LIVER411的文章：新药

特深沉

原文由LIVER411在英文区发表。



主题: Achillion initiates PII of HBV drugs  

liver411

Achillion公司的HBV药物开始二期实验





AddictedMember  发表于 2002-03-01.06:28:17　　　 　　　　　　　　　　　

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Thursday February 28, 10:30 am Eastern Time

Press Release



SOURCE: Achillion Pharmaceuticals

来源： Achillion药品公司

Achillion Pharmaceuticals Initiates Phase 2 Study of Lead Product Candidate in Hepatitis B Patients



Achillion药品公司开始了对一种HBV领先产品进行二期实验。



NEW HAVEN, Conn., Feb. 28 /PRNewswire/ -- Achillion Pharmaceuticals, a privately held pharmaceutical company focused on the discovery, development and commercialization of innovative anti-infective agents, today announced the commencement of a Phase 2 clinical study with the Company's lead product candidate, ACH-126,443 (Beta-L-Fd4C) in patients with chronic hepatitis B infection.



NEW HAVEN, Conn., Feb. 28 /PRNewswire消息— Achillion药品公司，一家私营药物公司，致力于

研发和商品化抗感染药物。今天，该公司宣布了公司的首要候选产品，ACH-126,443

(Beta-L-Fd4C)，在HBV慢性HBV感染者中开始了二期临床实验。



This phase 2 study (Study 443-003) will help identify the optimal dose of ACH-126,443 to treat patients chronically infected with hepatitis B virus (HBV), defined as the dose which most effectively suppresses hepatitis B DNA levels (viral load) while providing the best safety profile. This double-blind study will evaluate several doses of ACH-126,443 administered once a day to patients with chronic HBV infection, compared with lamivudine (3TC), and placebo. The 443-003 study will be conducted in multiple centers across central and eastern Europe under Achillion's Investigational New Drug application (IND) filed with the US Food and Drug Administration.



该项2P实验（项目号443-003）将帮助确定ACH-126,443治疗慢性HBV感染者的最佳剂量，也就

是在最安全的情况下，最高效地抑制HBV DNA水平（病毒载量）。这项双盲研究将评估

ACH-126,443 每天给予HBV患者的不同剂量，并同拉米夫定和安慰剂对比。 443-003项目的研究

将在中欧和东欧的多个中心进行，按Achillion公司新药调查程序，并在美国FDA存档。



"In two years from the launch of Achillion, we have advanced ACH-126,443 from early pre-clinical testing into Phase 2 efficacy trials. This rapid entry into clinical development underscores the value of the experience of our team to deliver major milestones successfully,'' said William G. Rice, Achillion's Chief Executive Officer. ``Chronic hepatitis B infection is a silent epidemic with an enormous need for additional and superior therapeutics. With existing treatments, the medical needs of patients are often not met due to adverse side effects or loss of efficacy because of viral resistance.''



Achillion公司的CEO， William G. Rice，说：“从Achillion开办的两年内，我们推进了

ACH-126,443从前期临床到二期功效实验。这样的高速进入临床阶段更确证了我们工作的价值具有

里程碑意义。慢性HBV感染是种沉默的流行病，更需要特别和高效的治疗。以现有的疗法，病人

所需的治疗很难满足，原因是有副作用，或因病毒抗药性致使丧失疗效。”



"The pre-clinical data on ACH-126,443 indicate potency against HBV strains that are both sensitive and resistant to lamivudine, the only currently approved oral anti-HBV drug,'' commented Lisa M. Dunkle, MD, Senior Vice President of Drug Development for Achillion. " Our previous clinical studies have demonstrated very promising safety and antiviral activity of the compound. We look forward to the data from this current study to provide more definitive information regarding the safety and efficacy of several doses of ACH-126,443.''



