J. Mcintyre, J. Castaǹer
2005
Citations
0
Influential Citations
1
Citations
Quality indicators
Journal
Drugs of The Future
Abstract
The nucleoside reverse transcriptase inhibitors (NRTIs) are widely used in combination with protease inhibitors and non-nucleoside RT inhibitors (NNRTIs) in regimens of highly active antiretroviral therapy (HAART) for the treatment of human immunodeficiency virus (HIV) infection. However, these regimens may lack efficacy, or initially successful regimens may fail because of significant cross-resistance among agents of the same class. The development of second-generation NRTIs has focused on the resistance profile and the requirement for suppression of mutant variants likely to be present in NRTI-experienced patients. Dexelvucitabine (Reverset™) is a cytidine nucleoside analogue that combines potency against wild-type, zidovudine- and lamivudine-resistant variants of HIV reverse transcriptase. It is a potent inhibitor of HIV-1 replication in vitro, with activity against recombinant zidovudine- and lamivudine-resistant viruses. A phase lib study conducted in 199 treatment-experienced patients who were viremic on their current regimen showed a decrease in mean viral load of 1.2 log 10 copies/ml and indicated that dexelvucitabine provided sustained antiviral activity in patients with multiple resistance mutations, including M184V and K65R.