Activity of Adagrasib (MRTX849) in Brain Metastases: Preclinical Models and Clinical Data From Patients With KRASG12C-Mutant Non-Small Cell Lung CancerPreliminary Activity of Adagrasib in Brain Metastases
Sabari J, Velcheti V, Shimizu K, Strickland M, Heist R, Singh M, Nayyar N, Giobbie-Hurder A, Digumarthy S, Gainor J, Rajan A, Nieblas-Bedolla E, Burns A, Hallin J, Olson P, Christensen J, Kurz S, Brastianos P, Wakimoto H. Activity of Adagrasib (MRTX849) in Brain Metastases: Preclinical Models and Clinical Data From Patients With KRASG12C-Mutant Non-Small Cell Lung CancerPreliminary Activity of Adagrasib in Brain Metastases. Clinical Cancer Research 2022, 28: 3318-3328. PMID: 35404402, PMCID: PMC9662862, DOI: 10.1158/1078-0432.ccr-22-0383.Peer-Reviewed Original ResearchConceptsNon-small cell lung cancerKRAS-mutant non-small cell lung cancerBrain metastasesCerebrospinal fluidAntitumor activityUntreated BMCentral nervous system penetrationDose-dependent pharmacokineticsCell lung cancerKRASG12C inhibitorsPreliminary clinical dataRetrospective database queryCerebrospinal fluid concentrationsPharmacokinetic propertiesExtensive tissue distributionTumor regressionNSCLC xenograftsPreclinical modelsPoor prognosisPreclinical studiesAdagrasibExtended survivalLung cancerClinical dataLong half-life