| Bioactivity | VV116 (JT001) is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). VV116 retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19[1][2]. |
| Target | SARS-CoV-2, RSV |
| Invitro | 氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱[1]。氘代化合物的潜在优势：（1）延长体内半衰期。氘代化合物或能够延长化合物的药代动力学特征，即延长体内半衰期。由此可提高化合物安全性、有效性和耐受性，并增加给药的便捷性。（2）提高口服生物利用度。氘代化合物或能够减少肠壁和肝脏中不需要的代谢 (首过代谢) 程度，使得更大比例的未代谢药物到达作用的目标位置。生物利用度高决定其在低剂量下具有活性以及更好的耐受性。（3）改善代谢特征。氘代化合物或能够减少有毒或反应性代谢物的形成，改善药物代谢状况。（4）改进药品安全性。氘代化合物或能够减少或消除药物化合物的不良副作用，具有安全性。（5）保留治疗特性。氘代化合物有望保留和此前研究中氢类似物相似的生化效力和选择性。 Cell Viability Assay Cell Line: |
| In Vivo | VV116 (25, 50 and 100 mg/kg; PO; b.i.d for 4 days) exhibits a stronger activity and decreases the virus titers below the detection limit at 50 mg/kg, also reduces lung injury after RSV infection[1].VV116 (25, 50 and 100 mg/kg; PO; single dosage) exhibits favorable PK properties and good safety profile[1].Pharmacokinetic Parameters of VV116 (JT001) in Balb/c mice[1]. |
| Name | VV116 |
| Formula | C24H31DBrN5O7 |
| Molar Mass | 583.45 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Zhang R, et al. Oral remdesivir derivative VV116 is a potent inhibitor of respiratory syncytial virus with efficacy in mouse model. Signal Transduct Target Ther. 2022;7(1):123. Published 2022 Apr 16. [2]. Qian HJ, et al. Safety, tolerability, and pharmacokinetics of VV116, an oral nucleoside analog against SARS-CoV-2, in Chinese healthy subjects [published online ahead of print, 2022 Mar 16]. Acta Pharmacol Sin. 2022;1-9. |