Bepirovirsen 是一种针对所有 HBV 信使 RNA 的反义寡核苷酸 | MedChemExpress (MCE)

Bepirovirsen

CAS：1403787-62-1

品牌：MedChemExpress (MCE)

存储条件：Please store the product under the recommended conditions in the Certificate of Analysis.

生物活性： Bepirovirsen 是一种针对所有 HBV 信使 RNA 的反义寡核苷酸。 Bepirovirsen 导致 HBV 衍生 RNA、HBV DNA 和病毒蛋白减少。贝匹罗韦森可用于慢性 HBV 感染的研究。贝匹罗韦森结合位点序列 (GCACTTCGCTTCACCTCTGC)[1]。

体外：Bepirovirsen（16-250 nM；16 小时）可减少 HepG2.2.15 细胞中的乙型肝炎病毒 (HBV) RNA、DNA 和病毒蛋白[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Bepirovirsen (22-50 mg/kg/周; 皮下注射，第 1 周每周两次，第 2-4 周每周一次) 可减少 HBV 转基因小鼠的肝脏 HBV RNA 和 DNA[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male HBV transgenic mice (Tg[HBV 1.3 genome]Chi32 against C57BL/6 background) aged 7-12 weeks and weight 18-25 g[1]. Dosage: 22, 50 mg/kg/week Administration: Injected subcutaneously twice weekly for week 1 and once weekly for weeks 2-4 Result: Dose-dependently reduced hepatic levels of HBV DNA and HBV RNA in HBV transgenic mice. Reduced levels of serum HBV DNA, serum HBsAg and serum HBeAg. Clinical Trial

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参考文献：

[1]. Yuen MF, et al. Safety, tolerability and antiviral activity of the antisense oligonucleotide bepirovirsen in patients with chronic hepatitis B: a phase 2 randomized controlled trial. Nat Med. 2021 Oct;27(10):1725-1734.
[2]. Han K, et, al. Preclinical and Phase 1 Assessment of Antisense Oligonucleotide Bepirovirsen in Hepatitis B Virus-Transgenic Mice and Healthy Human Volunteers: Support for Clinical Dose Selection and Evaluation of Safety, Tolerability, and Pharmacokinetics of Single and Multiple Doses. Clin Pharmacol Drug Dev. 2022 Oct;11(10):1191-1202.