Adefovir Dipivoxil

Biological Activity

Adefovir Dipivoxil reduces Liver HBV DNA to <0.1 pg of viral DNA per mg of total DNA (pg/mg) in transgenic mice expressing hepatitis B virus. Adefovir Dipivoxil treatment also reduces serum HBV DNA to 3.5 log10 genomic equivalents (ge)/mL in transgenic mice expressing hepatitis B virus compared to 5.3 log10 ge/mL for the placebo control group. Adefovir Dipivoxil antiviral activity reaches near maximum viral reduction by day 10 in the liver and reaches an endpoint of liver virus inhibition at 1.0 mg/kg/day. Adefovir Dipivoxil works by blocking reverse transcriptase, an enzyme that is crucial for the hepatitis B virus (HBV) to reproduce in the body. Adefovir Dipivoxil is used for treatment of hepatitis B and herpes simplex virus infection.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information

References

Long-term therapy with adefovir dipivoxil in hepatitis B e antigen-negative patients developing resistance to lamivudine.
Manolakopoulos S,et.al. Aliment Pharmacol Ther. 2008 Feb 1;266-73. PMID: 17988233.

Adefovir dipivoxil for the treatment of hepatitis B e antigen-positive chronic hepatitis B.
Marcellin P,et.al. N Engl J Med. 2003 Feb 27;808-16. PMID: 12606735.

Characterizing antiviral activity of adefovir dipivoxil in transgenic mice expressing hepatitis B virus.
Julander JG,et.al. Antiviral Res. 2002 Jul;27-40. PMID: 12076749.