Debing Yannick, Vanrusselt Hannah, Degrauwe Lars, Silva de Oliveira Daniel Apolônio, Kariuki Christopher Kinyanjui, Ebwanga Ebanja Joseph, Bashir Shahbaz, Merckx Wouter, Thatikonda Santhosh Kumar, Rajwanshi Vivek, Gohil Vikrant, Hong Jin, Kum Dieudonné Buh, Acosta Sanchez Abel, Chanda Sushmita, Blatt Lawrence M, Jekle Andreas, Symons Julian A, Smith David B, Raboisson Pierre, Lin Tse-I, Beigelman Leonid, Paeshuyse Jan
Aligos Belgium BV, Leuven, Belgium.
Aligos Belgium BV, Leuven, Belgium.
Antiviral Res. 2024 Apr;224:105835. doi: 10.1016/j.antiviral.2024.105835. Epub 2024 Feb 23.
Nucleic acid polymers (NAPs) are an attractive treatment modality for chronic hepatitis B (CHB), with REP2139 and REP2165 having shown efficacy in CHB patients. A subset of patients achieve functional cure, whereas the others exhibit a moderate response or are non-responders. NAP efficacy has been difficult to recapitulate in animal models, with the duck hepatitis B virus (DHBV) model showing some promise but remaining underexplored for NAP efficacy testing. Here we report on an optimized in vivo DHBV duck model and explore several characteristics of NAP treatment. REP2139 was efficacious in reducing DHBV DNA and DHBsAg levels in approximately half of the treated ducks, whether administered intraperitoneally or subcutaneously. Intrahepatic or serum NAP concentrations did not correlate with efficacy, nor did the appearance of anti-DHBsAg antibodies. Furthermore, NAP efficacy was only observed in experimentally infected ducks, not in endogenously infected ducks (vertical transmission). REP2139 add-on to entecavir treatment induced a deeper and more sustained virological response compared to entecavir monotherapy. Destabilized REP2165 showed a different activity profile with a more homogenous antiviral response followed by a faster rebound. In conclusion, subcutaneous administration of NAPs in the DHBV duck model provides a useful tool for in vivo evaluation of NAPs. It recapitulates many aspects of this class of compound's efficacy in CHB patients, most notably the clear division between responders and non-responders.
核酸聚合物(NAPs)是治疗慢性乙型肝炎(CHB)的一种有吸引力的治疗方式,REP2139和REP2165已在CHB患者中显示出疗效。一部分患者实现了功能性治愈,而其他患者则表现出中度反应或无反应。NAP的疗效在动物模型中难以重现,鸭乙型肝炎病毒(DHBV)模型显示出一些希望,但在NAP疗效测试方面仍未得到充分探索。在此,我们报告一种优化的体内DHBV鸭模型,并探讨NAP治疗的几个特征。无论腹腔内给药还是皮下给药,REP2139在大约一半的治疗鸭中有效降低了DHBV DNA和DHBsAg水平。肝内或血清中的NAP浓度与疗效无关,抗DHBsAg抗体的出现也与疗效无关。此外,仅在实验感染的鸭中观察到NAP疗效,而在内源性感染的鸭(垂直传播)中未观察到。与恩替卡韦单药治疗相比,REP2139联合恩替卡韦治疗诱导了更深且更持久的病毒学反应。不稳定的REP2165显示出不同的活性谱,抗病毒反应更均匀,随后反弹更快。总之,在DHBV鸭模型中皮下给药NAP为体内评估NAP提供了一个有用的工具。它概括了这类化合物在CHB患者中疗效的许多方面,最显著的是反应者和无反应者之间的明显区分。