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tacrolimus + entecavir

Development stage: Unknown
Lead developer: Bristol Myers Squibb
Modality: Small Molecules
Administration: Oral

Overview

A combination therapy of tacrolimus and entecavir used primarily for treating hepatitis B virus-associated glomerulonephritis (HBV-GN), particularly in patients with biopsy-proven membranous nephropathy. Tacrolimus inhibits HBV entry into hepatocytes by targeting the HBV receptor, sodium taurocholate cotransporting polypeptide, while entecavir is a guanosine nucleoside analogue that inhibits HBV polymerase, blocking viral replication. The combination has shown improved efficacy in achieving proteinuria remission compared to entecavir monotherapy, with potentially synergistic antiviral effects.

Targets

NTCP (Na+-taurocholate cotransporting polypeptide)HBV Pol (Hepatitis B virus polymerase)

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