Drug intelligence / Profile preview

MK-3168

Development stage
Phase 1
Lead developer
Merck Research Laboratories
Modality
Small Molecules
Administration
Intravenous
01

Overview

MK‑3168 is a radiolabeled small molecule positron emission tomography (PET) tracer developed for imaging fatty acid amide hydrolase (FAAH) in the brain. FAAH is an integral membrane serine hydrolase responsible for the breakdown of endocannabinoids such as anandamide. Inhibition or occupancy of FAAH can be relevant to analgesia and anti-inflammatory effects, and PET tracers like MK‑3168 enable non-invasive measurement of FAAH availability and target engagement in both preclinical models and humans. The compound was designed to have high affinity for FAAH with suitable properties for brain imaging, using carbon‑11 labeling ([11C]MK‑3168). It has been used in clinical research to assess central nervous system target engagement by candidate FAAH inhibitors[1][4][6].

Other names
(1S,2S)-2-(4-(5-((5-Chloropyridin-2-yl)thio)-1-(11C)methyl–1H-imidazol–4–yl)phenyl)-N,N-dimethylcyclopropanecarboxamide
02

Targets

FAAH

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