sitamaquine

Sitamaquine is an orally active 8-aminoquinoline analog developed primarily for the treatment of visceral leishmaniasis. It was investigated by the Walter Reed Army Institute in collaboration with GlaxoSmithKline (formerly SmithKline Beecham). Sitamaquine acts as a small molecule antileishmanial agent, accumulating in Leishmania parasites through interactions with membrane phospholipids rather than via a transporter. Its mechanism involves inhibition of the mitochondrial respiratory chain complex II (succinate dehydrogenase), leading to disruption of parasite energy metabolism and induction of oxidative stress. Sitamaquine has a short elimination half-life, which may help prevent rapid resistance development. Clinical trials have reached phase II, but further development has been limited by adverse effects such as methemoglobinemia and nephrotoxicity[1][2][3][5][6].

Other names

sitamaquina