RO6889678

Description

RO6889678 is an inhibitor of HBV with a complex ADME profile. RO6889678 showed an intracellular enrichment of 78-fold in hepatocytes, with an apparent intrinsic clearance of 5.2 μl/min per mg protein and uptake and biliary clearances of 2.6 and 1.6 μl/min per mg protein, respectively. The induction potential of RO6889678 on cytochrome P450 (P450) enzymes and transporters at steady state was assessed and cotreatment with ritonavir revealed a complex drug-drug interaction with concurrent P450 inhibition and moderate UDP-glucuronosyltransferase induction.

in vitro

RO6889678 is a highly potent inhibitor of HBV capsid formation, with attributes that are favorable for targeting the liver while maintaining moderate peripheral exposure._x000D_ _x000D_ Reference: J Pharmacol Exp Ther. 2018 May;365(2):237-248. https://pubmed.ncbi.nlm.nih.gov/29453199/

target

RO6889678 is a highly potent HBV capsid formation inhibitor with a complex absorption, distribution, metabolism, and excretion (ADME) profile. RO6889678 is a potent inducer of CYP3A4 and coregulated proteins in human hepatocytes.