clioquinol

Trade name: nystaform

Small moleculeapproved

Approved

Jun 1, 1969

Clioquinol is a broad-spectrum antibacterial with antifungal properties, bacteriostatic. It is used as an antifungal and antiprotozoal topical drug OTC product for treatment of human infections. Previousely was used for wide number of intestinal disorders including lambliasis, shigellosis, balantidiral dysentery and some forms of diarrheas. The physiologic effect of clioquinol is by increased histamine release and cell-mediated immunity. It is a member of a family hydroxyquinolines which inhibit certain enzymes related to DNA replication. It is a copper, iron and zink chelating agent. It is an organic molecule with a quinolinic acid as its apparent core which itself is a neurotransmitter. In large doses it possesses neurotoxicity and may induce neurological disease such as subacute myelo-optic neuropathy by creating copper deficiency that leads to zink excess. SMON (Sub-Acute-Myelo-Optical-Neuropathy) - a polio-like disease began as an epidemic in 1959 in Japan was believed to be a Clioquinol caused. Clioquinol is a standardized chemical allergen. It has been resurrected as a potential treatment for Alzheimer's disease since it perturbs metallo-chemistry of amyloid and clioquinol treatment has been shown to be beneficial in a mouse model of Alzheimer's disease. — NCATS

Clinical trial activity

2 trials · 3 clinical orgs · 1 marketing orgs

Phase 1
1
Phase 2
1
Phase 3
1
Phase 4
0

Earliest trial started Aug 1, 2009 (NCT00963495)

Timeline

1960s

  1. Jun 1, 1969

    Earliest FDA Approval

2000s

  1. Jan 1, 2009

    Earliest Phase 1 Sponsor(trial)

2010s

  1. Jan 1, 2012

    Earliest Phase 3 Sponsor(trial)

Indications

Mechanism of action

  • IronCHELATING AGENT

    Iron chelating agent

    Used as antibiotic against diarrhea in the 70s, but nowadays considered in cancer treatments (off-label), for its chelator and ionophore properties with capacity to inhibit proteosome

  • CopperCHELATING AGENT

    Copper chelating agent

    Used as antibiotic against diarrhea in the 70s, but nowadays considered in cancer treatments (off-label), for its chelator and ionophore properties with capacity to inhibit proteosome

  • ZincCHELATING AGENT

    Zinc chelating agent

    Used as antibiotic against diarrhea in the 70s, but nowadays considered in cancer treatments (off-label), for its chelator and ionophore properties with capacity to inhibit proteosome

Combination products

Approval history

  • approvedJun 1, 1969

Chemistry & pharmacology

Loading structure…

SMILES

OC1=C2N=CC=CC2=C(Cl)C=C1I
Mol. weight
305.5 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • 5-chlor-7-jod-8-hydroxy-chinolin
  • 5-chlor-7-jod-8-hydroxy-chinolin
  • 5-chloro-7-iodo-8-hydroxyquinoline
  • 5-chloro-7-iodo-8-hydroxyquinoline
  • 5-chloro-7-iodo-8-quinolinol
  • 5-chloro-7-iodo-8-quinolinol
  • 5-chloro-7-iodoquinolin-8-ol
  • 5-chloro-7-iodoquinolin-8-ol
  • 5-chloro-8-hydroxy-7-iodoquinoline
  • 5-chloro-8-hydroxy-7-iodoquinoline
  • 7-iodo-5-chloro-8-hydroxyquinoline
  • 7-iodo-5-chloro-8-hydroxyquinoline
  • 7-iodo-5-chloroxine
  • 7-iodo-5-chloroxine
  • chloroiodoquin
  • chloroiodoquin
  • chloroiodoquin
  • chloroiodoquine
  • cleoquinol
  • clioquinol
  • clioquinol
  • clioquinol
  • clioquinol
  • clioquinol
  • clioquinol
  • clioquinol
  • clioquinol
  • clioquinol
  • clioquinol
  • clioquinolum
  • clioquinolum
  • cliquinol
  • domeform-hc
  • domeform-hc
  • iodochlorhydroxyquin
  • iodochlorhydroxyquin
  • iodochlorhydroxyquin
  • iodochlorhydroxyquin
  • iodochlorhydroxyquinoline
  • iodochlorhydroxyquinoline
  • iodochlorohydroxyquin
  • iodochlorohydroxyquin
  • iodochloroxyquinoline
  • iodochloroxyquinoline
  • nystaform
  • nystaform
  • oralcer
  • oralcer
  • quin-o-creme
  • quin-o-creme
  • vioform
  • vioform
  • vioform

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT01429701Phase 3May 1, 2012EMS S/A, Medicin Instituto da Pele
NCT00963495Phase 1Aug 1, 2009University of Toronto
Showing 2 of 2 trials
Page 1 / 1

Organizations

Research & Development (3)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
EMS S/AFor profit1112012
Medicin Instituto da PeleAcademic/Hospital1012012
University of TorontoAcademic/Hospital1112009
3 organizations
Page 1 / 1

Marketing (1)

OrganizationOrg typeRelationshipDate
BayerFor profitNDA