Prediction of Response to Therapy for Autoimmune/Inflammatory Diseases Using an Activated Macrophage-Targeted Radioimaging Agent

Mol Pharm. 2015 Oct 5;12(10):3547-55. doi: 10.1021/acs.molpharmaceut.5b00134. Epub 2015 Sep 17.

Abstract

The ability to select patients who will respond to therapy is especially acute for autoimmune/inflammatory diseases, where the costs of therapies can be high and the progressive damage associated with ineffective treatments can be irreversible. In this article we describe a clinical test that will rapidly predict the response of patients with an autoimmune/inflammatory disease to many commonly employed therapies. This test involves quantitative assessment of uptake of a folate receptor-targeted radioimaging agent ((99m)Tc-EC20) by a subset of inflammatory macrophages that accumulate at sites of inflammation. Murine models of four representative inflammatory diseases (rheumatoid arthritis, inflammatory bowel disease, pulmonary fibrosis, and atherosclerosis) show markedly decreased uptake of (99m)Tc-EC20 in inflamed lesions upon initiation of successful therapies, but no decrease in uptake upon administration of ineffective therapies, in both cases long before changes in clinical symptoms can be detected. This predictive capability should reduce costs and minimize morbidities associated with failed autoimmune/inflammatory disease therapies.

Keywords: EC20 radioimaging; activated macrophages; atherosclerosis; folate receptor targeting; idiopathic pulmonary fibrosis; inflammatory and autoimmune diseases; rheumatoid arthritis; ulcerative colitis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use*
  • Arthritis, Experimental / drug therapy
  • Atherosclerosis / drug therapy
  • Autoimmune Diseases / drug therapy*
  • Colitis, Ulcerative / drug therapy
  • Disease Models, Animal
  • Female
  • Flow Cytometry
  • Folate Receptors, GPI-Anchored / drug effects
  • Immunologic Factors / pharmacology
  • Immunologic Factors / therapeutic use*
  • Inflammation / drug therapy*
  • Macrophages / drug effects*
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred C57BL
  • Mice, Inbred DBA
  • Organotechnetium Compounds / pharmacology*
  • Pulmonary Fibrosis / drug therapy
  • Treatment Outcome

Substances

  • Anti-Inflammatory Agents
  • Folate Receptors, GPI-Anchored
  • Immunologic Factors
  • Organotechnetium Compounds
  • technetium 99m EC20 folate peptide