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Entecavir

Cat. No. M20468
Entecavir Structure
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Biological Activity

Entecavir, a new deoxyguanine nucleoside analogue, is a selective inhibitor of the replication of the hepatitis B virus (HBV).

Chemical Information
Molecular Weight 277.28
Formula C12H15N5O3
CAS Number 142217-69-4
Form Solid
Solubility (25°C) DMSO 55 mg/mL
Storage -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yi Yu, et al. Int J Immunopathol Pharmacol. Entecavir-associated thrombocytopenia

[2] Sung Won Lee, et al. Clin Mol Hepatol. Entecavir versus tenofovir in patients with chronic hepatitis B: Enemies or partners in the prevention of hepatocellular carcinoma

[3] Won-Mook Choi, et al. Clin Gastroenterol Hepatol. Effects of Tenofovir vs Entecavir on Risk of Hepatocellular Carcinoma in Patients With Chronic HBV Infection: A Systematic Review and Meta-analysis

[4] Jonggi Choi, et al. JAMA Oncol. Risk of Hepatocellular Carcinoma in Patients Treated With Entecavir vs Tenofovir for Chronic Hepatitis B: A Korean Nationwide Cohort Study

[5] A Billich. Curr Opin Investig Drugs. Entecavir (Bristol-Myers Squibb)

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