Cancer Genome and Epigenetics Program, NCI-Designated Cancer Center, Sanford Burnham, Prebys Medical Discovery Institute, La Jolla, California, USA.
Department of Neurology and Herbert Irving Comprehensive Cancer Center, Columbia University Medical Center, New York, New York, USA.
J Clin Invest. 2024 Mar 15;134(6):e179144. doi: 10.1172/JCI179144.
Diffuse intrinsic pontine glioma (DIPG) is a devastating brain tumor with a need for novel therapies. So far, monotherapies have failed to prolong survival for these patients, and combinatorial strategies have often shown severe, dose-limiting toxicities. In this issue of the JCI, Duchatel, Jackson, and colleagues address this challenge by introducing a drug combination that mitigates side effects and overcomes resistance. After identifying the PI3K/mTOR pathway as a therapeutic vulnerability, they treated DIPG-bearing mice with paxalisib and saw responses but also observed hyperglycemia as a severe side effect. Combining paxalisib with metformin mitigated this toxicity, but also upregulated protein kinase C (PKC) signaling. To tackle this mechanism of resistance, the authors added the PKC inhibitor enzastaurin to their drug combination and showed that this triple therapy led to improved survival. This approach paves the way for improved outcomes for patients with DIPG and other brain tumors.
弥漫性内在脑桥胶质瘤(DIPG)是一种具有破坏性的脑瘤,需要新的治疗方法。到目前为止,单一疗法未能延长这些患者的生存期,而联合治疗策略往往表现出严重的、剂量限制的毒性。在本期 JCI 中,Duchatel、Jackson 和同事们通过引入一种减轻副作用和克服耐药性的药物组合来应对这一挑战。在确定 PI3K/mTOR 通路是一种治疗弱点后,他们用帕拉西林治疗携带 DIPG 的小鼠,观察到了反应,但也观察到了严重的副作用——高血糖。将帕拉西林与二甲双胍联合使用可以减轻这种毒性,但也会上调蛋白激酶 C(PKC)信号。为了解决这种耐药机制,作者在药物组合中加入了 PKC 抑制剂恩杂鲁胺,结果表明这种三联疗法可提高生存率。这种方法为 DIPG 和其他脑肿瘤患者的改善预后铺平了道路。