Drug intelligence / Profile preview

LSN3316612

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Alpha Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

LSN3316612 is a highly selective and potent small-molecule ligand for O-GlcNAcase (OGA), developed for use as a positron emission tomography (PET) radioligand in neuroscience research[3][1]. The molecule is labeled with either fluorine-18 ([18F]LSN3316612) or carbon-11 ([11C]LSN3316612) radioisotopes for quantitative imaging of OGA enzyme occupancy in the human brain[1][3]. OGA modulates O-GlcNAcylation of proteins such as tau, which is implicated in neurodegenerative disorders like Alzheimer’s disease[3]. LSN3316612 demonstrates high affinity (IC50 = 1.9 nM), excellent selectivity for OGA, and favorable pharmacokinetics, enabling stable in vivo brain imaging[3][1]. The compound is designed primarily for research purposes to assess target engagement by OGA inhibitors in clinical and preclinical studies[3][1].

Other names
MNI-1068MNI1068MNI 1068[18F]MNI-1068
02

Targets

OGA (Protein O-GlcNAcase)

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