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chloroquine

Small moleculeapproved

Approved

Oct 31, 1949

Chloroquine (brand name Aralen) is indicated for the suppressive treatment and for acute attacks of malaria due to P. vivax, P.malariae, P. ovale, and susceptible strains of P. falciparum. The drug is also indicated for the treatment of extraintestinal amebiasis. In addition, chloroquine is in clinical trials as an investigational antiretroviral in humans with HIV-1/AIDS and as a potential antiviral agent against chikungunya fever. The mechanism of plasmodicidal action of chloroquine is not completely certain. However, is existed theory, that like other quinoline derivatives, it is thought to inhibit heme polymerase activity. The heme moiety consists of a porphyrin ring called Fe(II)-protoporphyrin IX (FP). To avoid destruction by this molecule, the parasite biocrystallizes heme to form hemozoin, a non-toxic molecule. Chloroquine enters the red blood cell, inhabiting parasite cell, and digestive vacuole by simple diffusion. Chloroquine then becomes protonated (to CQ2+), as the digestive vacuole is known to be acidic (pH 4.7); chloroquine then cannot leave by diffusion. Chloroquine caps hemozoin molecules to prevent further biocrystallization of heme, thus leading to heme buildup. Chloroquine binds to heme (or FP) to form what is known as the FP-Chloroquine complex; this complex is highly toxic to the cell and disrupts membrane function. — NCATS

Clinical trial activity

171 trials · 195 clinical orgs · 11 marketing orgs

Phase 1
24
Phase 2
75
Phase 3
55
Phase 4
38

Earliest trial started Nov 1, 1993 (NCT01019408)

Timeline

1940s

  1. Oct 31, 1949

    Earliest FDA Approval

  2. Oct 31, 1949

    Sanofi-Aventis — NDA Secondary Org

1970s

  1. Dec 11, 1974

    Impax Laboratories — Marketing Organization

  2. Jul 9, 1975

    Hikma — Marketing Organization

1980s

  1. Jan 13, 1982

    Teva — Marketing Organization

  2. Dec 21, 1982

    Watson Pharmaceuticals — Marketing Organization

1990s

  1. Jan 1, 1999

    Earliest Phase 1 Sponsor(trial)

2000s

  1. Jan 1, 2001

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2001

    Earliest Phase 3 Sponsor(trial)

  3. Dec 3, 2009

    IPCA Laboratories Ltd. — Marketing Organization

2010s

  1. Jan 21, 2011

    Natco Pharma — Marketing Organization

2020s

  1. Sep 3, 2021

    Suven Life Sciences Limited — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Combination products

  • aralen phosphate w/ primaquine phosphate

    with primaquine

Approval history

  • approvedOct 31, 1949

Chemistry & pharmacology

Loading structure…

SMILES

CCN(CC)CCCC(C)NC1=C2C=CC(Cl)=CC2=NC=C1
Mol. weight
319.872 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • aralen
  • aralen
  • aralen
  • arechin
  • avloclor
  • avloclor
  • chingamin phosphate
  • chloraquine
  • chloraquine
  • chloraquine
  • chlorochin
  • chlorochin
  • chlorochin
  • chlorochine
  • chlorochine
  • chloroquina
  • chloroquina
  • chloroquine
  • chloroquine
  • chloroquine
  • chloroquine
  • chloroquine
  • chloroquine
  • chloroquine
  • chloroquine
  • chloroquine bis(dihydrogenphosphate) dihydrate
  • chloroquine diphosphate
  • chloroquine diphosphate
  • chloroquine diphosphate
  • chloroquine diphosphate
  • chloroquine diphosphate
  • chloroquine diphosphate, (-)-isomer
  • chloroquine diphosphate, (+-)-isomer
  • chloroquine diphosphate, (+)-isomer
  • chloroquine hcl
  • chloroquine hcl
  • chloroquine hcl
  • chloroquine hydrochloride
  • chloroquine hydrochloride
  • chloroquine hydrochloride
  • chloroquine hydrochloride
  • chloroquine phosphate
  • chloroquine phosphate
  • chloroquine phosphate
  • chloroquine phosphate
  • chloroquine phosphate
  • chloroquine phosphate
  • chloroquine sulfate
  • chloroquine sulfate
  • chloroquine sulfate
  • chloroquine sulfate
  • chloroquine sulfate
  • chloroquine sulfate
  • chloroquine sulfate
  • chloroquine sulphate
  • chloroquine sulphate
  • chloroquine sulphate
  • chloroquinium
  • chloroquinium
  • chloroquinum
  • chloroquinum
  • cloroquina
  • cloroquina
  • delagil
  • khingamin phosphate
  • malarivon
  • n4-(7-chloro-4-quinolinyl)-n1,n1-diethyl-1,4-pentanediamine
  • n4-(7-chloro-4-quinolinyl)-n1,n1-diethyl-1,4-pentanediamine
  • n(4)-(7-chloro-4-quinolinyl)-n(1),n(1)-diethyl-1,4-pentanediamine, phosphate (1:2)
  • nsc-187208
  • nsc-187208
  • plasmodium falciparum nf54
  • resochin
  • unspecified phosphate of chloroquine diphosphate

