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selpercatinib
- Development stage
- Approved
- Lead developer
- Eli Lilly
- Modality
- Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Fragment-Derived Small Molecules → Multivalent & Scaffold-Based Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Selpercatinib is a highly selective small molecule inhibitor of the RET (rearranged during transfection) receptor tyrosine kinase. It is used as a targeted therapy for cancers driven by RET gene alterations, including non-small cell lung cancer (NSCLC), medullary thyroid cancer (MTC), other types of thyroid cancer, and certain solid tumors. Selpercatinib works by blocking the activity of abnormal RET proteins that drive tumor growth and proliferation. It was developed to provide greater specificity for RET compared to earlier multikinase inhibitors, reducing off-target toxicity. The drug is administered orally and requires confirmation of a RET gene alteration before use[1][3][5][7].
- Brand names
- RetevmoRetsevmo
- Other names
- selpercatinib
02
Targets
RET (Rearranged during transfection receptor tyrosine kinase)
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