NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations

NVL-520 是一种选择性、TRK 保留性、脑渗透性 ROS1 融合和继发性耐药突变抑制剂

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作者:Alexander Drilon #, Joshua C Horan #, Anupong Tangpeerachaikul #, Benjamin Besse, Sai-Hong Ignatius Ou, Shirish M Gadgeel, D Ross Camidge, Anthonie J van der Wekken, Linh Nguyen-Phuong, Adam Acker, Clare Keddy, Katelyn S Nicholson, Satoshi Yoda, Scot Mente, Yuting Sun, John R Soglia, Nancy E Kohl, J

Abstract

The combined preclinical features of NVL-520 that include potent targeting of ROS1 and diverse ROS1 resistance mutations, high selectivity for ROS1 G2032R over TRK, and brain penetration mark the development of a distinct ROS1 TKI with the potential to surpass the limitations of earlier-generation TKIs for ROS1 fusion-positive patients. This article is highlighted in the In This Issue feature, p. 517.

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