Curran Monique P, McKeage Kate
Wolters Kluwer Health, Adis, Auckland, New Zealand.
Drugs. 2009;69(7):859-88. doi: 10.2165/00003495-200969070-00006.
Bortezomib (VELCADE) is a proteasome inhibitor that not only targets the myeloma cell, but also acts in the bone marrow micro-environment, inhibiting the binding of myeloma cells to bone marrow stromal cells, as well as demonstrating anabolic effects on bone. Intravenous bortezomib, with or without dexamethasone, is effective and well tolerated in patients with relapsed/refractory multiple myeloma, as demonstrated in the phase II CREST and SUMMIT trials, and the phase III APEX trial, and is a recommended treatment for this patient group. Based on the results of another phase III trial, the combination of bortezomib plus pegylated liposomal doxorubicin is also a recommended treatment for patients with relapsed/refractory multiple myeloma. Other bortezomib-combination regimens have demonstrated promising response data in phase II trials in patients with relapsed/refractory disease, although response and survival data for these combinations need to be confirmed in larger phase III trials. Bortezomib was effective and well tolerated when used as part of a first-line regimen in previously untreated patients with multiple myeloma. In the phase III VISTA trial in elderly patients with previously untreated multiple myeloma not eligible for transplantation, bortezomib in combination with melphalan and prednisone was effective and well tolerated and is a recommended treatment regimen for this group of patients. Preliminary data from phase II/III trials in patients with previously untreated multiple myeloma indicate a promising role for the use of bortezomib combined with various other chemotherapeutic agents as induction therapy prior to transplantation.
硼替佐米（万珂）是一种蛋白酶体抑制剂，不仅作用于骨髓瘤细胞，还作用于骨髓微环境，抑制骨髓瘤细胞与骨髓基质细胞的结合，并对骨骼有合成代谢作用。在II期CREST和SUMMIT试验以及III期APEX试验中已证实，静脉注射硼替佐米，无论是否联合地塞米松，对于复发/难治性多发性骨髓瘤患者均有效且耐受性良好，是该患者群体的推荐治疗方法。根据另一项III期试验的结果，硼替佐米联合聚乙二醇化脂质体阿霉素也是复发/难治性多发性骨髓瘤患者的推荐治疗方法。其他硼替佐米联合方案在复发/难治性疾病患者的II期试验中已显示出有前景的反应数据，尽管这些联合方案的反应和生存数据需要在更大规模的III期试验中得到证实。硼替佐米作为初治多发性骨髓瘤患者一线治疗方案的一部分使用时，效果良好且耐受性佳。在针对不符合移植条件的初治老年多发性骨髓瘤患者的III期VISTA试验中，硼替佐米联合美法仑和泼尼松效果良好且耐受性佳，是该组患者的推荐治疗方案。在初治多发性骨髓瘤患者的II期/III期试验中的初步数据表明，硼替佐米联合各种其他化疗药物作为移植前诱导治疗具有广阔前景。
