Liu Fei-yan, Qiu Xiao-yan, Jiao Zheng
Yao Xue Xue Bao. 2016 Nov;51(11):1666-73.
Inosine 5’-monophosphate dehydrogenase(IMPDH) is a rate-limiting enzyme in de novo biosynthesis of guanine and plays an important role in cell proliferation. In clinic, IMPDH inhibitors are mainly used in fields of anticancer, antiviral, anti-parasitic, and immunosuppressive chemotherapy. However, since there are usually great inter- and intra-individual variability between drug concentration and clinical effect of IMPDH inhibitors, the enzyme activity of IMPDH may be applied as a specific biomarker and combined with the pharmacokinetics (PK) monitoring to improve efficacy and safety of IMPDH inhibitors. This review aims to discuss the assay of IMPDH activity measurement and its clinical application in recent years and provide valuable insights and theoretical basis for the development of IMPDH inhibitors’ pharmacodynamics monitoring.
肌苷5'-单磷酸脱氢酶（IMPDH）是鸟嘌呤从头生物合成中的限速酶，在细胞增殖中起重要作用。在临床上，IMPDH抑制剂主要用于抗癌、抗病毒、抗寄生虫和免疫抑制化疗领域。然而，由于IMPDH抑制剂的药物浓度与临床效果之间通常存在很大的个体间和个体内变异性，IMPDH的酶活性可作为一种特异性生物标志物，并与药代动力学（PK）监测相结合，以提高IMPDH抑制剂的疗效和安全性。本综述旨在探讨近年来IMPDH活性测定方法及其临床应用，为IMPDH抑制剂药效学监测的发展提供有价值的见解和理论依据。
