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Besifovir

Cat. No. M20972
Besifovir Structure
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Biological Activity

Besifovir is novel and potent acyclic nucleotide phosphonate used to treat hepatitis B virus (HBV) infection.

Chemical Information
Molecular Weight 299.22
Formula C10H14N5O4P
CAS Number 441785-25-7
Solubility (25°C) DMSO 60 mg/mL
Water 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Juhee Won, et al. Biomedicines. Susceptibility of Drug Resistant Hepatitis B Virus Mutants to Besifovir

[2] Hyung Joon Yim, et al. J Gastroenterol Hepatol. Besifovir therapy improves hepatic histology and reduces covalently closed circular DNA in chronic hepatitis B patients

[3] Jeong Eun Song, et al. Expert Opin Pharmacother. Besifovir dipivoxil maleate: a novel antiviral agent with low toxicity and high genetic barriers for chronic hepatitis B

[4] Do Seon Song, et al. Clin Mol Hepatol. Continuing besifovir dipivoxil maleate versus switching from tenofovir disoproxil fumarate for treatment of chronic hepatitis B: Results of 192-week phase 3 trial

[5] Lung-Yi Mak, et al. Expert Opin Drug Metab Toxicol. Pharmacokinetic evaluation of besifovir for the treatment of HBV infection

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