Design and optimisation of dendrimer-conjugated Bcl-2/xL inhibitor, AZD0466, with improved therapeutic index for cancer therapy
oleh: 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
| Format: | Article |
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| Diterbitkan: | Nature Portfolio 2021-01-01 |
Deskripsi
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.