An Open, Multicenter, Phase III Extension Clinical Trial to Evaluate the Long-term Safety of ASC40 (Denifanstat) Tablets in Patients With Moderate to Severe Acne Vulgaris

This is a multicenter, open-label study designed to determine the long-term safety of ASC40 (Denifanstat) tablets in patients with moderate to severe acne vulgaris enrolled in the ASC40-303 Phase III study. All subjects are eligible for study eligibility screening after enrollment in ASC40-303 Phase III study, and all eligible subjects with moderate to severe acne vulgaris will receive ASC40 (Denifanstat) tablets after signing informed consent. The investigational drug will be administered orally once daily (QD) for up to 40 weeks. There will be a total of 7 visits for screening and follow-up. The tests required by the program included routine blood tests, blood biochemistry, lipid profile, pregnancy test and urine routine, etc.

开始日期2024-04-24

申办/合作机构

歌礼药业（浙江）有限公司

CTR20240230 / Recruiting临床3期

评价ASC40（地尼法司他）片治疗中、重度寻常性痤疮患者的长期安全性的开放、多中心、III期延伸临床研究

观察长期使用ASC40（地尼法司他）片治疗中、重度寻常性痤疮患者的安全性

开始日期2024-04-18

申办/合作机构

歌礼生物科技（杭州）有限公司

CTR20233958 / Recruiting临床3期

评价 ASC40（地尼法司他）片治疗中、重度寻常性痤疮患者的疗效和安全性的多中心、随机、双盲、安慰剂对照的III期临床研究

主要目的：评价 ASC40（地尼法司他）片每日1次，治疗12周时，与安慰剂相比，治疗中、重度寻常性痤疮患者的疗效。次要目的：评价 ASC40（地尼法司他）片每日1次，治疗12周时，与安慰剂相比，治疗中、重度寻常性痤疮患者的安全性。

开始日期2024-01-23

申办/合作机构

歌礼生物科技（杭州）有限公司

100 项与地尼法司他相关的临床结果

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100 项与地尼法司他相关的转化医学

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100 项与地尼法司他相关的专利（医药）

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项与地尼法司他相关的文献（医药）

2024-03-01·Molecular oncology

Fatty acid synthase (FASN) signalome: A molecular guide for precision oncology

Article

作者: Serrano-Hervás, Eila ; Lupu, Ruth ; Llop-Hernández, Àngela ; López, Júlia ; Vander Steen, Travis ; Martin-Castillo, Begoña ; Menendez, Javier A ; Cuyàs, Elisabet ; Verdura, Sara ; Osuna, Sílvia ; Encinar, Jose Antonio

The initial excitement generated more than two decades ago by the discovery of drugs targeting fatty acid synthase (FASN)‐catalyzed de novo lipogenesis for cancer therapy was short‐lived. However, the advent of the first clinical‐grade FASN inhibitor (TVB‐2640; denifanstat), which is currently being studied in various phase II trials, and the exciting advances in understanding the FASN signalome are fueling a renewed interest in FASN‐targeted strategies for the treatment and prevention of cancer. Here, we provide a detailed overview of how FASN can drive phenotypic plasticity and cell fate decisions, mitochondrial regulation of cell death, immune escape and organ‐specific metastatic potential. We then present a variety of FASN‐targeted therapeutic approaches that address the major challenges facing FASN therapy. These include limitations of current FASN inhibitors and the lack of precision tools to maximize the therapeutic potential of FASN inhibitors in the clinic. Rethinking the role of FASN as a signal transducer in cancer pathogenesis may provide molecularly driven strategies to optimize FASN as a long‐awaited target for cancer therapeutics.

2024-02-01·Recent patents on anti-cancer drug discovery

Fatty Acid Synthase (FASN): A Patent Review Since 2016-Present

Article

作者: Karthikeyan, Chandrabose ; Moorthy, Narayana Subbiah Hari Narayana ; Singh, Shailendra

Abstract::

Fatty acid synthase (FASN), is a key metabolic enzyme involved in fatty acid biosynthesis and is an essential target for multiple disease progressions like cancer, obesity, NAFLD, etc. Aberrant expression of FASN is associated with deregulated energy metabolism of cells in these diseases. This article provides a summary of the most recent developments in the discovery of novel FASN inhibitors with potential therapeutic uses in cancer, obesity, and other metabolic disorders such as nonalcoholic fatty liver disease from 2016 to the present. The recently published patent applications and forthcoming clinical data of FASN inhibitors from both academia and the pharma industries are also highlighted in this study. The implication of FASN in multiple diseases has provided an impetus for developing novel inhibitors by both pharma companies and academia. Critical analysis of the patent literature reveals the exploration of diverse molecular scaffolds to identify potential FASN inhibitors that target the different catalytic domains of the enzyme. In spite of these multifaceted efforts, only one molecule, TVB-2640, has reached phase II trials for non-alcoholic steatohepatitis (NASH) and many malignancies. However, the combined efforts of pharma companies to produce several FASN inhibitors might facilitate the clinical translation of this unique class of inhibitors. Nevertheless, concerted efforts towards developing multiple FASN inhibitors by pharma companies might facilitate the clinical translation of this novel class of inhibitors.

