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KI0866Hepsera100 mg$200
Hepsera1 g$592

Chemical Characteristic

Product NameHepsera
SynonymsAdefovir dipivoxil
CAS No.142340-99-6
Molecular Weight 501.47
FormulaC20H32N5O8P
Chemical Name9-(2[bis(Pivaloyloxymethoxy)phosphorylmethoxy]ethyl)adenine
Smilesn1cnc2c(c1N)ncn2CCOCP(=O)(OCOC(=O)C(C)(C)C)OCOC(=O)C(C)(C)C
Chemical Structure

Biological activities

Hepsera is an oral prodrug of adefovir, a phosphonate nucleotide analogue of AMP with potent activity against the polymerase activity of hepadnaviruses, retroviruses, and herpesviruses. Hepsera inhibits wild-type and mutant HBV DNA polymerases (M552I, M552V, L528M, L528M and M552V) with IC50 of 0.10, 0.13, 0.22, 0.23 and 0.079µM, respectively.[1] Hepserais is used for the treatment of HBV and human immunodeficiency virus (HIV) infections. Hepsera is a selective inhibitor of viral polymerases and reverse transcriptases (RT), and has broad-spectrum antiviral activity. [2] Hepsera has in vivo activity against both lamivudine-resistant HBV and wild-type HBV. Oral administration of hepsera leads to enhanced delivery of adefovir to the systemic circulation.[3]

References

[1] Xiong X, et al. Mutations in hepatitis B DNA polymerase associated with resistance to lamivudine do not confer resistance to adefovir in vitro. Hepatology. 1998, 28 (6): 1669-1673.
[2] Schiff ER, et al. Adefovir dipivoxil therapy for lamivudine-resistant hepatitis B in pre- and post-liver transplantation patients. Hepatology. 2003, 38(6): 1419-1427.
[3] Perrillo R, et al. Adefovir dipivoxil for the treatment of lamivudine-resistant hepatitis B mutants. Hepatology. 2000, 32(1): 129-134.

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