Novel Anticancer Pro-Drugs Activated by Hydrogen Peroxide

OTT1277

Applications

Anticancer drugs

Key Features

  • Safer – prodrugs are specifically designed only to be toxic for cancer cells 
  • Specific activation – targeted specifically to the tumor microenvironment 
  • Versatile – triggers can be added to a wide variety of already known cancer drugs 
  • Multifunctional – compounds contain multiple effectors for fighting cancer cells  
  • Better drug properties – prodrug design can aid in pharmaceutical problems of poor solubility, poor chemical stability, insufficient absorption, inadequate blood-brain barrier permeability, and pre-systemic metabolism 

Technology

An inventor at the University of Wisconsin-Milwaukee has developed pro-drug compounds that contain “triggers” activated by high levels of hydrogen peroxide deep inside a tumor and provide a new alternative for clinical use. They are ideal for cancer treatment due to their lack of toxicity in the body until they are located within the tumor microenvironment. and contain multiple potent effectors, some of which have been designed to cause DNA damage within the tumor leading to cell death.  Several of these compounds have undergone initial testing through the National Cancer Institute’s NCI 60-Cell Line Screen and show promise in causing cell growth inhibition or death in Leukemia, Non-Small Cell Lung Cancer, and breast cancer.  Invitro cytotoxicity assays with H2O2 inducible compounds have shown growth inhibition of cancer cells at less than 1 micromolar and they induced apoptosis in primary leukemic lymphocytes. A nude mouse xenograft trial for breast cancer showed significant decreases in tumor size in treated mice. 

Intellectual Property

United States Utility Patent, Anti-Cancer Agents: 8,962,670

Inventor(s)

Xiaohua Peng, Yunyan Kuang, Sheng Cao, Yibin Wang