Aprotinin is a polypeptide with serine protease inhibitory activity of key enzymes associated with inflammatory, fibrinolytic, and hemostatic pathways. The drug binds directly to the fibrinolytic plasmin at the lower plasmin-inhibiting dose (plasma concentration, 137 KIU/mL), and the inflammatory mediator, kallikrein, using the higher kallikrein-inhibiting dose (plasma concentration, >250 KIU/mL). Aprotinin inhibits platelet glycoprotein loss (GpIb and GpIIb/IIIa receptors) associated with cardiopulmonary bypass and has been described as platelet sparing. Current literature supports direct anti-inflammatory effects through modulation of neutrophil activation, attachment, and transmigration, with resultant blunting in the rise of proinflammatory cytokine levels and deleterious tissue damaging enzymes. The pharmacologic properties of aprotinin may lead clinicians to consider this therapy for use as a hemostatic and anti-inflammatory agent in surgeries beyond its established use in coronary artery bypass graft surgery.