Full Prescribing Information

Activase® (Alteplase) is a tissue plasminogen activator produced by recombinant DNA technology.

Status Activase is approved for treating acute myocardial infarction (AMI), or heart attacks, acute ischemic stroke, and acute, massive pulmonary embolism. Activase is the first therapy to be indicated for the management of stroke.

Proposed Mechanism of Action Activase works by stimulating the body's own clot-dissolving mechanism by activating plasminogen, a naturally occurring substance secreted by endothelial cells in response to injury to the artery walls that contributes to clot formation.

AMI, Stroke and Pulmonary Embolism Heart attack, or acute myocardial infarction, is caused when a blood clot obstructs a coronary artery supplying blood to the heart. This causes an inadequate flow of oxygenated and nutrient rich blood and results in the death of a portion of the heart muscle. Stroke is the number one cause of adult disability in America, with more than three million people living with the effects of stroke; more than one million of whom are severely impaired. About 80 percent of all strokes are acute ischemic strokes caused by a blood clot stopping or diminishing blood flow to an area of the brain. Thus, acute ischemic stroke, or "brain attack," has comparable physiological cause as an acute myocardial infarction, or heart attack. Pulmonary embolism is the blocking of the pulmonary artery by foreign matter such as a blood clot.

Safety Information There are risks involved with Activase treatment. Because Activase is a clot buster, the most common side effect is bleeding, including bleeding in the brain, called intracranial hemorrhage (ICH). Not all patients with acute ischemic stroke will be able to use Activase, including patients with recent or ongoing bleeding; recent (within 3 months) brain or spinal surgery, a serious head injury, or previous stroke; uncontrolled high blood pressure; or problems with blood clotting.

All thrombolytic agents increase the risk of bleeding, including intracranial bleeding, and should be used only in eligible patients. In addition, thrombolytic therapy increases the risk of stroke, including hemorrhagic stroke, in elderly patients (>75 years).