2023-07-05·Clinical cancer research : an official journal of the American Association for Cancer Research

Phase II Investigation of TVB-2640 (Denifanstat) with Bevacizumab in Patients with First Relapse High-Grade Astrocytoma.

Article

作者: Madhusudanannair-Kunnuparampil, Vinu ; Michalek, Joel ; Diaz Duque, Adolfo Enrique ; Chen, Yidong ; Caflisch, Laura ; Brenner, Andrew ; Kelly, William ; Floyd, John ; Pathuri, Sarath Chand ; Konkel, Brandon

PURPOSE:

Glioblastoma represents the most common primary brain tumor. Although antiangiogenics are used in the recurrent setting, they do not prolong survival. Glioblastoma is known to upregulate fatty acid synthase (FASN) to facilitate lipid biosynthesis. TVB-2640, a FASN inhibitor, impairs this activity.

PATIENTS AND METHODS:

We conducted a prospective, single-center, open-label, unblinded, phase II study of TVB-2640 plus bevacizumab in patients with recurrent high-grade astrocytoma. Patients were randomly assigned to TVB-2640 (100 mg/m2 oral daily) plus bevacizumab (10 mg/kg i.v., D1 and D15) or bevacizumab monotherapy for cycle 1 only (28 days) for biomarker analysis. Thereafter, all patients received TVB-2640 plus bevacizumab until treatment-related toxicity or progressive disease (PD). The primary endpoint was progression-free survival (PFS).

RESULTS:

A total of 25 patients were enrolled. The most frequently reported adverse events (AE) were palmar-plantar erythrodysesthesia, hypertension, mucositis, dry eye, fatigue, and skin infection. Most were grade 1 or 2 in intensity. The overall response rate (ORR) for TVB-2640 plus bevacizumab was 56% (complete response, 17%; partial response, 39%). PFS6 for TVB-2640 plus bevacizumab was 31.4%. This represented a statistically significant improvement in PFS6 over historical bevacizumab monotherapy (BELOB 16%; P = 0.008) and met the primary study endpoint. The observed OS6 was 68%, with survival not reaching significance by log-rank test (P = 0.56).

CONCLUSIONS:

In this phase II study of relapsed high-grade astrocytoma, TVB-2640 was found to be a well-tolerated oral drug that could be safely combined with bevacizumab. The favorable safety profile and response signals support the initiation of a larger multicenter trial of TVB-2640 plus bevacizumab in astrocytoma.

