학술논문
Design and optimisation of dendrimer-conjugated Bcl-2/xL inhibitor, AZD0466, with improved therapeutic index for cancer therapy
Document Type
article
Author
Claire M. Patterson; Srividya B. Balachander; Iain Grant; Petar Pop-Damkov; Brian Kelly; William McCoull; Jeremy Parker; Michael Giannis; Kathryn J. Hill; Francis D. Gibbons; Edward J. Hennessy; Paul Kemmitt; Alexander R. Harmer; Sonya Gales; Stuart Purbrick; Sean Redmond; Matthew Skinner; Lorraine Graham; J. Paul Secrist; Alwin G. Schuller; Shenghua Wen; Ammar Adam; Corinne Reimer; Justin Cidado; Martin Wild; Eric Gangl; Stephen E. Fawell; Jamal Saeh; Barry R. Davies; David J. Owen; Marianne B. Ashford
Source
Communications Biology, Vol 4, Iss 1, Pp 1-14 (2021)
Subject
Language
English
ISSN
2399-3642
Abstract
Claire Patterson et al. present the design and development of AZD0466, a drug-dendrimer conjugate, and use preclinical and mathematical models to determine the optimal release rate of the drug from the dendrimer carrier for maximal therapeutic index in terms of anti-tumour efficacy and cardiovascular tolerability. This study identifies this promising dual Bcl-2/Bcl-xL inhibitor for progression to clinical development.