Multi-Target CCR5/CXCR4 Chemokine Compounds for the Treatment of HIV


Chemical compounds that bind to both CCR5 and CXCR4 chemokine GPCRs as therapeutics to block HIV entry and infection.

Key Benefits

  • Targets both chemokine receptors used for cell entry by HIV: CCR5 & CXCR4.
  • Eliminates the requirement of a tropism pre-test used for drug administration of single chemokine agents.
  • Does not interfere with CXCR4-based G-protein coupled receptor signaling, suggesting they may be HIV-chemokine selective and reduce toxic side effects.
  • May provide better drug resistance profile versus other HIV medications.

Market Summary

 Highly active antiretroviral therapy (HAART) has limited HIV infection in developed countries and normally includes several antiretroviral agents that act on different stages of the HIV life-cycle. Combinations of antiretroviral agents form multiple obstacles to HIV replication to keep the viral load low and reduce the possibility of a superior mutation. However, due to the short life cycle and high error rate, HIV still generates drug-resistant strains in patients who do not take their regimen regularly, creating the need for new anti-HIV drugs. There are currently only two FDA-approved HIV entry inhibitors and neither inhibitor targets CXCR4. Furthermore, as the CXCR4-using variant of the virus highly correlates to the development of AIDS, an agent that targets this mechanism is an urgent and unmet need.

Technical Summary

Emory University researchers have identified compounds which potentially bind to both CCR5 and CXCR4 chemokine receptors. Initial results for some of the lead compounds show they do not interfere with CXCR4-based G-protein (GPCR) mediated signaling and therefore may have reduced toxic side effects. There are several lead compound series that have shown activity against both tropic forms of the virus in vitro. This technology may lead to anti-HIV drugs with lower resistance profiles.

Developmental Stage

Lead compounds have been identified and experiments are planned to improve anti-viral potency as well as performing further mechanistic studies.

Patent Information

App Type Country Serial No. Patent No. File Date Issued Date Patent Status
Nationalized PCT - United States United States 15/311,573 10,450,293 11/16/2016 10/22/2019 Issued
EP Registered Country France 15793622.0 3143005 11/25/2016 7/7/2021 Issued
EP Registered Country Germany 15793622.0 3143005 11/25/2016 7/7/2021 Issued
EP Registered Country United Kingdom 15793622.0 3143005 11/25/2016 7/7/2021 Issued
Nationalized PCT - Foreign EP 15793622.0 3143005 11/25/2016 7/7/2021 Issued
Tech ID: 14127
Published: 1/8/2016