140

项与地尼法司他相关的新闻（医药）

2024-06-10

·空之客

【药海听涛】GLP-1也不是万能的：2024年欧肝会NASH药物数据更新

好像自从GLP-1成为医药界顶流以来，但凡被它“临幸”过的领域就要寸草不生，其中NASH就是很多人说是下一个“被GLP-1打没了的市场”。恰逢今年的EASL，几个重要的NASH在研管线都首次公布了病理数据，我们可以横向比较一下，在这个领域GLP-1是否还是万能的？ 1 THR-β 在Madrigal的Resmetirom带头大哥，成为首个获批的NASH治疗药物后，THR-β自然而然成为这个适应症绝对的显学，而继续光大门楣的任务就落到新贵Viking身上。本次会议Viking公布了VK-2809的2b期临床VOYAGE研究的52周病理结果，在每日一次10mg/5mg/2.5mg/1mg和安慰剂组中，NASH缓解且纤维化不恶化的患者比例为75.0%/63.0%/65.4%/71.4%/29.3%、最高剂量组相比安慰剂组高45.7%，纤维化改善且NASH不恶化的患者比例为56.8%/51.9%/44.2%/57.1%/34.1%，最高剂量组相比安慰剂高22.7%。安全性方面也相对可接受，虽然不良反应发生率偏高，但最高剂量组因不良反应而停药的比例不到10%、且与安慰剂组相差不大。 https://ir.vikingtherapeutics.com/2024-06-04-Viking-Therapeutics-Announces-Positive-52-Week-Histologic-Data-from-Phase-2b-VOYAGE-Study-of-VK2809-in-Patients-with-Biopsy-Confirmed-Non-Alcoholic-Steatohepatitis-NASH 与之相比，本门大师兄Resmetirom就有点黯然失色了，最高剂量组在两个终点的安慰剂修正比例分别为20.2%和11.7%，都远低于VK-2809。 https://www.nejm.org/doi/10.1056/NEJMoa2028395 VK-2809这次的临床数据其实可以说是超预期的，不仅显著优于同靶点已获批的Resmetirom，而且从两个终点的绝对值来看也处于整个NASH在研药物的领先位置。不过蹊跷之处在于逆天的安慰剂效应（两个终点安慰剂组响应率为29%和34%），导致相对来看有效性没有那么惊艳，而且剂量依赖性也不明显，可能都成为数据发布后股价大跌的一些解释。 2 GLP-1 在GLP-1的封神之路上，NASH应该是除减重以外最大的适应症机会之一，Semaglutide已经一马当先（尽管结果也不算很理想，见后文），紧随其后的是两个双靶点Tirzepatide和Survodutide。本次会议Eli Lilly公布了Tirzepatide的2期临床SYNERGY-NASH研究的52周病理结果，在每周一次15mg/10mg/5mg和安慰剂组中，NASH缓解且纤维化不恶化的患者比例为73.3%/62.8%/51.8%/13.2%、最高剂量组相比安慰剂组高60.1%，纤维化改善且NASH不恶化的患者比例为51.0%/51.3%/54.9%/29.7%、最高剂量组相比安慰剂高21.3%。虽然安全性尚未具体披露，但入组190例患者到最后只有157例完成治疗接受肝穿，脱落率还是有点偏高了。 https://events-distribution.easl.eu/from.storage?image=mIoM6rsplpmkPbT9D4cRMhCdB962jqqPLI0ekg3BGloLb0klBbYoN9dNVhvU-7Oz0 本次会议BI也公布了Survodutide的2期临床48周病理结果，在每周一次6.0mg/4.8mg/2.4mg和安慰剂组中，NASH缓解且纤维化不恶化的患者比例为43%/62%/47%/14%、最优剂量组相比安慰剂组高48%，纤维化改善且NASH不恶化的患者比例为32.4%/36.1%/34.2%/17.6%、最优剂量组相比安慰剂高18.5%。安全性就有点堪忧，不仅不良反应发生率高达93-97%，而且因不良反应而停药的比例也在16-23%。 https://www.nejm.org/doi/10.1056/NEJMoa2401755 与新一代的这两个双靶点GLP-1相比，Semaglutide此前公布的数据同样也都是明显处于下风，最高剂量组在两个终点的安慰剂修正比例分别为42%和10%。 https://www.nejm.org/doi/10.1056/NEJMoa2028395 从GLP-1这几个药物的NASH临床结果中，可以读出一些共性的问题：1）首先看起来GLP-1药物对于纤维化的改善不太在行，相对而言在NASH缓解上表现要好不少；2）其次GLP-1药物有效性的剂量依赖程度很低，三个药物都出现了随着剂量升高而效果增加不明显、甚至倒挂的情况，可能说明其作用机制与想象中存在较大差异；3）这三个临床，在NASH缓解且纤维化不恶化终点的安慰剂效应都控制到比较低（13-17%），但在另一边纤维化改善且NASH不恶化终点的安慰剂组都响应率偏高（S药和T药分别33%和30%），这对于统计学显著性与否产生了很关键的作用。 3 FGF-21 Akero在今年三月公布了Efruxifermin的2b期临床HARMONY试验的96周病理结果，在每日一次50mg/28mg和安慰剂组中，纤维化改善且NASH不恶化的患者比例为75%/46%/24%、最高剂量组相比安慰剂高达51%，NASH缓解且纤维化不恶化的患者比例为57%/62%/24%、最高剂量组相比安慰剂组高达33%。安全性方面略有点尴尬，SAE和因不良反应而停药的比例都超过10%。 https://ir.akerotx.com/static-files/c76e5581-39ab-4d46-a6c7-b5893f7a2210 另一家企业89Bio在今年五月公布了Pegozafermin的2b期临床ENLIVEN试验的24周病理结果（又在本次会议公布了48周非病理结果），在每两周一次44mg、每周一次30mg/15mg和安慰剂组中，纤维化改善且NASH不恶化的患者比例为27%/26%/22%/7%、最高剂量组相比安慰剂高20%，NASH缓解且纤维化不恶化的患者比例为26%/23%/37%/2%、最高剂量组相比安慰剂组高24%。安全性方面则相当优秀，特别是每两周一次的剂量组，不良反应发生率67%、停药比例仅2%。 https://www.nejm.org/doi/full/10.1056/NEJMoa2304286 FGF-21的有效性在两个终点之间相对均衡，而Efruxifermin很明显更加突出，其改善纤维化能力是目前的全场最佳；然而除了同样存在剂量依赖性不足的问题外，Efruxifermin最大的蹊跷在于24周和96周在NASH终点的倒挂，以及安全性的隐忧。 4 横向对比在纤维化改善且NASH不恶化终点上，Efruxifermin处在一骑绝尘的位置（哪怕是结合96周和24周的数据），VK-2809和Tirzepatide看绝对值本来也有希望、但在奇高的安慰剂效应抵消之下显得较为平庸，另有Denifanstat也值得关注，至少目前这几个后来者都优于已获批的Resmetirom。在NASH缓解且纤维化不恶化终点上，GLP-1们就比较优秀，VK-2809也很能打，Efruxifermin则呈现吊诡的“长短倒挂”，同样地也都优于Resmetirom。综上所述，NASH目前仍处于群雄逐鹿的蛮荒状态，既没有因为首个获批的药物而定鼎大局，也没有看出会被GLP-1扫穴犁庭之势，这几家正在推进的三期临床都还有充分的竞争机会。往期NASH药物相关文章：【药海听涛】最后的烛火能否燃到黎明：NASH领域再现希望【药海听涛】弦歌不辍还是功败垂成：NASH药物近期主要进展【药海听涛】Madrigal鼙鼓动地来，惊破NASH羽衣曲【药海听涛】以往不谏，来者可追：NASH研发方向的新旧交替

