McCormack Paul L, Keating Gillian M
Wolters Kluwer Health/Adis, Auckland, New Zealand.
Drugs. 2006;66(17):2269-79; discussion 2280-2. doi: 10.2165/00003495-200666170-00010.
Tacrolimus is a calcineurin inhibitor recently approved in the US and throughout the EU for the prevention of allograft rejection in heart transplant recipients. It is commonly administered orally for long-term immunosuppression. The incidence of mild to severe acute rejection in the first 6 months following heart transplantation was significantly lower in tacrolimus recipients than in ciclosporin recipients (54% vs 66%) in a large, phase III trial conducted in Europe. A large, phase III trial conducted in the US did not show a significant difference between tacrolimus and ciclosporin in the incidence of severe rejection or haemodynamic compromise rejection requiring treatment within the first 6 months post-transplant (22% vs 32%), but did show a significant difference in the incidence at 1 year (23% vs 37%). In phase III trials, 1-year patient survival was similar between tacrolimus and ciclosporin recipients in the EU (93% vs 92%) and the US (95% vs 90%). Tacrolimus was shown to be effective in the prevention of rejection in paediatric and African American heart transplant recipients. The tolerability profile of tacrolimus in heart transplant recipients was broadly similar to that of ciclosporin, although tacrolimus was usually associated with lower incidences of post-transplant hypertension and dyslipidaemia.
他克莫司是一种钙调神经磷酸酶抑制剂，最近在美国和整个欧盟被批准用于预防心脏移植受者的同种异体移植排斥反应。它通常口服用于长期免疫抑制。在欧洲进行的一项大型III期试验中，心脏移植后前6个月，接受他克莫司治疗的患者中轻度至重度急性排斥反应的发生率显著低于接受环孢素治疗的患者（54%对66%）。在美国进行的一项大型III期试验中，他克莫司和环孢素在移植后前6个月内严重排斥反应或需要治疗的血流动力学受损排斥反应的发生率方面没有显著差异（22%对32%），但在1年时的发生率有显著差异（23%对37%）。在III期试验中，欧盟（分别为93%和92%）和美国（分别为95%和90%）接受他克莫司和环孢素治疗的患者1年生存率相似。他克莫司在预防儿科和非裔美国心脏移植受者的排斥反应方面被证明是有效的。他克莫司在心脏移植受者中的耐受性概况与环孢素大致相似，尽管他克莫司通常与移植后高血压和血脂异常的发生率较低有关。
