Lumicitabine (ALS-008176) is an inhibitor of the respiratory syncytial virus ( RSV ) polymerase. In Vitro Lumicitabine is an orally bioavailable prodrug of the novel RSV replication inhibitor ALS-008112, a cytidine nucleoside analogue. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Lumicitabine demonstrates excellent anti-RSV efficacy and safety in a phase 2 clinical RSV challenge study. It exhibits good oral bioavailability and a high level of 2c-TP in vivo . Lumicitabine has excellent stability profiles in formulations (>24 h storage stability in 0.5% methylcellulose aqueous formulation at rt) and simulats gastric and intestinal fluids (half-life >2 h). Its solubility is adequate to support oral administration in solutions with relatively low percentage of organic solvent and in aqueous suspensions. High levels of NMP and NTP are obtained following oral administration of Lumicitabine to monkeys. In an adult human challenge study, Lumicitabine has shown efficacy against RSV infection . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal administration Rats: Lumicitabine are formulated as solutions in PEG400-based vehicles. Pharmacokinetic studies are conducted at 5 mg/kg and for oral PK studies the prodrugs are administered at 5 mg/kg parent nucleoside equivalent doses. Blood samples are typically collected at various time points up to 24 h post dose for rat . Monkeys: Lumicitabine are formulated as solutions in PEG400-based vehicles. Pharmacokinetic studies are conducted at 5 mg/kg and for oral PK studies the prodrugs are administered at 5 mg/kg parent nucleoside equivalent doses. Blood samples are typically collected at various time points up to 12 h post dose for Monkeys . aladdin has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid
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Lumicitabine
CAS number:1445385-02-3 molecular formula:C18H25ClFN3O6
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| Chinese alias | 鲁米他滨 | ||
| English alias | ALS-8176 | ALS-008176 | DTXSID801028057 | HY-12983A | BNW5PQ52G1 | DB14808 | UNII-BNW5PQ52G1 | 1445385-02-3 | A908658 | [(2R,3R,4R,5R)-5-(4-amino-2-oxo-1,2-dihydropyrimidin-1-yl)-2-(chloromethyl)-4-fluoro-3-[(2-methylpropanoyl)oxy]oxolan-2-yl]methyl 2-met | ||
| CAS number | 1445385-02-3 | molecular formula | C18H25ClFN3O6 |
| molecular weight | 433.86 g/mol | Exact mass | ≥99% |
| PSA | 121.000 Ų | logp | 1.5 |
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