Drug intelligence / Profile preview

adefovir + entecavir

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

Adefovir + entecavir is a combination of two antiviral small molecules used primarily for the treatment of chronic hepatitis B virus (HBV) infection. Both drugs are nucleoside/nucleotide analog reverse transcriptase inhibitors that target HBV polymerase but act via different mechanisms. Adefovir dipivoxil is a prodrug converted to adefovir, an acyclic nucleotide analog of adenosine monophosphate; it inhibits HBV DNA polymerase by competing with deoxyadenosine triphosphate and causing DNA chain termination after incorporation into viral DNA[5]. Entecavir is a guanosine nucleoside analogue that selectively inhibits all three steps in the replication process of HBV by competing with deoxyguanosine triphosphate and inhibiting base priming, reverse transcription from pregenomic RNA, and synthesis of the positive strand of HBV DNA[6]. The combination therapy has been shown to improve clinical outcomes in patients with hepatitis B cirrhosis or those resistant to other antivirals such as lamivudine or entecavir alone[1][2]. This regimen can reduce serum inflammatory markers and improve liver function in affected patients[1].

Brand names
HepseraBaraclude
Other names
adefovir dipivoxil
02

Targets

HBV Pol (Hepatitis B virus polymerase)

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