Drug intelligence / Profile preview

mefloquine

Development stage
Approved
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

Mefloquine is an antimalarial drug used for both the prevention and treatment of malaria, a serious infection caused by Plasmodium parasites transmitted through mosquito bites. It is available as an oral tablet and was previously marketed under the brand name Lariam, though generic versions are now common. Mefloquine works primarily by inhibiting protein synthesis in Plasmodium falciparum, the parasite responsible for most severe cases of malaria, through direct binding to its 80S ribosome. This action disrupts polypeptide elongation during translation, ultimately killing the parasite[6][8]. The drug has also been shown to have off-target effects on several human neurotransmitter receptors and transporters, which may contribute to its neurological and psychiatric side effects[7]. Mefloquine was approved by the FDA in 1989.

Brand names
Lariam
Other names
mefloquine hydrochloride
02

Targets

Pf80S (Plasmodium falciparum cytoplasmic ribosome)

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