该公司药物研发副总裁，医学博士 Lisa M. Dunkle说，“ACH-126,443的前期临床数据显示抗HBV

的能力很强，无论对拉米敏感品系或抗药性品系。拉米是目前唯一被批准的口服抗HBV药物。我

们先前的临床研究证明该化合物很好的安全性预期和抗病毒性。我们期待当前的研究能提供关于

ACH-126,443安全和功效的更多准确信息。



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About ACH-126,443



ACH-126,443 is an L-nucleoside antiviral agent administered orally once daily that has demonstrated in vitro activity against both wild-type and lamivudine-resistant strains of HBV. Clinical studies are planned in 2002 to evaluate the efficacy of the agent in patients with lamivudine-resistant strains of HBV. Chronic HBV infection is a life-threatening disease that affects more than 350 million individuals worldwide. It is a common cause of liver damage and the leading cause of liver cancer. The World Health Organization lists chronic HBV as the ninth leading cause of death worldwide.



ACH-126,443是一种L-核苷类抗病毒药，每天一次给用药量，在实验室中显示能对抗HBV野生株

和拉米夫定耐药品系。计划在2002年进行临床研究，来评估对抗拉米品系的HBV患者功效。慢性

HBV感染是种致命的疾病，感染了世界上超过35亿个体。它是肝损伤和肝癌的主因。世界卫生组

织把慢性HBV列为世界上第9大死亡原因。



Pre-clinical studies have also demonstrated that ACH-126,443 effectively inhibits HIV, including lamivudine-resistant and multi-drug resistant strains. Achillion is also conducting studies to evaluate ACH-126,443 in patients with HIV infection. Over 36 million people worldwide were estimated by the National Institutes of Health to be living with HIV/AIDS at the end of 2000, with approximately 5.3 million new infections having occurred in 2000. Through 2000, the HIV/AIDS epidemic had resulted in over 20 million deaths worldwide.



前期临床研究还显示CH-126,443能有效地抑制HIV，包括拉米耐药型，和多种药物耐药型。

Achillion公司还开展了ACH-126,443对HIV感染者的评估研究。国家卫生研究所估计，到2000年

底，全世界有超过3千6百万人携带HIV/AIDS，其中5百30万是在2000年内新感染的。2000年

中，HIV/AIDS疾病造成世界上2千万人死亡。



Achillion is a privately held pharmaceutical company focused on the discovery, development and commercialization of innovative small molecule drugs that combat drug resistance in infectious diseases, with a particular emphasis on antiviral drugs to treat diseases caused by hepatitis B and C viruses (HBV and HCV), HIV and herpes viruses. Achillion's drug development pipeline is led by the product candidate, ACH-126,443 (Beta-L-Fd4C), which is currently in human clinical trials for the treatment of chronic hepatitis B and HIV infections. Achillion's drug discovery expertise embodies both a conventional medicinal chemistry approach directed at classic anti-infective molecular targets, and its novel Zinc Finger Targeting (ZFT) drug discovery technology developing small molecules that target zinc finger motifs unique to particular pathogens.



Achillion药品公司，一家私营药物公司，致力于研发和商品化革新的小分子药物，抗击耐药型感染

疾病，特别重视治疗HBV，HCV，HIV，及疱疹的抗病毒药物。Achillion公司的药物研发途径是

由候选药物引导，ACH-126,443 (Beta-L-Fd4C),现已进行治疗HBV，HIV感染的临床实验。

Achillion公司的药物研究专门技术体现在，一方面，有传统的化学方法对准传统的抗感染分子目

标，另一方面，他的新颖的锌指针靶（ZFT）药物寻找技术，通过瞄准锌指针图形，可发展对应

唯一病原体的小分子。



This news release contains certain forward-looking statements that involve risks and uncertainties. Such statements are only predictions and the company's actual results may differ materially from those anticipated in these forward-looking statements. Factors that may cause such differences include the risk that products that appeared promising in early research and clinical trials do not demonstrate safety or efficacy in larger-scale clinical trials and the risk that the company will not obtain approval to market its products.



