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. 2011 Mar;7(1):8-14.
doi: 10.2174/157340711795163866.

CRLX101 (formerly IT-101)-A Novel Nanopharmaceutical of Camptothecin in Clinical Development

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Free PMC article

CRLX101 (formerly IT-101)-A Novel Nanopharmaceutical of Camptothecin in Clinical Development

Cissy Young et al. Curr Bioact Compd. 2011 Mar.
Free PMC article

Abstract

CRLX101 (formerly IT-101) is a first-in-class nanopharmaceutical, currently in Phase 2a development, which has been developed by covalently conjugating camptothecin (CPT) to a linear, cyclodextrin-polyethylene glycol (CD-PEG) co-polymer that self-assembles into nanoparticles. As a nanometer-scale drug carrier system, the cyclodextrin polymeric nanoparticle technology, referred to as "CDP", has unique design features and capabilities. Specifically, CRLX101 preclinical and clinical data confirm that CDP can address not only solubility, formulation, toxicity, and pharmacokinetic challenges associated with administration of CPT, but more importantly, can impart unique biological properties that enhance CPT pharmacodynamics and efficacy.

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Figures

Fig. (1)
Fig. (1)
Schematic diagram of CRLX101, a nanopharmceutical comprised of camptothecin conjugated to a linear, cyclodextrin-polyethylene glycol (CD-PEG) co-polymer and formulated into nanoparticles.
Fig. (2)
Fig. (2)
Cryo-TEM of CRLX101.

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