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AACR Annual Meeting Presentation

11, May 2015
Abstract Number:
4471
         
Presentation Title:
The antitumor activity of hyaluronic acid nimesulide-NH2 bioconjugate (CA102N) in human colorectal cancer (CRC)
         
Presentation Time:
Tuesday, Apr 21, 2015, 1:00 PM - 5:00 PM
         
Location:
Section 30
         
Poster Board Number:
28
         
Author Block:
Eskouhie Tchaparian. HolyStone Healthcare, Taipei, Taiwan
         
Abstract Body:
Carrier mediated drug delivery systems are promising next generation therapeutics for targeted delivery and improved efficacy and safety of cytotoxic drugs. Hyaluronic Acid conjugated drugs (HACD) are novel carrier-mediated drug delivery systems (Targeting Carrier™) characterized by CD44-mediated endocytosis of Hyaluronic Acid (HA) and intracellular drug release. The present study investigates the in vitro and in vivo antitumor activity of CA102N, an HA- Cyclooxygenase-2 inhibitor conjugate, HA-Nimesulide, currently in preclinical development. Cyclooxygenase-2 (COX-2) inhibitors are a class of compounds that are associated with anticancer properties. CA102N was able to selectively inhibit HCT116 and HT29, CRC cancer cell growth in vitro with an IC50 of 57.7 and 77.14 μM respectively. In in vivo studies, strong anti-tumor effects and rapid tumor shrinkage was observed within 3 days posttherapy in mice bearing HT-29 xenografts treated with either 1.5 or 4.5 mg/kg of relative amount of the conjugate. Further, full and sustained regression of tumors was also attained during the entire observational period (14 days) after the last dose. No treatment related toxicity was noticed in mice. HACD drug delivery systems may offer great advantages in the development of a new class of bioconjugated drugs for intracellular delivery and enhanced safety of potent cytotoxic drugs.
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