tafenoquine succinate

Trade name: arakoda

Small moleculeapprovedOrphan Drug FDABreakthrough Therapy FDA

Approved

Jul 20, 2018

Tafenoquine is anti-malaria drug originated in Walter reed army institute of research and developed by GSK and 60 Degrees Pharmaceuticals. In 2018 United States Food and Drug Administration (FDA) approved single dose tafenoquine for the radical cure (prevention of relapse) of Plasmodium vivax malaria. Tafenoquine, an 8-aminoquinoline antimalarial, is active against all the stages of Plasmodium species that include the hypnozoite (dormant stage) in the liver. Studies in vitro with the erythrocytic forms of Plasmodium falciparum suggest that tafenoquine may exert its effect by inhibiting hematin polymerization and inducing apoptotic like death of the parasite. In addition to its effect on the parasite, tafenoquine causes red blood cell shrinkage in vitro. Tafenoquine is active against pre-erythrocytic (liver) and erythrocytic (asexual) forms as well as gametocytes of Plasmodium species that include P. falciparum and P. vivax. The activity of tafenoquine against the pre-erythrocytic liver stages of the parasite, prevents the development of the erythrocytic forms of the parasite. — NCATS

Clinical trial activity

33 trials · 28 clinical orgs · 2 marketing orgs

Phase 1
6
Phase 2
18
Phase 3
6
Phase 4
7

Earliest trial started May 1, 1997 (NCT02491606)

Timeline

1990s

  1. Jan 1, 1997

    Earliest Phase 2 Sponsor(trial)

2000s

  1. Jan 1, 2009

    GlaxoSmithKline — Earliest Phase 1 Sponsor(trial)

2010s

  1. Jan 15, 2013

    Orphan Drug Designation

  2. Jan 1, 2015

    GlaxoSmithKline — Earliest Phase 3 Sponsor(trial)

  3. Jul 20, 2018

    Earliest FDA Approval

  4. Jul 20, 2018

    GlaxoSmithKline — NDA Secondary Org

  5. Aug 8, 2018

    60 Degrees Pharmaceuticals LLC — First NDA Organization

  6. Aug 8, 2018

    60 Degrees Pharmaceuticals LLC — NDA Secondary Org

  7. Aug 8, 2018

    60 Degrees Pharmaceuticals LLC — NDA Organization

Indications

Mechanism of action

  • Plasmodium falciparum antagonist

  • Unspecified targetOTHER

    Unknown

    Hypothesized that redox cycling of the drug and oxidation of the redox product generates reactive oxygen species that provide the killing effect.

    Active against the pre-erythrocytic and erythrocytic stages.

Approval history

  • approvedPriority reviewBreakthroughJul 20, 2018

Chemistry & pharmacology

Loading structure…

SMILES

COc1cc(C)c2c(Oc3cccc(C(F)(F)F)c3)c(OC)cc(NC(C)CCCN)c2n1
Mol. weight
463.5 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • butanedioic acid, compd. with n4-(2,6-dimethoxy-4-methyl-5-(3-(trifluoromethyl)phenoxy)-8-quinolinyl)-1,4-pentanediamine (1:1)
  • n(4)-(2,6-dimethoxy-4-methyl-5-((3-trifluoromethyl)phenoxy)-8-quinolinyl)-1,4-pentanediamine
  • sb-252263aab
  • sb-252263aab
  • tafenoquine
  • tafenoquine
  • tafenoquine
  • tafenoquine
  • tafenoquine
  • tafenoquine
  • tafenoquine maleate
  • tafenoquine succinate
  • tafenoquine succinate
  • tafenoquine succinate
  • tafenoquine succinate
  • tafenoquine succinate
  • tafenoquine succinate
  • wr 238605
  • wr-238605
  • wr-238605
  • wr-238605

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07060794Phase 4Nov 30, 2025Menzies School of Health Research
NCT07060404Phase 2/Phase 3 (Phase 3)Aug 31, 2025Curtin University, Government of Papua New Guinea, Menzies School of Health Research
NCT07052162Phase 4Jul 31, 2025Curtin University, Government of Papua New Guinea, University of Western Australia
NCT06656351Phase 2Feb 28, 202560 Degrees Pharmaceuticals LLC
NCT06666491Phase 3Nov 7, 2024GlaxoSmithKline
NCT06575647Phase 4Oct 1, 2024Mahidol University
NCT06207370Phase 2Jun 17, 202460 Degrees Pharmaceuticals LLC
NCT06148792Phase 3Apr 1, 2024Addis Ababa University, Arba Minch University, Ethiopia, Curtin University, Fundação de Medicina Tropical Dr. Heitor Vieira Dourado, Government of Papua New Guinea, Menzies School of Health Research, University of Melbourne
NCT05947812Phase 2Aug 1, 202360P Australia Pty Ltd
NCT05788094Phase 4Jun 26, 2023Mahidol University
NCT05203744Phase 4May 10, 2022Government of Australia, United States Navy
NCT04984759Phase 4Nov 1, 2021Mahidol University, University of Oxford
NCT05081089Phase 2Oct 12, 2021Malaria Research and Training Center, Bamako, Mali, University of London
NCT04704999Phase 4Oct 1, 2021Mahidol University, PATH, University of Oxford
NCT04411836Phase 3Jan 1, 2021Addis Ababa University, Ethiopian Public Health Institute, Mahidol University, Menzies School of Health Research, National Centre for Parasitology, Entomology and Malaria Control, Cambodia, Universitas Sumatera Utara, University of Melbourne
NCT04533347Phase 2Oct 31, 202060 Degrees Pharmaceuticals LLC, Peachtree BioResearch Solutions Inc.
NCT04609098Phase 2Oct 29, 2020Malaria Research and Training Center, Bamako, Mali, University of London
NCT02802501Phase 3Jan 15, 2018GlaxoSmithKline, Medicines for Malaria Venture
NCT03320174Phase 2Oct 5, 201760 Degrees Pharmaceuticals LLC
NCT02563496Phase 2Feb 6, 2017GlaxoSmithKline, Medicines for Malaria Venture
Showing 20 of 33 trials
Page 1 / 2

Organizations

Research & Development (28)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
GlaxoSmithKlineFor profit121132003
Medicines for Malaria VentureAcademic/Hospital9032009
Mahidol UniversityAcademic/Hospital6232003
60 Degrees Pharmaceuticals LLCFor profit5522017
Menzies School of Health ResearchAcademic/Hospital4322021
United States ArmyGovernment4411997
Curtin UniversityAcademic/Hospital3222024
Government of Papua New GuineaGovernment3022024
SmithKline BeechamFor profit3011997
Addis Ababa UniversityAcademic/Hospital2012021
Malaria Research and Training Center, Bamako, MaliAcademic/Hospital2012020
United States NavyGovernment2121998
University of LondonAcademic/Hospital2212020
University of MelbourneAcademic/Hospital2012021
University of OxfordAcademic/Hospital2212021
60P Australia Pty LtdFor profit1112023
Arba Minch University, EthiopiaAcademic/Hospital1012024
Ethiopian Public Health InstituteAcademic/Hospital1012021
Fundação de Medicina Tropical Dr. Heitor Vieira DouradoAcademic/Hospital1012024
Government of AustraliaGovernment1012022
28 organizations
Page 1 / 2

Marketing (3)

OrganizationOrg typeRelationshipDate
60 Degrees Pharmaceuticals LLCFor profitNDA2Aug 8, 2018
60 Degrees Pharmaceuticals LLCFor profitNDAAug 8, 2018
GlaxoSmithKlineFor profitNDA2Jul 20, 2018