1578153-27-1

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.

RO6889678 是一种高效的 HBV 衣壳结构抑制剂，具有复杂的吸收、分布、代谢和排泄 (ADME) 特征。RO6889678 是人肝细胞中 CYP3A4 和共调节蛋白的有效诱导剂。RO6889678 通过 CYP3A4 介导的氧化和 UDP-葡萄糖醛酸基转移酶 UGT1A3 和 UGT1A1 介导的直接葡萄糖醛酸化作用进行代谢。