Preclinical comparison of the blood brain barrier (BBB) permeability of osimertinib with other EGFR TKIs.

Conclusion These preclinical studies indicate that osimertinib can achieve significant exposure in the brain compared with the other EGFR-TKIs tested and supports the ongoing clinical evaluation of osimertinib for the treatment of EGFRm brain metastasis. This work also demonstrates the link between low in-vitro transporter efflux ratios and increased brain penetrance in-vivo supporting the use of in-vitro transporter assays as an early screen in drug discovery. PMID: 33028591 [PubMed - as supplied by publisher]

https://www.ncbi.nlm.nih.gov/pubmed/33028591?dopt=Abstract

Source: Clinical Cancer Research - October 7, 2020 Category: Cancer & Oncology Authors: Colclough N, Chen K, Johnström P, Strittmatter N, Yan Y, Wrigley GL, Schou M, Goodwin RJA, Varnäs K, Adua SJ, Zhao M, Nguyen DX, Maglennon GA, Barton P, Atkinson J, Zhang L, Janefeldt A, Wilson J, Smith A, Takano A, Arakawa R, Kondrashov M, Malmquist J, Tags: Clin Cancer Res Source Type: research