Drug intelligence / Profile preview

MK-0952

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

Overview

MK-0952 is a selective and orally active phosphodiesterase type 4 (PDE4) inhibitor developed by Merck for the potential treatment of cognitive impairment associated with Alzheimer's disease and mild cognitive impairment. As a small molecule drug with high potency (IC50 ~0.5–0.6 nM), it was designed to modulate cyclic AMP signaling in the central nervous system to enhance long-term memory and cognitive function[1][4][5]. The mechanism involves inhibition of PDE4 enzymes that degrade cAMP; this leads to increased cAMP levels in neurons and downstream effects on synaptic plasticity and anti-inflammatory pathways[6][8]. Despite promising preclinical results for memory enhancement and neuroprotection[6], clinical development was discontinued after phase II trials for Alzheimer's disease due to lack of efficacy or other strategic reasons[3][5][7].

Other names
934995-87-6UNII-N48GH1UIR0UNII-N-48GH1UIR0UNII-N 48GH1UIR0N48GH1UIR0N-48GH1UIR0N 48GH1UIR0Cyclopropanecarboxylic acid, 2-(3'-(3-((cyclopropylamino)carbonyl)-4-oxo-1,8-naphthyridin-1(4H)-yl)-3-fluoro(1,1'-biphenyl)-4-yl)-, (1R,2R)
02

Targets

PDE4 (Phosphodiesterase 4A1)

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