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Association details:
| Biomarker: | KIF5B-RET fusion + RET G810C |
|---|---|
| Cancer: | Solid Tumor |
| Drug: | HSN608 (RET inhibitor, c-Abl tyrosine kinase inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Targeting RET Solvent-Front Mutants with Alkynyl Nicotinamide-Based Inhibitors
Published date:
06/01/2023
Excerpt:
Surprisingly, the G810V mutant found in a clinical study was not resistant to selpercatinib or pralsetinib. Besides G810C/R/S, G810D also conferred selpercatinib/pralsetinib resistance….In cell-derived xenograft tumors driven by KIF5B-RET (G810C) that contains the most frequently observed solvent-front mutant in selpercatinib-treated patients, HSN608, HSL476, and HSL468 significantly suppressed and caused regression of the selpercatinib-resistant tumors.
DOI:
10.1158/1535-7163.MCT-22-0629
