Indoleamine 2,3-dioxygenase 1（IDO1）与广泛的恶性肿瘤免疫逃逸高度相关，由于它在通过色氨酸（Trp）耗竭和琥珀酸酰化酶（Kyn）积累引起的免疫抑制中扮演着重要的角色。IDO1抑制剂与其他治疗方法的组合是免疫治疗的一种有前途的策略，尽管仍面临着相当大的挑战。本综述聚焦于通过Espacenet和Google学者检索的专利出版物，并涉及2018-2022年期间具有潜在抗癌利用价值的IDO1抑制剂。尽管一流的IDO1抑制剂依柏卡度胺结合Pembrolizumab的临床试验失败，但已进行了大量研究，以追求更有效的基于IDO1的免疫调节治疗方案。结晶学研究的推动下，已生产了大量具有新结构和设计理念的IDO1抑制剂，显示出巨大的研究潜力。关于IDO1抑制剂与其他靶向药物的联合、更精确地选择患者、鉴定更可靠的生物标志物用于评价IDO1治疗以及探索可能的毒性影响，是推动IDO1基础免疫治疗从实验室走向床边的关键因素。

Indoleamine 2,3-dioxygenase 1 (IDO1) is highly related to the immune evasion of a wide range of malignancies due to its role in the immune suppression caused by the depletion of tryptophan (Trp) and the accumulation of kynurenine (Kyn). The combination of IDO1 inhibitors with other treatments represents a promising strategy in immunotherapy, although considerable challenges lie ahead.This review focuses on patent publications searched from Espacenet and Google Scholar, and related to IDO1 inhibitors with potential anti-cancer utilization during the period 2018-2022.Despite the clinical trial failure of the first-in-class IDO1 inhibitor epacadostat in combination with pembrolizumab, numerous studies have been carried on to pursue more efficient IDO1-based immune-modulating therapeutic solutions. A large number of IDO1 inhibitors with new structures and design concepts have been produced with the impetus of crystallographic studies, and have shown great research potential. The elaboration on the combination of IDO1 inhibitors with other targeting agents, the more precise selection of patients, the identification of more reliable biomarkers for evaluating the IDO1 treatment, and the investigation of possible toxicity, are critical factors to promote IDO1-based immunotherapies from bench to bedside.