Alteplase

Alteplase is a recombinant tissue plasminogen activator (rt-PA) used as a thrombolytic agent. It cleaves plasminogen to form plasmin, an enzyme involved in the degradation of fibrin clots. In the absence of fibrin, the alteplase-mediated conversion of plasminogen is limited, thanks to the high affinity between alteplase and fibrin. Alteplase is a purified glycoprotein of 527 amino acids expressed in Chinese hamster ovary (CHO) cells. It was first approved by the FDA in 1987 for the management of thromboembolic disease, including acute myocardial infarction (AMI). The use of alteplase to manage AMI has decreased thanks to the availability of safer treatments such as angioplasty and stenting. However, its use for the treatment of acute ischemic stroke (AIS) has increased over the years. New thrombolytic agents derived from tissue plasminogen activator, such as desmoteplase, tenecteplase and reteplase, have also been developed. Alteplase is also available as Cathflo Activase (intracatheter instillation) for the restoration of function to central venous access devices.

Alteplase is indicated for the treatment of acute ischemic stroke (AIS) and for use in acute myocardial infarction (AMI) for the reduction of mortality and incidence of heart failure. Alteplase is also indicated for the lysis of acute massive pulmonary embolism, defined as acute pulmonary emboli obstructing blood flow to a lobe or multiple lung segments, and acute pulmonary emboli accompanied by unstable hemodynamics.