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

Cissy      Young; Thomas      Schluep; Jungyeon      Hwang; Scott      Eliasof

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 (CDPEG) 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.

Keywords: Nanopharmaceutical, oncology, camptothecin, topoisomerase 1