Article
Molecular Characteristics of Repotrectinib That Enable Potent Inhibition of TRK Fusion Proteins and Resistant Mutations.
Molecular cancer therapeutics - 1 Dec 2021
Murray Brion W, Rogers Evan, Zhai Dayong, Deng Wei, Chen Xi, Sprengeler Paul A, Zhang Xin, Graber Armin, Reich Siegfried H, Stopatschinskaja Shanna, Solomon Benjamin, Besse Benjamin, Drilon Alexander
Abstract excerpt
NTRK chromosomal rearrangements yield oncogenic TRK fusion proteins that are sensitive to TRK inhibitors (larotrectinib and entrectinib) but often mutate, limiting the durability of response for NTRK + patients. Next-generation inhibitors with compact macrocyclic structures (repotrectinib and selitrectinib) were designed to avoid resistance mutations. Head-to-head potency comparisons of TRK inhibitors and...
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