tafenoquine succinate
Trade name: arakoda
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
Earliest trial started May 1, 1997 (NCT02491606)
Timeline
1990s
- Jan 1, 1997
Earliest Phase 2 Sponsor(trial)
2000s
- Jan 1, 2009
GlaxoSmithKline — Earliest Phase 1 Sponsor(trial)
2010s
- Jan 15, 2013
Orphan Drug Designation
- Jan 1, 2015
GlaxoSmithKline — Earliest Phase 3 Sponsor(trial)
- Jul 20, 2018
Earliest FDA Approval
- Jul 20, 2018
GlaxoSmithKline — NDA Secondary Org
- Aug 8, 2018
60 Degrees Pharmaceuticals LLC — First NDA Organization
- Aug 8, 2018
60 Degrees Pharmaceuticals LLC — NDA Secondary Org
- Aug 8, 2018
60 Degrees Pharmaceuticals LLC — NDA Organization
Indications
Approved for
Mechanism of action
- Plasmodium falciparumANTAGONIST
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
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
- ChEMBLCHEMBL298470 ↗
- WikipediaTafenoquine ↗
- NCATSDL5J0B8VSS ↗
- ChEMBLCHEMBL2364635 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07060794 | Phase 4 | Nov 30, 2025 | Menzies School of Health Research |
| NCT07060404 | Phase 2/Phase 3 (Phase 3) | Aug 31, 2025 | Curtin University, Government of Papua New Guinea, Menzies School of Health Research |
| NCT07052162 | Phase 4 | Jul 31, 2025 | Curtin University, Government of Papua New Guinea, University of Western Australia |
| NCT06656351 | Phase 2 | Feb 28, 2025 | 60 Degrees Pharmaceuticals LLC |
| NCT06666491 | Phase 3 | Nov 7, 2024 | GlaxoSmithKline |
| NCT06575647 | Phase 4 | Oct 1, 2024 | Mahidol University |
| NCT06207370 | Phase 2 | Jun 17, 2024 | 60 Degrees Pharmaceuticals LLC |
| NCT06148792 | Phase 3 | Apr 1, 2024 | Addis 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 |
| NCT05947812 | Phase 2 | Aug 1, 2023 | 60P Australia Pty Ltd |
| NCT05788094 | Phase 4 | Jun 26, 2023 | Mahidol University |
| NCT05203744 | Phase 4 | May 10, 2022 | Government of Australia, United States Navy |
| NCT04984759 | Phase 4 | Nov 1, 2021 | Mahidol University, University of Oxford |
| NCT05081089 | Phase 2 | Oct 12, 2021 | Malaria Research and Training Center, Bamako, Mali, University of London |
| NCT04704999 | Phase 4 | Oct 1, 2021 | Mahidol University, PATH, University of Oxford |
| NCT04411836 | Phase 3 | Jan 1, 2021 | Addis 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 |
| NCT04533347 | Phase 2 | Oct 31, 2020 | 60 Degrees Pharmaceuticals LLC, Peachtree BioResearch Solutions Inc. |
| NCT04609098 | Phase 2 | Oct 29, 2020 | Malaria Research and Training Center, Bamako, Mali, University of London |
| NCT02802501 | Phase 3 | Jan 15, 2018 | GlaxoSmithKline, Medicines for Malaria Venture |
| NCT03320174 | Phase 2 | Oct 5, 2017 | 60 Degrees Pharmaceuticals LLC |
| NCT02563496 | Phase 2 | Feb 6, 2017 | GlaxoSmithKline, Medicines for Malaria Venture |
Organizations
Research & Development (28)
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| 60 Degrees Pharmaceuticals LLC | For profit | NDA2 | Aug 8, 2018 |
| 60 Degrees Pharmaceuticals LLC | For profit | NDA | Aug 8, 2018 |
| GlaxoSmithKline | For profit | NDA2 | Jul 20, 2018 |