Department of Leukemia, The University of Texas MD Anderson Cancer Center, Houston, TX, USA.
Blood Cancer J. 2023 Sep 11;13(1):142. doi: 10.1038/s41408-023-00911-w.
FLT3 is the most frequently mutated gene in acute myeloid leukemia (AML), with FLT3 internal tandem duplication (ITD) mutations being associated with a more aggressive clinical course. While two large, randomized clinical trials have shown a survival benefit with the frontline use of an oral FLT3 inhibitor (midostaurin or quizartinib) in patients with FLT3-mutated AML, the role of FLT3 inhibitors in older adults with newly diagnosed FLT3-mutated AML remains unclear. A definitive improvement in survival has not been observed in intensively treated patients over 60 years of age receiving frontline FLT3 inhibitors. Furthermore, many patients with FLT3-mutated AML are unsuitable for intensive chemotherapy due to age and/or comorbidities, and this population represents a particular unmet need. For these older patients who are unfit for intensive approaches, azacitidine + venetoclax is a new standard of care and is used by many clinicians irrespective of FLT3 mutation status. However, FLT3-ITD mutations confer resistance to venetoclax and are a well-established mechanism of relapse to lower-intensity venetoclax-based regimens, leading to short durations of remission and poor survival. Preclinical and clinical data suggest synergy between FLT3 inhibitors and venetoclax, providing rationale for their combination. Novel strategies to safely incorporate FLT3 inhibitors into the standard hypomethylating agent + venetoclax backbone are now being explored in this older, less fit population with newly diagnosed FLT3-mutated AML, with encouraging early results. Herein, we discuss the frontline use of FLT3 inhibitors in older adults with FLT3-mutated AML, including the potential role of FLT3 inhibitors in combination with intensive chemotherapy and as part of novel, lower-intensity doublet and triplet regimens in this older population.
FLT3 是急性髓系白血病(AML)中最常发生突变的基因,FLT3 内部串联重复(ITD)突变与更具侵袭性的临床病程相关。虽然两项大型随机临床试验表明,在伴有 FLT3 突变的 AML 患者中,一线使用口服 FLT3 抑制剂(米哚妥林或quizartinib)具有生存获益,但 FLT3 抑制剂在新诊断为伴有 FLT3 突变的 AML 的老年患者中的作用仍不清楚。在接受一线 FLT3 抑制剂治疗的 60 岁以上强化治疗患者中,并未观察到生存的显著改善。此外,由于年龄和/或合并症,许多伴有 FLT3 突变的 AML 患者不适合强化化疗,而这部分患者存在特定的未满足的需求。对于不适合强化治疗的这些老年患者,阿扎胞苷+维奈托克是一种新的标准治疗方法,许多临床医生无论 FLT3 突变状态如何,都在使用它。然而,FLT3-ITD 突变赋予了对维奈托克的耐药性,并且是复发至强度较低的维奈托克为基础的方案的一种既定机制,导致缓解持续时间短,生存状况较差。临床前和临床数据表明 FLT3 抑制剂与维奈托克具有协同作用,为它们的联合应用提供了依据。目前,在新诊断的伴有 FLT3 突变的 AML 的老年、身体状况较差的患者中,正在探索将 FLT3 抑制剂安全地纳入标准低甲基化剂+维奈托克方案的新策略,并取得了令人鼓舞的早期结果。在此,我们讨论了在伴有 FLT3 突变的 AML 的老年患者中一线使用 FLT3 抑制剂的情况,包括在这一老年人群中,FLT3 抑制剂与强化化疗联合应用以及作为新型低强度二联和三联方案的一部分的潜在作用。