Tafenoquine
Small molecule targets TMPRSS2 via inhibition
Regulatory milestones approvals, filings & regulatory actions · 1 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Approved | US (FDA) | KRINTAFEL | — | 2018-07-20 | fda.gov ↗ |
Trials 31 · a red edge is where a trial was stopped
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 01 trial | ||||||
| Phase 0 | NCT07373743 | May 2026 → Mar 2027 expected | — | State University of New York - Upstate Medical University | Not yet recruiting | No outcome recorded |
| Phase 14 trials | ||||||
| Phase 1 | NCT02751294 | May → Aug 2016 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 1 | NCT02658435 | Feb 2016 → Sep 2017 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 1 | NCT02184637 | Jul 2014 → Apr 2015 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 1 | NCT01928914 | Jul 2011 → Jun 2012 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 210 trials | ||||||
| Phase 2 | NCT06656351 | Nov 2025 → Feb 2027 expected | babesiosis | 60 Degrees Pharmaceuticals LLC | Recruiting | No outcome recorded |
| Phase 2 | NCT05947812 | Aug 2023 → Apr 2024 | COVID-19 | 60P Australia Pty Ltd | Unknown | No outcome recorded |
| Phase 2 | NCT05081089 | Oct → Dec 2021 | Plasmodium falciparum malaria | London School of Hygiene and Tropical Medicine | Completed | No outcome recorded |
| Phase 2 | NCT04609098 | Oct → Dec 2020 | Plasmodium falciparum malaria | London School of Hygiene and Tropical Medicine | Completed | No outcome recorded |
| Phase 2 | NCT02563496 | Feb 2017 → Dec 2019 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 2 | NCT01376167 | Apr 2014 → Nov 2016 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 2 | NCT01290601 | Sep 2003 → Jan 2005 | Plasmodium vivax malaria | U.S. Army Medical Research and Development Command | Terminated | No outcome recorded |
| Phase 2 | NCT02488980 | May → Oct 2000 | Plasmodium falciparum malaria | U.S. Army Medical Research and Development Command | Completed | No outcome recorded |
| Phase 2 | NCT02488902 | Aug → Sep 1998 | malaria | U.S. Army Medical Research and Development Command | Completed | No outcome recorded |
| Phase 2 | NCT02491606 | May → Sep 1997 | malaria | U.S. Army Medical Research and Development Command | Completed | No outcome recorded |
| Phase 2/31 trial | ||||||
| Phase 2/3 | NCT07060404 | Apr → Dec 2026 expected | — | Curtin University | Not yet recruiting | No outcome recorded |
| Phase 36 trials | ||||||
| Phase 3 | NCT06666491 | Nov 2024 → May 2026 overdue | Plasmodium vivax malaria | GlaxoSmithKline | Recruiting | No outcome recorded |
| Phase 3 | NCT05690841 | Oct 2024 → May 2027 expected | Plasmodium vivax malaria | University of California, San Francisco | Recruiting | No outcome recorded |
| Phase 3 | NCT06148792 | May 2024 → Mar 2027 expected | Plasmodium vivax malaria | Menzies School of Health Research | Recruiting | No outcome recorded |
| Phase 3 | NCT04411836 | Apr 2021 → Sep 2024 | Plasmodium vivax malaria | Menzies School of Health Research | Completed | No outcome recorded |
| Phase 3 | NCT02802501 | Apr 2018 → Aug 2019 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 3 | NCT02216123 | Apr 2015 → Nov 2016 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 47 trials | ||||||
| Phase 4 | NCT07060794 | Jun 2026 → Jun 2028 expected | Plasmodium vivax malaria | Menzies School of Health Research | Not yet recruiting | No outcome recorded |
| Phase 4 | NCT07403643 | Apr → Dec 2026 expected | malaria | Curtin University | Not yet recruiting | No outcome recorded |
| Phase 4 | NCT07052162 | Oct 2025 → Mar 2026 overdue | — | Curtin University | Recruiting | No outcome recorded |
