Drug intelligence / Profile preview

[U-2H]pyruvate

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

Overview

[U-2H]pyruvate is a uniformly deuterium-labeled metabolic probe used in deuterium magnetic resonance spectroscopy (2H-MRS) for the non-invasive imaging of metabolic fluxes. It serves as a diagnostic tool to monitor the conversion of pyruvate to lactate, a process catalyzed by lactate dehydrogenase (LDH) that is typically upregulated in cancer cells due to the Warburg effect. Research, particularly at the University of California, San Francisco (UCSF), has demonstrated its utility in brain tumor models (such as glioblastoma and oligodendroglioma) to assess tumor burden, metabolic reprogramming, and early response to treatment, including TERT inhibitors and standard-of-care chemoradiation. Unlike 13C-labeled probes which require hyperpolarization, 2H-labeled substrates like [U-2H]pyruvate can be detected using standard clinical MR scanners, facilitating its translation into clinical practice for monitoring tumor immortality and metabolic status.

Other names
uniformly deuterated pyruvatedeuterated pyruvate[U-2H]pyruvic acid
02

Targets

LDH (L-lactate dehydrogenase A chain)MCT4 (Monocarboxylate transporter 4)PDH E1 (Pyruvate dehydrogenase E1 component)PROC (Protein C)

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