In vivo fluorescence imaging of breast tumor-bearing mice after intravenous administration of Cy7.5 and dextran-lipid-Cy7.5.
The Dextran Docetaxel Conjugate A CQ-0527 eliminated all solid tumors in mice models and outperforms docetaxel without toxic signs
Comparison with drug concentrations of dextran lipid docetaxel conjugate LLG and the original drug docetaxel (DTX) in tumor tissues and normal tissues
After more than 20 years of research and hard work, our company has developed innovative technologies to overcome many of the challenges associated with polysaccharide drug conjugtes. We have achieved significant breakthroughs in the fields of polysaccharide functionalization, position-specific taxane functionalization, and the synthesis of polysaccharide-based polymer-drug conjugates. In particular, our first-in-class new drug candidate, CQ-0527, which targets tumors via macropinocytosis pathway, has entered the preclinical study phase.
Our in vivo imaging and anticancer experiments reveal that supramolecular dextran docetaxel (DTX) conjugates exhibit exceptional tumor-targeting capabilities. In breast tumor xenografted mouse models, low doses of these novel dextran-DTX conjugates completely eradicated solid tumors without notable toxicity. In lung cancer xenografted mouse models, our conjugates surpassed both the Tween-80 DTX formulation and Abraxane—a widely recognized, human albumin-bound paclitaxel standard in chemotherapy—excelling in tumor targeting, efficacy, safety, solubility, and formulation. At equivalent DTX doses, the dextran-DTX-treated group demonstrated over twice the efficacy of the standard DTX formulation. At equitoxic doses, the polysaccharide-DTX group achieved 2.3 times greater efficacy than controls. Furthermore, a single dose of our conjugates outperformed a double dose of Abraxane by 2.5 times in efficacy, underscoring their superior therapeutic potential.
In summary, our invented tumor targeting supra-molecular dextran docetaxel conjugates have superior properties as a promising anticancer drug candidate such as improved tumor targeting, reduced drug toxicities, and enhanced drug safety without causing immunogenicity and hypersensitivity. As a result, these excellent drug properties associated with our invented drug candidate may greatly improve the therapeutic efficacy in patients with much better patient compliance and with much fewer side effects; therefore, a better therapeutic index can be achieved. In all, these excellent drug properties associated with the patented innovative dextran docetaxel conjugates will enable it to be developed into a new generation of best in class (BIC) of taxane anticancer drugs.