Clevudine

Biological Activity

Clevudine (L-FMAU) is a nucleoside analogue with unnatural L-configuration, which has strong anti-HBV activity, long half-life and low toxicity. Clevudine is a non-competitive inhibitor that binds not to viral DNA but to the polymerase.

Chemical Information

Molecular Weight	260.22
Formula	C10H13FN2O5
CAS Number	163252-36-6
Solubility (25°C)	52 mg/mL in DMSO
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 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 Compound A of 10 mg/kg.

References

[1] Tak WY, et al. Hepatol Int. A randomized, open-label study comparing low-dose clevudine plus adefovir combination therapy with clevudine monotherapy in naïve chronic hepatitis B patients.