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Chapter 8. Polymeric Nanoparticles and Cancer: Lessons Learnt from CRLX101

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.

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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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Davis, Mark E.0000-0001-8294-1477
Additional Information:© 2016 Royal Society of Chemistry.
Series Name:RSC Drug Discovery Series
Issue or Number:51
Record Number:CaltechAUTHORS:20160729-120515808
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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
Deposited By: Ruth Sustaita
Deposited On:29 Jul 2016 19:56
Last Modified:11 Nov 2021 04:12

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