NEO 212 Shows Efficacy In Treating Breast Cancer That Has Metastasized To The Brain

A Novel Temozolomide–Perillyl Alcohol Conjugate Exhibits Superior Activity against Breast Cancer Cells In Vitro and Intracranial Triple-Negative Tumor Growth In Vivo.

Authors: Thomas C. Chen^1,2, Hee-Yeon Cho¹, Weijun Wang¹, Manasai Barath³, Natasha Sharma⁴, Florance M. Hofman², and Axel H. Schönthal³.

Currently, there is no effective therapy for breast cancer that has spread to the brain. This is primarily due to the inability of breast cancer drugs from effectively reaching intracranial metastases due to the Blood-Brain Barrier (BBB). Although Temozolomide (TMZ), which is the gold standard for chemotherapeutic treatment of glioblastomas is able to penetrate the BBB, most trails that have been done to test whether TMZ has efficacy for brain metastases of breast cancer have shown mixed results that ranged from “encouraging activity” to “no objective responses.” In an effort to generate an agent with greater activity against intracranial breast metastases, NeOnc Technologies has performed a study testing its NEO 212 conjugate of TMZ and Peryllil Alcohol (POH) to see if increased anticancer activity in a variety of breast cancer cell lines would be effective.

In the study looking at the impact of NEO 212 on intracranial tumors with triple-negative breast cancer, it was shown that the conjugate provided considerably greater therapeutic efficacy than TMZ alone. In the study, the median survival benefit of the test animals was extended from 6 days, with TMZ alone, to 28 days using the NEO 212 TMZ/POH conjugate. At the same time, the test animals seemed to be able to tolerate the NEO 212 treatments without severe side-effects.

Departments of ¹Neurosurgery, ²Pathology, and ³ Molecular Microbiology & Immunology, and ⁴Pharmaceutical Sciences, University of Southern California, Los Angeles, CA.