selpercatinib (Pending FDA Approval)

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Dosing & Uses

Non-small Cell Lung Cancer

Pending FDA approval for advanced RET fusion-positive non-small cell lung cancer (NSCLC)

Thyroid Cancer

Pending FDA approval for RET-mutant medullary thyroid cancer (MTC) and RET fusion-positive thyroid cancer

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Pharmacology

Mechanism of Action

Rearranged during transfection (RET) kinase inhibitor

Genomic alterations in RET kinase, which include fusions and activating point mutations, lead to overactive RET signaling and uncontrolled cell growth

RET fusion cancers and RET-mutant MTC are primarily dependent on this single activated kinase for their proliferation and survival; this dependency, often referred to as "oncogene addiction," renders such tumors highly susceptible to small molecule inhibitors targeting RET

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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.