Tafenoquine

Tafenoquine is an 8-aminoquinoline antimalarial drug [see Microbiology ( 12.4 )] .

• ARAKODA is indicated for the prophylaxis of malaria in patients aged 18 years and older. ARAKODA is an antimalarial indicated for the prophylaxis of malaria in patients aged 18 years and older.ICD-10: B54

• ARAKODA is contraindicated in: • patients with G6PD deficiency or unknown G6PD status due to the risk of hemolytic anemia [see Warnings and Precautions ( 5.2 )] . • breastfeeding by a lactating woman when the infant is found to be G6PD deficient or if the G6PD status of the infant is unknown [see Warnings and Precautions ( 5.3 ), Use in Specific Populations ( 8.2 )] .contraindicated

• All patients must be tested for glucose-6-phosphate dehydrogenase (G6PD) deficiency prior to prescribing ARAKODA. ( 2.1 ) • Pregnancy testing is recommended for females of reproductive potential prior to initiating treatment with ARAKODA. ( 2.1 ) Regimen Name Timing Dosage Loading regimen For each of the 3 days before travel to a malarious area 200 mg (2 of the 100 mg tablets) once daily for 3 days Maintenance regimen While in the malarious area 200 mg (2 of the 100 mg tablets) once weekly – start 7 days after the last loading regimen dose Terminal prophylaxis regimen In the week following exit from the malarious area 200 mg (2 of the 100 mg tablets) one-time 7 days after the last maintenance dose • Administer ARAKODA with food. ( 2.2 ) • See full prescribing information for instructions on how to replace missed doses. ( 2.2 ) 2.1 Tests to be Performed Prior to ARAKODA Dose Initiation All patients must be tested for glucose-6-phosphate dehydrogenase (G6PD) deficiency prior to prescribing ARAKODA [see Contraindications ( 4 ), Warnings and Precautions ( 5.1 )] . Pregnancy testing is recommended for females of reproductive potential prior to initiating treatment with ARAKODA [see Use in Specific Populations ( 8.1 and 8.3 )] . 2.2 Recommended Dosage and Administration Instructions The recommended dosage of ARAKODA is described in Table 1 below. ARAKODA can be administered for up to 6 months of continuous dosing.

• Hemolytic Anemia : G6PD testing must be performed before prescribing ARAKODA due to the risk of hemolytic anemia. Monitor patients for signs or symptoms of hemolysis. ( 5.1 ) • G6PD Deficiency in Pregnancy or Lactation : ARAKODA may cause fetal harm when administered to a pregnant woman with a G6PD-deficient fetus. ARAKODA is not recommended during pregnancy. A G6PD-deficient infant may be at risk for hemolytic anemia from exposure to ARAKODA through breast milk. Check infant’s G6PD status before breastfeeding begins. ( 5.2 , 8.1 , 8.2 ) • Methemoglobinemia : Asymptomatic elevations in blood methemoglobin have been observed. Initiate appropriate therapy if signs or symptoms of methemoglobinemia occur. ( 5.3 ) • Psychiatric Effects : Serious psychotic adverse reactions have been observed in patients with a history of psychosis or schizophrenia, at doses different from the approved dose. If psychotic symptoms (hallucinations, delusions, or grossly disorganized thinking or behavior) occur, consider discontinuation of ARAKODA therapy and, evaluation by a mental health professional as soon as possible. ( 5.4 ) • Hypersensitivity Reactions : Serious hypersensitivity reactions have been observed with administration of ARAKODA. If hypersensitivity reactions occur, institute appropriate therapy. ( 5.5 ) • Delayed Adverse Reactions : Due to the long half-life of ARAKODA (approximately 17 days), psychiatric effects, hemolytic anemia, methemoglobinemia, and hypersensitivity reactions may be delayed in onset and/or duration.

The following clinically significant adverse reactions observed with ARAKODA are discussed in detail in the Warnings and Precautions section: • Hemolytic Anemia [see Warnings and Precautions ( 5.2 )] • Methemoglobinemia [see Warnings and Precautions ( 5.3 )] • Psychiatric Effects [see Warnings and Precautions ( 5.4 )] • Hypersensitivity Reactions [see Warnings and Precautions ( 5.5 )] The most common adverse reactions (incidence ≥1%) were: headache, dizziness, back pain, diarrhea, nausea, vomiting, increased alanine aminotransferase (ALT), motion sickness, insomnia, depression, abnormal dreams, anxiety. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact 60 Degrees Pharmaceuticals at 1-888-834-0225 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of tafenoquine was studied in clinical trials at various doses and regimens in 3,184 subjects. The recommended ARAKODA regimen was evaluated in 825 subjects in 5 controlled clinical trials (Trials 1, Trial 2, Trial 3, Trial 4 and Trial 5). The mean duration of exposure to ARAKODA in these five clinical trials was 21 weeks (range 10-29 weeks). Trial 1, 2 and 4 were conducted in healthy semi-immune volunteers in Ghana or Kenya and were placebo-controlled; a mefloquine arm was included in Trials 2 and 4 as a benchmark.

