Jerome Lipper Multiple Myeloma Center, Dana-Farber Cancer Institute, Harvard Medical School Boston, MA, USA.
Ther Clin Risk Manag. 2008 Feb;4(1):129-36. doi: 10.2147/tcrm.s1445.
Lenalidomide (also known as Revlimid((R)), CC-5013) is an immunomodulatory derivative of thalidomide and has more potent anti-tumor and anti-inflammatory effects than thalidomide. The molecular mechanisms of anti-tumor activity of lenalidomide have been extensively studied in multiple myeloma (MM) both preclinical models and in clinical trials. Lenalidomide: directly triggers growth arrest and/or apoptosis of drug resistant MM cells; inhibits binding of MM cells to bone marrow (BM) extracellular matrix proteins and stromal cells; modulates cytokine secretion and inhibits angiogenesis in the BM milieu; and augments host anti-tumor immunity. Lenalidomide achieved responses in patients with relapsed refractory MM. Moreover, lenalidomide with dexamethasone (Dex) demonstrates more potent anti-MM activities than Dex both in vitro and in randomized phase III clinical trials. Specifically, the combination improved overall and extent of response, as well as prolonged time to progression and overall survival, resulting in FDA approval of lenalidomide with Dex for therapy MM relapsing after prior therapy.
来那度胺（也称为雷利度胺（Revlimid((R))），CC-5013）是沙利度胺的免疫调节衍生物，具有比沙利度胺更强的抗肿瘤和抗炎作用。来那度胺在多发性骨髓瘤（MM）的临床前模型和临床试验中，其抗肿瘤活性的分子机制已经得到了广泛研究。来那度胺：直接触发耐药 MM 细胞的生长停滞和/或凋亡；抑制 MM 细胞与骨髓（BM）细胞外基质蛋白和基质细胞的结合；调节 BM 环境中的细胞因子分泌和抑制血管生成；并增强宿主抗肿瘤免疫。来那度胺在复发性难治性 MM 患者中取得了疗效。此外，来那度胺联合地塞米松（Dex）在体外和随机 III 期临床试验中均表现出比 Dex 更强的抗 MM 活性。具体而言，该联合方案改善了总体反应程度以及进展时间和总生存期，导致 FDA 批准来那度胺联合 Dex 治疗先前治疗后复发的 MM。
