Drug intelligence / Profile preview

lecozotan + cholinesterase inhibitor

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Lecozotan + cholinesterase inhibitor refers to the combination of *lecozotan*, a selective serotonin 5-HT1A receptor antagonist, with a cholinesterase inhibitor (e.g., donepezil, rivastigmine, or galantamine), for potential use in treating mild to moderate Alzheimer’s disease. Lecozotan acts by competitively antagonizing 5-HT1A receptors, resulting in enhanced glutamate and acetylcholine release in the hippocampus—both neurotransmitter systems implicated in cognitive function[2][3][4][6]. Cholinesterase inhibitors prevent the breakdown of acetylcholine, further supporting cholinergic neurotransmission. The combination is hypothesized to have a synergistic effect on cognitive symptoms in Alzheimer’s disease by dual enhancement of cholinergic signaling[1][5].

02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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