Development of 2-Deoxy-2-[(18)F]fluororibose for Positron Emission Tomography Imaging Liver Function in Vivo.

Positron emission tomography (PET) is a molecular imaging technique that can provide information on cellular functions in vivo. The PET imaging probe [18F]-FDG is used clinically to detect, stage, and monitor cancer. Life-threatening acute liver failure can be triggered by a variety of factors, including common drugs such as Tylenol. PET imaging is rarely used to monitor liver diseases, in part due to a lack of specific imaging agents for liver function. PET imaging of the liver could have an important impact on the diagnosis and treatment of such conditions as acute liver failure and hepatocellular carcinoma. Here we report a new PET imaging probe, 2-deoxy-2-[18F]fluororibose ([18F]-2-DFR), for use in imaging liver function. We synthesized [18F]-2-DFR from a carefully prepared molecular precursor, designed to withstand the harsh reaction conditions of late-stage fluorination. [18F]-2-DFR accumulated preferentially in the mouse liver and was metabolized by enzymes that metabolize ribose. Notably [18F]-2-DFR PET imaging could distinguish between healthy liver and liver damaged by acetaminophen. [18F]-2-DFR is expected to be a useful PET probe for imaging and quantifying liver functions in vivo, with likely significant clinical utility.