School of Pharmacy, Guilin Medical University, Guilin, Guangxi, China.
J Viral Hepat. 2021 Jun;28(6):852-858. doi: 10.1111/jvh.13490. Epub 2021 Feb 28.
With extensive research on the pathogenesis and treatment of hepatitis B virus (HBV) and hepatitis D virus (HDV) infections, the current treatment of interferon and nucleoside or nucleotide analogues provides reasonable control of viral replication in chronic hepatitis B (CHB). However, drug resistance may occur as a result of long-term treatment, and continuous covalently closed circular DNA (cccDNA) can cause disease relapse after drug withdrawal. Therefore, there is an urgent need for safe and effective antiviral drugs or methods to treat HBV and HDV infections. Myrcludex B is the first entry inhibitor that can inactivate HBV and HDV receptors, compete with HBV for the sodium-taurocholate co-transporting polypeptide, which has been identified as the bona fide receptor for HBV and HDV, block HBV infection in hepatocytes, and participate in HBV transcriptional suppression. Myrcludex B plays an important role in the inhibition of HBV replication and is a potential drug for phase III clinical trials. In this article, we review the progress on the efficacy and clinical application of myrcludex B in recent years.
经过对乙型肝炎病毒（HBV）和丁型肝炎病毒（HDV）感染的发病机制和治疗的广泛研究，目前干扰素和核苷（酸）类似物的治疗为慢性乙型肝炎（CHB）的病毒复制提供了合理的控制。然而，长期治疗可能会导致耐药性的产生，并且持续的共价闭合环状 DNA（cccDNA）可导致停药后疾病复发。因此，迫切需要安全有效的抗病毒药物或方法来治疗 HBV 和 HDV 感染。Myrcludex B 是第一个能够使 HBV 和 HDV 受体失活的进入抑制剂，与 HBV 竞争用于牛磺胆酸钠共转运多肽，该受体已被确定为 HBV 和 HDV 的真正受体，可阻止 HBV 感染肝细胞，并参与 HBV 转录抑制。Myrcludex B 在抑制 HBV 复制方面发挥着重要作用，是一种有潜力进入 III 期临床试验的药物。本文综述了近年来 Myrcludex B 在疗效和临床应用方面的进展。
