Development and optimization of [68Ga]Ga-DOTA-EMP-100 for non-invasive PET imaging and targeted radioligand therapy of c-MET overactivation in cancer

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Abstract

Background. Overactivation of the HGF/c-MET pathway is implicated in various cancers, making its inhibition a promising therapeutic strategy. While several MET-targeting agents are currently approved or in advanced clinical development, patient selection often relies on invasive tissue-based assays. The development of a specific c-MET radioligand for PET imaging and radioligand therapy represents a non-invasive alternative, enabling real-time monitoring of target expression and offering a pathway to personalized treatment. Results. An optimized formulation of [⁶⁸Ga]Ga-DOTA-EMP-100, using 40 µg of precursor, provided the best outcome in terms of radiochemical performance. Process validation across three independent productions confirmed a consistent radiochemical yield of 64.5%, high radiochemical purity (100%), and a molar activity of 53.41 GBq/µmol. Conclusions. [⁶⁸Ga]Ga-DOTA-EMP-100 was successfully synthesized with high purity and reproducibility, supporting its potential for multi-dose application in clinical PET imaging and targeted radioligand therapy.

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