Tafenoquine, sold under the brand name Krintafel among others, is a medication used to prevent and to treat

malaria Malaria is a Mosquito-borne disease, mosquito-borne infectious disease that affects vertebrates and ''Anopheles'' mosquitoes. Human malaria causes Signs and symptoms, symptoms that typically include fever, Fatigue (medical), fatigue, vomitin ...

. With respect to acute malaria, it is used together with other medications to prevent relapse by ''

Plasmodium vivax ''Plasmodium vivax'' is a protozoal parasite and a human pathogen. This parasite is the most frequent and widely distributed cause of recurring malaria. Although it is less virulent than ''Plasmodium falciparum'', the deadliest of the five huma ...

''. 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 Methemoglobinemia, or methaemoglobinaemia, is a condition of elevated methemoglobin in the blood. Symptoms may include headache, dizziness, shortness of breath, nausea, poor muscle coordination, and blue-colored skin (cyanosis). Complications ma ...

, trouble sleeping, and

anaphylaxis Anaphylaxis (Greek: 'up' + 'guarding') is a serious, potentially fatal allergic reaction and medical emergency that is rapid in onset and requires immediate medical attention regardless of the use of emergency medication on site. It typicall ...

. 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. The

mechanism of action In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical Drug interaction, interaction through which a Medication, drug substance produces its pharmacological effect. A mechanism of action usually includes mention o ...

is unclear but it is effective both in the liver and bloodstream. A possible mechanism of action and other novel perspectives have been published. Tafenoquine was approved for medical use in Australia and in the United States in 2018. 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 eliminating the hypnozoite stage of ''

'' and '' Plasmodium ovale'' that is responsible for relapse of these malarial infections, 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 (2–3 weeks) 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 Chloroquine is an antiparasitic medication that treats malaria. It works by increasing the levels of heme in the blood, a substance toxic to the malarial parasite. This kills the parasite and stops the infection from spreading. Certain types ...

, that kills the parasites in the bloodstream. There is a need to determine whether or not tafenoquine kills the numerous, non-circulating asexual ''P. vivax'' parasites that are now known to occur in the spleen, bone marrow, and possibly elsewhere in chronic infections.

Chemistry

Tafenoquine contains a stereocenter and consists of two enantiomers. This is a mixture of (''R'') - and the (''S'') - Form:

History

Tafenoquine was approved for medical use in Australia and in the United States in 2018. Tafenoquine was given an

orphan drug An orphan drug is a medication, pharmaceutical agent that is developed to treat certain rare medical conditions. An orphan drug would not be profitable to produce without government assistance, due to the small population of patients affected by th ...

designation and was granted

breakthrough therapy Breakthrough therapy is a United States Food and Drug Administration designation that expedites drug development that was created by Congress under Section 902 of the 9 July 2012 Food and Drug Administration Safety and Innovation Act. The FDA's "b ...

status in 2013 in the United States.

Society and culture

One version is made by

GlaxoSmithKline GSK plc (an acronym from its former name GlaxoSmithKline plc) is a British Multinational corporation, multinational Pharmaceutics, pharmaceutical and biotechnology company with headquarters in London. It was established in 2000 by a Mergers an ...

. While another is made by 60 Degrees Pharmaceutical.

Names

Etaquine was a generic name proposed by WRAIR, and subsequently rejected by

CDER The Center for Drug Evaluation and Research (CDER, pronounced "see'-der") is a division of the U.S. Food and Drug Administration (FDA) that monitors most drugs as defined in the Food, Drug, and Cosmetic Act. Some biological products are also le ...

. Trade names * Kozenis (Australia) * Kodatef (Australia) * Arakoda (USA), Krintafel (USA)

References

External links

* {{Portal bar , Medicine Antimalarial agents Drugs developed by GSK plc Orphan drugs Phenol ethers Quinolines Trifluoromethyl compounds Wikipedia medicine articles ready to translate Diaryl ethers