Drug intelligence / Profile preview

[18F]AG-120

Development stage
Preclinical
Lead developer
Helmholtz-Zentrum Dresden-Rossendorf
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

[18F]AG-120 is a fluorine-18 labeled radiopharmaceutical tracer developed for positron emission tomography (PET) imaging of mutant isocitrate dehydrogenase 1 (mIDH1) in gliomas. It is a radiolabeled derivative of ivosidenib (AG-120), an FDA-approved small molecule inhibitor of mIDH1. Developed by researchers at the Helmholtz-Zentrum Dresden-Rossendorf (HZDR) and ROTOP Pharmaka, [18F]AG-120 is designed to non-invasively assess the IDH1R132H mutation status in brain tumors, aiding in patient stratification and treatment monitoring. Preclinical studies have demonstrated target-specific internalization in vitro and high metabolic stability in vivo, although its blood-brain barrier penetration is limited unless co-administered with a P-glycoprotein inhibitor like cyclosporine A.

Other names
18F-AG-12018F-AG12018F-ivosidenib[18F]ivosidenib
02

Targets

IDH1 (Isocitrate dehydrogenase [NADP] cytoplasmic)

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