P-selectin Inhibitor for the Treatment of Sickle Cell Disease

Application

A glycopeptide inhibitor of p-selectin for the treatment of sickle cell disease.

Key Benefits

  • Blocks the activity of P-selectin with nM affinity.
  • Potential treatment for vaso-occlusive crisis associated with sickle cell disease.
  • Inhibits the earliest stage of leukocyte activation helping to prevent immune response.

Market Summary

Sickle cell anemia, a serious disorder in which the body makes sickle-shaped red blood cells, affects thousands of Americans and a majority of these are African Americans. The most common clinical manifestation of sickle cell disease is vaso-occlusive crisis, which results in an average of 2.5 hospital visits per year for sickle cell patients in the U.S. Current treatments for vaso-occlusive crisis, such as opioids and rehydration, are primarily focused only the management of symptoms.

Technical Summary

P-selectin is a constitutively expressed carbohydrate-binding protein that helps activate leukocytes to initiate the inflammatory response in mammals. The best characterized ligand for P-selectin is called P-selectin glycoprotein ligand-1 (PSGL-1) which is expressed on the surface membranes of all leukocytes. PSGL-1 supports leukocyte recruitment in both innate and adaptive arms of the immune response. Because PSGL-1 plays an important role in vascular endothelial signaling, a PSGL-1 mimetic with the ability to block the activity of P-selectin has the potential to treat multiple indications, such as sickle cell anemia vaso-occlusive crisis, vascular inflammation, and thrombosis.

Developmental Stage

In vivo studies in mice show efficient blockade of P-selectin-dependent binding of leukocytes to the activated endothelium of blood vessels.

Patent Information

App Type Country Serial No. Patent No. File Date Issued Date Patent Status
Nationalized PCT - Foreign Canada 2,914,470 2,914,470 12/2/2015 9/27/2022 Issued
Nationalized PCT - United States United States 14/895,606 10,253,071 12/3/2015 4/9/2019 Issued
Nationalized PCT - Foreign EP 14806846.3 3004139 12/11/2015 5/6/2020 Issued
EP Registered Country France 14806846.3 3004139 12/11/2015 5/6/2020 Issued
EP Registered Country Germany 14806846.3 3004139 12/11/2015 5/6/2020 Issued
EP Registered Country Netherlands 14806846.3 3004139 12/11/2015 5/6/2020 Issued
EP Registered Country United Kingdom 14806846.3 3004139 12/11/2015 5/6/2020 Issued
EP Registered Country Switzerland 14806846.3 3004139 12/11/2015 5/6/2020 Issued
Divisional United States 16/352,585   3/13/2019   Pending
Tech ID: 13089
Published: 12/4/2013