| Identification | Back Directory | [Name]
L-Valine, ester with 2',3'-dideoxy-3'-fluoroguanosine 5'-[(2S)-2-hydroxypropanoate] | [CAS]
1001670-19-4 | [Synonyms]
Lagociclovir valactate
L-Valine, ester with 2',3'-dideoxy-3'-fluoroguanosine 5'-[(2S)-2-hydroxypropanoate] | [Molecular Formula]
C18H25FN6O6 | [MOL File]
1001670-19-4.mol | [Molecular Weight]
440.43 |
| Hazard Information | Back Directory | [Uses]
Lagociclovir valactate is a prodrug of Lagociclovir (HY-14844). Lagociclovir valactate is an orally active anti-HBV agent[1]. | [in vivo]
Lagociclovir valactate (20 or 60 mg/kg; p.o.; daily for 10 weeks) shows anti-woodchuck hepatitis virus (WHV) activity in woodchucks[1]. | Animal Model: | Woodchucks with chronic WHV infection[1] | | Dosage: | 20 or 60 mg/kg | | Administration: | Oral, daily for 10 weeks | | Result: | Reduced WHV viremia effectively and maintained WHV DNA at a very low level. |
| Animal Model: | Woodchucks[1] | | Dosage: | 10 or 40 mg/kg | | Administration: | Oral (Pharmacokinetic Analysis) | | Result: | Average pharmacokinetic parameters for Lagociclovir after oral administration of Lagociclovir valactate to healthy and chronically WHV infected woodchucks[1]
| Pharmacokinetic
parameter for Lagociclovir | Healthy woodchucks (n = 4) receiving Lagociclovir valactate at 10 mg/kg | Healthy woodchucks (n = 4) receiving Lagociclovir valactate at 40 mg/kg | WHV-infected woodchucks (n = 14) receiving Lagociclovir valactate at 60 mg/kg | | Cmax (μM) | 0.54 ± 0.14 | 2.10 ± 1.5 | 3.50 ± 1.9 | | Tmax (h) | 4.10 ± 1.0 | 3.30 ± 1.5 | 2.90 ± 1.1 | | AUC0-∞ (μM ? h/liter) | 5.15 ± 1.0 | 10.50 ± 4.2 | 20.1 ± 11.3 | | t1/2 (h) | 5.44 ± 1.2 | 4.20 ± 1.6 | 4.7 ± 0.8 |
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| [References]
[1] Michalak TI, et al. Profound antiviral effect of oral administration of MIV-210 on chronic hepadnaviral infection in a woodchuck model of hepatitis B. Antimicrob Agents Chemother. 2009 Sep;53(9):3803-14. DOI:10.1128/AAC.00263-09 |
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