Drug intelligence / Profile preview

hyperpolarized [2-13C] pyruvate

Development stage
Phase 1
Lead developer
GE Healthcare
Modality
Small Molecules
Administration
Intravenous
01

Overview

Hyperpolarized [2-13C] pyruvate is a specialized, investigational imaging agent used in magnetic resonance imaging (MRI) to noninvasively probe real-time metabolic processes in vivo. The compound consists of pyruvic acid labeled with the stable isotope carbon-13 at the second carbon position and is rendered hyperpolarized using dynamic nuclear polarization techniques immediately prior to administration. This dramatically increases its MR signal, enabling sensitive detection of downstream metabolites after intravenous injection. Unlike the more common HP [1‑13C]pyruvate, which primarily tracks glycolytic conversion to lactate and alanine, HP [2‑13C]pyruvate allows direct observation of metabolic flux through both glycolysis and the tricarboxylic acid (TCA) cycle by following label incorporation into metabolites such as glutamate and acetyl-carnitine. This provides unique insights into mitochondrial function, oxidative metabolism, anaplerosis/cataplerosis, and gluconeogenesis that are not accessible with other tracers[1][2][4]. It has been used in early-phase human studies for brain metabolism research[1][2], as well as preclinical studies investigating hepatic gluconeogenesis[4]. The agent is not commercially available; it must be prepared on-site due to its short-lived polarization state. Preparation typically uses GMP/GLP-grade reagents from suppliers like MilliporeSigma/Merck KGaA or ISOTEC Stable Isotope Division[2]. Hyperpolarization equipment such as GE Healthcare’s SPINlab dDNP polarizer is commonly employed for clinical research use[1][2].

Other names
HP [2–13C]pyruvatehyperpolarized carbon 13 pyruvate (specific to the 2-position labeling)[2–13C]pyruvic acid (when referring to precursor)
02

Targets

LDH (L-lactate dehydrogenase A chain)PDH (Pyruvate dehydrogenase complex)PROC (Protein C)

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