Tenecteplase

Tenecteplase is an engineered, second-generation tPA-derived thrombolytic produced in a CHO cell line [39]. The 527-amino acid glycoprotein differs from native tPA by (1) substitution of Thr103 with Asn, (2) substitution of Asn117 with Glu, and (3) replacement of residues 296 to 299 with four Ala residues. The first two modifications reside in the K1 domain whereas residues 296 to 299 reside in the protease domain. The changes have been introduced by site-directed mutagenesis of a cDNA coding for native tPA. The therapeutic rationale for developing Tenecteplase was the generation of a tPA variant that can be administered intravenously as a rapid single-dose bolus injection [40]. The product is manufactured by Genentech. It is marketed in the United States under the trade name TNKase and in Europe as Metalyse (Table 3.3).

Tenecteplase is indicated in the treatment of AMI. The indication wording in the United States is "for the reduction of mortality associated with AMI." The EU wording is "for the thrombolytic treatment of suspected myocardial infarction with persistent ST evaluation or recent left Bundle Branch Block within 6 h after the onset of AMI symptoms" [41]. A single-dose bolus based upon the patient's weight but not exceeding a total dose of 50 mg is generally administered over a 5 sec period.

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