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06666491Phase 3Nov 7, 2024GlaxoSmithKline
NCT06083688Phase 4Oct 31, 2024Kamuzu University of Health Sciences, University of Liverpool
NCT06076837Phase 1Dec 31, 2023Agenus Inc., HonorHealth Research Institute, TGen Drug Development, University of Arizona
NCT05788094Phase 4Jun 26, 2023Mahidol University
NCT05980156Phase 4Feb 13, 2023Doris Duke Charitable Foundation, Kamuzu University of Health Sciences, University of Maryland
NCT06044805Phase 4Dec 19, 2022Ethiopian Public Health Institute, Wollega University
NCT05647330Phase 2Dec 15, 2022Henan Medical University
NCT05244954Phase 4Feb 1, 2022Doris Duke Charitable Foundation, Kamuzu University of Health Sciences, University of Maryland
NCT05443178Phase 1Jan 4, 2022University of Zurich
NCT04704999Phase 4Oct 1, 2021Mahidol University, PATH, University of Oxford
NCT04443270Phase 1Jul 27, 2020CMN "20 de Noviembre"
NCT04447534Phase 3Jun 23, 2020Tanta University
NCT04403555Phase 2/Phase 3 (Phase 3)Jun 1, 2020Tanta University
NCT04397679Phase 1May 20, 2020National Cancer Institute (NCI), Wayne State University
NCT04382846Phase 3May 8, 2020Tanta University
NCT04360759Phase 3May 1, 2020University of Cape Town
NCT04333732Phase 3Apr 30, 2020Bill and Melinda Gates Foundation, University of London, Washington University in St. Louis, Wits University
NCT04333628Phase 2/Phase 3 (Phase 3)Apr 30, 2020Emek Medical Center, T MAY BIOPHARMA LTD.
NCT04303507N/AApr 30, 2020University of Oxford
NCT04349371Phase 2Apr 30, 2020Columbia University
Showing 20 of 171 trials
Page 1 / 9

Organizations

Research & Development (195)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Institute of Allergy and Infectious Diseases (NIAID)Government12952005
PfizerFor profit121232003
University of LondonAcademic/Hospital121041993
Mahidol UniversityAcademic/Hospital11232003
University of OxfordAcademic/Hospital111142007
GlaxoSmithKlineFor profit8732003
Medicines for Malaria VentureAcademic/Hospital8232007
Centers for Disease Control and Prevention (CDC)Government6622003
Menzies School of Health ResearchAcademic/Hospital6532004
Tanta UniversityAcademic/Hospital6612020
Radboud UniversityAcademic/Hospital5512011
United States ArmyGovernment5322003
World Health OrganizationGovernment5031993
Fundação de Medicina Tropical Dr. Heitor Vieira DouradoAcademic/Hospital4422018
Maastricht UniversityAcademic/Hospital4422013
University of Sao PauloAcademic/Hospital4332002
Washington University in St. LouisAcademic/Hospital4432006
Wellcome TrustAcademic/Hospital4032004
Bandim Health ProjectGovernment3312001
Bill and Melinda Gates FoundationAcademic/Hospital3022014
195 organizations
Page 1 / 10

Marketing (11)

OrganizationOrg typeRelationshipDate
BayerFor profitNDA—
HikmaFor profitMKTGJul 9, 1975
IPCA Laboratories Ltd.For profitMKTGDec 3, 2009
Impax LaboratoriesFor profitMKTGDec 11, 1974
MD PharmaFor profitMKTG—
Natco PharmaFor profitMKTGJan 21, 2011
Puracap PharmaceuticalFor profitMKTG—
Sanofi-AventisFor profitNDA2Oct 31, 1949
Suven Life Sciences LimitedFor profitMKTGSep 3, 2021
TevaFor profitMKTGJan 13, 1982
Watson PharmaceuticalsFor profitMKTGDec 21, 1982