Department of Hematology, VU University Medical Center, Amsterdam, The Netherlands.
Department of Clinical Chemistry and Hematology, University Medical Center Utrecht, Utrecht, The Netherlands.
Leukemia. 2015 Oct;29(10):2039-49. doi: 10.1038/leu.2015.123. Epub 2015 May 15.
Daratumumab is an anti-CD38 monoclonal antibody with lytic activity against multiple myeloma (MM) cells, including ADCC (antibody-dependent cellular cytotoxicity) and CDC (complement-dependent cytotoxicity). Owing to a marked heterogeneity of response to daratumumab therapy in MM, we investigated determinants of the sensitivity of MM cells toward daratumumab-mediated ADCC and CDC. In bone marrow samples from 144 MM patients, we observed no difference in daratumumab-mediated lysis between newly diagnosed or relapsed/refractory patients. However, we discovered, next to an expected effect of effector (natural killer cells/monocytes) to target (MM cells) ratio on ADCC, a significant association between CD38 expression and daratumumab-mediated ADCC (127 patients), as well as CDC (56 patients). Similarly, experiments with isogenic MM cell lines expressing different levels of CD38 revealed that the level of CD38 expression is an important determinant of daratumumab-mediated ADCC and CDC. Importantly, all-trans retinoic acid (ATRA) increased CD38 expression levels but also reduced expression of the complement-inhibitory proteins CD55 and CD59 in both cell lines and primary MM samples. This resulted in a significant enhancement of the activity of daratumumab in vitro and in a humanized MM mouse model as well. Our results provide the preclinical rationale for further evaluation of daratumumab combined with ATRA in MM patients.
达雷妥尤单抗是一种抗 CD38 单克隆抗体,对多发性骨髓瘤(MM)细胞具有溶细胞活性,包括 ADCC(抗体依赖性细胞毒性)和 CDC(补体依赖性细胞毒性)。由于达雷妥尤单抗治疗 MM 的反应存在明显的异质性,我们研究了 MM 细胞对达雷妥尤单抗介导的 ADCC 和 CDC 敏感性的决定因素。在 144 名 MM 患者的骨髓样本中,我们观察到新诊断或复发/难治性患者之间达雷妥尤单抗介导的细胞裂解无差异。然而,除了效应物(自然杀伤细胞/单核细胞)与靶标(MM 细胞)比值对 ADCC 的预期作用外,我们还发现 CD38 表达与达雷妥尤单抗介导的 ADCC(127 名患者)以及 CDC(56 名患者)之间存在显著关联。同样,用表达不同 CD38 水平的同源 MM 细胞系进行的实验表明,CD38 表达水平是达雷妥尤单抗介导的 ADCC 和 CDC 的重要决定因素。重要的是,全反式维甲酸(ATRA)增加了 CD38 表达水平,但也降低了两种细胞系和原发性 MM 样本中补体抑制蛋白 CD55 和 CD59 的表达。这导致达雷妥尤单抗在体外和人源化 MM 小鼠模型中的活性显著增强。我们的研究结果为进一步评估达雷妥尤单抗与 ATRA 在 MM 患者中的联合应用提供了临床前依据。