VV116 (Synonyms: JT001)

VV116 (JT001) is an orally active nucleoside antiviral agent against SARS-CoV-2 and respiratory syncytial virus (RSV) infection. VV116 has favorable oral bioavailability, excellent in vitro antiviral activity and selectivity[1][2].

VV116 (0-1000 μM; 48 hours) can inhibit RSV replication in A549 cells[1].

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]. PO (25 mg/kg) PO (50 mg/kg) PO (100 mg/kg) T_{max (h)0.42 ± 0.140.42 ± 0.140.42 ± 0.14Cmax (ng/mL)5360 ± 56011617 ± 344324017 ± 6521AUC0-t (ng/mL.h)11461 ± 101324594 ± 105947799 ± 6545 AUC0-∞ (ng/mL.h)11534 ± 99224739 ± 102848014 ± 6696MRT0-∞ (ng/mL.h)2.25 ± 0.322.15 ± 0.262.28 ± 0.53Tmax (h)2.30 ± 1.103.27 ± 1.924.25 ± 0.53}

[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.