已发表的消息，包括预先声明含有风险和不确定性。该声明只是预报，公司的实际结果可能和预期

的声明有很大不同。可能造成差异的因素包括，早期研究的表现的预期，不能在临床实验或大规模

临床实验中证实其安全性和功效。风险还有，该公司不能获得销售他们产品的批准。

特深沉

以下为该公司网页内容



Beta-L-Fd4C (ACH-126,443)is an L-nucleoside with in vitro activity against wild-type strains of hepatitis B (HBV) and human immunodeficiency

virus (HIV), as well as strains of HBV and HIV that are resistant to certain currently used therapies. Research conducted with Beta-L-Fd4C

indicates that it inhibits viral replication by inhibiting reverse transcriptase in HIV and DNA polymerase in HBV.

Achillion is currently evaluating Beta-L-Fd4C in chronically infected HBV patients in a phase 1b/2 clinical trial. Additional phase 2 studies are

planned for Beta-L-Fd4C in 2002, evaluating the compound in chronic HBV patients.



Clinical and pre-clinical data collected to date indicates that Beta-L-Fd4C can be dosed as one pill once a day, may be used in combination

therapy, and has an excellent side effect profile. The L-nucleoside configuration of the compound may provide protection against mitochondrial



toxicity, a serious side effect often seen with D-nucleosides。

The current worldwide market for HBV is estimated at $650 million annually, however, due to the low efficacy, poor tolerability and rapid

emergence of resistance with current HBV therapeutics (lamivudine and interferon), most clinicians are reserving treatment for late stage disease,

thus these agents have very poor market penetration.   Annual sales of lamivudine for HIV and HBV are over $1.2 billion annually. Achillion

believes that a compound with robust antiviral activity against wild type and resistant HBV & HIV will help address a serious global epidemic and

current unmet medical need.



Beta-L-Fd4C (ACH-126,443)是一种L-核苷，在实验室中，具有对抗野生株HBV和HIV的能力，包

括目前的治疗中有抗药性的品系。对Beta-L-Fd4C 的研究指出，它通过抑制HIV的逆转录酶和

HBV的DNA聚合酶来抑制病毒复制。



Achillion公司现已就 Beta-L-Fd4C进行了对慢性HBV感染者的1b/2期临床实验。另外，正计划在

2002年开展2期研究。评估对慢性HBV感染的影响。



临床和先期临床收集的数据指出，Beta-L-Fd4C可以用每天一片的剂量给药，可用于联合治疗，有

良好的副作用评价。该化合物的L-核苷构造可能会提供对线粒体毒性的保护（一种在D-核苷上常

见的严重副作用）。目前，全世界每年HBV药物估计有 $65亿的市场。然而，由于目前HBV治疗

（拉米和干扰素）的低效，耐受性差（译注：副作用？）和快速产生抗药性，多数临床医师推迟治

疗到下一阶段疾病。所以，这些药的市场渗透率很低。拉米夫定每年用于HBV和HIV的销量超过

$12亿。Achillion 公司相信，一种对HBV&HIV 野生株和耐药株有很强抗病毒能力的化合物，会帮

助解决全球性严重传染病和当前对治疗药物的需求。

特深沉

感觉一场瓜分中国HBV市场的竞赛正在很多生化公司进行。谁先研究出高效的药物，谁就能从HBV身上大捞特捞。



不过，到了那天，我们又要“量中华之物力，结与国之欢心”了。

liver411

谢谢你, 辛苦了!

难兄难弟

希望能找到根本的药物

可可

我们论坛真是人才倍出.

非常感谢特深沉兄.

medline

特深沉兄的付出真是没说的。

已经看到过几篇翻译稿了

rainbow

我们大家都是战友，是不是该由我们自己来研制，用自己做试验，搞出个特效药呢？

hezhanjian

美女美女我爱你，就像老鼠爱大米

消灭HBV

非常感谢