A Phase 1, Open-Label Window-of-Opportunity Study to Assess the Pharmacokinetics, Pharmacodynamics and Central Nervous System (CNS) Penetration of Xevinapant in Preoperative Subjects With Recurrent High-Grade Glioma (rHGG)

Researchers will investigate the ability of Xevinapant to cross the blood-brain barrier and exert anti-tumor effects on rHGG through activation of apoptosis. Researchers hypothesize that oral administration of Xevinapant has acceptable safety and tolerability in patients with recurrent HGG and demonstrate pharmacokinetic and pharmacodynamic effects in HGG tumors. To that end, Researchers will engage in a phase I "window of opportunity" translational clinical trial in patients undergoing a clinically-indicated craniotomy for resection of recurrent tumors to evaluate the impact of treatment on rHGG.

开始日期2024-07-22

申办/合作机构

H. Lee Moffitt Cancer Center & Research Institute, Inc.

[+1]

NCT06084845

/ Withdrawn临床2期IIT

Phase II Trial of Xevinapant and Chemoradiotherapy in Adjuvant Treatment for Patients With Head and Neck Squamous Cell Carcinoma With High Risk Pathologic Features

This phase II trial compares the effect of usual radiation therapy with cisplatin/carboplatin (chemoradiation) to the addition of xevinapant with chemoradiation in patients with head and neck cancer. Radiation therapy uses high energy x-rays, particles, or radioactive seeds to kill cancer cells and shrink tumors. Cisplatin is in a class of medications known as platinum-containing compounds. It works by killing, stopping or slowing the growth of cancer cells. Carboplatin is in a class of medications known as platinum-containing compounds. It works in a way similar to the anticancer drug cisplatin, but may be better tolerated than cisplatin. Carboplatin works by killing, stopping or slowing the growth of cancer cells. Xevinapant is a first-in-class antagonist of inhibitor of apoptosis (programmed cell death) proteins (IAPs), which leads to tumor cell death and enhances tumor cell sensitivity to chemotherapy and radiotherapy. Giving xevinapant with chemoradiation may be more effective in preventing head and neck cancer from growing or spreading than chemoradiation alone.

开始日期2024-04-12

申办/合作机构

ECOG-ACRIN Medical Research Foundation, Inc.

[+1]

NCT06110195

/ Active, not recruiting临床1期IIT

A Phase I Study of Xevinapant With Radiation and Concurrent Carboplatin and Paclitaxel in Patients Ineligible for Cisplatin With Locoregionally Advanced Squamous Cell Carcinoma of the Head and Neck

The goal of this clinical trial is to determine the best safe dose of xevinapant that can be given in combination with chemotherapy and radiation in patients with head and neck cancer. Up to 4 doses of xevinapant will be tested in the dose escalation portion of the study. After the best safe dose is found during escalation, an additional group of participants will be enrolled at that dose to learn more about the treatment combination (dose expansion).
The main question[s] it aims to answer are:
what is the maximum safe dose that can be given
what dose should be used in subsequent (phase 2) trials
Participants will receive xevinapant in combination with paclitaxel and carboplatin chemotherapy and radiation. Treatment will be given in 3-week cycles for 3 cycles.

开始日期2024-01-24

申办/合作机构

The University of Chicago

[+1]

100 项与 Xevinapant 相关的临床结果

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100 项与 Xevinapant 相关的转化医学

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100 项与 Xevinapant 相关的专利（医药）

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268

项与 Xevinapant 相关的文献（医药）

2024-11-22·JCI Insight

HIV-1 latency reversal agent boosting is not limited by opioid use

Article

作者: Corry, Heather ; Olson, Alex ; Lilie, Tyler J. ; Tsibris, Athe ; Taylor, Jessica ; Bouzy, Jennifer ; Lin, Nina ; Coxen, Kendyll ; Asundi, Archana ; Clayton, Kiera ; Lilie, Tyler ; Jordan, Hannah ; Roche, Samantha

