Intravenous Formulation of HET0016 Decreased Human Glioblastoma Growth and Implicated Survival Benefit in Rat Xenograft Models

Autor: Meshal Alsulami, Thaiz F. Borin, Bhagelu R. Achyut, Austin M. Guo, Meenu Jain, Roxan Ara, Wilson B. Chwang, Asm Iskander, Adarsh Shankar, Iryna Lebedyeva, Mohammad H. Rashid, Hassan Bagher-Ebadian, Ali S. Arbab, Zhi Wenbo, Meser M. Ali, Kartik Angara, Nipuni Dhanesha H Gamage
Rok vydání: 2017
Předmět:
Zdroj: Scientific Reports
ISSN: 2045-2322
DOI: 10.1038/srep41809
Popis: Glioblastoma (GBM) is a hypervascular primary brain tumor with poor prognosis. HET0016 is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth. Therefore, to explore novel treatments, we have generated an improved intravenous (IV) formulation of HET0016 with HPßCD and tested in animal models of human and syngeneic GBM. Administration of a single IV dose resulted in 7-fold higher levels of HET0016 in plasma and 3.6-fold higher levels in tumor at 60 min than that in IP route. IV treatment with HPßCD-HET0016 decreased tumor growth, and altered vascular kinetics in early and late treatment groups (p
Databáze: OpenAIRE