The core expertise of our team lies in drug design and synthesis, cell toxicity testing, in vitro stability assays of drugs, animal efficacy evaluation, and pharmacokinetic studies. The novel conjugate can be delivered to cancer cells by glucose transporters and activated by enzymatic proteins in the tumor microenvironment. This activation releases the cytotoxic agent and the glucose transporter inhibitor, resulting in a synergistic effect and achieving specific cancer cell killing.

Our team first developed a novel conjugate that contained a glucose transporter inhibitor (targeting moiety) and cytotoxic agent. Compound 10 is capable of specifically activating within the tumor and releasing the active drug SN38. In an orthotopic colorectal cancer animal model, Compound 10 exhibits superior anti-tumor activity compared to the clinically used Irinotecan. Furthermore, it demonstrates good safety characteristics, making it a promising candidate for cancer therapy.

Compound 10 demonstrates excellent anti-tumor activity with high specificity and safety, making it suitable for colorectal cancer patients and those who have developed resistance to 5-FU or Irinotecan. Moreover, cancer patients with overexpression of glucose transporters, such as pancreatic cancer patients, are expected to benefit from this compound. This invention is tech-transferred to ImmunAdd Inc., with over NTD 10 million licensing fee. PCT application was applied in Mar 2022