A pentapeptide enabled AL3810 liposome-based glioma-targeted therapy with immune opsonic effect attenuated.

Author: Jinyang LI ¹ ; Jiasheng LU ¹ ; Haiyan GUO ¹ ; Jianfen ZHOU ¹ ; Songli WANG ¹ ; Kuan JIANG ¹ ; Zhilan CHAI ¹ ; Shengyu YAO ¹ ; Xiaoyi WANG ¹ ; Linwei LU ² ; Cao XIE ¹ ; Yi CHEN ³ ; Weiyue LU ¹
Author Information

1. Department of Pharmaceutics, School of Pharmacy, Fudan University & Key Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education and PLA, Shanghai 201203, China.
2. The Institutes of Integrative Medicine of Fudan University, Shanghai 200041, China.
3. Chinese Academy of Sciences Shanghai Institute of Materia Medica, Shanghai 201203, China.
Publication Type:Journal Article
Keywords: Anti-glioma efficacy; Immune opsonization; Immunogenicity; Liposome; c(RGDyK); mn
From: Acta Pharmaceutica Sinica B 2021;11(1):283-299
CountryChina
Language:English
Abstract: AL3810, a molecular dual inhibitor of the vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR), has earned the permission of phase II clinical trial for tumor treatment by China FDA. As a reversible ATP-competitive inhibitor, AL3810 targets ATP-binding site on intracellular region of VEGFR and FGFR, whereas, AL3810 lacking interplay with extracellular region of receptors rendered deficient blood-brain tumor barrier (BBTB) recognition, poor brain penetration and unsatisfactory anti-glioma efficacy. Integrin