Development of Novel Epidermal Growth Receptor-Based Radiopharmaceutical: Imaging Agents for Breast Cancer
Abstract
The goal of this research is to develop nuclear medicine imaging agents, to aid in the early detection, diagnosis and treatment of breast cancer, based on the epidermal growth factor receptor (EGFr) biomarker. EUF receptors are upregulated in 45% of breast tumors and tumors possessing these receptors fail to respond to conventional treatment correlating with decreased patient survivability. Our approach is to design and synthesize small molecule inhibitors of the EGFr tyrosine kinase (tk) suitable for labeling with single photon and positron-emitting radioisotopes and evaluate the imaging potential of these new molecules. The initial evaluation includes the full chemical characterization of the new molecules, an assessment of their lipophilicity, determination of their ability to inhibit EGFr tk activity and measurement of their affinity for the EGFr tk. Those compounds which possess suitable potency and binding characteristics will be radiolabeled and subjected to a secondary evaluation in in vitro cell studies and in vivo distribution studies in tumor bearing mice. The expected outcome of this research is the development of one or two radiolabeled tracers to be carried forward to preclinical EGFr imaging.
Document Details
- Document Type
- Technical Report
- Publication Date
- Sep 01, 1999
- Accession Number
- ADA384549
Entities
People
- Henry F VanBrocklin
Organizations
- University of California, Berkeley