異檸檬酸脫氫酶（IDH）1和2是細(xì)胞代謝的關(guān)鍵酶，參與多個(gè)生理過(guò)程。IDH突變（mIDH）在腫瘤發(fā)展中起關(guān)鍵或決定性作用，是膠質(zhì)瘤藥物開(kāi)發(fā)的重要靶點(diǎn)。制藥企業(yè)不斷開(kāi)發(fā)針對(duì)mIDH的抑制劑，Ivosidenib和Enasidenib已被FDA批準(zhǔn)用于治療復(fù)發(fā)難治性急性髓細(xì)胞性白血病（AML），并進(jìn)一步開(kāi)展針對(duì)膠質(zhì)瘤的試驗(yàn)；Olutasidenib，Vorasidenib，NOA-16等正在進(jìn)行Ⅰ/Ⅱ期臨床試驗(yàn)；AGI-5198，GSK-321等止步于臨床前研究。對(duì)這些小分子抑制劑和疫苗的臨床前研究成果及臨床試驗(yàn)進(jìn)展進(jìn)行總結(jié)，以期為膠質(zhì)瘤藥物開(kāi)發(fā)提供參考。

Isocitrate dehydrogenase (IDH) 1 and 2 are key enzymes in cell metabolism,which participate in multiple physiological processes. Mutant IDHs (mIDH) play a key or decisive role in tumor development and have become a kind of important targets for glioma drug. Pharmaceutical companies continue to develop inhibitors against mIDH. Ivosidenib and Enasidenib have been approved by the FDA for the treatment of relapsed or refractory acute myeloid leukemia (AML), which are continued to be studied in trials in glioma; Olutasidenib, Vorasidenib, NOA-16 and some other inhibitors are under phase Ⅰ/Ⅱ clinical trials; AGI-5198, GSK-321, etc. have stopped in preclinical research. In this review, we summarize the preclinical research results and clinical trial progress of some small molecule inhibitors and vaccines, hoping to provide a reference for the development of glioma drugs.

R979.1

天津市科技計(jì)劃項(xiàng)目（17ZXXYSY00050）