This invention provides methods, formulations and kits to reduce the toxicity of flavopiridol and analogs thereof. Disclosed are therapeutics and treatment methods employing such drugs in combination with agents that increase conjugative enzyme activity or glucuronosyltransferase activity, and agents that decrease biliary transport protein activity, such as cyclosporine A, the resultant effects of which are to decrease the significant side effects previously associated with treatment using these drugs. The invention also characterizes specific isoforms of glucuronyltransferase enzymes involved in glucuronidation of flavopiridols and their analogs.
本发明提供了降低
黄连素及其类似物毒性的方法、制剂和试剂盒。本发明公开了采用这类药物与增加共轭酶活性或
葡萄糖醛酸基转移酶活性的药剂和降低胆汁转运蛋白活性的药剂(如
环孢素 A)联合使用的治疗方法和治疗方法,其结果是减少了以前使用这类药物治疗时的显著副作用。本发明还描述了参与黄烷醇及其类似物
葡萄糖醛酸化的
葡萄糖醛酸转移酶的特异异构体。