Drug intelligence / Profile preview

tacrine

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Tacrine is a small molecule drug and the first centrally acting reversible acetylcholinesterase inhibitor approved for the treatment of mild to moderate Alzheimer's disease. It works by inhibiting acetylcholinesterase, thereby increasing levels of acetylcholine in the brain and enhancing cholinergic neurotransmission. Tacrine does not cure Alzheimer's disease or halt its progression but may temporarily improve cognitive function in some patients. The drug was marketed under the brand name Cognex but was withdrawn from the US market in 2012 due to concerns about hepatotoxicity (liver toxicity). Tacrine also exhibits activity against butyrylcholinesterase and has additional effects on muscarinic receptors, monoamine oxidases (MAO-A and MAO-B), potassium channels, sodium channels, calcium channels at high doses, and can modulate other neurotransmitter systems[1][2][6].

Brand names
Cognex
Other names
tacrinetetrahydroaminoacridineTHA
02

Targets

MAOA (Monoamine oxidase A)MAOB (Monoamine oxidase B)ButyrylcholinesteraseAcetylcholinesterase

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