Drug intelligence / Profile preview

metrifonate

Development stage
Discontinued
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

Metrifonate is an irreversible organophosphate acetylcholinesterase inhibitor and a prodrug that is non-enzymatically converted into the active metabolite dichlorvos. It was originally introduced as an insecticide (trichlorfon) in 1952 and later developed for human use in the treatment of urinary schistosomiasis caused by *Schistosoma haematobium*. Metrifonate selectively inhibits cholinesterase activity in schistosomes more than in humans due to its conversion to dichlorvos. It has also been investigated for Alzheimer's disease because it increases brain acetylcholine levels through long-lasting cholinesterase inhibition. While generally well-tolerated at therapeutic doses with mild and transient side effects such as nausea or diarrhea, its use has been discontinued or banned in many countries due to safety concerns and regulatory restrictions[1][2][3][4][5][7].

Brand names
ChlorophosMazotenDimetoxChlorakTrichlorfonBovinoxDioxaphos
Other names
trichlorphon
02

Targets

AcetylcholinesteraseButyrylcholinesterase

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