Pharmacology · Anticoagulants, Antiplatelets and Thrombolytics

Tenecteplase differs from alteplase in a way that allows single-bolus administration in myocardial infarction. The relevant modification is:

  • A Fusion with a monoclonal antibody fragment
  • B Removal of the kringle domain, abolishing fibrin binding
  • C Conjugation with polyethylene glycol to prevent clearance
  • D Substitution of amino acids conferring longer half-life and greater fibrin specificity
Correct answer: D. Substitution of amino acids conferring longer half-life and greater fibrin specificity

Explanation

Tenecteplase is a genetically engineered alteplase variant with defined amino acid substitutions that increase fibrin specificity roughly 14-fold, increase resistance to PAI-1, and prolong the half-life from about 5 minutes to 20 minutes or more, permitting a single weight-adjusted bolus instead of an infusion. It retains the kringle domains needed for fibrin binding, and neither pegylation nor antibody fusion is involved.

Reference: Goodman and Gilman's The Pharmacological Basis of Therapeutics, 14th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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