Opioid use may affect the HIV-1 reservoir and its reversal from latency. We studied 47 virally suppressed people with HIV (PWH) and observed that lower concentration of HIV-1 latency reversal agents (LRAs), used with small molecules that did not reverse latency, synergistically increased the magnitude of HIV-1 reactivation ex vivo, regardless of opioid use. This LRA boosting, which combined a second mitochondria-derived activator of caspases mimetic or low-dose PKC agonist with histone deacetylase inhibitors, generated more unspliced HIV-1 transcription than PMA with ionomycin (PMAi), the maximal known HIV-1 reactivator. LRA boosting associated with greater histone acetylation, modulated surface activation-induced markers, and altered T cell production of TNF-α, IL-2, and IFN-γ. HIV-1 reservoirs in PWH contained unspliced and polyadenylated virus mRNA, the ratios of which were greater in resting than total CD4+ T cells and corrected to 1:1 with PMAi exposure. We characterized treated suppressed HIV-1 infection as a period of inefficient, not absent, virus transcription. Multiply spliced HIV-1 transcripts and virion production did not consistently increase with LRA boosting, suggesting the presence of a persistent posttranscriptional block. LRA boosting can be leveraged to probe mechanisms of an effective cellular HIV-1 latency reversal program.

2024-10-02·INTERNATIONAL JOURNAL OF RADIATION BIOLOGY

Study on the sensitizing effect of SM-1 combined with irradiation on head and neck squamous cell carcinoma

Article

作者: Xiao, Yan-Tao ; Wang, Dan-Dan ; Hou, Wen-Bin ; Liu, Gai-Ting ; Li, Yi-Liang ; Hu, Tong ; Gou, Wen-Feng ; Zuo, Dai-Ying

PURPOSE:

Head and neck squamous cell carcinoma (HNSCC) is globally prevalent with high recurrence, low survival rate, and poor quality of life for patients. Derived from PAC-1, SM-1 can activate procaspase-3 and induce apoptosis in cancer cells to exert anti-tumor effects. However, the inhibitory effect of SM-1 on HNSCC after combination with radiation are unclear. This study aims to investigate the radiosensitizing effect of SM-1 on HNSCC in vitro and in vivo.

METHODS:

MTT method was used to detect the effect of SM-1 on the viability of HNSCC cell lines (HONE1, HSC-2, and CAL27). The effects of SM-1 combined with radiation on the survival index of HONE1, HSC-2, and CAL27 cell lines were determined by colony formation assay. Flow cytometry was used to investigate the effects of SM-1 and radiation combination on cell apoptosis and cell cycle, and western blot experiments were performed to detect the expression of apoptosis and cell cycle-related proteins. Finally, a xenograft tumor model of CAL27 was established to evaluate the anti-tumor effect of SM-1 combined with radiation in vivo.

RESULTS:

In vitro, SM-1 effectively inhibited the activity of HNSCC cell lines HONE1, HSC-2, and CAL27 cells, and synergistically showed anti-proliferation activity during combined irradiation. Meanwhile, anti-tumor effect of SM-1 on HNSCC was higher than that of Debio1143, and the radiosensitivity of cells was greatly increased. Flow cytometry and western blot analysis showed that SM-1 induced G2/M phase arrest of head and neck squamous cell carcinoma cells via inhibiting the expression of CyclinB1 and CDC2. Moreover, SM-1 activated caspase-3 activity and up-regulated the cleaved form of PARP1 to induce cell apoptosis. In vivo, SM-1 combined irradiation showed a good anti-tumor effect.

CONCLUSION:

SM-1 enhances HNSCC cell radiation sensitivity in vitro and in vivo, supporting its potential as a radiosensitizer for clinical trials in combination with radiotherapy.

