Ziresovir

Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein ( RSV F ) protein inhibitor. Ziresovir shows anti-RSV activity ( EC 50 =3 nM) and highlights pharmacokinetics in animal species In Vitro Ziresovir shows different efficacy in Wild Type (WT) and Mutant Strains RSV with EC 50 /EC 90 values (μM) of 0.003/0.005 (WT), 2.1/10.0 (D486N), and >10/>10 (D489A), respectively. RO-0529 (100 nM; 4 d) inhibits RSV F protein-induced cell–cell fusion process, and suppresses the syncytia formation induced by the RSV F protein. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Ziresovir (12.5 mg/kg, 50 mg/kg; p.o.; twice daily; 4 d) results reduction of RSV titer in mouse lung . Ziresovir (10 mg/kg; p.o.; single dose) exhibits good oral exposure and bioavailability with F(%) of 32% in male Wistar-Han rats . Ziresovir (150 mg/kg; p.o.; single dose) demonstrates a high tissue distribution to lung than plasma in CD-1 Mice . Pharmacokinetics of Ziresovir in male Wistar-Han rats Dose (mg/kg) AUC 0-24h (p.o.) (ng·h/mL) CL (mL/min/kg) T 1/2 (i.v.) (h) V ss (L/kg) F (%) 2 mg/kg (iv) or 10 mg/kg (po) 906 58 1.2 3.9 32 Pharmacokinetics of Ziresovir in CD-1 Mice Dose (mg/kg) AUC 0-24h (p.o.) (μg·h/L) tissue/lasma AUC 0-24h ratio (μg·h/L) T 1/2 (h) T max (h) C max (μg/L) plasma 8,380 1 1.02 0.25 5090 lung 72,400 8.6 3.31 1 22700 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/c mice infected by RSV Dosage: 12.5 mg/kg, 50 mg/kg Administration: Oral gavage; twice daily; 4 days Result: Resulted >1 log unit of viral titer reduction in the lung of infected mice at the dose level as low as 12.5 mg/kg. Reduced viral titer to 1.9 log units compared to vehicle at 50 mg/kg dose. IC50& Target:RSV F protein (respiratory syncytial virus fusion protein), EC50: 3 nM (RSV F)

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