| Phase 4 | NCT06575647 | Feb → Oct 2025 | Plasmodium vivax malaria | Shoklo Malaria Research Unit | Completed | No outcome recorded |
| Phase 4 | NCT04984759 | Jul 2023 → Jun 2025 | — | University of Oxford | Withdrawn | No outcome recorded |
| Phase 4 | NCT05788094 | Jun 2023 → Feb 2026 overdue | Plasmodium vivax malaria | Shoklo Malaria Research Unit | Recruiting | No outcome recorded |
| Phase 4 | NCT05203744 | May → Dec 2022 | — | Naval Medical Research Center | Unknown | No outcome recorded |
| Phase not applicable1 trial | ||||||
| — | NCT05540470 | Sep 2022 → Mar 2025 | Plasmodium vivax malaria | Cayenne Hospital | Completed | No outcome recorded |
| Phase not stated1 trial | ||||||
| — | NCT06478641 | — | babesiosis | 60 Degrees Pharmaceuticals LLC | Available | No outcome recorded |
Also used as a comparator or background therapy in 8 trials
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 12 trials | ||||||
| Phase 1 | NCT01205178 Comparator | Jul 2009 → Apr 2013 | malaria | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 1 | NCT00871156 Comparator | Mar → Aug 2009 | malaria | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 24 trials | ||||||
| Phase 2 | NCT07430592 Comparator | Jul 2026 → Nov 2028 expected | Plasmodium vivax malaria | R. Kiplin Guy | Not yet recruiting | No outcome recorded |
| Phase 2 | NCT06207370 Comparator | Jun 2024 → Mar 2027 expected | babesiosis | 60 Degrees Pharmaceuticals LLC | Recruiting | No outcome recorded |
| Phase 2 | NCT04533347 Comparator | Feb 2021 → Jun 2022 | COVID-19 | 60 Degrees Pharmaceuticals LLC | Completed | No outcome recorded |
| Phase 2 | NCT03320174 Comparator | Oct 2017 → Jul 2021 | — | 60 Degrees Pharmaceuticals LLC | Completed | No outcome recorded |
| Phase 41 trial | ||||||
| Phase 4 | NCT04704999 Comparator | Jul 2024 → Oct 2027 expected | Plasmodium vivax malaria | University of Oxford | Recruiting | No outcome recorded |
| Phase not applicable1 trial | ||||||
| — | NCT07533136 Comparator | May 2026 → Oct 2028 expected | Plasmodium vivax malaria | Walter Reed Army Institute of Research (WRAIR) | Not yet recruiting | No outcome recorded |
Evidence & citations 15 cited values
Every value below carries the sentence it was read from. 42 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | Tafenoquine | “SB-252263 (Tafenoquine, TQ) is an 8-aminoquinoline (8-AQ) antimalarial drug being developed by GlaxoSmithKline (GSK), the U.S. Army Medical Research and Materiel Command...” NCT01205178 ↗39“The fMDA regimen will include 25mg/kg chloroquine (CQ) plus a single 300mg dose of tafenoquine (TQ) for individuals age ≥16 years, and 25mg/kg of CQ plus 7 days of 0.5mg/kg/day...” PMID 40321759 ↗ Apr 2025 “2. OR tafenoquine (TQ) (150 mg tablets): 2 tablets as a single dose (orally),” NCT05540470 ↗ “SJ733 combined with Tafenoquine” NCT07430592 ↗ “Tafenoquine” NCT00871156 ↗ |
| Known as | ARAKODA | “The goal of this clinical trial is to learn how people's different genetic makeups affects how their bodies convert the FDA approved drug ARAKODA (tafenoquine) to its active form.” NCT07373743 ↗ |
| Known as | KODATEF | “Tafenoquine KODATEF® 100 mg film-coated tablets will be purchased from Biocelect (Suite 5.02, Level 5, 139 Macquarie Street, Sydney NSW, 2000 Australia), 450 mg (4 1/2 tablets)...” NCT05788094 ↗1“Tafenoquine KODATEF® 100 mg film-coated tablets will be purchased from Biocelect” NCT06575647 ↗ |
| Known as | Krintafel | ChEMBL registry synonym — accepted as the source's own label CHEMBL298470 ↗ |
| Known as | SB-252263-AAB | ChEMBL registry synonym — accepted as the source's own label CHEMBL298470 ↗ |
| Known as | SB-252263-AX | ChEMBL registry synonym — accepted as the source's own label CHEMBL298470 ↗ |
