| Description | Tenofovir amibufenamide (HS-10234) is a Tenofovir prodrug, an antiviral compound with oral activity. Tenofovir amibufenamide inhibits hepatitis B virus (HBV) and can be used in chronic hepatitis B (CHB) studies. |
| In vitro | 在 HBV 阳性的 HepG2.2.15 细胞中，TMF 和 Tenofovir amibufenamide 对 HBV DNA 复制的抑制作用明显强于 TDF。处理 9 天后，TMF 的抗 HBV 活性略强于 Tenofovir amibufenamide（EC50 为 7.29 ± 0.71 nM 对 12.17 ± 0.56 nM）。三种 TFV 酯原药的回调效应依次为 TMF > Tenofovir amibufenamide > TDF。TMF 的这些优势被认为是由于其在临床前动物（SD 大鼠、C57BL/6 小鼠和小猎犬）中更高的生物利用度和更好的靶向负荷，尤其是药理活性代谢物 TFV-DP 的肝脏水平更高，而这与抗 HBV 的疗效密切相关。[1] |
| In vivo | 对 Tenofovir amibufenamide 组（25 毫克，96 周）和 TDF 组的安全性进行了全面评估，重点关注骨骼、肾脏和代谢参数。肾脏安全性评估采用非指数估计肾小球滤过率，Tenofovir amibufenamide 组的肾小球滤过率下降幅度小于 TDF 组（P=0.01）。在骨矿物质密度方面，接受 Tenofovir amibufenamide 治疗的患者在第 96 周时脊柱、髋部和股骨颈密度的下降水平明显低于接受 TDF 治疗的患者。此外，第48周后，各组患者的血脂指标均保持稳定，而体重变化仍呈相反趋势。与TDF相比，Tenofovir amibufenamide在第96周时保持了相似的疗效，并且在骨骼和肾脏安全性方面继续保持优势[2]。 |
| Target activity | Anti-HBV:7.29 ± 0.71 nM(EC50) |
| Synonyms | HS-10234 |
| molecular weight | 490.49 |
| Molecular formula | C22H31N6O5P |
| CAS | 1571076-26-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 180.0 mg/mL (367.0 mM), Sonication is recommended. |
| References | 1. Hong X, et al. Improved pharmacokinetics of tenofovir ester prodrugs strengthened the inhibition of HBV replication and the rebalance of hepatocellular metabolism in preclinical models. Front Pharmacol. 2022;13:932-934. 2. Liu Z, et al. Randomised clinical trial: 48 weeks of treatment with tenofovir amibufenamide versus tenofovir disoproxil fumarate for patients with chronic hepatitis B. Aliment Pharmacol Ther. 2021;54(9):1134-1149. 3. Zhihong Liu, et al. Randomised clinical trial: 48 weeks of treatment with tenofovir amibufenamide versus tenofovir disoproxil fumarate for patients with chronic hepatitis B. Aliment Pharmacol Ther. 2021 Nov;54(9):1134-1149. 4. Hong Zhang, et al. Randomised clinical trial: safety, efficacy and pharmacokinetics of HS-10234 versus tenofovir for the treatment of chronic hepatitis B infection. Aliment Pharmacol Ther. 2021 Jan;53(2):243-252. |