2024-06-10·ONCOGENE

Correction: Therapeutic targeting of necroptosis by Smac mimetic bypasses apoptosis resistance in acute myeloid leukemia cells

作者: Safferthal, C ; Rohde, K ; Fulda, S

109

项与 Xevinapant 相关的新闻（医药）

2025-03-10

·药时代

2024年全球十大药物临床试验失败案例

在2024年，全球制药行业经历了诸多挫折，许多备受期待的药物在临床试验中“夭折”。这些失败不仅给药企带来了巨大的经济损失，也凸显了药物研发的复杂性和不确定性。下面，让我们一起来看看去年一整年较为突出的十起失败案例：（1）Emraclidine 适应症：精神分裂症研发公司：艾伯维形式/靶点：M4选择性正向变构调节剂艾伯维（AbbVie）在2023年12月宣布以87亿美元收购Cerevel Therapeutics，看中的正是其精神分裂症药物Emraclidine。Emraclidine是一种M4选择性正向变构调节剂，艾伯维希望通过这一收购复制其他成功药物的路径。然而，事情并未如预期发展。在2024年，艾伯维报告了Emraclidine在两项II期临床试验中的失败，表明该药物未能达到预期的疗效。这一结果不仅让艾伯维的收购计划蒙上阴影，还导致公司在2025年初计入了35亿美元的减值支出。尽管如此，艾伯维并未完全放弃Emraclidine，其首席科学官Roopal Thakkar在J.P. Morgan医疗保健会议上表示，公司计划将该药物作为现有疗法的辅助药物进行测试，并考虑未来重新尝试单一疗法。（2）Losmapimod（洛批莫德）适应症：面肩胛肱型肌营养不良症研发公司：Fulcrum Therapeutics/赛诺菲形式/靶点：p38α/β丝裂原活化蛋白激酶抑制剂 Losmapimod是一种p38α/β丝裂原活化蛋白激酶（MAPK）抑制剂，由Fulcrum Therapeutics开发，用于治疗面肩肱型肌营养不良症（Facioscapulohumeral Muscular Dystrophy，FSHD）。这种罕见病是一种遗传性肌肉疾病，主要影响面部、肩部和上肢的肌肉，导致患者逐渐失去肌肉力量和功能。 2024年，赛诺菲（Sanofi）与Fulcrum Therapeutics达成合作，赛诺菲支付了8000万美元，获得了Losmapimod在美国以外地区的开发和商业化权利。这一合作基于对Losmapimod在早期临床试验中显示出的潜力的期待，尤其是在抑制炎症和改善肌肉功能方面的潜在效果。然而，Losmapimod的研发之路并非一帆风顺。早在2021年，该药物在2b期临床试验中就未能达到主要终点，显示出对患者生物标志物的显著影响不足。尽管如此，Fulcrum仍然对Losmapimod的潜力保持信心，并决定推进其进入III期临床试验，希望通过更广泛的患者群体验证其疗效。 2024年，Losmapimod的III期临床试验结果令人失望。试验结果显示，该药物未能显著改善患者的肌肉功能或减缓疾病进展。这一失败不仅让赛诺菲的8000万美元投资面临风险，也使Fulcrum不得不重新评估其研发战略。 Losmapimod的失败对Fulcrum Therapeutics产生了深远影响。公司不得不裁员40%，并将研发重点转向其他项目。这一事件也凸显了罕见病治疗领域的高风险性，尤其是在临床试验阶段，药物的疗效和安全性仍存在诸多不确定性。（3）Dalzanemdor 适应症：阿尔兹海默病、亨廷顿氏症和帕金森疾病研发公司：Sage Therapeutics 形式/靶点：NMDA受体正向变构调节剂 2024年，Sage Therapeutics在神经退行性疾病治疗领域遭遇了重大挫折，其核心药物Dalzanemdor在针对帕金森病、阿尔茨海默病和亨廷顿病的II期临床试验中连续三次失败。这一系列失败不仅对Sage的股价造成了沉重打击，也严重动摇了市场对其研发能力的信心。首先，4月公布的帕金森病II期PRECEDENT研究结果显示，Dalzanemdor未能在轻度认知障碍患者中显示出与安慰剂相比的统计学显著差异。随后，10月公布的阿尔茨海默病II期LIGHTWAVE研究也未能达到主要终点，药物在改善患者智力方面未显示出显著效果。