Emtricitabine/tenofovir disoproxil fumarate: in combination with a protease inhibitor in HIV-1 infection.
Emtricitabine, a nucleoside reverse transcriptase inhibitor (RTI), and tenofovir disoproxil fumarate (tenofovir DF), a nucleotide RTI, as a fixed-dose combination tablet (emtricitabine/tenofovir DF) for once-daily oral administration, are used as the nucleoside/nucleotide RTI backbone in combination with other antiretroviral agents, including ritonavir-boosted protease inhibitors (PIs), in the treatment of adults with HIV-1 infection. Emtricitabine and tenofovir DF show good activity against laboratory strains and clinical isolates of HIV-1 in vitro, although strains with resistance to emtricitabine or tenofovir have also been reported. Regimens consisting of once-daily emtricitabine/tenofovir DF 200 mg/300 mg plus lopinavir/ritonavir (in the randomized, double-blind, placebo-matched, multicentre HEAT study) or boosted atazanavir or efavirenz (in the randomized, partially-blind, multicentre ACTG 5202 trial) were effective in the initial treatment of patients with HIV-1 infection (with screening plasma HIV-1 RNA levels of >or=100,000 copies/mL in ACTG 5202). In other randomized studies, emtricitabine/tenofovir DF 200 mg/300 mg once daily was an effective backbone for boosted PI-based regimens in the initial treatment of HIV-1 infection. Treatment-experienced patients with HIV-1 infection also experienced beneficial virological effects when treated with similar regimens. Emtricitabine/tenofovir DF in combination with various boosted PIs was generally well tolerated by adults with HIV-1 infection.
Wolters Kluwer Health, Adis, Auckland, New Zealand. demail@adis.co.nz
Caroline M
CM
Perry
D000225:Adenine / Q000009:adverse effects / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use; D019380:Anti-HIV Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D003841:Deoxycytidine / Q000009:adverse effects / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use; D004338:Drug Combinations; D004359:Drug Therapy, Combination; D000068679:Emtricitabine; D015658:HIV Infections / Q000188:drug therapy* / Q000503:physiopathology; D017320:HIV Protease Inhibitors / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D063065:Organophosphonates / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D000068698:Tenofovir
D019380:Anti-HIV Agents; D004338:Drug Combinations; D017320:HIV Protease Inhibitors; D063065:Organophosphonates; D003841:Deoxycytidine; D000068698:Tenofovir; D000068679:Emtricitabine; D000225:Adenine