Tafenoquine

Products

Tafenoquine was approved in the United States in 2018 in tablet form (Krintafel, Arakoda).

Structure and properties

Tafenoquine (C24H28F3N3O3, Mr = 463.5 g/mol) is an 8-aminoquinoline derivative present in the drug as tafenoquine succinate. It is a derivative of primaquine. The drug was first synthesized in 1978 at the Walter Reed Army Institute of Research in the United States.

Effects

Tafenoquine has antiparasitic properties against all stages of . It is also effective against hypnozoites in the liver, the resting forms of the malaria parasite that trigger relapses. Tafenoquine has a long half-life of 15 days.

Indications

  • Tafenoquine is used for the eradication of (causative agent of malaria), with the aim of preventing relapses.
  • Tafenoquine is also approved for malaria prophylaxis.

Dosage

According to the professional information.

Contraindications

  • Hypersensitivity, including to related agents.
  • Glucose-6-phosphate dehydrogenase deficiency.
  • Pregnancy, lactation

Full precautions can be found in the drug label.

Interactions

Drug-drug interactions have been described with substrates of OCT2 and MATE transporters such as dofetilide and metformin. Tafenoquine is an inhibitor of these transporters.

Adverse effects

The most common potential adverse effects include dizziness, nausea, vomiting, headache, and reduced hemoglobin levels.