RO6889678 是高效的HBV衣壳结构抑制剂，其吸收、分布、代谢和排泄特征较为复杂。它可通过 CYP3A4 介导的氧化作用进行代谢，以及通过 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。它是一种诱导剂，可作用于人肝细胞中 CYP3A4 和共调节蛋白。

RO6889678 is HBV inhibitor with a complex ADME profile.

RO6889678, a novel inhibitor of HBV with a complex absorption, distribution, metabolism, and excretion (ADME) profile.?RO6889678 showed an intracellular enrichment of 78-fold in hepatocytes, with an apparent intrinsic clearance of 5.2 l/min per mg protein and uptake and biliary clearances of 2.6 and 1.6 l/min per mg protein, respectively.?When apparent intrinsic clearance was incorporated into a PBPK model, the simulated oral human profiles were in good agreement with observed data at low doses but were underestimated at high doses due to unexpected overproportional increases in exposure with dose.?In addition, 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.

1578153-27-1

C21H20ClFN4O5S

494.92

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years