11月，亨廷顿病的II期DIMENSION试验再次失败，进一步证实了Dalzanemdor在神经退行性疾病治疗中的局限性。这些连续的失败反映出神经退行性疾病治疗领域的复杂性和高风险性。尽管Sage在药物设计上采用了NMDA受体正向变构调节剂这一创新靶点，但临床试验结果表明，该药物在改善患者认知功能和延缓疾病进展方面未能达到预期效果。此外，这些失败也凸显了在神经退行性疾病领域，药物研发需要更精准的患者选择和更严格的临床试验设计。尽管Sage在Dalzanemdor项目上遭遇了挫折，但公司仍在努力推进其他研发管线，例如产后抑郁症药物Zurzuvae，这表明Sage并未完全放弃在神经科学领域的布局。然而，未来Sage能否在其他项目上取得突破，仍充满不确定性。（4）Ocedurenone 适应症：慢性肾病研发公司：诺和诺德形式/靶点：新型非甾体类盐皮质激素受体拮抗剂 2024年，诺和诺德（Novo Nordisk）在慢性肾病（CKD）治疗领域的希望因Ocedurenone的III期临床试验失败而破灭。这款新型非甾体类盐皮质激素受体拮抗剂曾被寄予厚望，诺和诺德在2023年10月以13亿美元的高价从KBP Biosciences引进该药物，旨在挑战拜耳的同类药物Kerendia。然而，Ocedurenone在2024年6月公布的III期CLARION-CKD试验中未能达到主要终点——降低慢性肾病患者的蛋白尿和稳定肾功能。这一失败对诺和诺德造成了重大打击。公司在2024年上半年财报中披露，因Ocedurenone项目失败导致了57亿丹麦克朗（约合8.02亿美元）的减值损失。此外，诺和诺德还因认为KBP在合作中隐瞒了关键信息，包括II期临床试验中期分析显示药物无效的结果以及合规性问题，而对其提起诉讼。尽管如此，诺和诺德并未放弃其他适应症的探索，但最终在2024年11月彻底放弃了Ocedurenone项目。 Ocedurenone的失败也凸显了创新药研发领域的高风险性，尤其是在临床试验阶段。尽管诺和诺德对Ocedurenone的潜力充满信心，认为其具有显著的疗效和安全性优势，但最终未能在关键的III期试验中证明其价值。（5）GSK3943104 适应症：单纯疱疹病毒感染研发公司：GSK 形式/靶点：重组蛋白疫苗 2024年，葛兰素史克（GSK）在生殖器疱疹疫苗的研发上再次遭遇挫折。其候选疫苗GSK3943104在II期临床试验中未能减少复发性生殖器疱疹的发作次数，导致GSK放弃了这一关键研究计划。单纯疱疹病毒（HSV）感染是一个全球性重大医疗需求，全球约有5亿人受到这种终身无法治愈的感染影响。尽管GSK在2010年曾放弃过一款预防女性生殖器疱疹的疫苗研发，但公司对HSV感染的研究兴趣并未减退。此次失败后，GSK表示将继续跟踪参与者，以获取复发性生殖器疱疹的数据，并为未来HSV相关研究提供参考。这一挫折也使得HSV疫苗研发领域的公司数量减少，BioNTech和Moderna的早期疫苗项目可能成为此次挫折的潜在受益者。（6）Vibostolimab (维博利单抗) 适应症：高风险切除黑色素瘤研发公司：默沙东形式/靶点：抗TIGIT抗体默沙东（Merck & Co.）的抗TIGIT抗体药物Vibostolimab在2024年的临床试验中遭遇了重大挫折。该药物原本被设计用于高风险黑色素瘤术后的辅助治疗，但在III期试验中因“免疫介导的不良事件”导致停药率过高，最终不得不提前终止试验。此外，Vibostolimab联合派姆单抗（pembrolizumab）用于肺癌治疗的III期研究也因不良事件发生率高于预期且未能提高患者生存率而受阻。尽管罗氏（Roche）的同类药物tiragolumab在食管癌试验中取得了一定进展，但在肺癌试验中也遭遇了连续失败。这些连续的失败不仅凸显了TIGIT靶点在免疫肿瘤学领域的开发难度，也反映了免疫检查点抑制剂在不同癌症类型中的疗效可能存在显著差异。公司最终决定停止进一步的研究与开发。（7）Simufilam 适应症：轻度至中度阿尔兹海默病研发公司：Cassava Sciences 形式/靶点：细丝蛋白A（Filamin A protein） Cassava Sciences开发的Simufilam曾被视为阿尔茨海默病治疗的希望，但其III期临床试验未能达到主要终点，导致公司股价暴跌85%。