Comparative in vitro study of anticoagulant activity of RA36 DNA aptamer in human, rabbit, and rat blood plasma
Savchik, E.I.; Kalinina, T.B.; Drozd, N.N.; Makarov, V.A.; Zav'ialova, E.G.; Lapsheva, E.N.; Babiĭ, A.V.; Mudrik, N.N.; Pavlova, G.V.; Golovin, A.V.; Kopylov, A.M.
Eksperimental'naia i Klinicheskaia Farmakologiia 75(11): 13-18
2012
ISSN/ISBN: 0869-2092 PMID: 23323327 Document Number: 661202
DNA aptamer RA36 with a molecular weight of 10000 is direct-acting anticoagulant whose efficacy is lower than that of recombinant hirudin and unfractionated heparin (UFH) in blood clotting time (BCT), activated blood recalcification time (ABRT), recalcification time (RT), prothrombin time (PT), and activated partial thromboplastin time (APTT) tests. The anticoagulant effect of RA36 is comparable with that of UFH in the thrombin time (TT) test, but is lower than the effect of recombinant hirudin. Analysis of the blood and plasma anticoagulant activity during intravenous bolus administration of aptamer RA36 in rabbits and rats is based on the use ABRT (in blood case) and APTT/RT (in plasma case) tests. The range of doses for evaluation of pharmacodynamic parameters of RA36 during intravenous bolus administration in rabbits and rats is 3 - 34 mg/kg and 1 - 27 mg/kg, respectively. Accordingly, designed dose range for humans is 1 -29 mg/kg.