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selpercatinib + trastuzumab deruxtecan
- Development stage
- Preclinical
- Lead developer
- Eli Lilly
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
A combination therapy consisting of selpercatinib, a selective RET kinase inhibitor, and trastuzumab deruxtecan, an antibody-drug conjugate. This combination targets both RET fusion proteins and HER2-expressing cancer cells simultaneously. The trastuzumab component binds to HER2 receptors while the deruxtecan component causes DNA damage after internalization. Selpercatinib inhibits RET kinase activity, blocking downstream signaling pathways.
02
Targets
FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)ERBB2 (Erb-b2 receptor tyrosine kinase 2)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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