Mendez-Lopez Max, Sutter Tabea, Driessen Christoph, Besse Lenka
Department of Medical Oncology and Hematology, Cantonal Hospital St Gallen, St Gallen, Switzerland.
Clin Adv Hematol Oncol. 2019 Nov;17(11):615-623.
Outcomes in multiple myeloma (MM) patients have improved in recent years owing to the introduction of new drugs. Among them, proteasome inhibitors and immunomodulatory imide drugs have become central in the management of newly diagnosed and relapsed MM. However, resistance to these classes of agents develops in most patients and ultimately leads to death from relapsed/refractory disease. A need exists for new classes of antimyeloma drugs, especially ones that are active in the multirefractory setting. The conventional drug development process, which involves extensive preclinical and clinical testing prior to assessment of clinical activity, has fallen short in delivering adequately safe and active novel drug candidates. HIV protease inhibitors such as nelfinavir are safe, US Food and Drug Administration-approved agents that have been shown to have potent antimyeloma activity in both preclinical models and patients with refractory disease. The repurposing of HIV protease inhibitors for treatment of MM is promising in light of their antimyeloma activity in conjunction with their global availability, established safety, and relatively low cost. This review will summarize the preclinical and clinical data available on HIV protease inhibitors for the treatment of refractory MM.
近年来,由于新药的问世,多发性骨髓瘤(MM)患者的预后有所改善。其中,蛋白酶体抑制剂和免疫调节性酰亚胺药物已成为新诊断和复发MM治疗的核心。然而,大多数患者会对这些药物产生耐药性,最终导致复发/难治性疾病死亡。因此,需要新型抗骨髓瘤药物,尤其是在多药难治情况下仍具有活性的药物。传统的药物开发过程,即在评估临床活性之前进行广泛的临床前和临床试验,在提供足够安全且有效的新型候选药物方面存在不足。诸如奈非那韦等HIV蛋白酶抑制剂是经美国食品药品监督管理局批准的安全药物,已证明在临床前模型和难治性疾病患者中均具有强大的抗骨髓瘤活性。鉴于HIV蛋白酶抑制剂具有抗骨髓瘤活性,且全球均可获得、安全性已确立且成本相对较低,将其重新用于治疗MM颇具前景。本综述将总结关于HIV蛋白酶抑制剂治疗难治性MM的临床前和临床数据。