Drug intelligence / Profile preview

activated protein c

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Replacement Enzymes → Therapeutic Enzymes → Recombinant Proteins and Enzymes
Administration
Intravenous, Subcutaneous
01

Overview

Activated protein C (APC) is a serine protease with potent anticoagulant and anti-inflammatory properties. It is the enzymatically active form of protein C, a vitamin K-dependent glycoprotein synthesized in the liver. Upon activation by thrombin-thrombomodulin complex on endothelial cells, APC inactivates coagulation factors Va and VIIIa, reducing thrombin formation and thus clot formation. In addition to its anticoagulant effects, APC has anti-inflammatory actions by inhibiting tumor necrosis factor production and leukocyte adhesion to selectins. Recombinant forms such as drotrecogin alfa (marketed as Xigris) were developed for severe sepsis but withdrawn due to lack of efficacy. Human plasma-derived concentrates (e.g., Ceprotin) are approved for congenital protein C deficiency to prevent or treat venous thrombosis and purpura fulminans[2][4][5][7].

Brand names
XigrisCeprotin
Other names
drotrecogin alfarecombinant human activated protein cautoprothrombin IIAblood coagulation factor XIV
02

Targets

PAI-1 (Plasminogen activator inhibitor type 1)F5a (Coagulation Factor Va)F8 (Coagulation Factor VIIIa)

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