Derivatives as CXCR4 Modulators for the Treatment of Inflammation and Metastasis


Amide derivatives as chemokine receptor type 4 (CXCR4) modulators for the treatment of inflammation or prevention of cancer cell metastasis.

Key Benefits

  • Excellent binding affinity, compared to currently available compounds targeting CXCR4 receptor.
  • Stability in plasma compared to protein/peptide agonists of CXCR4, these amide derivatives can be cost effective, and easier to handle and store.
  • Compounds show reduced cytotoxicity issues and no mobilization of stem cells/tumors.

Market Summary

CXCR4 receptors play a crucial role in recruitment of inflammatory cells to inflammation sites at the beginning of the disease process. Overexpression of CXCR4 receptors is correlated with cancer metastasis and prognosis. Expression of CXCR4 is increased in many types of cancer such as breast, pancreatic, and colon among others. Modulating CXCR4 functions present a new avenue for effective anti-cancer and anti-inflammation strategies. Almost all drugs targeting CXCR4 receptors are currently in discovery or preclinical phase in a few selected preclinical animal models of inflammation.

Technical Summary

Emory researchers have developed partial CXCR4 antagonists with potential in treating medical disorders such as inflammation and metastatic tumors. These novel amide-sulfamide derivatives were developed using virtual high-throughput screening method and show excellent efficacy against CXCR4 and blocking CXCL12. The compounds show increased CXCR4 inhibition for inflammation and reduced risk of serious side effects or cytotoxicity. These CXCR4 antagonists also have potential in cancer treatment as a combination therapy with other anticancer molecules. The compounds have been tested and selected through two animal models of basic inflammation.

Developmental Stage

Early pre-clinical development.


Bai, R. et al. (2017). European Journal of Medicinal Chemistry, 126, 464-475.
Bai, R. et al. (2018) European Journal of Medicinal Chemistry. 150, 195-205.

Patent Information

App Type Country Serial No. Patent No. File Date Issued Date Patent Status
Nationalized PCT - United States United States 16/085,099 10,669,270 9/14/2018 6/2/2020 Issued
Nationalized PCT - Foreign EP 17767332.4   10/9/2018   Pending
Tech ID: 16021
Published: 4/24/2017