临床2期ASH会议临床结果细胞疗法

2024-06-10

·GlobeNewswire-Health Care

Sagimet Biosciences to Host Conference Call and Webcast to Discuss Recently Presented Data from ITT and F3 Patient Population in Phase 2b FASCINATE-2 Clinical Trial of Denifanstat

Call scheduled on Thursday, June 13, 2024 at 9.30 AM PT / 12:30 PM ETSAN MATEO, Calif., June 10, 2024 (GLOBE NEWSWIRE) -- Sagimet Biosciences Inc. (Sagimet, Nasdaq: SGMT), a clinical-stage biopharmaceutical company developing novel fatty acid synthase (FASN) inhibitors designed to target dysfunctional metabolic and fibrotic pathways, today announced that it will host a conference call and webcast on Thursday, June 13, 2024, at 9.30 AM PT / 12:30 PM ET. The event will feature Rohit Loomba, M.D., M.H.Sc., Professor of Medicine, Chief, Division of Gastroenterology and Hepatology, and Director, MASLD Research Center, University of California San Diego, who was the Principal Investigator on the Phase 2b FASCINATE-2 clinical trial and serves as a scientific advisor for Sagimet on its ongoing development of denifanstat. Dr. Loomba will discuss positive data from Sagimet’s FASCINATE-2 Phase 2b clinical trial of denifanstat versus placebo in biopsy-confirmed metabolic dysfunction-associated steatohepatitis (MASH) patients which he recently presented at the European Association for the Study of the Liver (EASL) Congress in Milan, Italy. Sagimet’s lead drug candidate, denifanstat, is an oral, once-daily pill and selective FASN inhibitor in development for the treatment of MASH. Participants will have the opportunity to participate in a chat-based Q&A session. Conference Call and Webcast InformationThe live webcast and replay may be accessed by visiting the Sagimet website here. The dial-in number is 1-877-407-0779 (U.S./Canada) or 1-201-389-0914 (international). The conference ID for all callers is 13747107. The Call me™ link may be accessed here. Participants can use guest dial-in numbers above and be answered by an operator or they can click the Call me™ link for instant telephone access to the event (dial-out). The Call me™ link will be made active 15 minutes prior to scheduled start time. About Rohit Loomba, MD Rohit Loomba, MD, M.H.Sc., is a board-certified gastroenterologist. His expertise includes treating and managing many types of chronic liver disease, such as metabolic dysfunction-associated steatotic liver disease (MASLD), nonalcoholic steatohepatitis, chronic hepatitis, cirrhosis, and hemochromatosis. As a transplant hepatologist, Dr. Loomba works with transplant surgeons in the pre and postoperative care of liver transplant patients. As a professor in the Division of Gastroenterology, Dr. Loomba instructs students, residents and fellows in the Department of Medicine at UC San Diego School of Medicine. His research focuses on all aspects of MASLD, including prevalence in aging, epidemiology, genetic and environmental predisposition and progression. Dr. Loomba is the founding director of the UCSD MASLD Research Center where a multi-disciplinary team of researchers are conducting cutting edge research in all aspects of MASLD including non-invasive biomarkers, genetics, epidemiology, clinical trial design, imaging end-points, and integrated OMICs using microbiome, metabolome and lipidome. This integrated approach has led to several innovative applications such as establishment of MRI-PDFF as a non-invasive biomarker of treatment response in early phase trials in MASH, which has now been adopted in more than a hundred clinical trials conducted worldwide. He holds several patents on non-invasive biomarkers of MASH and fibrosis. His research is funded by the National Institutes of Health as a Principal Investigator including two R01s, three U01 (two NIDDK and one from NIAAA), clinical core director of P30 (NIDDK) and project director P01 (NHLBI) grant mechanisms, Foundation of NIH, as well as several large multicenter, multi-million dollar investigator initiated research projects funded by the industry. He is the Principal Investigator, UCSD, for the NIDDK-sponsored MASH Clinical Research Network and the Liver Cirrhosis Network. Dr. Loomba has published more than 500 peer-reviewed manuscripts in his field. He is an elected member of the American Society of Clinical Investigation and the Association of American Physicians. He has been continuously listed among the top 0.1% percent of highly cited scientists across fields of sciences. Dr. Loomba’s disclosure of conflicts of interest (COI) can be found in the EASL presentation which is available in the Posters & Publications section of Sagimet’s website at www.sagimet.com. About the Phase 2b FASCINATE-2 Clinical Trial The Phase 2b FASCINATE-2 clinical trial was a 52-week randomized, double-blind, placebo-controlled trial that evaluated the safety and histological impact of denifanstat compared to placebo in 168 biopsy-confirmed MASH patients with moderate-to-severe fibrosis (stage F2 or F3) with NAS ≥4. Patients were randomized 2:1 to receive 50 mg denifanstat or placebo, taken orally