新药跟踪II(10/14/02): Coviracil(FTC, emtricitabine~恩曲他滨/鸟环核苷)

liver411

Triangle制药公司的核苷类似物Coviracil(FTC, emtricitabine~恩曲他滨/鸟环核苷)两年来临床试验结果显示能降低慢性感染病人的乙肝病毒水平并抗药性小...

Coviracil Is an Effective HBV Therapy with Low Resistance Rates Following 2 Years of Therapy

By Brian Boyle, MD

Hepatitis B virus (HBV) infection is both a common and potentially fatal viral infection. Effective treatment options for this condition have been limited to this point; however, the number of effective agents for the treatment of this condition has steadily grown over the past few years.

Some exciting drugs in the pipeline are moving through clinical trials and one of these drugs, Coviracil (emtricitabine, FTC) is a nucleoside analogue (NA) that has potent activity against HBV and HIV. While Coviracil has a resistance profile similar to Epivir (lamivudine, 3TC), preliminary data from a study evaluating Coviracil in patients with chronic HBV indicated that it is very effective treatment of HBV and that there was a low rate of resistance development. Further follow-up of this study was presented at the 42nd ICAAC.

The Study, FTCB-102, is a randomized, double-blind, dose ranging trial comparing 3 once-daily doses (25, 100, 200mg) of FTC for 1 year in 98 patients. After 1 year of therapy, all patients were switched to a 200mg once-daily dose of Coviracil.

Using an Intent-to-Treat analysis, after 2 years of treatment with Coviracil, 42% of the patients had undetectable HBV levels, 76% had normalized their ALT levels, 51% had seroconverted to HBeAg negative and 29% to HBeAb positive. The patients who received 200mg of Coviracil for 2 years had a lower rate of Coviracil resistance (19%) than patients who received 25 or 100mg for the first year followed by 200mg (20% and 37% respectively). The Coviracil therapy was extremely well tolerated.

The authors conclude, "[Coviracil] produced a sustained virologic and serologic response (29% HBeAg conversion). At 2 years the incidence of mutations was low (19%) among the patients receiving 200mg for the duration of the study, suggesting that potent viral suppression limits the emergence of resistant variants. These data are consistent with an HIV clinical trial, regarding the rate of developing the M184V mutation."

10/14/02

Reference
H Mommeja Marin and others. Antiviral Activity and Incidence of Resistance after Treatment for Two Years with Emtricitabine in Patients with Chronic Hepatitis B. Abstract V-239. 42nd ICAAC. September 27-30, 2002. San Diego, CA. (Hepatitis.com, 42nd ICCAAC Summary)


*Reproduction of articles for personal or educational use is encouraged but please indicate the source of the article.

rising

HBV感染是一种常见且极具危险性的病毒感染，其有效的治疗选择一直有限，但是在过去的几年中对HBV感染有效的治疗药物已逐步增多。

一些研究中的令人振奋的药物正在通过临床试验，其中Coviracil(FTC, emtricitabine~恩曲他滨/鸟环核苷)是一种核苷类似物，具有强大的抗HBV、HIV活性。但其拥有和Epivir (lamivudine, 3TC)类似的抗药性，在一项评价Coviracil治疗慢性HBV感染病人的研究中，初步的数据表明它对HBV感染非常有效，抗药性发生率较低。进一步的随方研究有第42届ICAAC上交流。


在这项为期1年共98名患者的研究（FTCB-102）中，采用随机、双盲的方法，对每日一次、共三种剂量（25，100，200mg）进行比较研究。1年的治疗后，所有病人转换为每日一次、200mg剂量的Coviracil。

通过意图治疗分析，经过2年的Coviracil治疗，42%的病人HBV水平检测不出，76%的病人ALT正常，51%的病人血清HBeAg 转阴， 29%的病人HBeAb阳性。Coviracil耐药方面，服用Coviracil200mg2年的病人（19%）要低于第1 年服用25mg或100mg、第2年改为200mg的病人（分别为20%、37%）。Coviracil的治疗耐受性极好。

作者总结到：[Coviracil]产生了持续的病毒学和血清学应答（29%的病人HBeAg转换）。2年的研究中接受200mg的病人的变异率是低的（19%），提示其对病毒的强有力抑制作用限制了耐药株的出现。在M184V变异的发生方面，这些数据与一项HIV的临床试验是一致的。
10/14/02

参考（略）

请多指正。

可可

谢谢rising.以后请多帮忙。

rococo

"29%的人HBEAB阳性.",这应该是目前最伟大的HBV疗效了吧.这药是第几期药试啊.

unpigdual

“29%的病人HBeAb阳性”不算什么伟大吧，就是29%的血清转换率，现有药物足以达到这一水平了。

风中之子

如果是hbsab，那才让人兴奋呢@^@

rococo

噢!误会,谢了!

mingbai

唉!!!还是没有发明根治乙肝的药.就算这种药抗病毒有多强,安全性有多高又有什么用,我们面临的最大难题还不是身体上的,而是心理上的-----社会的歧视.我看,医学界如果同情我们的话,倒不如发明一种逃避体检的药,让我们活得有尊严.

unpigdual

这是不可能的。首先在国外没有这种歧视问题，所以国外的研究人员不可能去研制这种东西。国内的医生是想着怎么样赚钱，哪有心思去搞这种东西，就算搞出来，国家也要禁止的。

dsyman

我现在只想能有阻止向硬化和演变成ca的药物就很满足了