Nelfinavir mesylate

Author: Tebas P.   Powderly W.G.  

Publisher: Informa Healthcare

ISSN: 1465-6566

Source: Expert Opinion on Pharmacotherapy, Vol.1, Iss.7, 2000-12, pp. : 1429-1440

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Abstract

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.