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selumetinib + radioactive iodine therapy
- Development stage
- Unknown
- Lead developer
- AstraZeneca
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral
01
Overview
**Selumetinib + radioactive iodine therapy** is an experimental combination therapy for differentiated thyroid cancer (DTC), especially for patients at high risk of primary treatment failure following surgery. Selumetinib is a potent, highly selective allosteric inhibitor of MEK1 and MEK2 kinases—components of the MAPK/ERK pathway—developed to restore the ability of thyroid cancer cells to uptake radioactive iodine by inhibiting pathway-driven repression of sodium-iodide symporter gene expression. The approach is based on increasing tumor iodine avidity, thereby improving the efficacy of a therapeutic dose of oral radioactive iodine-131 (RAI; ^131I). In clinical settings, selumetinib is administered orally for several weeks preceding and following a single, high-dose radioactive iodine treatment.[1][2][3]
- Brand names
- Koselugo
- Other names
- selumetinib plus radioactive iodine therapyselumetinib + RAIselumetinib + iodine-131selumetinib + ^131I
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)NIS (Human sodium iodide symporter)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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