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LOXO-260
- Development stage
- Phase 1
- Lead developer
- Eli Lilly
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
LOXO-260 is an orally bioavailable, highly potent, and selective small molecule inhibitor of the rearranged during transfection (RET) receptor tyrosine kinase. It was specifically designed to target both fusion products and mutated forms of RET, including solvent front and gatekeeper mutations that confer resistance to first-generation selective RET inhibitors such as selpercatinib. The drug was developed for use in patients with advanced or metastatic cancers harboring RET gene alterations—such as non-small cell lung cancer (NSCLC), medullary thyroid cancer (MTC), papillary thyroid carcinoma, and other solid tumors—who have progressed on prior selective RET inhibitor therapy. Its mechanism involves inhibition of aberrant RET signaling pathways that drive tumor growth in these genetically defined cancers[3][7][9].
- Other names
- LOXO-260LOXO260LOXO 260LY3838915LY-3838915LY 3838915
02
Targets
RET (Rearranged during transfection receptor tyrosine kinase)
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