once daily. An end-of-trial biopsy was assessed by a central pathologist for histological endpoints. Liver biopsies were also analyzed using AI-based digital pathology. About Sagimet Biosciences Sagimet is a clinical-stage biopharmaceutical company developing novel fatty acid synthase (FASN) inhibitors that are designed to target dysfunctional metabolic pathways in diseases resulting from the overproduction of the fatty acid, palmitate. Sagimet’s lead drug candidate, denifanstat, is an oral, once-daily pill and selective FASN inhibitor in development for the treatment of MASH. FASCINATE-2, a Phase 2b clinical trial of denifanstat in MASH with liver biopsy-based primary endpoints, was successfully completed with positive results. For additional information about Sagimet, please visit www.sagimet.com. About MASH MASH is a progressive and severe liver disease which is estimated to impact more than 115 million people worldwide, for which there is only one recently approved treatment in the United States and no currently approved treatments in Europe. In 2023, global liver disease medical societies and patient groups formalized the decision to rename non-alcoholic fatty liver disease (NAFLD) to metabolic dysfunction-associated steatotic liver disease (MASLD) and nonalcoholic steatohepatitis (NASH) to metabolic dysfunction-associated steatohepatitis (MASH). Additionally, an overarching term, steatotic liver disease (SLD), was established to capture multiple types of liver diseases associated with fat buildup in the liver. The goal of the name change was to establish an affirmative, non-stigmatizing name and diagnosis. Forward-Looking Statements This press release contains forward-looking statements within the meaning of, and made pursuant to the safe harbor provisions of, The Private Securities Litigation Reform Act of 1995. All statements contained in this press release, other than statements of historical facts or statements that relate to present facts or current conditions, including but not limited to, statements regarding: the expected timing of the presentation of data from ongoing clinical trials, Sagimet’s clinical development plans and related anticipated development milestones, Sagimet’s cash and financial resources and expected cash runway. These statements involve known and unknown risks, uncertainties and other important factors that may cause Sagimet’s actual results, performance or achievements to be materially different from any future results, performance or achievements expressed or implied by the forward-looking statements. In some cases, these statements can be identified by terms such as “may,” “might,” “will,” “should,” “expect,” “plan,” “aim,” “seek,” “anticipate,” “could,” “intend,” “target,” “project,” “contemplate,” “believe,” “estimate,” “predict,” “forecast,” “potential” or “continue” or the negative of these terms or other similar expressions. The forward-looking statements in this press release are only predictions. Sagimet has based these forward-looking statements largely on its current expectations and projections about future events and financial trends that Sagimet believes may affect its business, financial condition and results of operations. These forward-looking statements speak only as of the date of this press release and are subject to a number of risks, uncertainties and assumptions, some of which cannot be predicted or quantified and some of which are beyond Sagimet’s control, including, among others: the clinical development and therapeutic potential of denifanstat or any other drug candidates Sagimet may develop; Sagimet’s ability to advance drug candidates into and successfully complete clinical trials, including its Phase 3 denifanstat program; Sagimet’s relationship with Ascletis, and the success of its development efforts for denifanstat; the accuracy of Sagimet’s estimates regarding its capital requirements; and Sagimet’s ability to maintain and successfully enforce adequate intellectual property protection. These and other risks and uncertainties are described more fully in the “Risk Factors” section of Sagimet’s most recent filings with the Securities and Exchange Commission and available at www.sec.gov. You should not rely on these forward-looking statements as predictions of future events. The events and circumstances reflected in these forward-looking statements may not be achieved or occur, and actual results could differ materially from those projected in the forward-looking statements. Moreover, Sagimet operates in a dynamic industry and economy. New risk factors and uncertainties may emerge from time to time, and it is not possible for management to predict all risk factors and uncertainties that Sagimet may face. Except as required by applicable law, Sagimet does not plan to publicly update or revise any forward-looking statements contained herein, whether as a result of any new information, future events, changed circumstances or otherwise. Contact:Joyce Allaire LifeSci Advisors JAllaire@lifesciadvisors.com

