Drug intelligence / Profile preview

[2H9]-choline

Development stage
Preclinical
Lead developer
University of California, San Francisco
Modality
Small Molecules
Administration
Intravenous
01

Overview

[2H9]-choline is a deuterium-labeled metabolic imaging probe used in deuterium magnetic resonance spectroscopy (DMRS) to assess phospholipid biosynthesis. It serves as a substrate for choline kinase α (CKα), which phosphorylates it into [2H9]-phosphocholine. Since CKα is frequently upregulated in cancers to support high membrane turnover, the conversion rate of [2H9]-choline provides a non-invasive readout of tumor metabolic activity and proliferation. Research at UCSF has demonstrated its utility in monitoring tumor burden and early therapeutic response in glioma models, where it can detect metabolic changes following temozolomide treatment before anatomical changes are visible on standard imaging.

Other names
N,N,N-trimethyl-d9-cholinedeuterated choline
02

Targets

Kennedy pathway enzymesCHDH (Choline dehydrogenase)CHKA (Choline kinase)CCT (T-complex protein Ring Complex)

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