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.
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.
Authors: Stuart D Dowall; Andrew Bosworth; Robert Watson; Kevin Bewley; Irene Taylor; Emma Rayner; Laura Hunter; Geoff Pearson; Linda Easterbrook; James Pitman; Roger Hewson; Miles W Carroll Journal: J Gen Virol Date: 2015-12 Impact factor: 3.891
Authors: John G Ayisi; Anna M van Eijk; Robert D Newman; Feiko O ter Kuile; Ya Ping Shi; Chunfu Yang; Margarette S Kolczak; Juliana A Otieno; Ambrose O Misore; Piet A Kager; Renu B Lal; Richard W Steketee; Bernard L Nahlen Journal: Emerg Infect Dis Date: 2004-04 Impact factor: 6.883