Current status of antiretroviral therapy

Abstract

At present, there are 22 FDA-approved antiretroviral agents, which are categorised into four classes of drugs. Several others are in various stages of basic and clinical development. The authors of this paper review the general characteristics of each class of antiretrovirals, as well as individual investigational agents that are in advanced clinical development. A brief synopsis of US and WHO antiretroviral treatment guidelines is also provided.

Keywords::

• antiretrovirals
• antiretroviral therapy
• chemokine receptor antagonists
• entry inhibitors
• fusion inhibitors
• highly active antiretroviral therapy
• HIV
• integrase inhibitors
• maturation inhibitors
• non-nucleoside analogue reverse transcriptase inhibitors
• nucleoside analogue reverse transcriptase inhibitors
• protease inhibitors
• treatment guidelines

Notes

Zalcitabine is planned to be discontinued in 2006. Amprenavir has been discontinued by the manufacturer.

*Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of all nucleoside analogues and are believed to be caused by NRTI/NtRTI-induced mitochondrial damage. The deoxynucleoside analogue reverse transcriptase inhibitors (zalcitabine, stavudine, didanosine) have a higher potential to cause mitochondrial DNA depletion than other NRTI/NtRTIs.

NNRTI: Non-nucleoside analogue reverse transcriptase inhibitor; NRTI: Nucleoside/nucleotide analogue reverse transcriptase inhibitor; NtRTI: Nucleotide reverse transcriptase inhibitor.