Nelfinavir mesylate.
Nelfinavir is an inhibitor of the HIV-1 and HIV-2 protease, with good in vivo activity in HIV-infected patients. Nelfinavir is used in combination with other antiretroviral medications as part of a potent antiretroviral regimen. When used in this manner, 50-75% of patients who are naïve to antiretroviral therapy have plasma HIV RNA levels below the limit of detection (< 400 copies) after 12 months of treatment. This use of nelfinavir in combination regimens is associated with an increase of almost 200/mm3 CD4+ lymphocytes at 12 months of therapy. Initial trials and clinical experience indicate that nelfinavir is equipotent to other potent protease inhibitors (PIs). The drug is well-tolerated, with mild diarrhoea being the most common side effect in 12-20% of patients. Virologic failure of nelfinavir is associated with genotypic and phenotypic changes that have a unique pattern that may retain susceptibility to other PIs. The results of small, non-controlled trials suggest these failures can be rescued with a second protease-based regimen. Due to the above characteristics, nelfinavir has become the most frequently prescribed first line PI.
Tebas
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Division of Infectious Diseases, Washington University School of Medicine, Box 8051, St. Louis, MO 63110, USA. tebas@im.wustl.edu
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D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D004338:Drug Combinations; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D017320:HIV Protease Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D019888:Nelfinavir / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*
D004338:Drug Combinations; D017320:HIV Protease Inhibitors; D019888:Nelfinavir