SBIR Phase I: Rationally-designed, modular imaging agents for the targeted detection of tumors.

This NSF SBIR Phase I project takes a unique holistic approach to both tumor imaging and cancer drug delivery. This approach harnesses cancer cell proteins already in the body to allow selective delivery of tumor imaging agents or cancer-killing drugs to, and into, cancer cells. By choosing cancer-specific targeting proteins, the drugs will be transported primarily into cancer cells and undesirable off-target enrichment will be diminished. The goal is to mitigate drug uptake in non-cancerous fast-growing cells like; heart cells, bone marrow, skin or hair follicles. Treated patients will benefit from improved effectiveness of their cancer therapies. Such selective delivery should permit lower dosages of drug to be administered while also lowering the risks of unwanted, problematic side-effects. This cost-effective approach is well supported by the NSF?s core mission for the technical development of innovative drug delivery systems. It remains challenging to provide sensitive tumor diagnosis and near-simultaneous assessments of response to cancer treatments in treated individuals. Of all the standard monitoring modalities, radiographic examination has been the most widely used to measure treatment response. However, some studies suggest up to 10-40% of cancers may not be measurable by currently available technologies. Various delivery approaches have been used to take advantage of endogenous molecules to transport imaging agents or drugs with increased specificity into cancer cells. Most of these approaches utilize macromolecular ligands or cell surface receptor binding approaches. This proposal takes a mechanistically innovative small-molecule approach. By harnessing the activities of endogenous inflammatory proteins produced in abundance by cancer cells and by cells within the tumor micro-environment, small molecule cancer drugs can be transported with efficiency to the site of their intended effect. Selective and accurate placement of a chemically-related diagnostic agent into cancer cells should allow a cost-effective, more personalized and exceedingly sensitive view of treatment response.