临床2期临床结果

2024-06-06

·药明康德

GSK达成5000万美元寡核苷酸公司收购协议；显著缓解MASH与肝纤维化，口服小分子临床积极数据公布

▎药明康德内容团队编辑 GSK达成5000万美元寡核苷酸疗法公司收购协议 GSK今天宣布以高达5000万美元（约合3900万英镑）的款项收购了致力于开发寡核苷酸疗法的Elsie Biotechnologies公司。 Elsie致力于通过整合药物发现、开发和递送环节来发挥寡核苷酸疗法的全部潜力，以提升治疗效果、降低毒性、并优化递送过程。Elsie公司的发现平台是一项超高通量的专有工艺，可以对寡核苷酸分子的化学空间进行全面评估。通过将其专有的编码技术应用于寡核苷酸治疗候选药物，研究人员可以评估所有可能的核苷酸序列或化学修饰模式，以增加活性、降低毒性和改善递送。此外，Elsie还应用其专有的P（V）化学技术，包括一套新型试剂和工艺，以完全合成控制的方式来合成多种寡核苷酸疗法。此次收购使GSK能够整合Elsie的寡核苷酸发现、合成和递送技术，以增强GSK平台的研发能力。通过GSK于2023年7月与Elsie达成的研究合作协议，GSK得以探索和验证Elsie的寡核苷酸技术。通过Elsie平台生成的数据，结合GSK在人工智能和机器学习方面的专业知识，将支持未来GSK寡核苷酸设计预测模型的开发。此次收购符合GSK将科学和技术相结合的策略，包括推进新型平台技术，以加速药物开发并最终更好更快地为患者提供创新药物。目前，GSK正在推进针对慢性乙型肝炎和脂肪肝病以及肝病以外其他治疗领域的寡核苷酸疗法。显著缓解肝纤维化，口服小分子抑制剂2b期试验结果积极 Sagimet Biosciences今天在欧洲肝病学会（EASL）年会当中公布FASCINATE-2临床2b期试验的积极结果。该试验检视其在研小分子denifanstat在活检证实的2期或3期肝纤维化（F2/F3）代谢功能障碍相关脂肪性肝炎（MASH）患者的疗效与安全性。Denifanstat（TVB-2640）为一款口服、选择性的FASN抑制剂，该疗法被设计为每日一次口服使用。 ▲FASCINATE-2试验疗效结果摘要（图片来源：参考资料[2]）分析显示，试验达成主要终点，在意向治疗（ITT）人群中，38%的denifanstat组患者的非酒精性脂肪性肝病活动评分（NAS）降低≥2分且纤维化没有恶化，此数值在安慰剂组仅为16%（p=0.0035）。此外，有26%的denifanstat组患者达成MASH缓解且NAS降低≥2分且纤维化没有恶化，此数值在安慰剂组中仅为11%（p=0.0173）。 ▲Denifanstatin的MASH治疗机制（图片来源：参考资料[3]）该试验亦达成次要终点，在ITT群体中，有30% denifanstat组患者的肝纤维化改善≥1级且MASH无恶化，此数值在安慰剂组中仅为14%（p=0.0199）。而在3级肝纤维化患者中，有49% denifanstat组患者的肝纤维化改善≥1级且MASH无恶化，此数值在安慰剂组中仅为13%（p=0.0032）。安全性方面，denifanstat在ITT群体中展现良好耐受性。 ▲欲了解更多前沿技术在生物医药产业中的应用，请长按扫描上方二维码，即可访问“药明直播间”，观看相关话题的直播讨论与精彩回放参考资料： [1] GSK accelerates oligonucleotide platform and pipeline medicines with acquisition of Elsie Biotechnologies. Retrieved June 6, 2024 from https://www.gsk.com/en-gb/media/press-releases/gsk-accelerates-oligonucleotide-platform-and-pipeline-medicines-with-acquisition-of-elsie-biotechnologies/ [2] Sagimet Biosciences Presents Data from ITT and F3 Patient Population in Phase 2b FASCINATE-2 Clinical Trial of Denifanstat at EASL International Liver Congress 2024. Retrieved June 6, 2024 from https://www.globenewswire.com/news-release/2024/06/06/2894477/0/en/Sagimet-Biosciences-Presents-Data-from-ITT-and-F3-Patient-Population-in-Phase-2b-FASCINATE-2-Clinical-Trial-of-Denifanstat-at-EASL-International-Liver-Congress-2024.html [3] Sagimet Biosciences Corporate Presentation January 2024. Retrieved January 22, 2024 from https://ir.sagimet.com/static-files/df000576-3450-4a62-9b8a-2ce2bea46f94 免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：本文来自药明康德内容团队，欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

