Tafenoquine


Tafenoquine, sold under the brand name Krintafel among others, is a medication used to prevent and to treat malaria. With respect acute malaria it is used together with other medications to prevent relapse by Plasmodium vivax. It may be used to prevent all types of malaria. It is taken by mouth.
Common side effects include vomiting, headache, and dizziness. Other side effects may include methemoglobinemia, trouble sleeping, and anaphylaxis. In people with G6PD deficiency, red blood cell breakdown may occur. Use in pregnancy is not recommended. Tafenoquine is in the 8-aminoquinoline family of medications. How it works is unclear but it is effective both in the liver and blood.
Tafenoquine was approved for medical use in Australia and in the United States in 2018. In the United States, as of 2019, a course of treatment costs about US$43. Tafenoquine is related to primaquine.

Medical use

Prevention

Tafenoquine may be used to prevent all types of malaria. For this use 200 mg 3 days before travel then 200 mg per week until one week after travel is recommended.

Treatment

Tafenoquine is used for the treatment of the hypnozoite stages of Plasmodium vivax and Plasmodium ovale that are responsible for relapse of these malaria species even when the blood stages are successfully cleared. Primaquine for 14 days can also be used for this. The advantage of tafenoquine is that it has a long half-life and therefore a single treatment is sufficient. For this use a single dose of 300 mg is recommended. It is used with another medication, such as chloroquine, that kills the malaria in the blood.

Chemistry

Tafenoquine contains a stereocenter and consists of two enantiomers. This is a mixture of - and the - Form:

History

Tafenoquine was approved for medical use in Australia and in the United States in 2018. Tafenoquine was given an orphan drug designation and was granted breakthrough therapy status in 2013 in the United States.

Society and culture

One version is made by GlaxoSmithKline. While another is made by 60 Degrees Pharmaceutical.

Names

Etaquine was a generic name proposed by WRAIR, and subsequently rejected by CDER.
Trade names