不仅如此，该公司还因2b期数据误导性陈述面临美国证券交易委员会的调查。在III期试验中，Simufilam未能显著改善患者的认知功能，这一结果让市场对其前景失去信心。尽管Simufilam的失败早有预兆，但其股价的暴跌和随后的裁员仍凸显了阿尔茨海默病治疗领域的高风险性。Cassava Sciences不得不重新审视其研发策略，以应对这一挑战。（8）Fordadistrogene movaparvovec（莫哌达基）适应症：杜氏肌营养不良症（DMD）研发公司：默克形式/靶点：基因疗法辉瑞的基因疗法Fordadistrogene Movaparvovec用于治疗杜氏肌营养不良症（DMD），但在III期临床试验中未能改善患者的运动功能。该药物在研发过程中一直存在安全性问题，导致试验进度受阻。最终，辉瑞在2024年6月宣布放弃该项目，导致公司财务损失2.3亿美元，并在北卡罗来纳州的制造业务中裁员150人。这一失败凸显了基因治疗在罕见病领域的挑战，尤其是在确保疗效和安全性方面的双重压力。（9）Xevinapant 适应症：头颈部鳞状细胞癌研发公司：默克形式/靶点：细胞凋亡蛋白抑制剂默克集团（Merck KGaA）的细胞凋亡蛋白抑制剂Xevinapant在III期临床试验中未能延长头颈部鳞状细胞癌患者的无事件生存期。尽管公司高管曾对Xevinapant的成功充满信心，但最终试验结果未能达到预期目标。这一失败不仅抵消了默克每1.5年推出一款新药的目标，也凸显了肿瘤学领域的研发风险。尽管如此，默克在其他肿瘤学项目中仍取得了一些进展，例如CSF-1R抑制剂匹米替尼（pimicotinib）在罕见癌症中的成功。（10）Suzetrigine 适应症：疼痛性腰骶神经根病研发公司：Vertex Pharmaceuticals 形式/靶点：NaV1.8疼痛信号抑制剂 Vertex Pharmaceuticals的NaV1.8疼痛信号抑制剂Suzetrigine在2024年经历了一段跌宕起伏的旅程。尽管Suzetrigine的II期临床试验并未达到预期效果，导致Vertex公司股价下跌，但该药物最终在2025年1月获得FDA批准，用于治疗中度至重度急性疼痛。这一批准标志着几十年来人类在疼痛缓解方面取得的第一项重大研究进展。 Suzetrigine的II期临床试验主要针对的是腰骶神经根病（lumbosacral radiculopathy），一种疼痛性的脊柱疾病。临床试验结果显示，与基线相比，患者的疼痛指数平均下降了2.02点，达到了临床试验的主要目标。然而，安慰剂组中的100名参与者的疼痛指数也下降了1.98点，这一结果引发了投资者的恐慌，导致Vertex的股价在数据公布后不久下跌了15%。不过，自从去年12月中旬达到低点以来，受到FDA批准的Journavx上市的推动，公司股价已经上涨了20%以上。 Vertex随后进行了事件分析来了解临床试验中发生了什么，并揭示了不同研究低点中安慰机组参与者的可变性。据公司介绍，在大约40%的安慰剂组参与者反应较低的地点，两个试验组的结果之间存在着“更大的分离”。尽管这些试验并未表明Suzetrigine比广泛使用的止痛药维柯丁（Vicodin）更有效，但该公司对这种药物的信心最终在2025年1月得到了回报。FDA批准该药物用于治疗中度至重度急性疼痛，这一成功为疼痛管理领域带来了新的希望。参考资料： 2024's top 10 clinical trial flops 本文仅用于学术分享，转载请注明出处。若有侵权，请联系微信：bioonSir 删除或修改！封面图来源：123rf Newco的三个宿命，以及LIDNewco的诞生 2025-03-09 “做药的” 跟 “做机器人的” 合资开了家新公司...... 2025-03-08 特朗普时代，NewCo模式危矣！ 2025-03-07 版权声明/免责声明本文为授权转载文章。本文仅作信息交流之目的，不提供任何商用、医用、投资用建议。文中图片、视频、字体、音乐等素材或为药时代购买的授权正版作品，或来自微信公共图片库，或取自公司官网/网络，部分素材根据CC0协议使用，版权归拥有者，药时代尽力注明来源。如有任何问题，请与我们联系。衷心感谢! 药时代官方网站:www.drugtimes.cn 联系方式: 电话:13651980212 微信:27674131 邮箱:contact@drugtimes.cn 点击，查看更多精彩！

