NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations.
Alexander E DrilonJoshua C HoranAnupong TangpeerachaikulBenjamin BesseSai-Hong Ignatius OuShirish M GadgeelD Ross CamidgeAnthonie J van der WekkenLinh Nguyen-PhuongAdam AckerClare KeddyKatelyn S NicholsonSatoshi YodaScot MenteYuting SunJohn R SogliaNancy E KohlJames R PorterMatthew D ShairViola W ZhuMonika A DavareAaron N HataHenry E PelishJessica J LinPublished in: Cancer discovery (2023)
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.
Keyphrases
- cell death
- dna damage
- reactive oxygen species
- end stage renal disease
- white matter
- chronic kidney disease
- ejection fraction
- machine learning
- newly diagnosed
- oxidative stress
- stem cells
- resting state
- tyrosine kinase
- prognostic factors
- drug delivery
- bone marrow
- cancer therapy
- minimally invasive
- brain injury
- robot assisted