Drug intelligence / Profile preview

alteplase + tenecteplase (Genentech)

Development stage
Unknown
Lead developer
Genentech
Modality
Therapeutic Enzymes → Recombinant Proteins and Enzymes
Administration
Intravenous
01

Overview

alteplase + tenecteplase refers to a combination or comparative grouping of two recombinant tissue plasminogen activators (rt-PA) used as thrombolytic agents. Alteplase (Activase) is a 527-amino acid glycoprotein that binds to fibrin in a thrombus and converts trapped plasminogen to plasmin, initiating local fibrinolysis. Tenecteplase (TNKase) is a bioengineered variant of alteplase containing three sets of mutations: a substitution of threonine 103 with asparagine, a substitution of asparagine 117 with glutamine, and a tetra-alanine substitution at amino acids 296-299. These modifications result in a longer plasma half-life, allowing for single-bolus administration, and significantly higher fibrin specificity compared to alteplase. Both drugs are primarily indicated for the management of acute myocardial infarction, while alteplase is also the standard of care for acute ischemic stroke and pulmonary embolism. Tenecteplase is increasingly utilized off-label for stroke due to its practical advantages in emergency settings.

Brand names
ActilyseMetalyseCathflo Activase
Other names
tissue plasminogen activatorrecombinant tissue plasminogen activator
02

Targets

PLG (Plasminogen)Fibrin (Factor Ia)

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