Apixaban, also known as BMS-56224701, is an anticoagulant for the treatment of venous thromboembolic events. Apixaban is a direct factor Xa inhibitor. Apixaban was approved in 2012. Apixaban is indicated for the following: (1) To lower the risk of stroke and embolism in patients with nonvalvular atrial fibrillation. (2) Deep vein thrombosis (DVT) prophylaxis. DVT's may lead to pulmonary embolism (PE) in knee or hip replacement surgery patients. (3) Treatment of both DVT and PE. (4) To reduce the risk of recurring DVT and PE after initial therapy.
Sun, Xiaoqing; Hong, Zexin; Liu, Moyi; Guo, Su; Yang, Di; Wang, Yong; Lan, Tian; Gao, Linyu; Qi, Hongxia; Gong, Ping; Liu, Yajing. Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity. Bioorganic & Medicinal Chemistry. Volume 25. Issue 10. Pages 2800-2810. Journal; Online Computer File. (2017).
: Pinto, Donald J. P.; Orwat, Michael J.; Koch, Stephanie; Rossi, Karen A.; Alexander, Richard S.; Smallwood, Angela; Wong, Pancras C.; Rendina, Alan R.; Luettgen, Joseph M.; Knabb, Robert M.; He, Kan; Xin, Baomin; Wexler, Ruth R.; Lam, Patrick Y. S. Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl]phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa. Journal of Medicinal Chemistry. Volume 50. Issue 22. Pages 5339-5356. Journal. (2007).
Nevuluri, Narasimha Rao; Rapolu, Rajesh Kumar; Iqbal, Javed; Kandagatla, Bhaskar; Sen, Saikat; Dahanukar, Vilas H.; Oruganti, Srinivas. A morpholine-free process amenable convergent synthesis of apixaban: a potent factor Xa inhibitor. Monatshefte fuer Chemie. Volume 148. Issue 8. Pages 1477-1482. Journal; Online Computer File. (2017).
Tao, Hai-yan; Mi, Bin; Guo, Guo-xian; Gong, Ping. Synthesis of apixaban. Zhongguo Yaowu Huaxue Zazhi. Volume 23. Issue 5. Pages 385-389. Journal. (2013)
Gu, Xifeng; Xu, Jun; Lu, Ming. Synthesis method of apixaban from its precursor. Assignee ChemFuture PharmaTech (Jiangsu) Ltd., Peop. Rep. China. CN 103896940. (2014).
