The anti-HIV-1 activity of chloroquine

Background: there is a dramatic need for drugs with anti-HIV-1 activity that are affordable for resource-poor countries. Chloroquine (CQ) is one such drug. Objectives: to review the data indicating that CQ has anti-HIV-1 activity. Results: chloroquine (CQ) and its derivative hydroxychloroquine (HCQ) are endowed with a broad anti-HIV-1 activity inhibiting X4, R5, and X4/R5 stains in lymphocytic and monocytic cells. Interestingly, CQ is capable of inhibiting HIV-1 replication at concentrations within the range reported in plasma of individuals chronically treated with doses of the drug which have well-known and limited toxicity. These effects have been confirmed in vivo in two clinical trials. The principal mechanism of HIV-1 inhibition by CQ seems to be an effect on gp120 on a post-transcriptional level. Because CQ and HCQ appear to have a novel site of action (i.e. post-transcriptional inhibition of gp120), these drugs may be particularly useful in combination with other anti-retroviral agents (e.g. ZDV, ddI and HU). Conclusion: combining these drugs with other anti-HIV-1 agents, especially HU and ddI, may be an interesting option for the treatment for HIV-1 infected individuals in the developing world.