在美国第一阶段试验中，第一个受试者服用了Gannex的FXR激动

StephenW

First Subject Dosed with Gannex's FXR Agonist ASC42 in a U.S. Phase I Trial

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Ascletis Pharma Inc.

Dec 27, 2020, 19:30 ET

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SHANGHAI, Dec. 27, 2020 /PRNewswire/ -- Gannex, a wholly owned company of Ascletis Pharma Inc. (HKEX: 1672) and fully dedicated to the R&D and commercialization of new drugs in the field of NASH, announces today dosing of first subject with its NASH drug candidate ASC42, a Farnesoid X Receptor (FXR) agonist, in a U.S. Phase I Trial.

This U.S. phase I trial is a randomized, double-blind, placebo-controlled, single and multiple dose escalation study to evaluate safety, tolerability, pharmacokinetics and pharmacodynamics (biomarkers - FGF19 and C4) of ASC42 in healthy subjects. This trial also investigates the food effect on ASC42 exposure.

ASC42 is an in-house developed，novel non-steroidal, selective and potent FXR agonist. ASC42 received Fast Track designation from the U.S. Food and Drug Administration (FDA) for NASH. The oral tablet formulation of ASC42 has been developed with the in-house proprietary technology and is stable at room temperature.

"We are excited about the initiation of U.S. Phase I trial for ASC42 in 2020," said Dr. Handan He, Chief Scientific Officer of Ascletis, "This is an important milestone for our R&D team that discovered and developed ASC42, with the potential to be the best-in-class FXR agonist for NASH."

"As a novel FXR agonist, ASC42 has demonstrated robust preclinical anti-inflammatory and anti-fibrotic effect," said Melissa Palmer, MD, Chief Medical Officer of Gannex. "Combining ASC42 with ASC40, a fatty acid synthase (FASN) inhibitor or ASC41, a thyroid hormone receptor beta (THR-β) agonist will provide exciting therapeutic options for NASH patients."

About Ascletis

Ascletis is an innovative R&D driven biotech and listed on Hong Kong Stock Exchange (1672.HK). Ascletis is committed to developing and commercializing innovative drugs in the areas of viral hepatitis, NASH and HIV/AIDS for unmet medical needs in China and globally. Led by a management team with deep expertise and a proven track record, Ascletis has developed into a fully integrated platform covering the entire value chain from discovery and development to manufacturing and commercialization.

Ascletis has three marketed products and thirteen R&D pipeline drug candidates or combination therapies (nine of them developed in-house). 1. Viral hepatitis: (i) Hepatitis B: focus on breakthrough therapies for HBV clinical cure with subcutaneously injected PD-L1 antibody - ASC22 and Pegasys® as cornerstone drugs. (ii) Hepatitis C: successfully launched all oral regimen of ASCLEVIR® and GANOVO® combination (RDV/DNV regimen); and ASC18 fixed dose combination (FDC) is an upgraded version of RDV/DNV regimen with bridging study finished. 2. NASH: Gannex, a wholly-owned company of Ascletis, is fully dedicated to the R&D and commercialization of new drugs in the field of NASH. Gannex has three clinical stage drug candidates against three different targets – FASN, THR-beta and FXR, and three pre-clinical stage combination therapies. 3. HIV/AIDS: ASC09F is a FDC treatment of HIV targeting protease. The clinical trial application of ASC09F has been approved. For more information, please visit www.ascletis.com.

SOURCE Ascletis Pharma Inc.
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StephenW

在美国第一阶段试验中，第一个受试者服用了Gannex的FXR激动剂ASC42

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Ascletis Pharma Inc.

2020年12月27日，美国东部时间19:30

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2020年12月27日，上海，美通社/-Gannex是Ascletis Pharma Inc.（HKEX：1672）的全资子公司，全力致力于NASH领域新药的研发和商业化，今天宣布首批给药在美国第一阶段试验中，将其受试者与NASH候选药物ASC42（一种法尼醇X受体（FXR）激动剂）结合使用。

这项美国I期试验是一项随机，双盲，安慰剂对照，单次和多次剂量递增研究，旨在评估健康受试者中ASC42的安全性，耐受性，药代动力学和药效学（生物标志物-FGF19和C4）。该试验还研究了食物对ASC42暴露的影响。

ASC42是内部开发的新型非甾体，选择性和强效FXR激动剂。 ASC42获得了美国食品药品监督管理局（FDA）对NASH的快速通道认证。 ASC42的口服片剂已采用内部专有技术开发，并在室温下稳定。

Ascletis首席科学官Handan He博士说：“我们对2020年美国ASC42一期试验的启动感到兴奋，这对于我们研发团队开发并拥有ASC42的潜力是一个重要的里程碑。成为NASH上最好的FXR激动剂。”

Gannex首席医学官医学博士Melissa Palmer表示：“作为一种新型的FXR激动剂，ASC42已表现出强大的临床前抗炎和抗纤维化作用。 “将ASC42与脂肪酸合酶（FASN）抑制剂ASC40或甲状腺激素受体β（THR-β）激动剂ASC41结合使用将为NASH患者提供令人兴奋的治疗选择。”

关于Ascletis

Ascletis是一家创新的研发驱动型生物技术，已在香港联合交易所（1672.HK）上市。 Ascletis致力于在病毒性肝炎，NASH和HIV / AIDS领域开发创新药物并将其商业化，以满足中国和全球尚未满足的医疗需求。在拥有深厚专业知识和成功经验的管理团队的带领下，Ascletis已发展成为一个完全集成的平台，涵盖了从发现，开发到制造和商业化的整个价值链。

Ascletis有3种上市产品和13种R＆D管线候选药物或联合疗法（其中9种是在内部开发的）。 1.病毒性肝炎：（i）乙型肝炎：专注于突破性疗法，以皮下注射的PD-L1抗体-ASC22和Pegasys®作为基础药物，可用于HBV临床治愈。 （ii）丙型肝炎：成功启动了ASCLEVIR®和GANOVO®联合治疗的所有口服方案（RDV / DNV方案）； ASC18固定剂量组合（FDC）是RDV / DNV方案的升级版，已完成桥接研究。 2. NASH：Gannex是Ascletis的全资公司，完全致力于NASH领域中新药的研发和商业化。 Gannex针对三种不同目标（FASN，THR-beta和FXR）具有三种临床阶段候选药物，以及三种临床前阶段联合疗法。 3. HIV / AIDS：ASC09F是FDC治疗HIV靶向蛋白酶。 ASC09F的临床试验应用已获得批准。有关更多信息，请访问www.ascletis.com。

消息来源Ascletis Pharma Inc.
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