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本帖最后由 StephenW 于 2013-10-28 16:46 编辑
回复 咬牙硬挺 的帖子
这个药物是否真是靶向药物?是的.
还是挂着羊头卖狗肉的核苷?这种药物属于一家美国公司Metabasis Therapeutics 和 Valeant Pharmaceuticals.他们进行所有的第1和第2阶段临床试验. 效果能否高于恩替卡韦和替诺福韦?我不知道。它应该是优于阿德福韦酯(Hepsera), 降低Hepsera的肾脏毒性.现有Hepsera高剂量导致毒性.
看你转发的论文里有在肝脏转化为阿德福韦,是怎么一回事?
Pradefovir and Hepsera are both prodrugs of 9 -[2 (Phosphonomethoxy) ethyl] adenine (PMEA), or adefovir. When the prodrug is converted to adefovir in patients with hepatitis B, it acts in the liver and leads to decreased viral levels. Pradefovir is a HepDirect prodrug that after oral administration is absorbed rapidly after which it is taken up by the liver and converted to the active form, adefovir. Hepsera, on the other hand, is converted to adefovir throughout the bloodstream. As a result of this difference in distribution, higher dosing of pradefovir is possible due to the reduced systemic and renal adefovir levels, providing potentially improved efficacy relative to Hepsera in the treatment of hepatitis B, based on results of a Phase 2 clinical trial, which is further discussed in the clinical trials section below.
pradefovir和Hepsera(阿德福韦酯)是阿德福韦的前药9 - [2 - (磷酰甲氧基)乙基]腺嘌呤(PMEA). 当该前药被转换为阿德福韦,它的作用在肝脏,导致病毒水平降低。 pradefovir是一个HepDirect的前体药物,口服后迅速被吸收后,它是在肝脏,转换为活性形式,阿德福韦。阿德福韦酯,在另一方面,被转换为阿德福韦在整个血液。这两种不同的分布,更高pradefovir药量是可能的,因为减少全身和肾的阿德福韦水平,提供潜在改进阿德福韦酯的相对B型肝炎治疗中的效力,基于2阶段临床试验,结果进一步临床试验中的一节讨论.
国内巧立名目瞒天过海的科研项目太多 - 这药是被国内购买的.
吉利德(Gilead)现在临床测试泰诺福韦前药 - TAF.
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