Overview
Dabigatran is a novel oral anticoagulant that directly inhibits thrombin (factor IIa), offering advantages over traditional vitamin K antagonists like warfarin. Developed by Boehringer Ingelheim and marketed as Pradaxa, it was first approved by the FDA in 2010 for stroke prevention in non-valvular atrial fibrillation. As a prodrug (dabigatran etexilate), it is converted to active dabigatran after oral administration. Unlike warfarin, it has predictable pharmacokinetics, doesn't require routine INR monitoring, and has fewer food and drug interactions, making it a preferred choice for many patients.
Physical and Chemical Properties
Dabigatran etexilate mesylate is a white to off-white crystalline powder with poor aqueous solubility but good permeability, classified as BCS class II. The compound is hygroscopic and requires careful moisture control during manufacturing and storage. The active form, dabigatran, has a molecular weight of 471.50 g/mol and binds reversibly to thrombin's active site. Its plasma protein binding is relatively low (35%), contributing to its consistent anticoagulant effect. The drug shows pH-dependent solubility, being more soluble in acidic environments which aids its absorption in the stomach.
Main Applications
The primary clinical use of dabigatran is for stroke prevention in patients with non-valvular atrial fibrillation, where it has demonstrated superior efficacy to warfarin with similar bleeding risks in major trials. It's also approved for treatment and secondary prevention of deep vein thrombosis (DVT) and pulmonary embolism (PE). In orthopedic settings, dabigatran serves as an alternative to low molecular weight heparins for venous thromboembolism prophylaxis after hip or knee replacement surgery. Off-label uses include bridging therapy in some perioperative settings, though this requires careful hematologist supervision due to bleeding risks.
Safety and Storage
Dabigatran carries a boxed warning for spinal/epidural hematoma risk during neuraxial anesthesia and for premature discontinuation increasing stroke risk. Major bleeding events, while comparable to warfarin, require specific reversal strategies (idarucizumab). Storage of bulk material requires controlled room temperature (15-30°C) in tightly closed containers with desiccants. Finished products are typically packaged in moisture-resistant blister packs to maintain stability. Shelf life is generally 24-36 months when stored properly, with particular attention to humidity control in tropical climates.
B2B Procurement Guide
Pharmaceutical buyers should verify API suppliers' compliance with current Good Manufacturing Practices (cGMP) and request detailed certificates of analysis including impurity profiles. For generic procurement, bioequivalence documentation is essential. Bulk purchases should consider lead times (typically 8-12 weeks for API) and may benefit from long-term contracts given price fluctuations. Quality audits are recommended for new suppliers, with particular attention to particle size distribution controls which affect bioavailability. For formulation development, excipient compatibility studies are crucial due to dabigatran's moisture sensitivity.
Related Manufacturers
- 主营：乙二醇、二甲基亚砜、丙二醇、精对苯二甲酸、己二酸、聚乙烯醇、聚乙二醇、木质素、甘油、三甘醇、己内酰胺、叔十二硫醇、白油、对苯二甲酸二甲酯、4-丁二醇
- 主营：硼酸酐、阻聚剂、己二酸、达比加群酯中间体N、氯化锂、发泡剂、乙二醇、醋酸铜、硅酸钠、正癸醇、新癸酸、环烷油、腰果酚、十二醇、酒石酸、碳酸锂、三甘醇、油菜酸、二甘醇、碳酸钾、甲酸钠、硅酸镁、棕榈油、6-氯嘌呤、微晶石蜡、磷酸一铵
- 主营：达比加群酯中间体II、阿昔洛韦侧链、化工原料
- 主营：四乙酰核糖、双乙酰阿昔洛韦、三乙酰更昔洛韦、达比加群酯中间体II、N4-乙酰胞嘧啶、胞苷、腺嘌呤、吡唑胺、对羟基苯乙酮、半胱胺盐酸盐、钼酸钠、碳酸锆
- 主营：肉桂醛、肉桂酸、汉防己甲素、达比加群酯中间体1、阻燃剂、褪黑素、甘氨酸、增塑剂
- 主营：中间体、天然产物、植物提取物、功能性原料、稀有人参皂苷、淫羊藿、橄榄苦苷、定制、研发、生产
- 主营：古龙酸、6-疏基瞟呤、紫草素、达比加群乙基酯、6-氯嘌呤、菲啰嗪一钠盐、6-二氟-4-羟基苯腈
- 主营：1-苯丙醇、1-萘甲醚、科隆试剂、达比加群、罗恩试剂、金刚烷醇、1-溴十八烷、2-恶唑烷酮、1-甲酰哌啶、2-氟苯甲醛、2-甲基吡嗪、2-氮己环酮、1-溴金刚烷、阿拉丁试剂、麦克林试剂、科密欧试剂、大小化工试剂
- 主营：1689-89-0、酒石酸、61438-64-0、甲磺酸达比加群酯872728、81810-66-4、17316-67-5、31430-15-6、68786-66-3、42461-84-7、115550-35-1、217500-96-4、101831-37-2、129496-10-2、沃尼妙林、丹诺沙星、非泼罗尼、加米霉素、能霉素钠、达氟沙星、奥苯达唑、粘杆菌素、双氢链霉素、酸泰妙菌素、盐酸四咪唑、盐酸沙拉沙星
- 主营：羟基磷灰石头、二醋酸纤维素、甲基丙烯酸镁、达比加群酯中间体、间苯二甲酸二甲酯、苯代三聚氰胺、苄索氯铵、柏木脑、乳酸铵、咪唑、明胶、靛红酸酐、DL-苹果酸、异噻唑啉酮、抗氧化剂1135、海藻酸
- 主营：阻燃剂、催化剂、洗涤剂、硫酸铵、醋酸镧、起泡剂、清洗剂、碳酸钙、抗氧剂、灭火剂、交联剂、粘合剂、封头剂、丙二醇、酸二氢铝、聚乙烯醇、对氯溴苯、生物试剂、息香乙醚、异戊二醇、香精香料、4-丁二醇、2-氯丙烯腈、2-己基癸酸、二甲胺硼烷
- 主营：砷酸锂、白云石、水合物、氮化锌、144205-68-5、二叔丁基、利多卡因、碳化钨钴、泛影葡胺、化合物库、1093222-27-5、羟基苯基、八钼酸铵、生化试剂、苯甲酸乙酯、熊去氧胆酸、胆酸二水合、乙酰丙酮锌、湿法云母粉、六氟磷酸盐、干法云母粉、苯碳酸甲酯、脱氧胆酸二水、氨基二琥珀酸、对乙酰氨基苯酚
- 主营：达比加群高纯试剂、大小化工试剂
- 主营：拆分剂、硫酸铵、硫酸锌、棕榈醇、醋酸盐、乙基醚、结晶粉、氯化钾、异辛醇、钨酸钠、气流粉、丙二醇、乙酸钾、调味剂、三胺五、中间体、一水肌酸、四硼酸钾、三乙醇胺、三磷酸钠、柠檬酸钠、油酸乙酯、樟脑磺酸、植物油酸、异己二醇
- 主营：硫酸汞、硝酸汞、雷尼镍、达比加群分析纯、二十烷、丁二酸、硫化银、正己醇、硫酸镉、铋酸钠、苯甲醇、硅酸钠、正辛酸、硫酸镁、磷钨酸、滑石粉、草酸锡、蓖麻油、椰子油、钒试剂、异辛醇