临床2期并购临床3期临床结果临床失败

2025-03-06

·FierceBiotech

Merck KGaA fails midphase lupus trial, says totality of data support further development

The importance of enpatoran to Merck has increased as other prospects have flamed out. \n One of Merck KGaA’s leading immunology assets has flunked a phase 2 lupus trial. Despite the primary endpoint miss, Merck has concluded further development is warranted in light of responses seen in subgroups and a recent win in another form of the disease.Merck tested its oral TLR7/8 inhibitor enpatoran in two forms of lupus. The company reported positive phase 2 data from the cohort of cutaneous lupus erythematosus (CLE) patients late last year. Thursday, Merck revealed the systemic lupus erythematosus (SLE) cohort was less successful. The SLE arm missed its primary endpoint, which assessed responses on a composite scale after 24 weeks of daily dosing.The German drugmaker said it saw “promising responses” in predefined subgroups of patients. Considering the subgroup responses, CLE results and safety profile, Merck judged that the totality of data supports further development.Merck is yet to share the data underpinning its conclusion, with updates to date limited to qualitative assessments of the results. Peter Guenter, CEO of healthcare at Merck, disclosed the CLE success at the company’s Capital Markets Day in October, telling analysts the trial found “very strong and unambiguous proof of concept in cutaneous lupus.” Enpatoran, which Merck is also studying in idiopathic inflammatory myopathies, is one of the two most advanced assets in the company’s neurology and immunology pipeline. Cladribine, the other advanced candidate, is in phase 3 development as a treatment for generalized myasthenia gravis.The importance of enpatoran and cladribine to Merck has increased as other prospects have flamed out. Four years ago, Merck named enpatoran, evobrutinib and xevinapant as three important clinical programs that it expected to help fuel its “next wave of growth.” Evobrutinib failed a phase 3 trial in late 2023 and was quickly axed, while Merck dropped xevinapant in June 2024 after an interim phase 3 analysis.

