Article
Identification of M4205─A Highly Selective Inhibitor of KIT Mutations for Treatment of Unresectable Metastatic or Recurrent Gastrointestinal Stromal Tumors.
Journal of medicinal chemistry - 23 Feb 2023
Blum Andreas, Dorsch Dieter, Linde Nina, Brandstetter Susanne, Buchstaller Hans-Peter, Busch Michael, Glaser Nina, Grädler Ulrich, Ruff Aaron, Petersson Carl, Schieferstein Hanno, Sherbetjian Eva, Esdar Christina
Abstract excerpt
The treatment of gastrointestinal stromal tumors (GISTs) driven by activating mutations in the KIT gene is a prime example of targeted therapy for treatment of cancer. The approval of the tyrosine kinase inhibitor imatinib has significantly improved patient survival, but emerging resistance under treatment and relapse is observed. Several additional KIT inhibitors have been approved; still, there is a high unmet...
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