Winkler M, Christians U
Klinik für Abdominal- und Transplantationschirurgie, Medizinische Hochschule, Hannover, Germany.
Drug Saf. 1995 May;12(5):348-57. doi: 10.2165/00002018-199512050-00006.
Tacrolimus is a new macrolide immunosuppressant that was isolated from Streptomyces tsukubaensis in 1984. In vitro, on a molecular basis, tacrolimus is 50 to 100 times more potent that cyclosporin. Since 1989, numerous clinical trials have been completed comparing the usefulness of tacrolimus with that of cyclosporin for baseline immunosuppression in solid organ transplantation. Almost all of these studies demonstrated the superior immunosuppressive potency of tacrolimus. However, in most of these trials, tacrolimus-based immunosuppression was associated with a higher overall frequency of drug-related adverse effects compared with cyclosporin. Based on the efficacy and tolerability profile of tacrolimus that has been demonstrated in the various clinical trials so far, tacrolimus is a relevant alternative to cyclosporin for baseline immunosuppression in liver transplantation. In addition to primary immunosuppression, conversion from cyclosporin to tacrolimus should be performed during episodes of severe graft rejection (e.g. resistant to steroid bolus therapy). The future role of tacrolimus for baseline immunosuppression in kidney and thoracic organ transplantation has yet to be defined by ongoing studies.
他克莫司是一种新型大环内酯类免疫抑制剂，于1984年从筑波链霉菌中分离出来。在体外，从分子层面来看，他克莫司的效力比环孢素强50至100倍。自1989年以来，已经完成了许多临床试验，比较他克莫司和环孢素在实体器官移植中进行基础免疫抑制的有效性。几乎所有这些研究都证明了他克莫司具有更强的免疫抑制效力。然而，在大多数这些试验中，与环孢素相比，基于他克莫司的免疫抑制与药物相关不良反应的总体发生率更高有关。根据迄今为止在各种临床试验中所证明的他克莫司的疗效和耐受性特征，他克莫司是肝移植中用于基础免疫抑制的环孢素的一种相关替代药物。除了初始免疫抑制外，在严重移植排斥反应（如对大剂量类固醇治疗耐药）发作期间，应从环孢素转换为他克莫司。他克莫司在肾移植和胸器官移植中用于基础免疫抑制的未来作用仍有待正在进行的研究所明确。
