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回复 zhihan1248 的帖子
A recent paper studied the effect of most FDA approved drugs on the inhibition of NTCP, the now known entry receptor for HBV. Ezetimibe was found to have a 50%inhibition conc of 25micromolar, while irbesartan, a commonly used angiotensin inhibitor to reduce blood pressure, was found to inhibit at 11.9 micromolar. Both compounds have similar MW, but irbesartan is given at up to 300mg per day, while exetimibe is dosed at 10mg. Thus the combination of 30fold higher approved dose and the double micromolar inhibition potency makes, in theory, irbesartan 60 fold more potent to inhibit Hbv entry. Of course, binding of these drugs to plasma proteins could cause substsntial differences in the available concentration on the hepatocyte membrane receptor, and the pharmacokinetics could further influence the in vivo efficscy. Tests in chimeric mice are urgently needed to determine the in vivo efficacy of this common, mostly beneficial medication on HBV reinfection
最近的一项研究NTCP，现在已知的条目HBV受体抑制效果最FDA批准的药物。依折麦布，发现有50％抑制浓度的25micromolar，，而厄贝沙坦，常用的血管紧张素抑制剂降低血压，被发现能抑制11.9微摩尔。两种化合物都具有相似的分子量，但厄贝沙坦300毫克，每天，而exetimibe剂量在10毫克。批准的剂量高30fold的和双微摩尔抑制效力，使得这样的组合，在理论上，厄贝沙坦60倍，更有效抑制乙肝病毒的条目。当然，与血浆蛋白结合的这些药物可能会导致在可用的浓度对肝细胞的膜受体的substsntial差异，和药代动力学的进一步影响体内efficscy。嵌合体小鼠的测试，迫切需要确定这个共同的，大多是有益药物在体内的疗效HBV再感染.
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楼主: StephenW
发表于 2013-4-29 00:33
:饮酒可杀死肝细胞, 更新肝细胞 - 因此，降低cccDNA的数量
