ANTICOAGULANT WITH DIRECT ACTION BASED ON MODULAR BIVALENT DNA OF APTAMER SELECTIVE TO THROMBIN Russian patent published in 2017 - IPC A61K31/00 C12Q1/68 C12N15/11 C12N15/115 G01N33/86 

FIELD: biotechnology.

SUBSTANCE: method for chemical modification of an antithrombin aptamer and for preparation of a new antithrombin aptamer with anticoagulant properties and prolonged antithrombotic activity is described. The invention describes an aptameric DNA oligonucleotide specifically binding to thrombin and having a nucleotide sequence of the general formula GGTTGGTGTGGTTGGTGGTTGGTGTGGTTGG, wherein at least one of the nucleotides is modified to bind to the polyethylene glycol molecule and increase the time of oligonucleotide residence in the blood stream. In the preferred versions of the invention, the modification is made by thymine at 7, 9, 16, 23 and/or 25 positions. The invention can be used as an anticoagulant and antithrombotic drug for prevention or treatment of thromboses of various nature.

EFFECT: improved pharmacokinetic parameters, low toxicity and high affinity for human thrombin.

11 cl, 5 dwg, 2 ex