CXCR4-Targeting Molecules for Tumor Metastasis and PET Imaging

Application

Positron emission tomography (PET) imaging agents with high specificity for metastatic cancer.

Key Benefits

¹⁸F-labeled CXCR4 (partial) antagonist without stem cell mobilizing property is safe to be given to patient multiple times.
Identifies tumor location non-invasively and provides an indication of tumor’s metastatic potential.

Market Summary

Cancers are a large family of diseases affecting tens of millions of people worldwide each year. Nearly 14 million new worldwide cancer cases are diagnosed each year, and nearly 90% of all cancer deaths are due to metastasis. Positron Emission Tomography (PET) is a commonly used non-invasive imaging technique that reliably differentiates tumors from post-surgical changes or radiation necrosis, distinguishing between benign and malignant lesions based on specific biomarkers. The majority of clinical PET studies use a glucose-based metabolic tracer, ¹⁸F-Fluorodeoxyglucose, which detects cancer cells with high metabolism. Unlike metabolic tracers, CXCR4 expression has potential to be a powerful biomarker to detect the presence and lethal metastases of numerous tumors, and even predict metastasis (metastatic potential), but most CXCR4 antagonists have drawbacks of having property of stem cell mobilization.

Technical Summary

Emory inventors have developed a unique class of molecules that have characteristics of partial inhibition of CXCR4 function, lacking stem cell mobilizing property through rigorous drug screening assays. The lack of stem cell mobilization make these partial antagonists safer to use in multiple imaging sessions. Some molecules with rapid clearance from the blood and unseen toxicity even at high concentration were carefully selected in in vivo PET imaging studies. New methods based on click-chemistry labeling enable the final molecules to be labeled in a one-step process. These molecules have been investigated for uptake kinetics and distribution.