaluation of the potential pharmacokinetic interactions between emtricitabine and zidovudine in healthy volunteers [abstract no. A1620 plus poster]. 43rd Annual Interscience Conference on Antimicrobial Agents and Chemotherapy; 2003 Sep 14-17; Chicago
30. Blum MR, Begley J, Zong J, et al. Lack of a pharmacokinetic interaction between emtricitabine and tenofovir DF when co-administered to steady state in healthy volunteers [abstract no. A-1621 plus poster]. 43rd Annual Interscience Conference on Antimicrobial Agents and Chemotherapy; 2003 Sep 14-17; Chicago
31. Wang LH, Blum MR, Hui J, et al. Lack of significant pharmacokinetic interactions between emtricitabine and other nucleoside antivirals in healthy volunteers [abstract no. A-505]. 41st Interscience Conference on Antimicrobial Agents and Chemotherapy; 2001 Sep 22-25; Chicago
32. Wang LH, Begley J, St Claire III RL. Pharmacokinetic and pharmacodynamic characteristics of emtricitabine supports its once daily dosing for the treatment of HIV infection. AIDS Res Hum Retroviruses 2004; 20 (11): 1173-82
33. Painter GR, St Clair M, Ching S, et al. 524W91: anti-HIV, anti-hepatitis B virus. Drugs Future 1995 Aug; 20: 761-5
34. Rousseau FS, Kahn JO, Thompson M, et al. Prototype trial design for rapid dose selection of antiretroviral drugs: an example using emtricitabine (Coviracil). J Antimicrob Chemother 2001 Oct; 48 (4): 507-13
35. Wang LH, Wiznia AA, Rathore MH, et al. Pharmacokinetics and safety of single oral doses of emtricitabine in human immunodeficiency virus-infected children. Antimicrob Agents Chemother 2004 Jan; 48 (1): 183-91
36. Molina JM, Peytavin G, Perusat S. Pharmacokinetics of emtricitabine, didanosine and efavirenz administered once-daily for the treatment of HIV-infected adults (pharmacokinetic sub-study of the ANRS 091 Trial). HIV Med 2004; 5 (2): 99-104
37. Molina JM, Ferchal F, Rancinan C, et al. Once-daily combination therapy with emtricitabine, didanosine, and efavirenz in human immunodeficiency virus-infected patients. J Infect Dis 2000; 182 (2): 599-602
38. Molina JM, Noe E, Raffi F, et al. Once-daily combination therapy with emtricitabine (FTC), didanosine (ddl) and efavirenz (EFV) in treatment naive HIV-infected adults: 3-year follow-up of the MONTANA (ANRS 091) trial [abstract no. 594 plus poster presented at the 2nd International AIDS Society Conference on HIV Pathogenesis and Treatment; 2003 Jul 13-16; Paris]. Antivir Ther 2003; 8 Suppl. 1: S346
39. Sanne I, Anderson J, Kargl D, et al. Evaluation of emtricitabine within a triple NRTI HAART regimen [abstract no. H-868 plus poster]. 43rd Interscience Conference on Antimicrobial Agents and Chemotherapy; 2003 Sep 14-17; Chicago
40. Sanne I, Van Der Horst C, Shaw A, et al. Two randomized, controlled, equivalence trials of emtricitabine to lamivudine [abstract no. 4432 plus poster]. 14th International AIDS conference; 2002 July 7-12; Barcelona
41. Gathe J, Podzamczer D, Johnson M, et al. Once-daily vs twice-daily lopinavir/ritonavir in antiretroviral-naive patients: 48-week results [abstract no. 570]. 11th Conference on Retroviruses and Opportunistic Infections; 2004 Feb 8-11; San Francisco
