Gritli, Ismael and Garmey, Edward Graeme and Eliasof, Scott and Tellez, Andres and Davis, Mark E. and Yun, Yen (2016) Chapter 8. Polymeric Nanoparticles and Cancer: Lessons Learnt from CRLX101. In: Nanomedicines. RSC Drug Discovery Series. No.51. Royal Society of Chemistry , Cambridge, UK, pp. 199-232. ISBN 978-1-84973-947-4. https://resolver.caltech.edu/CaltechAUTHORS:20160729-120515808
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Abstract
CRLX101 (formerly IT-101) is a novel cyclodextrin-based polymer that self-assembles into nanoparticles. CRLX101 is covalently conjugated to the hydrophobic topoisomerase 1 (TOP1)-inhibitor camptothecin (CPT) resulting in stabilized structure and increased water solubility. Extensive preclinical studies of CRLX101 demonstrated delayed renal clearance and a prolonged plasma half-life. The nanoparticle passively accumulates in tumour tissue through the enhanced permeability and retention effect and slowly releases active CPT leading to enhanced TOP1 inhibition, potential hypoxia inducible factor-1α (HIF-1α) effect, cancer stem cell targeting, and increased antitumour activity against multiple human tumour xenografts. More than 200 human cancer patients have been treated with CRLX101 in phase I/IIa and phase II clinical trials. In this chapter we explore a wide range of anti-cancer nanotherapeutic strategies to inhibit TOP1, HIF-1α and cancer stem cells. Moreover, we discuss the therapeutic value of combining HIF-1α inhibition with antiangiogenics. Finally, we return to CRLX101 and cover in detail the latest preclinical and clinical evaluations and discuss future directions.
| Item Type: | Book Section | |||||||||
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| Additional Information: | © 2016 Royal Society of Chemistry. | |||||||||
| Series Name: | RSC Drug Discovery Series | |||||||||
| Issue or Number: | 51 | |||||||||
| Record Number: | CaltechAUTHORS:20160729-120515808 | |||||||||
| Persistent URL: | https://resolver.caltech.edu/CaltechAUTHORS:20160729-120515808 | |||||||||
| Official Citation: | Chapter 8 Polymeric Nanoparticles and Cancer: Lessons Learnt from CRLX101 Ismael Gritli, Edward Garmey, Scott Eliasof, Andres Tellez, Mark E. Davis and Yen Yun Nanomedicines: Design, Delivery and Detection, 2016, 199-232 DOI:10.1039/9781782622536-00199 | |||||||||
| Usage Policy: | No commercial reproduction, distribution, display or performance rights in this work are provided. | |||||||||
| ID Code: | 69313 | |||||||||
| Collection: | CaltechAUTHORS | |||||||||
| Deposited By: | Ruth Sustaita | |||||||||
| Deposited On: | 29 Jul 2016 19:56 | |||||||||
| Last Modified: | 03 Oct 2019 10:21 |
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