| Known as | SB252263 | “A Phase 1, Multi-center, Single-masked, Randomized, Placebo-controlled, Parallel-group Study to Investigate the Ophthalmologic Safety and Pharmacodynamics of 300mg Single Doses...” NCT02658435 ↗10“SB-252263 (Tafenoquine, TQ) is an 8-aminoquinoline (8-AQ) antimalarial drug being developed by GlaxoSmithKline (GSK), the U.S. Army Medical Research and Materiel Command...” NCT01205178 ↗ “A Multi-centre, Double-blind, Randomised, Parallel-group, Active Controlled Study to Evaluate the Efficacy, Safety and Tolerability of Tafenoquine (SB-252263, WR238605) in...” NCT01376167 ↗ “An Open Label, Non-comparative, Multicenter Study to Assess the Pharmacokinetics, Safety and Efficacy of Tafenoquine (SB-252263, WR238605) in the Treatment of Pediatric...” NCT02563496 ↗ “A Randomized, Double Blind, Placebo Controlled Evaluation of Weekly Tafenoquine (WR 238605/SB252263) Compared to Mefloquine for Chemosuppression of Plasmodium Falciparum in...” NCT02488980 ↗ “A Five-cohort, Randomized, Open-label, Parallel-group Study to Evaluate the Pharmacokinetics of a Single Dose of Tafenoquine (SB252263) 300mg” NCT02184637 ↗ “Evaluation of Weekly Tafenoquine (SB 252263 / WR 238605) Compared to Placebo for Chemosuppression of Plasmodium Falciparum in Western Kenya” NCT02491606 ↗ “Single Oral 300 mg Doses of Tafenoquine (SB-252263) Tablets + 30 mg Tafenoquine Stable Isotope Labelled (SIL) Solution” NCT02751294 ↗ “SB-252263 (tafenoquine, TQ) is a new 8-aminoquinoline antimalarial drug being developed by GlaxoSmithKline” NCT01928914 ↗ “Tafenoquine (SB-252263, WR238605) Co-administered With Dihydroartemisinin-piperaquine (DHA-PQP)” NCT02802501 ↗ “Tafenoquine (SB-252263, WR238605)” NCT02216123 ↗ |
| Known as | Tafenoquina | ChEMBL registry synonym — accepted as the source's own label CHEMBL298470 ↗ |
| Known as | tafenoquine succinate | “Tablet contains TQ as tafenoquine succinate.” NCT02658435 ↗ |
| Known as | TFQ | “We identified antimalarial drug tafenoquine (TFQ), which is approved for radical cure of Plasmodium vivax and malaria prophylaxis, as a top candidate to inhibit Mpro protease activity.” PMID 35101449 ↗ Jan 20221“Ph 2B/3 Tafenoquine (TFQ) Study in Prevention of Vivax Relapse” NCT01376167 ↗ |
| Known as | WR 238605 | “A Multi-centre, Double-blind, Randomised, Parallel-group, Active Controlled Study to Evaluate the Efficacy, Safety and Tolerability of Tafenoquine (SB-252263, WR238605) in...” NCT01376167 ↗5“An Open Label, Non-comparative, Multicenter Study to Assess the Pharmacokinetics, Safety and Efficacy of Tafenoquine (SB-252263, WR238605) in the Treatment of Pediatric...” NCT02563496 ↗ “A Randomized, Double Blind, Placebo Controlled Evaluation of Weekly Tafenoquine (WR 238605/SB252263) Compared to Mefloquine for Chemosuppression of Plasmodium Falciparum in...” NCT02488980 ↗ “Evaluation of Weekly Tafenoquine (SB 252263 / WR 238605) Compared to Placebo for Chemosuppression of Plasmodium Falciparum in Western Kenya” NCT02491606 ↗ “Tafenoquine (SB-252263, WR238605) Co-administered With Dihydroartemisinin-piperaquine (DHA-PQP)” NCT02802501 ↗ “Tafenoquine (SB-252263, WR238605)” NCT02216123 ↗ |
| Action | Inhibit | “We also found that TFQ inhibited human transmembrane protease serine 2 (TMPRSS2).” PMID 35101449 ↗ Jan 2022 |
| Modality | Small molecule | “SB-252263 (Tafenoquine, TQ) is an 8-aminoquinoline (8-AQ) antimalarial drug” NCT01205178 ↗ |
| Route | Oral | “Patients received 3-day chloroquine plus oral single-dose tafenoquine as dispersible tablets (50 mg) or film-coated tablets (150 mg).” PMID 34871570 ↗ Dec 2021 |
| Target | TMPRSS2 | “We also found that TFQ inhibited human transmembrane protease serine 2 (TMPRSS2).” PMID 35101449 ↗ Jan 2022 |