Tafenoquine
Small molecule targets TMPRSS2 via inhibition
Regulatory milestones approvals, filings & regulatory actions · 2 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Filed Plasmodium vivax malaria 1 milestone | |||||
| Filed | US (FDA) | — | Plasmodium vivax malaria | 2017-11-28 | “announced the submission of a new drug application (NDA) by GSK to the United States Food and Drug Administration (FDA), seeking approval of single-dose tafenoquine” gsk.com ↗ |
| Approved Indication not stated 1 milestone | |||||
| Approved | US (FDA) | KRINTAFEL | — | 2018-07-20 | fda.gov ↗ |
Trials 32
| 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 · 1 met primary | ||||||
| Phase 1 | NCT02751294 | May → Aug 2016 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | Met primary |
| 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 211 trials · 1 met primary · 1 missed | ||||||
| Phase 2 | NCT07835321 | Sep 2026 → Dec 2029 expected | Plasmodium vivax malaria | University of Oxford | Not yet recruiting | No outcome recorded |
| 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 | Missed primary |
| 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 | Met primary |
| 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 · 1 met primary · 2 missed | ||||||
| Phase 3 | NCT06666491 | Nov 2024 → May 2027 expected | 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 | Missed primary |
| Phase 3 | NCT02802501 | Apr 2018 → Aug 2019 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | Met primary |
| Phase 3 | NCT02216123 | Apr 2015 → Nov 2016 | Plasmodium vivax malaria | GlaxoSmithKline | Completed | Missed primary |
| 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 |
| Comparator or background therapy8 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 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 4 | NCT04704999 Comparator | Jul 2024 → Oct 2027 expected | Plasmodium vivax malaria | University of Oxford | Recruiting | No outcome recorded |
| — | NCT07533136 Comparator | May 2026 → Oct 2028 expected | Plasmodium vivax malaria | Walter Reed Army Institute of Research (WRAIR) | Not yet recruiting | No outcome recorded |
News releases announcing trial results or a regulatory action · 11
| Date | Issuer | Release |
|---|---|---|
| 2024-12-04 | GlaxoSmithKline | Regulatory First single-dose medicine for P. vivax malaria prequalified by WHO and included in WHO Guidelines gsk.com ↗
GSK plc (LSE/NYSE: GSK) and Medicines for Malaria Venture (MMV) announced today that the World Health Organization (WHO) has awarded prequalification to tafenoquine, the first single-dose medicine for the prevention of relapse of Plasmodium vivax (P. vivax) malaria. |
| 2021-01-08 | GlaxoSmithKline | Regulatory GSK, MMV filing for Kozenis (tafenoquine) in paediatric populations with Plasmodium vivax malaria accepted by Australian Therapeutic Goods Administration gsk.com ↗
the Australian Therapeutic Goods Administration (TGA) accepted the submission of a Category 1 application to extend the indication of single-dose Kozenis (tafenoquine) to paediatric populations |
| 2020-11-19 | GlaxoSmithKline | Results GSK and MMV present positive data on treatment for Plasmodium vivax malaria in children from 6 months up to 15 years of age gsk.com ↗
GSK and Medicines for Malaria Venture (MMV) today presented positive data from the TEACH study of tafenoquine, an 8-aminoquinoline, for the prevention of relapse (radical cure) of Plasmodium vivax (P. vivax) malaria in children and adolescents. |
| 2019-01-16 | GlaxoSmithKline | Results Two positive phase III studies of tafenoquine for the radical cure of Plasmodium vivax malaria published in The New England Journal of Medicine gsk.com ↗
Using a confirmed FDA-preferred analysis (Kaplan Meier analysis), a significantly greater proportion of patients in the tafenoquine group remained relapse-free over the 6-month follow-up period compared with patients in the placebo group (62.4% vs 27.7%), with an odds ratio of 0.3, p<0.001. |
| 2018-09-21 | GlaxoSmithKline | Regulatory Kozenis (tafenoquine) approved by the Australian Therapeutic Goods Administration for the radical cure of P. vivax malaria gsk.com ↗
GSK and Medicines for Malaria Venture (MMV) today announced that the Australian Therapeutics Good Administration (TGA) has approved single-dose Kozenis (tafenoquine) for the radical cure (prevention of relapse) of Plasmodium vivax (P. vivax) malaria |
| 2018-07-20 | GlaxoSmithKline | Regulatory US FDA approves Krintafel (tafenoquine) for the radical cure of P. vivax malaria gsk.com ↗
Today’s approval of Krintafel, the first new treatment for Plasmodium vivax malaria in over 60 years, is a significant milestone for people living with this type of relapsing malaria. |
| 2018-07-12 | GlaxoSmithKline | Regulatory US FDA Advisory Committee endorses the effectiveness and safety of single-dose tafenoquine for the radical cure of P. vivax malaria gsk.com ↗
The positive vote is an important step towards tafenoquine becoming a significant addition to the global anti-malaria arsenal. |
| 2017-12-14 | GlaxoSmithKline | Regulatory GSK submits regulatory application for single-dose tafenoquine for the treatment of Plasmodium vivax malaria to Australia’s Therapeutic Goods Administration gsk.com ↗ |
| 2017-11-28 | GlaxoSmithKline | Regulatory GSK submits US regulatory application for single-dose tafenoquine for Plasmodium vivax malaria gsk.com ↗
This regulatory filing marks a significant and historical milestone in our global health efforts. |
| 2017-06-12 | GlaxoSmithKline | Results GSK and MMV announce positive headline phase III results showing single-dose tafenoquine reduces risk of relapse in patients with Plasmodium vivax malaria gsk.com ↗
GSK and Medicines for Malaria Venture (MMV) today announced positive results from two phase III studies of tafenoquine, an investigational 8-aminoquinoline, for the prevention of relapse of Plasmodium vivax (P.vivax) malaria. |
| 2013-12-20 | GlaxoSmithKline | Regulatory GSK and MMV announce FDA Breakthrough Therapy designation for tafenoquine for Plasmodium vivax malaria gsk.com ↗
GlaxoSmithKline (GSK) and Medicines for Malaria Venture (MMV) announced today that the U.S. Food and Drug Administration (FDA) has granted Breakthrough Therapy designation for tafenoquine, an investigational medicine for the treatment and relapse prevention of Plasmodium vivax malaria. |
All press releases naming this drug 12 releases
Evidence & citations 15 cited values
Every value below carries the sentence it was read from. 43 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 ↗40“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 | “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 | 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 | 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 | WR238605 | “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 |