Curr Cancer Drug Targets. 2012 May;12(4):372-90. doi: 10.2174/156800912800190893.
Thal has antiangiogenic and immunomodulatory activity. Clinical research provided clear evidence that Thal belongs to the most active drugs for the treatment of multiple myeloma e.g. leading to decrease of monoclonal protein of at least 50 % in 30 % of patients with relapsed or refractory multiple myeloma. Randomized trials that were designed based on a large body of evidence from phase II trials determined that Thal significantly increases total response rate, progression-free and in some studies overall survival in combination regimens (dexamethason and or chemotherapy) for relapsed as well as newly diagnosed patients and was therefore approved for first-line treatment of Multiple Myeloma. Strict guidelines apply due to the teratogenic effects of Thal and to monitor and prevent other potential adverse events as neuropathy and thrombosis has been recognized by leading organizations as part of the treatment concept for patients with relapsed or refractory disease. The success of Thal has sparked the development of Thal analogues with Lenalidomide (Len) the most advanced compound which was approved for relapsed multiple myeloma. As Len has a lower incidence of polyneuropathy, constipation and somnolence compared to Thalidomid but at least equal if not higher efficacy Len is meanwhile used more frequently in clinical routine and has advantages in combination therapies with Bortezomib. Additional randomized studies will now define the status of Thal and Len for maintenance therapy and their optimal integration in multi-agent treatment regimen.
沙利度胺具有抗血管生成和免疫调节活性。临床研究提供了明确的证据，表明沙利度胺属于治疗多发性骨髓瘤最有效的药物之一，例如在 30%的复发性或难治性多发性骨髓瘤患者中，导致单克隆蛋白减少至少 50%。基于 II 期试验的大量证据设计的随机试验表明，沙利度胺联合地塞米松和/或化疗方案显著提高了总缓解率、无进展生存期，在某些研究中还提高了总体生存率，因此被批准用于复发性和初发性多发性骨髓瘤的一线治疗。由于沙利度胺具有致畸作用，因此需要严格遵守指南，以监测和预防其他潜在的不良反应，如周围神经病和血栓形成。这些不良反应已被主要组织认可为复发或难治性疾病治疗方案的一部分。沙利度胺的成功激发了沙利度胺类似物的开发，来那度胺（Len）是最先进的化合物，已被批准用于复发性多发性骨髓瘤。与沙利度胺相比，来那度胺的周围神经病、便秘和嗜睡发生率较低，但疗效至少相当，如果不是更高，因此来那度胺在临床常规中更频繁地使用，并在与硼替佐米联合治疗中具有优势。目前正在进行额外的随机研究，以确定沙利度胺和来那度胺在维持治疗中的地位，以及它们在多药治疗方案中的最佳整合。
