Small interfering RNA (siRNA) is mainly involved in RNA interference for stopping gene translation by targeting and degrading HBV-transcribed mRNA. Targeting and stability in siRNA can be enhanced via chemical modification, combination use and improved delivery system. Clinical studies have identified JNJ-3989 (ARO-HBV) and ARB-1740 as well-tolerated siRNA drugs, which significantly reduce HBsAg levels. This article expounds the main mechanisms of siRNA in inhibiting HBsAg expression, improving target and stability as well as relevant preclinical and clinical studies.
小干扰RNA（siRNA）主要参与RNA干扰，通过靶向HBV转录的mRNA并对其进行降解来阻止基因翻译。通过对siRNA进行化学修饰、结合使用和改进其传递体系，可增强siRNA的靶向性和稳定性。JNJ-3989（ARO-HBV）、ARB-1740作为耐受性良好、明显降低HBsAg水平的siRNA药物已进入临床研究。现主要阐述siRNA抑制HBsAg表达的机制、siRNA靶向性和稳定性的提高以及相关的临床前和临床研究。.
Keywords: Hepatitis B surface antigen; Hepatitis B, chronic; RNA, small Interfering.