ABCB1 and ABCG2 regulation at the blood-brain barrier: potential new targets to improve brain drug delivery

JA Schulz, AMS Hartz, B Bauer - Pharmacological Reviews, 2023 - ASPET
The drug efflux transporters ABCB1 and ABCG2 at the blood-brain barrier limit the delivery
of drugs into the brain. Strategies to overcome ABCB1/ABCG2 have been largely …

Improving CNS delivery to brain metastases by blood–tumor barrier disruption

SA Sprowls, TA Arsiwala, JR Bumgarner, N Shah… - Trends in cancer, 2019 - cell.com
Brain metastases encompass nearly 80% of all intracranial tumors. A late stage diagnosis
confers a poor prognosis, with patients typically surviving less than 2 years. Poor survival …

Preclinical comparison of the blood–brain barrier permeability of osimertinib with other EGFR TKIs

N Colclough, K Chen, P Johnström, N Strittmatter… - Clinical Cancer …, 2021 - AACR
Purpose: Osimertinib is a potent and selective EGFR tyrosine kinase inhibitor (EGFR-TKI) of
both sensitizing and T790M resistance mutations. To treat metastatic brain disease, blood …

EGFR, the Lazarus target for precision oncology in glioblastoma

B Lin, J Ziebro, E Smithberger, KR Skinner… - Neuro …, 2022 - academic.oup.com
The Lazarus effect is a rare condition that happens when someone seemingly dead shows
signs of life. The epidermal growth factor receptor (EGFR) represents a target in the fatal …

Efficacy of neratinib plus capecitabine in the subgroup of patients with central nervous system involvement from the NALA trial

SA Hurvitz, C Saura, M Oliveira, ME Trudeau… - The …, 2021 - academic.oup.com
Background Neratinib has efficacy in central nervous system (CNS) metastases from HER2-
positive metastatic breast cancer (MBC). We report outcomes among patients with CNS …

Drug concentration asymmetry in tissues and plasma for small molecule–related therapeutic modalities

D Zhang, CECA Hop, G Patilea-Vrana, G Gampa… - Drug Metabolism and …, 2019 - ASPET
The well accepted “free drug hypothesis” for small-molecule drugs assumes that only the
free (unbound) drug concentration at the therapeutic target can elicit a pharmacologic effect …

Advances in the management of non-small-cell lung cancer harbouring EGFR exon 20 insertion mutations

JL Low, SM Lim, JB Lee, BC Cho… - … Advances in Medical …, 2023 - journals.sagepub.com
Epidermal growth factor receptor (EGFR) mutation is one of the key oncogenic mutations in
non-small-cell lung cancer with adenocarcinoma histology. Exon 19 deletions and exon 21 …

Blood–brain barrier penetration prediction enhanced by uncertainty estimation

X Tong, D Wang, X Ding, X Tan, Q Ren, G Chen… - Journal of …, 2022 - Springer
Blood–brain barrier is a pivotal factor to be considered in the process of central nervous
system (CNS) drug development, and it is of great significance to rapidly explore the blood …

Repurposed anti-cancer epidermal growth factor receptor inhibitors: mechanisms of neuroprotective effects in Alzheimer's disease

HM Mansour, HM Fawzy, AS El-Khatib… - Neural regeneration …, 2022 - journals.lww.com
Numerous molecular mechanisms are being examined in an attempt to discover disease-
modifying drugs to slow down the underlying neurodegeneration in Alzheimer's disease …

Pathogenetic features and current management of glioblastoma

HM Nguyen, K Guz-Montgomery, DB Lowe, D Saha - Cancers, 2021 - mdpi.com
Simple Summary Glioblastoma (GBM) is the most common form of primary malignant brain
tumor with a devastatingly poor prognosis. Tumor heterogeneity (cellular, molecular and …