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selpercatinib + trastuzumab deruxtecan
- Development stage
- Preclinical
- Lead developer
- Eli Lilly
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- 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
ERBB2 (Erb-b2 receptor tyrosine kinase 2)FGFR1 (Fibroblast growth factor receptor 1)TOP1 (DNA Topoisomerase I)FGFR3 (Fibroblast growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)RET (Rearranged during transfection receptor tyrosine kinase)
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