治疗膀胱癌的吲哚胺2,3-双加氧酶1抑制剂—Linrodostat

Indoleamine 2,3-dioxygenase 1 inhibitor for the treatment of bladder cancer—Linrodostat

膀胱癌是泌尿系统最常见的恶性肿瘤之一,占我国泌尿生殖系统肿瘤发病率的第1位。吲哚胺2,3-双加氧酶1(IDO1)是一种细胞溶质酶,可以改善肿瘤微环境而使肿瘤细胞产生免疫抑制,Linrodostat是一种强效的IDO1口服抑制剂。在Ⅰ、Ⅱ期临床试验中,Linrodostat对人IDO1表现出很强的效力,并且在测试剂量下并未观察到临床显著的不良反应,表现出了符合期望的有效性与安全性。目前正在进行Ⅲ期临床试验。本文对其基本信息、作用机制、药物代谢动力学、临床疗效评价、安全性评价及用法用量等方面进行简要概括。

Bladder cancer is the most common malignant tumor of urinary system.The incidence rate of urogenital system tumors is the first in China.Indoleamine 2,3-dioxygenase 1(IDO1)is a cell solute enzyme,which can improve the tumor microenvironment and cause tumor cells to produce immunosuppression.Linrodostat is a potent oral inhibitor of IDO1.In its phase Ⅰ and Ⅱ clinical trials,Linrodostat showed strong efficacy on human IDO1.No clinically significant adverse reactions were observed at the test dose,showing the expected effectiveness and safety.Currently,the clinical phase Ⅲ trials are being carried out.This paper briefly summarizes its pharmacological mechanism,pharmacokinetics,clinical efficacy evaluation,adverse reactions,usage and dosage.