Drug Evaluations: Drug Evaluation Anti-infectives: Activity and role of lamivudine in the treatment of adults with human immunodeficiency virus type 1 infection: A review

Abstract

Lamivudine is a nucleoside analogue reverse transcriptase inhibitor of HIV-1, HIV-2 and Hepatitis B virus which demonstrates in vitro activity with a high therapeutic index in a range of T-lymphocyte and haematopoietic precursor cell lines. It is synergistic in vitro with zidovudine and a range of other antiretrovirals, including the proteinase inhibitor saquinavir, in two- and three-way combinations and is active against zidovudine-resistant virus. Whilst it exhibits excellent oral bioavailability, the CSF/plasma ratio of lamivudine is lower than those reported with other licensed antiretrovirals. In clinical use, lamivudine exhibits limited antiretroviral activity as a monotherapy, but in combination with zidovudine results in more substantial and durable responses in immunological and virological markers than zidovudine alone. Clinical end-point data from lamivudine trials are now awaited. Clinical trials in combination with zidovudine in patients both naive to and experienced with prior antiretroviral...