Barrientos Jacqueline C
CLL Research and Treatment Program, Division of Hematology/Oncology, Department of Medicine, Hofstra Northwell School of Medicine, Hofstra University, Lake Success, NY, USA.
Onco Targets Ther. 2016 May 18;9:2945-53. doi: 10.2147/OTT.S102573. eCollection 2016.
Idelalisib is a first-in-class, oral, selective phosphatidylinositol 3-kinase δ inhibitor that offers a chemotherapy-free option for patients with relapsed or refractory (R/R) indolent non-Hodgkin lymphoma (iNHL). Clinical trials in iNHL have evaluated idelalisib as monotherapy and as combination therapy with rituximab, bendamustine, and rituximab + bendamustine. When administered to heavily pretreated patients with R/R iNHL, idelalisib monotherapy or combination therapy showed durable antitumor activity accompanied by sustained or improved quality-of-life outcomes. Idelalisib has an acceptable safety profile; however, serious or fatal diarrhea/colitis, hepatoxicity, pneumonitis, and intestinal perforation have occurred in treated patients. Selective inhibition of phosphatidylinositol 3-kinase δ with idelalisib is a valuable addition to available treatment options for patients with iNHL, many of whom do not respond to or cannot tolerate chemoimmunotherapy. Two Phase III, randomized, placebo-controlled trials of idelalisib as combination therapy with rituximab or bendamustine + rituximab and a Phase I trial of idelalisib in combination with the Bruton's tyrosine kinase inhibitor ONO/GS-4059 in R/R B-cell malignancies are currently ongoing. A Phase III monotherapy trial in previously treated follicular lymphoma or small lymphocytic lymphoma is planned. The development of other kinase inhibitors for the treatment of iNHL raises the potential for new treatment combinations. Additional research is needed to determine optimal therapy (monotherapy vs combination regimens), treatment sequencing, and long-term management.
idelalisib是首个口服、选择性磷脂酰肌醇3激酶δ抑制剂,为复发或难治性(R/R)惰性非霍奇金淋巴瘤(iNHL)患者提供了一种无化疗的治疗选择。iNHL的临床试验评估了idelalisib单药治疗以及与利妥昔单抗、苯达莫司汀和利妥昔单抗+苯达莫司汀联合治疗的效果。在接受过大量治疗的R/R iNHL患者中,idelalisib单药治疗或联合治疗均显示出持久的抗肿瘤活性,同时生活质量持续改善或提高。idelalisib具有可接受的安全性;然而,接受治疗的患者中出现了严重或致命的腹泻/结肠炎、肝毒性、肺炎和肠穿孔。用idelalisib选择性抑制磷脂酰肌醇3激酶δ是iNHL患者现有治疗选择的一项重要补充,其中许多患者对化疗免疫疗法无反应或无法耐受。目前正在进行两项idelalisib与利妥昔单抗或苯达莫司汀+利妥昔单抗联合治疗的III期随机安慰剂对照试验,以及一项idelalisib与布鲁顿酪氨酸激酶抑制剂ONO/GS-4059联合用于R/R B细胞恶性肿瘤的I期试验。计划开展一项针对既往治疗过的滤泡性淋巴瘤或小淋巴细胞淋巴瘤的III期单药治疗试验。开发其他用于治疗iNHL的激酶抑制剂增加了新治疗组合的可能性。需要进一步研究以确定最佳治疗方案(单药治疗与联合治疗方案)、治疗顺序和长期管理。