BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate. It has shown antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action and predictable pharmacodynamic response.
|Preparation method||Human thrombin is dose-dependently and competitively inhibited by dabigatran (Table 2). This inhibition with a Ki of 4.5 nmol/L compares well to the Ki of melagatran (11.2 nmol/L). Real-time binding kinetics using surface plasmon resonance showed a rapid and reversible binding of dabigatran to thrombin.7 The concentration of dabigatran required tom double the in vitro coagulation time (EC2) in platelet poor plasma is species dependent and varies with the type of test (Table 3).|
|Animal models||rabbit model of venous thrombosis|
|Dosages||a single IV administration of 5, 10, 20, and 30 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Trocóniz et al. J Clin Pharmacol. Population pharmacokinetic analysis of the new oral thrombin inhibitor dabigatran etexilate (BIBR 1048) in patients undergoing primary elective total hip replacement surgery.
|Related Thrombopoietin/Thrombin Products|
Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist.
Heparin sodium salt(HY-17567A 150U/mg), a highly sulfated glycosaminoglycan, is widely used as an injectable anticoagulant, and has the highest negative charge density of any known biological molecule.
Eltrombopag olamine is a small-molecule, nonpeptide thrombopoietin receptor agonist with megakaryopoiesis-stimulating activity.
Dabigatran Etexilate is the procompound of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule.
Eltrombopag is a member of the biarylhydrazone class, which is a nonpeptide agonist of the thrombopoietin receptor (TpoR).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.