Drugs

Chloroquine

Chloroquine

Other Names: Aralen, CQ, chloroquine phosphate Drug Class: Immune Modulators Molecular Formula: C18 H26 Cl N3 Registry Number: 54-05-7 (CAS) Chemical Name: Quinoline, 7-chloro-4-((4-(diethylamino)-1-methylbutyl)amino)- Chemical Class: 4-aminoquinoline Phase of Development: Chloroquine is in Phase II development for HIV treatment.

(Compound details obtained from ChemIDplus Advanced,1 Retrovirology article,2 PLoS Medicine article,3 and ClinicalTrials.gov4)

What is chloroquine?

What is chloroquine?

Chloroquine is being investigated (studied) to treat HIV infection. As an HIV investigational drug, chloroquine is categorized as an immune modulator.2 Immune modulators (also called immunomodulators) are substances that help to activate, boost, or restore normal immune function.

Chloroquine is currently approved by the U.S. Food and Drug Administration (FDA) for the treatment of malaria and certain amoeba infections.5

Researchers have evaluated whether chloroquine can reduce immune system hyperactivity (also called immune activation) as part of a strategy to treat or cure HIV infection. Reducing immune activation may help to reduce latent HIV reservoirs and increase CD4 counts.2,6

To learn how investigational drugs are tested during clinical trials, read the AIDSinfo What is an Investigational HIV Drug? and HIV/AIDS Clinical Trials fact sheets.

Which clinical trials are studying chloroquine?

Which clinical trials are studying chloroquine?

Study Name: ACTG A5258; NCT00819390
Phase: II
Status: This study has been completed.
Location: United States
Purpose: The purpose of this study was to evaluate the safety and effectiveness of chloroquine in reducing immune activation in participants both on and off antiretroviral therapy (ART).4

Study Name: CTN 246; NCT02004314
Phase: Not available
Status: This study has been completed.
Location: Canada
Purpose: This study evaluated whether chloroquine could increase CD4 counts and reduce immune activation in participants on ART who had suppressed viral loads but low CD4 counts.7

Study Name: NCT00308620
Phase: I
Status: This study has been completed.
Location: United States
Purpose: The purpose of this study was to evaluate whether chloroquine could reduce viral loads and immune system activation in participants who had never been on ART or who were off ART for at least 16 months.6,8

For more details on the studies listed above, see the Health Professional version of this drug summary.

Other HIV-related studies of chloroquine have been completed. A completed study (NCT00972725) evaluated the effect of a single dose of chloroquine given before a booster dose of the investigational therapeutic HIV vaccine (F4/AS01β) on the immune system of healthy adults.9,10

What side effects might chloroquine cause?

What side effects might chloroquine cause?

One goal of HIV research is to identify new drugs that have fewer side effects. The following side effects were observed in some of the studies of chloroquine listed above.

ACTG A5258 (NCT00819390):
In this study, no chloroquine-related side effects were reported.4,11

CTN 246 (NCT02004314):
In this study, no serious side effects related to chloroquine were reported. But during the first week of treatment with chloroquine, 1 participant stopped the study because of moderately severe digestive (gastrointestinal) side effects.12

Additional information on side effects known to be associated with chloroquine can be found in the FDA-approved Full Prescribing Information for Chloroquine.5

Because chloroquine is still being studied, information on possible side effects of the drug is not complete. As testing of chloroquine continues, additional information on possible side effects will be gathered.

Where can I get more information about clinical trials studying chloroquine?

Where can I get more information about clinical trials studying chloroquine?

More information about chloroquine-related research studies is available from the AIDSinfo database of ClinicalTrials.gov study summaries. Click on the title of any trial in the list to see the ClinicalTrials.gov trial summary and more information about the study.

Some clinical trials may be looking for volunteer participants. Your health care provider can help you decide whether participating in a clinical trial is right for you. For more information, visit NIH Clinical Research Trials and You.

References

References

  1. United States National Library of Medicine. ChemIDplus Advanced: chloroquine. https://chem.nlm.nih.gov/chemidplus/rn/54-05-7. Accessed September 10, 2018.
  2. Savarino A, Shytaj IL. Chloroquine and beyond: exploring anti-rheumatic drugs to reduce immune hyperactivation in HIV/AIDS. Retrovirology. 2015;12:51.
  3. Delves M, Plouffe D, Scheurer C, et al. The activities of current antimalarial drugs on the life cycle stages of plasmodium: a comparative study with human and rodent parasites. PLoS Med. 2012;9(2):e1001169.
  4. AIDS Clinical Trials Group. A Phase II, double blind, randomized, exploratory study of chloroquine for reducing HIV-associated immune activation. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on January 8, 2009. NLM Identifier: NCT00819390. https://clinicaltrials.gov/ct2/show/NCT00819390. Accessed September 10, 2018.
  5. West-ward Pharmaceutical Corp. Chloroquine: full prescribing information. DailyMed. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9b585ad5-ae86-4403-b83f-8d8363d43da5. Published July 2010. Accessed September 10, 2018.
  6. Murray SM, Down CM, Boulware DR, et al. Reduction of immune activation with chloroquine therapy during chronic HIV infection. J Virol. 2010;84(22):12082-12086.
  7. CIHR Canadian HIV Trials Network. Chloroquine as a modulator of T cell immune activation to improve CD4 recovery in HIV-infected participants receiving antiretroviral therapy: a proof-of-concept study. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on November 27, 2013. NLM Identifier: NCT02004314. https://clinicaltrials.gov/ct2/show/NCT02004314. Accessed September 10, 2018.
  8. University of Minnesota - Clinical and Translational Science Institute. A randomized, pilot study of the anti-viral and anti-inflammatory effects of chloroquine in early HIV infection. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on March 27, 2006. NLM Identifier: NCT00308620. https://clinicaltrials.gov/ct2/show/NCT00308620. Accessed September 10, 2018.
  9. GlaxoSmithKline. A study to evaluate the safety and immunogenicity of a booster dose of GSK biologicals’ HIV candidate vaccine (732461) after administration of chloroquine in healthy adults. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on September 3, 2009. NLM Identifier: NCT00972725. https://clinicaltrials.gov/ct2/show/NCT00972725. Accessed September 10, 2018.
  10. Leroux-Roels G, Bourguignon P, Willekens J, et al. Immunogenicity and safety of a booster dose of an investigational adjuvanted polyprotein HIV-1 vaccine in healthy adults and effect of administration of chloroquine. Clin Vaccine Immunol. 2014;21(3):302-311.
  11. Jacobson JM, Bosinger SE, Kang M, et al. The effect of chloroquine on immune activation and interferon signatures associated with HIV-1. AIDS Res Hum Retroviruses. 2016;32(7):636-647.
  12. Routy J-P, Angel JB, Patel M, et al. Assessment of chloroquine as a modulator of immune activation to improve CD4 recovery in immune nonresponding HIV-infected patients receiving antiretroviral therapy. HIV Med. 16(1):48-56.

Last Reviewed: September 10, 2018