Today’s cyclodextrin is a reminder of a fascinating application of cyclodextrins, the project CRLX-101 by Ellipses Pharma. This is a unique technology proposing a conjugate of a cyclodextrin-containing polymer to camptothecin for anticancer therapy, particularly ovarian cancer.
CRLX101 (formerly IT-101) is a first-in-class nanopharmaceutical, currently in clinical 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.

Treatment of cancer using a cyclodextrin-containing polymer-topoisomerase inhibitor conjugate and a parp inhibitor