Department of Internal Medicine, Division of Hematology, and Oncology and Cell Therapy, Rush University Medical Center, Chicago, IL 60612, USA.
Department of Microbial Pathogens and Immunity, Rush University Medical Center, Chicago, IL 60612, USA.
Int J Mol Sci. 2024 Aug 30;25(17):9448. doi: 10.3390/ijms25179448.
FMS-like tyrosine kinase 3 (FLT3) mutations are genetic changes found in approximately thirty percent of patients with acute myeloid leukemia (AML). FLT3 mutations in AML represent a challenging clinical scenario characterized by a high rate of relapse, even after allogeneic hematopoietic stem cell transplantation (allo-HSCT). The advent of FLT3 tyrosine kinase inhibitors (TKIs), such as midostaurin and gilteritinib, has shown promise in achieving complete remission. However, a substantial proportion of patients still experience relapse following TKI treatment, necessitating innovative therapeutic strategies. This review critically addresses the current landscape of TKI treatments for FLT3+ AML, with a particular focus on gilteritinib. Gilteritinib, a highly selective FLT3 inhibitor, has demonstrated efficacy in targeting the mutant FLT3 receptor, thereby inhibiting aberrant signaling pathways that drive leukemic proliferation. However, monotherapy with TKIs may not be sufficient to eradicate AML blasts. Specifically, we provide evidence for integrating gilteritinib with mammalian targets of rapamycin (mTOR) inhibitors and interleukin-15 (IL-15) complexes. The combination of gilteritinib, mTOR inhibitors, and IL-15 complexes presents a compelling strategy to enhance the eradication of AML blasts and enhance NK cell killing, offering a potential for improved patient outcomes.
FMS 样酪氨酸激酶 3(FLT3)突变是约 30%急性髓系白血病(AML)患者中发现的遗传改变。AML 中的 FLT3 突变代表了一种具有挑战性的临床情况,其特征是复发率高,即使在异基因造血干细胞移植(allo-HSCT)后也是如此。FLT3 酪氨酸激酶抑制剂(TKI)的出现,如米哚妥林和吉特替尼,在实现完全缓解方面显示出了希望。然而,相当一部分患者在 TKI 治疗后仍会复发,这需要创新的治疗策略。这篇综述批判性地探讨了针对 FLT3+AML 的 TKI 治疗现状,特别关注吉特替尼。吉特替尼是一种高度选择性的 FLT3 抑制剂,已证明在靶向突变的 FLT3 受体方面有效,从而抑制驱动白血病增殖的异常信号通路。然而,TKI 的单一疗法可能不足以消除 AML blasts。具体而言,我们提供了将吉特替尼与哺乳动物雷帕霉素靶蛋白(mTOR)抑制剂和白细胞介素-15(IL-15)复合物联合使用的证据。吉特替尼、mTOR 抑制剂和 IL-15 复合物的联合使用提供了一种增强 AML blasts 消除和增强自然杀伤细胞杀伤的有吸引力的策略,为改善患者预后提供了潜力。