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selpercatinib + repaglinide
- Development stage
- Unknown
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Selpercatinib + repaglinide is a **combination** of two pharmaceutical small molecule drugs: selpercatinib, a selective inhibitor of the RET receptor tyrosine kinase used in the treatment of RET-driven cancers, and repaglinide, a meglitinide-class antihyperglycemic agent that stimulates pancreatic β-cell insulin release for glycemic control in type 2 diabetes. Selpercatinib blocks RET kinase signaling and may also inhibit VEGFR3, VEGFR1, and FGFR1-3 at high concentrations, impeding cell proliferation in cancers with RET alterations. Repaglinide works by closing ATP-dependent potassium channels in β-cells, causing insulin release dependent on glucose presence, specifically effective for postprandial glucose reduction. This combination is not a branded or approved fixed-dose pharmaceutical product and is referenced in drug interaction contexts, most notably with selpercatinib possibly increasing serum concentrations of repaglinide through metabolic interactions, elevating the risk of hypoglycemia[1][3][7].
- Other names
- selpercatinib + repaglinide
02
Targets
KATP channel (ATP-sensitive potassium channel)RET (Rearranged during transfection receptor tyrosine kinase)FGFR3 (Fibroblast growth factor receptor 3)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)
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