A Novel Composition for Selective Imaging and Therapy of Cancer

Reference #: 2015-028

OTC Contact: Ruchika Nijhara, Ph.D., MBA, CLP ( Directory Information | Send a Message )

Categories:  ”Cancer Therapeutics“, “Diagnostics


Standard chemotherapies are often limited due to side effects associated with off-target cytotoxicity of normal healthy cells. To alleviate this problem, researchers at Georgetown University have designed and synthesized a prodrug form of the tubulin-destabilizing agent combretastatin (CA-4) that contains an additional near-infrared (NIR) imaging moiety. The flurophore with the cleavable disulfide linker can be cleaved by intracellular glutathione (GSH) releasing the active drug. This release only occurs in the tumor cells as GSH is known to be upregulated in cancer cells over normal cells. The novel prodrug strategy allows CA-4 to be specific and selective for tumor cells and reduces off-target toxicities. Further, the present drug delivery system offers a theranostic agent wherein both a therapeutic effect and drug uptake-related imaging information are produced and can be used for monitoring of dosage levels. 


  • Therapeutic for solid tumors
  • Near-infrared imaging of solid tumors
  • Research tool


  • Specific and selective activation of cytotoxic CA-4 reduces toxic side effects with traditional chemotherapeutics
  • Near-infrared imaging moiety is released in the tumor, which allows for deep tissue penetrance and specificity


  • Lead compound synthesized
  • In vitro proof of concept demonstrated


Patent pending


Milton L. Brown, Yali Kong