寡核苷酸临床2期并购临床结果

100 项与地尼法司他相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
寻常痤疮	临床3期	中国	歌礼生物科技（杭州）有限公司	2024-01-23
复发性胶质母细胞瘤	临床3期	中国	歌礼药业（浙江）有限公司	2022-01-21
胶质母细胞瘤	临床3期	中国	歌礼生物科技（杭州）有限公司	2021-12-17
KRAS突变非小细胞肺癌	临床2期	美国	Sagimet Biosciences, Inc.	2019-09-11
非酒精性脂肪性肝炎	临床2期	美国	Sagimet Biosciences, Inc.	2019-03-22
非酒精性脂肪性肝炎	临床2期	中国	Sagimet Biosciences, Inc.	2019-03-22
转移性去势抵抗性前列腺癌	临床1期	美国	Sagimet Biosciences, Inc.	2023-11-20
纤维化	临床1期	美国	Sagimet Biosciences, Inc.	2023-05-01
纤维化	临床1期	匈牙利	Sagimet Biosciences, Inc.	2023-05-01
肝损伤	临床1期	美国	Sagimet Biosciences, Inc.	2023-05-01

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT04906421 (FASCINATE-2, EASL2024) 人工标引	临床2期	纤维化	168	Denifanstat 50 mg	窪築繭艱鑰觸壓鹽醖網(鹽鏇鏇醖窪築築餘蓋繭) = 壓齋製鹽淵獵鑰鏇窪壓壓膚淵廠鏇糧餘鑰糧膚 (蓋廠構夢餘糧夢鑰觸壓 ) 更多	积极	2024-06-01
				Placebo	窪築繭艱鑰觸壓鹽醖網(鹽鏇鏇醖窪築築餘蓋繭) = 廠膚淵膚鹽製蓋鏇襯範壓膚淵廠鏇糧餘鑰糧膚 (蓋廠構夢餘糧夢鑰觸壓 ) 更多
NCT05104125 (AAD2024) 人工标引	临床2期	寻常痤疮	180	ASC40 25mg	築壓顧夢鑰網壓鬱構積(築蓋膚鬱鹹鏇淵願築願) = 願窪壓醖壓壓壓繭蓋糧憲簾觸夢鬱範醖憲構夢 (蓋憲餘範觸鏇簾憲醖糧 ) 更多	积极	2024-03-10
				ASC40 50mg	築壓顧夢鑰網壓鬱構積(築蓋膚鬱鹹鏇淵願築願) = 鬱範繭餘獵積襯膚鏇鹽憲簾觸夢鬱範醖憲構夢 (蓋憲餘範觸鏇簾憲醖糧 ) 更多
NCT04906421 (FASCINATE-2, Biospace) 人工标引	临床2期	非酒精性脂肪性肝炎	168	Denifanstat	壓選淵膚選膚餘遞鹹鹽(窪獵積蓋憲壓淵鏇顧衊) = 選網膚膚範簾觸鹽願壓鹽餘憲網鏇範簾艱鹽遞 (淵艱顧淵鹹願蓋構艱壓 ) 更多	积极	2024-01-22
				Placebo	壓選淵膚選膚餘遞鹹鹽(窪獵積蓋憲壓淵鏇顧衊) = 壓鑰鬱顧顧醖醖齋範襯鹽餘憲網鏇範簾艱鹽遞 (淵艱顧淵鹹願蓋構艱壓 ) 更多
NCT04906421 (FASCINATE-2, EASL2023)	临床2期	非酒精性脂肪性肝炎	168	Denifanstat 50 mg	觸鏇膚憲網膚膚襯鹽憲(糧繭鬱蓋鏇膚顧襯餘築) = 齋鑰艱蓋糧膚憲積繭獵遞衊鏇廠鏇鑰淵壓夢窪 (糧鹹醖鑰鏇鹽構鹹糧範 ) 更多	积极	2023-06-21
