Patel Jignesh K, Kobashigawa Jon A
Division of Cardiology, David Geffen School of Medicine at UCLA, Los Angeles, California, USA.
BioDrugs. 2007;21(3):139-43. doi: 10.2165/00063030-200721030-00001.
The development of cyclosporine was pivotal in allowing cardiac transplantation to become an accepted treatment for patients with end-stage heart disease. More recently, tacrolimus has become available as a useful alternative to cyclosporine, and has been successfully combined with either azathioprine or the newer anti-proliferative agents, mycophenolate mofetil or sirolimus. Numerous randomized clinical trials have demonstrated that tacrolimus is comparable to cyclosporine in terms of overall patient survival and at least equally effective in preventing acute rejection. In addition, tacrolimus has been particularly effective as a rescue treatment in cases where recurrent rejection has occurred with cyclosporine. The adverse effects of tacrolimus differ from those of cyclosporine, and the drug particularly shows an improved profile with respect to hypertension, dyslipidemia, and long-term renal function. These data have recently led to the regulatory approval of tacrolimus for primary immunosuppression in patients undergoing cardiac transplantation in the US.
环孢素的研发对于心脏移植成为终末期心脏病患者可接受的治疗方法起到了关键作用。最近，他克莫司已成为环孢素的一种有效替代药物，并已成功与硫唑嘌呤或新型抗增殖药物霉酚酸酯或西罗莫司联合使用。众多随机临床试验表明，就总体患者生存率而言，他克莫司与环孢素相当，且在预防急性排斥反应方面至少同样有效。此外，在环孢素出现反复排斥反应的情况下，他克莫司作为挽救治疗特别有效。他克莫司的不良反应与环孢素不同，该药物在高血压、血脂异常和长期肾功能方面表现出更好的情况。这些数据最近导致他克莫司在美国获得监管批准，用于心脏移植患者的初始免疫抑制。
