CXCR4 Modulator for Preventing Cancer Metastasis


Amine derivatives as chemokine receptor type 4 (CXCR4) modulators to treat breast cancer and block tumor metastasis.

Key Benefits

  • New class of anti-cancer drugs targeting CXCR4 instead of COX pathway.
  • Partial antagonists are safer for use because they do not mobilize stem cells.

Market Summary

CXC chemokine receptor 4 (CXCR4) and stromal cell-derived factor 1 (SDF-1, also known as CXCL12) are a chemokine receptor and chemokine pair that play a critical role in cancer metastasis and inflammation. Expression of CXCR4 is increased in many types of cancer such as breast, pancreatic, and colon among others and overexpression of CXCR4 receptors is correlated with cancer metastasis and prognosis. Accumulating evidence suggests the involvement of CXCR4/SDF-1 interaction in the migration of tumor cells as well as various inflammatory diseases, including rheumatoid arthritis, autoimmune diseases, ischemic injuries, inflammatory bowel disease, and pneumonia. Modulating CXCR4 functions present a new avenue for effective anti-cancer and anti-inflammation strategies.

Technical Summary

CXCR4 inhibitors are promising agents for the treatment of breast cancer and prevention of cancer metastasis. A series of novel tertiary amine derivatives uniquely modulating CXCR4 were designed, synthesized, and evaluated. The central benzene ring linker and side chains were modified and optimized to study the structure–activity relationships. These partial antagonists are safer for long-term use than full antagonists because they do not mobilize stem cells. The compounds have been selected via in vitro testing to determine their CXCR4 modulating activities and potency. These compounds have the potential for complementary therapeutic strategy in cancer treatment, prevention of cancer metastasis, inflammatory diseases, and viral infections.

Developmental Stage

Selected compounds were tested in animal models of inflammation.


Bai, R. et al. (2017). European Journal of Medicinal Chemistry, 126, 464-475.
Bai, R. et al. (2016). European Journal of Medicinal Chemistry, 118, 340-350.

Patent Information

App Type Country Serial No. Patent No. File Date Issued Date Patent Status
Nationalized PCT - United States United States 15/745,291 10,709,697 1/16/2018 7/14/2020 Issued
Divisional United States 16/905,528 11,517,565 6/18/2020 12/6/2022 Issued
Tech ID: 15100
Published: 4/10/2017