OB-001 Enhances Osimertinib Brain Penetration: Preclinical Pharmacokinetics and Translational Rationale for EGFR-Mutant NSCLC with CNS Disease.

Abstract excerpt

Osimertinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with proven efficacy in EGFR-mutant non-small cell lung cancer (NSCLC), including patients with central nervous system (CNS) disease. However, pharmacokinetic (PK) studies demonstrate low CNS penetration (CSF:plasma 0.8%-22%), largely due to ABCB1/ABCG2 efflux. OB-001, a KinetiSol amorphous solid dispersion...

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