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

doi:10.1158/2159-8290.CD-22-0968

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Article

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

Cancer discovery - 1 Mar 2023

Drilon Alexander, Horan Joshua C, Tangpeerachaikul Anupong, Besse Benjamin, Ou Sai-Hong Ignatius, Gadgeel Shirish M, Camidge D Ross, van der Wekken Anthonie J, Nguyen-Phuong Linh, Acker Adam, Keddy Clare, Nicholson Katelyn S, Yoda Satoshi, Mente Scot, Sun Yuting, Soglia John R, Kohl Nancy E, Porter James R, Shair Matthew D, Zhu Viola, Davare Monika A, Hata Aaron N, Pelish Henry E, Lin Jessica J

Abstract excerpt

SIGNIFICANCE: 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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PMID: 36511802
DOI: 10.1158/2159-8290.CD-22-0968
PMCID: PMC9975673

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