Abstract
Abstract Docetaxel is one of the most commonly prescribed anticancer agents. While efficacious, the therapeutic benefits of docetaxel are often compromised by immunosuppression and neurotoxicity, incurring a discontinuation rate of over 25%. Cerulean has developed a novel class of tumor-targeted nanopharmaceuticals designed to enhance both efficacy and tolerability. CRLX301, a self-assembling docetaxel nanopharmaceutical, possesses significantly enhanced efficacy and improved pharmacokinetics compared to the parent drug. IND-enabling toxicity studies for CRLX301 are currently underway. Compared to docetaxel, CRLX301 showed a superior PK profile, with a significantly longer half-life and a >20-fold higher drug concentration in tumor tissue 7 days after a single administration. The improved PK and biodistribution of CRLX301 docetaxel translated into superior antitumor activity in murine syngeneic and human xenograft models. In the murine B16.F10 tumor model, median survival at the MTD exceeded 100 days for CRLX301 compared to 38 days for the parent drug docetaxel. CRLX301 also demonstrated superior efficacy over docetaxel in tumor models representative of other cancer types as well, including cure rates between 50 and 83% in xenograft models representing triple-negative breast and squamous non-small cell lung cancer tumors, compared to no cures for docetaxel. Further, in the human prostate xenograft tumor model DU-145, CRLX 301 achieved a 100% cure rate compared to a relatively poor cure rate of 25% with docetaxel, 146 days after three weekly doses at the MTD. In summary, CRLX301 represents a new and potent anticancer therapeutic that has the potential to be a best-in-class taxane. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 5643. doi:1538-7445.AM2012-5643
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