Chloroquine (diphosphate) is an antimalarial and anti-inflammatory drug widely used to treat malaria and rheumatoid arthritis. Chloroquine is an inhibitor of autophagy and toll-like receptors (TLRs).

Autophagy, TLRs^[1][2][3]

Chloroquine (CHQ, 20 μM) inhibits IL-12p70 release and reduces Th1-priming capacity of activated human monocyte-derived Langerhans-like cells (MoLC). Chloroquine (CHQ, 20 μM) enhances IL-1–induced IL-23 secretion in MoLC and subsequently increases IL-17A release by primed CD4⁺ T cells^[1]. Chloroquine (25 μM) suppresses MMP-9 mRNA expression in normoxia and hypoxia in parental MDA-MB-231 cells. Chloroquine has cell-, dose- and hypoxia-dependent effects on MMP-2, MMP-9 and MMP-13 mRNA expression^[2]. TLR7 and TLR9 inhibition using IRS-954 or chloroquine significantly reduces HuH7 cell proliferation in vitro^[3].

Chloroquine (80 mg/kg, i.p.) does not prevent the growth of the triple-negative MDA-MB-231 cells with high or low TLR9 expression levels in the orthotopic mouse model^[2]. TLR7 and TLR9 inhibition using IRS-954 or chloroquine significantly inhibits tumour growth in the mouse xenograft model. HCC development in the DEN/NMOR rat model is also significantly inhibited by chloroquine^[3].

