Pharmacokinetic properties of the temozolomide perillyl alcohol conjugate (NEO212) in mice.

ABSTRACT:

Background

NEO212 is a novel small-molecule anticancer agent that was generated by covalent conjugation of the natural monoterpene perillyl alcohol (POH) to the alkylating agent temozolomide (TMZ). It is undergoing preclinical development as a therapeutic for brain-localized malignancies. The aim of this study was to characterize metabolism and pharmacokinetic (PK) properties of NEO212 in preclinical models.

Methods

We used mass spectrometry (MS) and modified high-performance liquid chromatography to identify and quantitate NEO212 and its metabolites in cultured glioblastoma cells, in mouse plasma, brain, and excreta after oral gavage.

Results

Our methods allowed identification and quantitation of NEO212, POH, TMZ, as well as primary metabolites 5-aminoimidazole-4-car

SUBMITTER: Cho HY 

PROVIDER: S-EPMC7764505 | biostudies-literature | 2020 Jan-Dec

REPOSITORIES: biostudies-literature