生物活性

• 描述Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor Xa with K of 0.08 nM and 0.17 nM for Human Factor Xa and Rabbit Factor Xa, respectively. In vitro, Apixaban prolongs the clotting times of normal human plasma with the concentrations (EC) of 3.6 μM, 0.37 μM, 7.4 μM, and 0.4 μM, which are required respectively to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT) and HepTest. Besides, Apixaban shows the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays.

• 动物研究
  剂量	Rat: 0.1 mg/kg - 3 mg/kg[3] (i.v.) Rabbit: 0.015 mg/kg - 0.5 mg/kg[4] (i.v.) Horse: 0.15 mg/kg - 0.2 mg/kg[5] (p.o./i.v.)
  给药途径	i.v., p.o.
  动物药代数据	Animal Rats[3] Dogs[3] Dose 0.5 mg/kg (i.v.) 2 mg/kg (p.o.) 0.2 mg/kg (i.v.) 0.5 mg/kg (p.o.) Administration i.v. p.o. i.v. p.o. F 34% (p.o.) 88% (p.o.) AUC0→24h 2.0 μg·h/ml (i.v.) 2.7 μg·h/ml (p.o.) 3.9 μg·h/ml (i.v.) 8.0 μg·h/ml (p.o.) T1/2 1.9 h (i.v.) 3.2 h (p.o.) 5 h (i.v.) 5.8 h (p.o.) Tmax 0.5 h (p.o.) 1.0 h (p.o.) CL/F (CLTp) 0.87 ml/min/kg (i.v.) CL/F 4.3 ml/min/kg (i.v.) Protein binding (free drug %) 95.2 - 96.4% (i.v.) 91.0 - 93.7% (i.v.) MRT 1.2 h (i.v.) 3.2 h (p.o.) 5.8 h (i.v.) 8.0 h (p.o.) Vd 0.31 L/kg (i.v.) 0.30 L/kg (i.v.) Cmax 1.1 μg/ml (p.o.) 1.1 μg/ml (p.o.)