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01650558	University of Maryland|National Institute of Allergy and Infectious Diseases (NIAID)	HIV	November 2012	Not Applicable
NCT01662700	Mahidol University	Acute Uncomplicated Malaria With P.Vivax Infection	October 2012	Phase 4
NCT02496741	Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)	Glioma|Cholangiocarcinoma|Chondrosarcoma	November 2015	Phase 1|Phase 2
NCT02511054	National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC)	Malaria	July 21, 2015	Phase 1
NCT00455325	Washington University School of Medicine|National Heart, Lung, and Blood Institute (NHLBI)	Metabolic Syndrome X|Overweight|Hypertension|Dyslipidemias|Prediabetic State	March 2007	Phase 2
NCT02432417	Maastricht Radiation Oncology	Glioblastoma|Astrocytoma, Grade IV	January 2020	Phase 2
NCT02564471	State University of New York - Upstate Medical University|Walter Reed Army Institute of Research (WRAIR)|Kansas State University	Rabies	April 2016	Phase 4
NCT01546961	University of Oxford	Vivax Malaria	June 2011	Not Applicable
NCT01777477	University of Zurich	Pancreatic Cancer	July 2012	Phase 1
NCT00426439	Bandim Health Project	Malaria, Falciparum	December 2006	Phase 4
NCT01019408	London School of Hygiene and Tropical Medicine|European Union|United Nations High Commissioner for Refugees|World Health Organization	Malaria, Falciparum	November 1993	Phase 4
NCT00308620	University of Minnesota - Clinical and Translational Science Institute|Minnesota Medical Foundation	HIV Infections	March 2006	Phase 2|Phase 3
NCT02610686	National Institute of Malariology, Parasitology and Entomology, Vietnam|Institute of Tropical Medicine, Belgium	Plasmodium Vivax	March 2015	Phase 4
NCT01218893	Radboud University	Plasmodium Falciparum Malaria	April 2011	Not Applicable
NCT00224978	National Institute of Neurology and Neurosurgery, Mexico	Glioblastoma Multiforme	January 2005	Phase 3
NCT02118090	Institut Pasteur, Cambodia|National Institute of Allergy and Infectious Diseases (NIAID)	Vivax Malaria	May 2014	Phase 4
NCT00849602	University of Sao Paulo|Fundação de Amparo à Pesquisa do Estado de São Paulo	Dengue	February 2008	Phase 1|Phase 2
NCT00805519	Ardabil University of Medical Sciences	Osteoarthritis of the Knee	February 2009	Phase 4
NCT00290420	Institut de Recherche pour le Developpement|Instituto Nacional de Laboratorios de Salud (INLASA)|Pan American Health Organization|Ministry of Health, Bolivia	Malaria	March 2006	Phase 4
NCT01366235	Asan Medical Center	Healthy Volunteers	May 2011	Phase 1
NCT03278808	U.S. Army Medical Research and Materiel Command	Malaria	September 17, 2018	Phase 2
NCT01894633	Instituto Nacional de Cancerologia de Mexico	Brain Metastasis	May 2011	Phase 2
NCT02389374	Menzies School of Health Research|International Centre for Diarrhoeal Disease Research, Bangladesh	Malaria	August 2014	Phase 4
NCT00811096	Walter Reed Army Institute of Research (WRAIR)	Malaria, Vivax	November 2008	Phase 2
NCT02876549	University of Oxford|Mahidol Oxford Tropical Medicine Research Unit|Nangarhar University, Afghanistan	Vivax Malaria	September 1, 2016	Phase 4
NCT01103713	Pfizer	Asymptomatic Parasitemia In Pregnancy	March 2011	Phase 3
NCT00677833	Pfizer	Malaria, Falciparum	June 2008	Phase 2|Phase 3
NCT01376167	GlaxoSmithKline|Medicines for Malaria Venture	Malaria, Vivax	April 24, 2014	Phase 2
NCT01074905	University of Oxford|Mahidol University	Vivax Malaria	May 2010	Phase 3
NCT01727531	Main Line Health	Brain Metastasis	December 2008	Not Applicable
NCT00844207	Pfizer	Malaria	February 2009	Phase 1
NCT01785979	Lihir Medical Centre	Hyper-reactive Malarial Splenomegaly|Malaria|Anaemia	January 2016	Phase 3
NCT00127998	Centers for Disease Control and Prevention|Malaria Research and Training Center, Bamako, Mali	Malaria	July 2005	Not Applicable
NCT03529396	Fundação de Medicina Tropical Dr. Heitor Vieira Dourado|Oswaldo Cruz Foundation|Conselho Nacional de Desenvolvimento Científico e Tecnológico	Vivax Malaria|G6PD Deficiency	July 20, 2018	Phase 2
NCT00157859	Menzies School of Health Research|Wellcome Trust|National Health and Medical Research Council, Australia|National Institute of Health Research and Development (NIHRD), Indonesia	Falciparum Malaria|Vivax Malaria	April 2004	Not Applicable
NCT01640574	University of Oxford	Vivax Malaria	February 2012	Phase 3
NCT01023477	Inova Health Care Services|George Mason University|University of Pittsburgh|United States Department of Defense|U.S. Army Medical Research and Materiel Command	Carcinoma, Intraductal, Noninfiltrating|DCIS|Ductal Carcinoma In Situ	December 2009	Phase 1|Phase 2
NCT02080026	Radboud University|Bill and Melinda Gates Foundation	Malaria	June 2014	Not Applicable
NCT02773979	National Institute of Allergy and Infectious Diseases (NIAID)	Plasmodium Falciparum Infection	September 12, 2016	Phase 1
