NEO 212 Preferentially Concentrates In Brain Tumor Tissue For Delivery Of TMZ
Pharmacokinetic Properties Of The Temozolomide Perillyl Alcohol Conjugate (NEO212) In Mice.
Authors: Hee-Yeon Cho1, Steve Swenson1, Thu Zan Thein1, Weijun Wang1, Weijun Wang1, Neloni R. Wijeratne2, Nagore I. Marín-Ramos1, Jonathan E. Katz2, Florence M. Hofman1,4, Axel H. Schönthal3, and Thomas C. Chen1,4
In a study to further validate NEO 212’s development as a therapeutic for brain-localized malignancies, NeOnc Technologies was able to characterize
metabolism and pharmacokinetic properties of NEO212 in preclinical models.
In the study, mass spectrometry and modified high-performance liquid chromatography to identify and quantitate NEO212 and its metabolites in cultured glioblastoma cells, in mouse plasma, brain, and excreta. The hope was to determine the half-life of the therapeutic for cytotoxicity as well as its ability to target a tumor site without causing harm to surrounding normal brain tissue.
The study showed that the half-life of NEO 212 in the subject plasma was 94 min and that NEO212 preferentially concentrates in brain tumor tissue over normal brain tissue, and compared to TMZ alone, has a higher brain: plasma ratio revealing favorable features to encourage its further development as a brain-targeted therapeutic.