Open AccessPanobinostat penetrates the blood–brain barrier and achieves effective brain concentrations in a murine model
Author(s) -
Morgan J Homan,
Andrea Franson,
Karthik Ravi,
Holly Roberts,
Manjunath P. Pai,
Cai Liu,
Miao He,
Aleksas Matvekas,
Carl Koschmann,
Bernard L. Marini
Publication year - 2021
Publication title -
cancer chemotherapy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.112
H-Index - 111
eISSN - 1432-0843
pISSN - 0344-5704
DOI - 10.1007/s00280-021-04313-2
Subject(s) - panobinostat , pharmacokinetics , cmax , pharmacology , medicine , metabolite , chemistry , biochemistry , histone deacetylase , gene , histone
Panobinostat, an orally bioavailable pan-HDAC inhibitor, has demonstrated potent activity in multiple malignancies, including pediatric brain tumors such as DIPG, with increased activity against H3K27M mutant cell lines. Given limited evidence regarding the CNS penetration of panobinostat, we sought to characterize its BBB penetration in a murine model.