Article
The return of RET GateKeeper mutations? an in-silico exploratory analysis of potential resistance mechanisms to novel RET macrocyclic inhibitor TPX-0046.
Investigational new drugs - 1 Oct 2022
Repetto Matteo, Crimini Edoardo, Ascione Liliana, Boscolo Bielo Luca, Belli Carmen, Curigliano Giuseppe
Abstract excerpt
TPX-0046 is designed to overcome resistance to FDA approved RET inhibitors Selpercatinib and Pralsetinib. Early prediction of resistance mechanisms to investigational drugs may facilitate subsequent drug and trial designs. This study aims to predict potential mutations inducing resistance to TPX-0046. We conducted an in-silico analysis of TPX-0046 macrocyclic structure and predicted the binding mode on RET. We...
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