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. Hofman^1,4, Axel H. Schönthal³, and Thomas C. Chen^1,4

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.

 

 

¹Department of Neurosurgery, Keck School of Medicine, University of Southern California, Los Angeles, California, USA, ²Lawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, California, USA, ³Department of Molecular Microbiology and Immunology, Keck School of Medicine, University of Southern California, Los Angeles, California, USA, ⁴Department of Pathology, Keck School of Medicine, University of Southern California, Los Angeles, California, USA