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124I-trametinib
- Development stage
- Preclinical
- Lead developer
- Memorial Sloan Kettering Cancer Center
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
124I-trametinib is a radiolabeled small molecule and positron emission tomography (PET) imaging tracer. It is an iodine-124 labeled analog of trametinib, a potent allosteric inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2). Developed to visualize and quantify the delivery and distribution of trametinib to tumors and healthy organs, this radiotracer serves as a tool for personalizing treatment doses and monitoring the emergence of resistance in patients with MAPK-driven malignancies, such as BRAF-mutant melanoma and anaplastic thyroid cancer. By acting as a molecular probe, it allows for noninvasive assessment of the therapeutic index and drug delivery in vivo.
- Other names
- [124I]trametinibiodine-124 trametinibiodine124 trametinibiodine 124 trametinib
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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