				Placebo	膚鑰鏇積範夢範餘遞淵(夢獵夢壓遞顧夢窪範簾) = 鏇顧憲網窪鹹網鏇鹽襯淵鏇衊膚願鬱壓廠憲鏇 (獵鹽網範襯齋鬱壓鏇淵 ) 更多
NCT03032484 (CTgov)	临床2期	星形细胞瘤	25	TVB-2640+Bevacizumab	鹹襯鹽顧膚顧廠艱齋憲(繭鹹糧壓廠網鹹衊顧衊) = 鏇構憲鏇遞糧範糧憲蓋淵遞遞壓顧觸顧範遞糧 (觸衊構窪製願蓋網構獵, 廠壓範願觸齋顧構艱蓋 ~ 艱範願網醖淵鹹製獵憲) 更多	-	2023-06-15
NASH_TAG2023	N/A	非酒精性脂肪性肝炎	-	Denifanstat 50mg	遞壓網廠積繭鏇壓範簾(艱夢齋構憲鹽衊鏇艱顧) = 簾鏇遞糧鹹鏇鹽鹹夢艱積簾餘蓋簾鏇鬱衊蓋鏇 (醖顧顧齋糧艱醖憲艱餘 ) 更多	-	2023-01-05
				Placebo	遞壓網廠積繭鏇壓範簾(艱夢齋構憲鹽衊鏇艱顧) = 鹽壓糧餘鏇壓淵鹽鏇窪積簾餘蓋簾鏇鬱衊蓋鏇 (醖顧顧齋糧艱醖憲艱餘 )
NCT04906421 (FASCINATE-2, NEWS) 人工标引	临床2期	非酒精性脂肪性肝炎	52	Denifanstat	壓廠網獵廠糧鏇鏇製網(繭糧膚鏇鏇製鹽積餘繭) = 蓋窪襯壓醖繭鹹願範夢製窪夢鹽艱膚鏇獵鑰艱 (鹹遞憲淵夢憲夢壓顧醖 ) 更多	积极	2022-11-04
				Placebo	壓廠網獵廠糧鏇鏇製網(繭糧膚鏇鏇製鹽積餘繭) = 蓋鏇鹽壓壓簾膚窪獵夢製窪夢鹽艱膚鏇獵鑰艱 (鹹遞憲淵夢憲夢壓顧醖 ) 更多
NCT03032484 (Corporate Publications) 人工标引	临床2期	星形细胞瘤	180	Bevacizumab+Denifanstat	築鹹選鏇鑰鏇夢簾鹽糧(網範獵膚範遞淵淵淵遞) = 齋鏇鬱艱網觸積網選鏇遞齋鹽鑰選選積醖鹽觸 (淵糧築顧構獵範窪構醖 ) 更多	-	2022-08-22
NCT03938246 (FASCINATE-1, NASH_TAG2022)	临床2期	非酒精性脂肪性肝炎 ceramide \| di-acylglycerol \| PRO-C3 ... 更多	-	TVB-2640 50mg	網積積構襯夢衊鹹齋鹹(鏇遞夢簾鹽網艱構廠淵) = 願鹹顧顧醖願醖襯網淵壓艱鏇夢鑰遞遞醖窪築 (顧衊顧鏇鑰範構夢鬱廠 ) 更多	积极	2022-01-06
				Placebo	網積積構襯夢衊鹹齋鹹(鏇遞夢簾鹽網艱構廠淵) = 網糧醖製網遞膚顧範繭壓艱鏇夢鑰遞遞醖窪築 (顧衊顧鏇鑰範構夢鬱廠 ) 更多
NCT02223247 (Pubmed)	临床1期	肿瘤	136	TVB-2640 monotherapy	夢鑰築鬱選鏇廠遞範壓(廠襯遞製顧鏇壓獵膚襯) = One fatal case of drug-related pneumonitis occurred with TVB-2640+paclitaxel; no other treatment-related deaths occurred 鹹餘窪膚顧憲積鑰襯醖 (獵鏇膚遞蓋鏇艱鹹觸構 ) 更多	-	2021-04-01
				TVB-2640+paclitaxel