Patent analysis for coagulation factor Xa inhibitors / 中国药科大学学报

@#Anticoagulant drugs are widely used in the prevention and treatment of thromboembolic diseases. In recent years, coagulation factor Xa inhibitors have become a hot spot for the development of new anticoagulant drugs. However, the anticoagulant drugs currently used still have side-effects such as increased bleeding risk. This paper analyzes the patent applications of coagulation factor Xa inhibitors, and summarizes the development route of patent application of Bristol-Myers Squibb Company and Guangdong Dongyang Pharmaceutical Co. , Ltd. as representatives of key enterprises, in order to provide some useful references and recommendations for the development, patent protection countermeasure and intellectual property strategy of coagulation factor Xa for domestic pharmaceutical enterprises.

Series with complete resolution of left atrial appendage thrombi with apixaban in elderly patients

No abstract available.

Analysis of Novel Anticoagulants for Atrial Fibrillation – Pharmacokinetics and Pharmacological Considerations.

Atrial Fibrillation (AF) is the most common arrhythmia. AF is a major risk factor for stoke. Warfarin has been available for more than 60 years and until recently it was the only oral anticoagulant used for the prevention of stroke. Despite the extensive studies and proven efficacy, its utility is limited by multiple factors. Warfarin interacts with a multitude of drugs and foods, has a delayed onset of action, has a narrow therapeutic range, requires routine lab monitoring and exhibits variable responses in patients. The novel agents dabigatran, rivaroxaban and apixaban have the potential to have some of the limitations of warfarin. This article will discuss the pharmacokinetic and pharmacological considerations and different characteristics of the novel anticoagulants when used for the prevention of AF.

Advances in the research of factor Xa inhibitors / 中国药科大学学报

Factor Xa is a trypsin-like serine protease playing a pivotal role in the blood coagulation cascade.Factor Xa and its inhibitors are of great importance in the development of orally active antithrombotic agents and have aroused considerable attention from the pharmaceutical industry sector over the years.In this review,the structural characteristics of the factor Xa binding site are discussed and the X-ray information available together with the published structure-activity relationship data is used to identify the molecular interactions that are most important for tight enzyme-inhibitor binding,which would be useful in the structure-based drug design of novel factor Xa inhibitors.

Novel anticoagulant,direct factor Xa inhibitor:Rivaroxaban / 中国临床药理学与治疗学

Anticoagulants are recommended for the prevention and treatment of a wide variety of thromboembolic events.Although existing anticoagulants are effective,their usage is limited by parenteral administration or the requirement for frequent monitoring and subsequent dose adjustment.Therefore,there is an urgent need for novel,oral agents with a predictable anticoagulant action.Because of its key position in the coagulation cascade and its limited roles outside of coagulation,Factor Xa has presented as an attractive target for novel anticoagulants.As a result,the past decade has witnessed an explosion of research into small-molecule,oral,direct Factor Xa inhibitors,and some are now in clinical development.Rivaroxaban is currently furthest ahead in its developmental program,having entered phase III in 3 indications.It is hoped that,before long,these anticoagulants will allow us to enter an era of convenient,oral anticoagulation,without the need for regular monitoring or dose adjustment.