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.)

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02492828	-	-	Completed	-	-
  NCT01780987	Deep Vein Thrombosis ... more >> Pulmonary Embolism Collapse <<	Phase 3	Completed	-	Japan ... more >> Aichi Medical University Hospital Nagakute, Aichi, Japan, 480-1195 Toho University Sakura Medical Center Sakura, Chiba, Japan, 285-8741 Kokura Memorial Hospital Kitakyusyu, Fukuoka, Japan, 802-8555 Hiroshima General Hospital Hatsukaichi, Hiroshima, Japan, 738-8503 Teine Keijinkai Hospital Sapporo, Hokkaido, Japan, 006-8555 Kanazawa Medical University Hospital Kahoku-gun, Ishikawa, Japan, 920-0293 Yokohama Minami Kyousai Hospital Yokohama, Kanagawa, Japan, 236-0037 National Hospital Organization Yokohama Medical Center Yokohama, Kanagawa, Japan, 245-8575 Mie University Hospital Tsu, MIE, Japan, 514-8507 National Hospital Organization Okayama Medical Center Okayama City, Okayama, Japan, 701-1192 Kinki University Hospital Osakasayama, Osaka, Japan, 589-8511 National Cerebral and Cardiovascular Center Hospital Suita-shi, Osaka, Japan, 565-8565 St. Luke's International Hospital Chuo-ku, Tokyo, Japan, 104-8560 Nihon University Itabashi Hospital Itabashi-ku, Tokyo, Japan, 173-8610 National Hospital Organization Tokyo Medical Center Meguro-ku, Tokyo, Japan, 152-8902 Japanese Red Cross Musashino Hospital Musashino, Tokyo, Japan, 180-8610 Tokyo Medical University Hospital Shinjuku-ku, Tokyo, Japan, 160-0023 Fukushima Medical University Hospital Fukushima, Japan, 960-1295 Kumamoto University Hospital Kumamoto, Japan, 860-8556 Saiseikai Kumamoto Hospital Kumamoto, Japan, 861-4193 Collapse <<
  NCT02640222	-	-	Active, not recruiting	December 31, 2019	-

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