42. Molina JM, Ferchel F, Rancinan C, et al. Once-daily combination of emtricitabine, didanosine, and efavirenz vs continued PI-based HAART in HIV-infected adults with undetectable plasma HIV-RNA: 48-week results of a prospective randomized multicenter trial (ALIZE-ANRS 99) [abstract no. 551 plus poster]. 10th Conference on Retroviruses and Opportunistic Infections; 2003 Feb 10-14; Boston:
43. US FDA CDER. Clinical review: NDA 21-500 Emtriva® (emtricitabine) capsules for treatment of HIV-1 infection in adults [online]. Available from URL: http://www.fda.gov/cder/foi/ nda/2003/21-500_Emtriva_Medr_P1.pdf [and P2.pdf] [Accessed 2005 Apr 18]
44. Data on file, Gilead Sciences, Inc., 2005
45. Sanne I, Mommeja-Marin H, Hinkle J, et al. Severe hepatotoxicity associated with nevirapine use in HIV-infected subjects. J Infect Dis 2005 Mar 15; 191: 825-9
46. Nelson M, Schiavone M. Emtricitabine (FTC) for the treatment of HIV infection. Int J Clin Pract 2004 May; 58 (5): 504-10
47. Center for Drug Evaluation and Research (CDER) of the US Food and Drug Administration (US FDA). Guidance for industry, antiretroviral drugs using plasma HIV RNA measurements: clinical considerations for accelerated and traditional approval [online]. Available from URL: http://www.fda.gov/ cder/guidance/index.htm [Accessed 2005 May 23]
48. Levin J. TDF/FTC vs FD AZT/3TC combivir in ART naive: 48 weeks (Natap, 13Apr05) [online]. Available from URL: http://www.actions-traitements.org/breve. php3?id_breve=1692 [Accessed 2005 Jun 1]
49. FDA approves once daily Kaletra for therapy naive patients [online]. Available from URL: http://www.natap.org/2005/ HIV/050205_01.htm [Accessed 2005 May 23]
50. Powderly W, Mondou E, Shaw A, et al. Overview of the incidence of symptomatic hyperlactataemia with emtricitabine (FTC) [abstract no. 737]. Antiviral Ther 2003; 8 Suppl. 1: S389
51. Mondou E, Quinn JB, Shaw A, et al. Incidence of skin discoloration across phase 3 clinical trials of emtricitabine (FTC) [abstract no. WePeB5916]. 15th International AIDS Conference; 2004 Jul 11-16; Bangkok
52. Department of Health and Human Services (US). Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (March 23, 2004) [online]. Available from URL: http://aidsinfo.nih.gov/guidelines/adult/archive/ AA_032304.pdf [Accessed 2005 Jun 2]
53. UNAIDS. AIDS epidemic update: December 2004 [online]. Available from URL: http://www.unaids.org [Accessed 2005 Apr 14]
54. Boyle BA. The continuing evolution of HIV therapy. AIDS Read 2003 Dec; 13 (12): 576-8, 582
55. Stone VE, Hogan JW, Schuman P, et al. Antiretroviral regimen complexity, self-reported adherence, and HIV patients' understanding of their regimens: survey of women in the HER study. J Acquir Immune Defic Syndr 2001 Oct 1; 28 (2): 124-31
56. Yeni PG, Hammer SM, Hirsch MS, et al. Treatment for adult HIV infection: 2004 recommendations of the International AIDS Society-USA Panel. JAMA 2004 Jul 14; 292 (2): 251-65
57. Dando TM, Wagstaff AJ. Emtricitabine/tenofovir disoproxil fumarate. Drugs 2004; 64 (18): 2075-82
58. Gilead Sciences Inc. Gilead provides update on development of fixed-dose regimen of truvada (emtricitabine and tenofovir disoproxil fumarate) and sustiva (efavirenz) [online]. Available from URL: http://www.gilead.com/wt/sec/ pr_701414 [Accessed 2005 May 19]
59. British HIV Association (BHIVA). Guidelines for the treatment of HIV-infected adults with antiretroviral therapy: an update [online]. Available from URL: http://www.bhiva.org/ guidelines/2003/hiv/ [Accessed 2005 Apr 26]