Armoiry X, Aulagner G, Facon T
Pharmacy Department, Groupement Hospitalier Est, Hospices Civils de Lyon, Lyon, and Faculty of Pharmacy, Henri Poincaré University, Nancy, France.
J Clin Pharm Ther. 2008 Jun;33(3):219-26. doi: 10.1111/j.1365-2710.2008.00920.x.
Lenalidomide is an immunomodulatory drug derived from thalidomide. It was developed to maximize the anti-inflammatory and anti-neoplasic properties of thalidomide and to reduce its toxicity. The molecular mechanism of action of lenalidomide is unclear, but its therapeutic activity is mainly due to its well defined anti-inflammatory, immunomodulatory, anti-proliferative and anti-angiogenic properties. In relapsed or refractory multiple myeloma (MM), lenalidomide, combined with standard dose dexamethasone, is superior to dexamethasone alone in terms of time to progression, response rate and overall survival. The most commonly reported adverse events include haematological toxicity with manageable neutropenia and thrombopenia. Lenalidomide does not trigger the limiting toxicities of thalidomide: somnolence, neuropathy and constipation. Lenalidomide, in combination with dexamethasone, is indicated for the treatment of MM patients who have received at least one prior therapy and is administered orally at the dose of 25 mg q.d. for 21 days of 28-day cycles. The drug is being investigated for the treatment of newly diagnosed MM. In this review, we summarize the pharmacokinetic, pharmacodynamic and clinical trial data on lenalidomide.
来那度胺是一种从沙利度胺衍生而来的免疫调节药物。它的研发目的是最大化沙利度胺的抗炎和抗肿瘤特性，并降低其毒性。来那度胺的分子作用机制尚不清楚，但其治疗活性主要归因于其明确的抗炎、免疫调节、抗增殖和抗血管生成特性。在复发或难治性多发性骨髓瘤（MM）中，来那度胺与标准剂量地塞米松联合使用，在疾病进展时间、缓解率和总生存期方面优于单独使用地塞米松。最常报告的不良事件包括血液学毒性，中性粒细胞减少和血小板减少可控制。来那度胺不会引发沙利度胺的限制性毒性：嗜睡、神经病变和便秘。来那度胺与地塞米松联合使用，适用于至少接受过一种先前治疗的MM患者，以25mg每日一次的剂量口服，每28天为一个周期，共21天。该药物正在研究用于治疗新诊断的MM。在本综述中，我们总结了来那度胺的药代动力学、药效学和临床试验数据。
