Novel Radiopharmaceutical for Non-Invasive Imaging of Ferroptosis in Cancer Therapy

Stanford researchers in Prof. Corinne Beinat's lab have developed a novel radiotracer, [18F]hGTS13, for non-invasive imaging of system xc- activity, enabling the identification of ferroptosis-sensitive cancers and monitoring the efficacy of ferroptosis-inducing therapies. This technology facilitates personalized cancer treatment by assessing drug engagement and predicting therapeutic outcomes.

Ferroptosis, a form of regulated cell death driven by the iron-dependent accumulation of membrane lipid peroxides, has emerged as a promising target for cancer therapy, particularly in glioblastoma multiforme (GBM). However, the current state of the field lacks non-invasive imaging techniques to monitor the engagement of ferroptosis-inducing drugs and to identify patients who would benefit from such therapies. Existing radiotracers, like [18F]FSPG, have limitations in specificity and uptake in inflammatory cells, leading to suboptimal cancer imaging.

The novel radiotracer [18F]hGTS13 specifically targets system xc- to enable non-invasive imaging of ferroptosis in cancer cells. It offers improved radiosynthesis, enhanced specificity for cancer cells over inflammatory cells, and a high tumor-to-brain ratio in glioma models, making it a superior tool for personalized cancer treatment. Evidence from preclinical studies in rats demonstrates its effectiveness in distinguishing ferroptosis-sensitive and resistant cell lines and monitoring drug engagement, highlighting its ability to monitor drug engagement and efficacy in vivo, advancing the current state of cancer therapy.

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Stage of Development
Proof of concept - in vivo data in a rat model of glioma

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