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Alteplase, sold under the brand name Activase among others, is a biosynthetic form of human tissue-type plasminogen activator (t-PA). It is a thrombolytic medication used to treat acute ischemic stroke, acute ST-elevation myocardial infarction (a type of heart attack), pulmonary embolism associated with low blood pressure, and blocked central venous catheter. Alteplase is given by injection into a vein or artery. and is synthesized via recombinant DNA technology in Chinese hamster ovary cells (CHO). Alteplase causes the breakdown of a clot by inducing fibrinolysis.

thumb|Blood flow obstructed by coagulated blood that could potentially be reversed with alteplase.

Medical uses

Alteplase is indicated for the treatment of acute ischemic stroke, acute myocardial infarction, acute massive pulmonary embolism, and blocked catheters. Similar to other thrombolytic drugs, alteplase is used to dissolve clots to restore tissue perfusion, but this can vary depending on the pathology. Generally, alteplase is delivered intravenously into the body.

Ischemic stroke

In adults diagnosed with acute ischemic stroke, thrombolytic treatment with alteplase is the standard of care. Administration of alteplase is associated with improved functional outcomes and reduced incidence of disability.

Pulmonary embolism

As of 2019, alteplase is the most commonly used medication to treat pulmonary embolism. Alteplase has a short infusion time of 2 hours and a half-life of 4–6 minutes.

Systemic thrombolysis can quickly restore right ventricular function, heart rate, and blood pressure in patients with acute PE. However, standard doses of alteplase used in systemic thrombolysis may lead to massive bleeding, such as intracranial hemorrhage, particularly in older patients.

Blocked catheters

Alteplase can be used in small doses to clear blood clots that obstruct a catheter, reopening the catheter so it can continue to be used. Catheter obstruction is commonly observed with a central venous catheter. Currently, the standard treatment for catheter obstructions in the United States is alteplase administration. Novel alternatives to treat catheter occlusion, such as tenecteplase, reteplase, and recombinant urokinase, offer the advantage of shorter dwell times than alteplase. Contraindications for use of alteplase in people with a STEMI are similar to those of acute ischemic stroke. Adverse effects of alteplase include symptomatic intracranial hemorrhage and fatal intracranial hemorrhage. This sparked a medical paradigm shift as it redesigned stroke treatment in the emergency department to allow for timely assessment and therapy for ischemic stroke patients.

In May 1987, the US Food and Drug Administration (FDA) requested additional data for the drug rather than approve it outright, causing Genentech stock prices to fall by nearly one quarter. The decision was described as a surprise to the company as well as many cardiologists and regulators, and it generated significant criticism of the FDA.

After results from two additional trials were obtained, This was just seven years after the first efforts were made to produce recombinant t-PA, making it one of the fastest drug developments in history. However, alteplase continues to be cost-effective. Activase,

Controversies

Alteplase is underused in low- and middle-income countries. This may be due to its high cost and the fact that it is often not covered by health insurance.

There is a sex difference in the use of intravenous tissue plasminogen activator, as it is less likely to be used for women with acute ischemic stroke than men. However, this difference has been improving since 2008.