SHEN26

ATV006 is a potent, orally active antiviral agent and ester prodrugs of GS-441524. ATV006 inhibits the replication of SARS-CoV-2 and its variants. ATV006 can be used for SARS-CoV-2 research[1].

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> SARS-CoV

ATV006 (0.001-100 μM; 48 h; Vero E6 cells) inhibits the replication of authentic SARS-CoV-2 and its variants of concern. ATV006 has an overall >4-fold and >12-fold potency improvement in inhibiting the replication of Delta and Omicron variants, with EC50 values of 0.349 μM and 0.106 μM, respectively[1].

ATV006 (5-25 mg/kg; p.o. and i.v.; Sprague Dawley rats) has favorable pharmacokinetic profiles in rats with high oral bioavailability (F %) of 81.5% and maximum blood concentration (Cmax) of 8.2 μM[1]. ATV006 (250-500 mg/kg; p.o.; daily, for 4 days; hACE2 knock-in and Ad5-hACE2 mice) has antiviral activity and inhibits SARS-CoV-2 replication in mouse models[1]. ATV006 (100-250 mg/kg; p.o.; daily, for 10 days) reduces lung damage and protects K18-hACE2 mice[1]. ATV006 (10-150 mg/kg; p.o.; daily, for 3 days) reduces virus titers and lung damage caused by Delta variant infection in K18-hACE2 mice[1]. Animal Model: Sprague Dawley rats[1] Dosage: 5 and 25 mg/kg Administration: Oral administration (25 mg/kg) and intravenous injection (5 mg/kg) Result: 1.19 parameters i.v. (5 mg/kg) p.o. (25 mg/kg) AUClast (μM·h) 5.6 22.8 T1/2 (h) 1.5 1.2 Tmax (h) 0.5 Cmax (μM) 8.7 8.2 F % 81.5 Animal Model: hACE2 knock-in and Ad5-hACE2 mice[1] Dosage: 250 and 500 mg/kg Administration: Oral administration; daily, for 4 days Result: Inhibited gRNA and sgRNA, which is Biomarkers of coronavirus replication. Reduced the viral load and pathological damage of the lung. Animal Model: K18-hACE2 mice[1] Dosage: 100 and 250 mg/kg Administration: Oral administration; daily, for 10 days Result: Reduced viral RNA and increased the survival rate of mice. Reduced evidence of lung pathology and the production of inflammatory cytokines and chemokines in the lung tissues. Animal Model: K18-hACE2 mice[1] Dosage: 10, 30, 80 and 150 mg/kg Administration: Oral administration; daily, for 3 days Result: Reduced viral load in a dose-dependent manner and alleviated the symptoms in the lung.

[1]. Cao L, et, al. The adenosine analog prodrug ATV006 is orally bioavailable and has preclinical efficacy against parental SARS-CoV-2 and variants. Sci Transl Med. 2022 May 17:eabm7621.