NCT01178021	University of Oxford|National Malaria and Leishmaniasis Control Program, Afghanistan|Mahidol University	Vivax Malaria	August 2009	Phase 4
NCT00473837	Medical Research Council Unit, The Gambia	Malaria Anaemia	July 2007	Not Applicable
NCT02378532	Maastricht Radiation Oncology	Glioblastoma Multiforme	August 2016	Phase 1
NCT01422954	Radboud University|ZonMw: The Netherlands Organisation for Health Research and Development	Malaria|Plasmodium Falciparum	January 2012	Not Applicable
NCT00367653	Pfizer	Malaria	November 2006	Phase 3
NCT00131703	London School of Hygiene and Tropical Medicine|Ministry of Health, Ghana	Malaria|Pregnancy	March 2003	Phase 3
NCT02563496	GlaxoSmithKline|Medicines for Malaria Venture	Malaria, Vivax	February 6, 2017	Phase 2
NCT03070470	Food and Drug Administration (FDA)|Spaulding Clinical Research LLC	Drug-induced QT Prolongation|Pharmacokinetics|Pharmacodynamics	March 14, 2017	Phase 1
NCT00972725	GlaxoSmithKline	AIDS	December 1, 2009	Phase 2
NCT03449758	Sanofi|Regeneron Pharmaceuticals	Rheumatoid Arthritis	March 9, 2018	Phase 4
NCT02143934	Papua New Guinea Institute of Medical Research|Walter and Eliza Hall Institute of Medical Research|Swiss Tropical & Public Health Institute|Barcelona Centre for International Health Research	Plasmodium Vivax Infection|Plasmodium Vivax Clinical Episode|Plasmodium Falciparum Infection|Plasmodium Falciparum Clinical Episode	August 2009	Phase 4
NCT00282919	Pfizer	Falciparum Malaria	March 2006	Phase 2
NCT00137514	Bandim Health Project	Malaria, Falciparum	March 2001	Phase 4
NCT03687905	Tanta University	Proliferative Nephritis|Chloroquine Retinopathy	September 18, 2018
NCT01500980	Seattle Biomedical Research Institute	Malaria	December 2011	Phase 1
NCT00391313	Assistance Publique Hopitaux De Marseille	Chikungunya Virus	May 2006	Phase 3
NCT01443130	National Institute of Allergy and Infectious Diseases (NIAID)	Malaria	February 2012	Phase 3
NCT03243461	University of Göttingen|Deutsche Kinderkrebsstiftung|Hannover Clinical Trial Center GmbH	Glioblastoma WHO Grade IV|Diffuse Midline Glioma Histone 3 K27M WHO Grade IV|Anaplastic Astrocytoma WHO Grade III|Diffuse Intrinsic Pontine Glioma|Gliomatosis Cerebri	July 17, 2018	Phase 3
NCT00486694	London School of Hygiene and Tropical Medicine	Malaria, Vivax	March 2004	Phase 2
NCT00118807	London School of Hygiene and Tropical Medicine|Medical Research Council|National Malaria Control Programme, The Gambia	Malaria	August 2003	Phase 3
NCT00140517	London School of Hygiene and Tropical Medicine|DBL -Institute for Health Research and Development	Malaria in Pregnancy|Birth Weight|Anaemia	October 2002	Not Applicable
NCT00730366	Institute of Tropical Medicine, Belgium|University of Ouagadougou, Burkina Faso|National Laboratory of Public Health,Burkina Faso|Liverpool School of Tropical Medicine|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)	Malaria in Pregnancy	March 2004	Phase 3
NCT02043652	Centers for Disease Control and Prevention	Malaria	February 2014	Not Applicable
NCT00964691	Ministry of Health and Medical Services, Solomon Islands|World Health Organization	Malaria|Malaria in Pregnancy	August 2009	Phase 4
NCT02192944	University of Oxford	Healthy	July 2014	Phase 4
NCT02394197	LILIA GONZALEZ CERON|Instituto de Diagnóstico y Referencia Epidemiológicos (InDRE), Mexico|Centro Nacional de Vigilancia Epidemiológica y control de enfermedades (CENAVECE), Mexico|Jurisdicción Sanitaria VII, Chiapas, México|Pan American Health Organization|Instituto Nacional de Salud Publica, Mexico	Malaria	February 2008	Phase 4
NCT01103063	Pfizer|London School of Hygiene and Tropical Medicine|Medicines for Malaria Venture	Intermittent Preventive Treatment In Pregnancy (IPTp)	October 2010	Phase 3
NCT03503058	Sanaria Inc.|Eijkman Oxford Clinical Research Unit, Eijkman Institute|Indonesia University|Congressionally Directed Medical Research Programs	Malaria	March 2019	Phase 2
NCT01100060	Pfizer	Malaria Prophylaxis	April 2010	Phase 1
NCT01378286	Sanofi	Malaria	January 2012	Phase 3
NCT00442403	Université Victor Segalen Bordeaux 2	Malaria	April 2002	Phase 3
NCT01205178	GlaxoSmithKline|Medicines for Malaria Venture	Malaria	July 2, 2009	Phase 1
NCT02691910	Oswaldo Cruz Foundation|University of Sao Paulo	Malaria, Vivax	August 2014	Phase 2|Phase 3
NCT01290601	U.S. Army Medical Research and Materiel Command|GlaxoSmithKline	Malaria|Plasmodium Vivax	September 15, 2003	Phase 2
NCT02463331	University of Sao Paulo General Hospital	Autoimmune Hepatitis	May 2003	Phase 4
NCT02071537	University of Cincinnati	Malignant Neoplasm|Solid Tumors	May 2014	Phase 1
NCT02004314	CIHR Canadian HIV Trials Network	HIV	October 2009	Not Applicable