Lactation : Advise women not to breastfeed a G6PD-deficient infant or infant with unknown G6PD status during treatment and for 3 months after the last dose of ARAKODA. ( 5.2 , 8.2 ) 8.1 Pregnancy Risk Summary The use of ARAKODA during pregnancy may cause hemolytic anemia in a fetus who is G6PD-deficient. Treatment with ARAKODA during pregnancy is not recommended. If a pregnancy is detected during ARAKODA use, discontinue ARAKODA as soon as possible and switch to an alternative prophylactic drug for malaria during pregnancy [see Warnings and Precautions ( 5.2 )] . Available data with use of ARAKODA in pregnant women are insufficient to establish a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. In animal studies, there were increased abortions, with and without maternal toxicity when tafenoquine was given orally to pregnant rabbits at and above doses equivalent to about 0.4 times the clinical exposure based on body surface area comparisons. No fetotoxicity was observed at doses about 1.5 times the clinical exposure (based on body surface area comparisons) in a similar study in rats. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S.

Metabolism

Absorption A food effect study was not conducted with the 100 mg ARAKODA tablet. In majority of the clinical trials, tafenoquine was administered under fed conditions.

There were no reported cases of ARAKODA overdose. Hemoglobin decline and methemoglobinemia may be encountered in an overdose with ARAKODA. Treatment of overdosage consists of institution of appropriate symptomatic and/or supportive therapy.

• Jul 20, 2018NDANDA210795Glaxosmithkline
• Aug 8, 2018NDANDA21060760 Degrees Pharms

1. 1Depression2029%
2. 2Anxiety1826%
3. 3Post-traumatic Stress Disorder1521%
4. 4Anger1420%
5. 5Nausea1420%
6. 6Tinnitus1217%
7. 7Headache1116%
8. 8Suicide Attempt1116%
9. 9Dizziness1014%
10. 10Drug Ineffective1014%
11. 11Memory Impairment1014%
12. 12Mental Disorder1014%
13. 13Off Label Use1014%
14. 14Paranoia1014%
15. 15Brain Injury913%

The 10 most recently updated of 42 ClinicalTrials.gov registrations naming Tafenoquine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• FocaL Mass Drug Administration for Vivax Malaria Elimination
  Recruiting · Phase 3 · Interventional · 7,530 enrolled · University of California, San Francisco
  NCT05690841updated 2026-06-09
• This is a Clinical Study to Assess Whether the Combination of SJ733 and Tafenoquine Will be a Safe and Rapidly Acting Anti-malarial for the Radical Cure of P. Vivax Malaria
  Not yet recruiting · Phase 2 · Interventional · 104 enrolled · R. Kiplin Guy
  NCT07430592updated 2026-05-28
• Long-Term Safety Study of Tafenoquine
  Completed · Phase 2 · Interventional · 600 enrolled · 60 Degrees Pharmaceuticals LLC
  NCT03320174updated 2026-04-17
• Tafenoquine Combinations for Improved Radical Cure Efficacy of Plasmodium Vivax
  Not yet recruiting · Interventional · 300 enrolled · Walter Reed Army Institute of Research (WRAIR)
  NCT07533136updated 2026-04-16
• Radical Cure (RC) With Tafenoquine or Primaquine After Semi-quantitative G6PD Testing: A Feasibility Study in Peru
  Completed · Observational · 187 enrolled · Medicines for Malaria Venture
  NCT05361486updated 2026-03-20
• Pharmacokinetic (PK) Study of Tafenoquine in Healthy Adults
  Not yet recruiting · Early phase 1 · Interventional · 20 enrolled · State University of New York - Upstate Medical University
  NCT07373743updated 2026-03-20
• Investigating the Pharmacokinetics of Tafenoquine in Healthy Papua New Guinean Children
  Recruiting · Phase 4 · Interventional · 30 enrolled · Curtin University
  NCT07052162updated 2026-03-18
• Postpartum 8-aminoquinoline Breast Milk Study
  Not yet recruiting · Phase 2 · Phase 3 · Interventional · 60 enrolled · Curtin University
  NCT07060404updated 2026-03-18
• Tafenoquine and ACTs (TADORE- Plus)
  Not yet recruiting · Phase 4 · Interventional · 507 enrolled · Menzies School of Health Research
  NCT07060794updated 2026-03-18
• Investigating the Pharmacology of Tafenoquine in Papua New Guinean Children With Uncomplicated Malaria
  Not yet recruiting · Phase 4 · Interventional · 60 enrolled · Curtin University
  NCT07403643updated 2026-02-12

CPIC-curated drug–gene pairs for Tafenoquine. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• G6PDCPIC AFDA label: Testing Required
  G6PD

Frequently asked questions

How does Tafenoquine work?

Tafenoquine is an 8-aminoquinoline antimalarial drug [see Microbiology ( 12.4 )] .

What is Tafenoquine used for?

According to FDA labeling, Tafenoquine carries indications including: ARAKODA is indicated for the prophylaxis of malaria in patients aged 18 years and older. ARAKODA is an antimalarial indicated for the prophylaxis of malaria in patients aged 18 years and older.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tafenoquine?

Tafenoquine is classified as Aminoquinolines, Unknown Cellular or Molecular Interaction.

What are the brand names for Tafenoquine?

Tafenoquine is marketed under brand names including Arakoda, Kodatef, Krintafel.

What are the contraindications for Tafenoquine?

Tafenoquine labeling lists contraindications including: ARAKODA is contraindicated in: • patients with G6PD deficiency or unknown G6PD status due to the risk of hemolytic anemia [see Warnings and Precautions ( 5.2 )] . • breastfeeding by a lactating woman when the infant is found to be G6PD deficient or if the G6PD status of the infant is unknown [see Warnings and Precautions ( 5.3 ), Use in Specific Populations ( 8.2 )] .. Always consult the full prescribing information and a clinician.