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  BAY 94-9392

Description of BAY 94-9392: BAY 94-9392 ((4S)-(3-[18F]Fluoropropyl)-L-glutamic acid) is a new positron emitting tracer to target tumor specific metabolism. BAY 94-9392 appears to be a promising novel tumor imaging agent with a high cancer detection rate and favorable biodistribution in patients with NSCLC. However, the uptake of BAY 94-9392 in breast cancer patients is lower than FDG. More studies are needed to further investigate the underlying biological mechanisms and specificity in various cancer entities.

Current developer:    Bayer

(4S)-(3-[F-18]fluoropropyl)-L-glutamic acid (BAY 94-9392) was obtained with a radiochemical yield of > 40 % (d.c.) and purity of > 92 % (n = 40) via nucleophilic substitution. Transport of BAY 94-9392 is inhibited by p-carboxy-phenylglycine, L-glutamate and L-cystine but not by L- or D-aspartate, indicating specific transport via the sodium-independent xCT transporter (SLC7A11). Reduced uptake of BAY 94-9392 was observed in shRNA xCT knock down human A549 lung cancer cells. BAY 94-9392 shows high uptake and retention in a variety of tumor models. No metabolic degradation and a rapid renal clearance occurred in vivo. In contrast to FDG, BAY 94-9392 did not accumulate in induced inflammatory lesions. Conclusions: High metabolic stability, rapid excretion and xCT transporter mediated uptake of BAY 94-9392 led to excellent tumor specific visualization. Clinical investigations are in progress (source: J Nucl Med. 2011; 52 (Supplement 1):412).

 1: Koglin N, Mueller A, Berndt M, Schmitt-Willich H, Toschi L, Stephens AW, Gekeler V, Friebe M, Dinkelborg LM. Specific PET imaging of xC- transporter activity using a ¹⁸F-labeled glutamate derivative reveals a dominant pathway in tumor metabolism. Clin Cancer Res. 2011 Sep 15;17(18):6000-11. Epub 2011 Jul 12.  PubMed PMID: 21750203.

2. Norman Koglin1, Andre Mueller1, Mathias Berndt1, Heribert Schmitt-Willich1, Volker Gekeler1, Matthias Friebe1 and Ludger Dinkelborg1  Probes for Oncology I: F-18 and C-11 Labeled Radiopharmaceuticals for Tumor Imaging  BAY 94-9392 - A novel F-18 L-glutamate derivative for tumor-specific PET imaging. J Nucl Med. 2011; 52 (Supplement 1):412.