Abstract
The unique opportunity for aptamer uses in thrombotic events has sparked a considerable amount of research in the area. The short half-lives of unmodified aptamers in vivo remain one of the major challenges in therapeutic aptamers. Much of the incremental successful therapeutic aptamer stories were due to modifications in the aptamer bases. This mini-review briefly summarizes the successes and challenges in the clinical development of aptamers for thrombotic events, and highlights some of the most recent developments in using aptamers for anticoagulation monitoring.
Highlights
Antibodies and their variants, such as antigen-bind fragments (Fab) and single-chain variable fragments, have received considerable attention in the area of biomedicine
ARC-1779 is a DNA aptamer developed by the Archemix Corporation to target the human von Willebrand factor [23]. vWF interacts with GP1b on platelets to affect the P2Y12 receptor, which leads to platelet activation
REG1, known as pegnivacogin, is an RNA aptamer that acts as a direct factor IXa inhibitor [32]
Summary
Antibodies and their variants, such as antigen-bind fragments (Fab) and single-chain variable fragments (scFv), have received considerable attention in the area of biomedicine. There has been a modest increase in the number of biological drugs approved by the US FDA [1]. Almost all of the approved biologics are antibodies and antibody–drug conjugates, with a few additional enzyme products [1]. A largely under-explored area of biologics is nucleic acid-based aptamer therapies. The purpose of this review is to provide a summary and perspective of the clinical success and failure of aptamer-based therapeutic agents in the treatment and monitoring of thrombotic events
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