NCT00959517	London School of Hygiene and Tropical Medicine|HealthNet TPO	Uncomplicated Falciparum Malaria	July 2001	Phase 2
NCT03337152	PATH|Mahidol Oxford Tropical Medicine Research Unit	Malaria, Vivax|G6PD Deficiency	May 7, 2018	Phase 4
NCT01887821	Oxford University Clinical Research Unit, Vietnam|Institute of Malaria, Parasitology and Entomology, Ho Chi Minh City, Viet Nam|Hospital for Tropical Diseases, Ho Chi Minh City, Vietnam|Agency for Science, Technology and Research|Wellcome Trust	Plasmodium Vivax Malaria	February 2013	Phase 4
NCT00455403	Washington University School of Medicine|National Heart, Lung, and Blood Institute (NHLBI)|Singulex	Metabolic Syndrome X|Overweight|Hypertension|Dyslipidemias|Prediabetic State	April 2006	Not Applicable
NCT01941095	Hoffmann-La Roche	Rheumatoid Arthritis	November 20, 2013	Phase 3
NCT02932007	University of South Florida	Atrial Fibrillation	March 28, 2017	Phase 2
NCT01716260	Menzies School of Health Research|Ministry of Health, Bhutan	Vivax Malaria	January 2013
NCT01980745	University of Sao Paulo General Hospital	Hepatitis, Autoimmune	February 2002	Phase 4
NCT01680406	Centers for Disease Control and Prevention|Ethiopian Health and Nutrition Research Institute|Federal Minstry of Health of Ethiopia|Columbia University|Oromia Regional Health Bureau, Ethiopia|United States Agency for International Development (USAID)|Menzies School of Health Research	Plasmodium Vivax Infection	October 2012	Phase 4
NCT01784315	Ministry of Health, Bhutan|Asia Pacific Malaria Elimination Network|Menzies School of Health Research	Parasitemia	March 2013
NCT02348788	Menzies School of Health Research|Ministry of Health, Malaysia	Plasmodium Vivax Malaria Without Complication	January 2015	Phase 3
NCT03083847	National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC)	Malaria	June 5, 2017	Phase 1
NCT00379821	National Institute of Allergy and Infectious Diseases (NIAID)	Plasmodium Falciparum Infection	February 2007	Phase 3
NCT00819390	AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	March 2009	Phase 2
NCT02216123	GlaxoSmithKline|Medicines for Malaria Venture	Malaria, Vivax	April 30, 2015	Phase 3
NCT02001012	Menzies School of Health Research|Ministry of Health, Malaysia	Uncomplicated Knowlesi Malaria	January 2014	Phase 3
NCT00680732	Institute of Tropical Medicine, Belgium|Departments of Parasitology and Public Health, ITM, Antwerp, Belgium|Centre Muraz|Laboratoire National de Santé Publique, Ouagadougou, Burkina Faso	Malaria|Malaria in Pregnancy	June 2003	Phase 4
NCT00682578	University of Oxford|Wellcome Trust|Ministry of public Health Afghanistan	Uncomplicated Falciparum Malaria|Vivax Malaria	July 2007	Phase 3
NCT00440999	Medicines for Malaria Venture|Shin Poong Pharmaceuticals	Malaria	March 2007	Phase 3
NCT00169078	London School of Hygiene and Tropical Medicine	Malaria	July 2002	Not Applicable
NCT02698748	Centro de Investigacao em Saude de Manhica	Malaria	January 2015	Phase 2|Phase 3
NCT00125489	National Institute of Allergy and Infectious Diseases (NIAID)	Malaria|Plasmodium Falciparum Malaria	May 2005	Phase 4
NCT00082563	Pfizer	Malaria, Falciparum	August 2004	Phase 2
NCT01438177	New York University School of Medicine|Millennium Pharmaceuticals, Inc.	Multiple Myeloma	October 2011	Phase 2
NCT01708876	Menzies School of Health Research|Ministry of Health, Malaysia	Uncomplicated Plasmodium Knowlesi Malaria	October 2012	Phase 3
NCT01107145	Centers for Disease Control and Prevention	Plasmodium Vivax Malaria	February 2011	Phase 4
NCT01718054	London School of Hygiene and Tropical Medicine|Wellcome Trust	Sickle Cell Disease	August 2012	Phase 2|Phase 3
NCT01546389	National Institute of Allergy and Infectious Diseases (NIAID)	Malaria	April 2012	Phase 1
NCT02996695	National Institute of Allergy and Infectious Diseases (NIAID)	Plasmodium Falciparum Infection	April 6, 2017	Phase 1
NCT01078779	National University Hospital, Singapore	Influenza	November 2009	Phase 2
NCT01575782	Maastricht Radiation Oncology	Small Cell Lung Cancer	May 2014	Phase 1
NCT01236612	Radboud University	Plasmodium Falciparum Malaria	April 2011	Not Applicable
NCT00323375	Tulane University Health Sciences Center|National Institutes of Health (NIH)	Malaria	August 1999	Phase 1
NCT00132535	London School of Hygiene and Tropical Medicine|DBL -Institute for Health Research and Development|Uganda AIDS Commission	Malaria in Pregnancy|HIV Infections	August 2003	Not Applicable
NCT02333890	Ottawa Hospital Research Institute	Breast Cancer|Invasive Breast Cancer	July 2015	Phase 2
NCT02058173	Shiraz University of Medical Sciences	Hepatitis C Virus	January 2014	Phase 4

In Vitro: 

H₂O : ≥ 33 mg/mL (63.97 mM)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

* "≥" means soluble, but saturation unknown.

*Please refer to the solubility information to select the appropriate solvent.