临床3期临床2期临床结果

2025-03-06

·Firstwordpharma

Merck KGaA keeps schtum on ongoing SpringWorks talks

Merck KGaA on Thursday reported its annual results for 2024, although investors eager for an update on a potential deal with SpringWorks Therapeutics were left frustrated. The German drugmaker simply reaffirmed that it is in advanced discussions about a possible acquisition of SpringWorks, although there is no certainty that an agreement will be signed. Rumours of a transaction between the parties first surfaced on February 10, with Merck confirming later the same day that talks were ongoing. A purchase of SpringWorks would give Merck the oral gamma secretase inhibitor Ogsiveo (nirogacestat), which is approved for desmoid tumours, as well as the MEK inhibitor mirdametinib, currently under review by the FDA for neurofibromatosis type 1-associated plexiform neurofibromas.The acquisition of SpringWorks would revitalise Merck's pipeline, following a number of recent setbacks, including the failure of a pair of Phase III studies for its lead oncology candidate xevinapant. While the company's healthcare segment posted 5% growth last year to €8.5 billion ($9.2 billion), driven by oncology — which was up 10.5% to €2 billion — it is heavily reliant on its 20-year-old drug Erbitux.Erbitux biosimilars on the horizonThe anti-EGFR monoclonal antibody generated sales in 2024 of €1.2 billion, up 13.3% over the prior year. Merck noted that growth for Erbitux was led by Latin America, particularly Mexico, as well as Europe and China, tempered by negative pricing effects in Japan.Asked on an analyst call about the growth potential of Erbitux, particularly in China, Peter Guenter — CEO of Merck's healthcare unit — noted that sales of the product are forecast to increase this year, with biosimilars not expected to launch before 2026. Guenter indicated that China, which accounts for about 25% of Erbitux revenue, is "an important growth driver, but actually the brand is very dynamic across the world."While Erbitux faces competition in China from Simcere Pharmaceutical's Enlituo, Guenter clarified that the product — approved last June — is not classified as a biosimilar, but rather a non-comparable biologic. "And that has, of course, relatively important implications in terms of, you know, lack of substitution," Guenter explained, as well as inclusion on the reimbursement drug list and volume-based procurement programme.Merck's other key drug, the multiple sclerosis (MS) therapy Mavenclad, achieved blockbuster status in 2024 for the first time, posting an 11.1% increase in revenue to €1.1 billion. Meanwhile, its older MS treatment Rebif declined 11.6% to €626 million in line with the wider interferon market.For the current year, the firm expects sales in its healthcare unit to be between €8.3 billion and €8.9 billion, representing organic growth of up to 5%.Pipeline questions continueMerck also disclosed Thursday that the oral TLR7/8 inhibitor enpatoran failed to meet the primary endpoint of the systemic lupus erythematosus cohort of the mid-stage WILLOW study. Despite what Guenter called "a near miss" in the trial, the company plans further development of the drug, given "promising responses" in patient subgroups and the totality of data, including positive results from the cutaneous lupus erythematosus arm of WILLOW.Guenter explained "the good news is that we see clear responses in predefined subpopulations. So we can really say that the drug clearly hits the target." These subgroups include patients with skin manifestations within the lupus cluster, those with a strong interferon gene signature and also those with high steroid use at baseline.Meanwhile, chief financial officer Helene von Roeder noted that Inspirna "informed [us] about negative top-line data" from an ongoing Phase II trial of ompenaclid in RAS-mutated advanced or metastatic colorectal cancer. The SLC6A8 inhibitor — also known as RGX-202 — was the focus of a licensing agreement between the parties last year. However, von Roeder indicated that the mid-stage failure means "we will not exercise the US option" on the drug, but will instead record an impairment charge of around €15 million in the current quarter.

上市批准临床2期并购引进/卖出临床3期

100 项与 Xevinapant 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
头颈部鳞状细胞癌	临床3期	中国	默克雪兰诺（北京）医药研发有限公司	2022-10-06
头颈部鳞状细胞癌	临床3期	中国台湾	默克雪兰诺（北京）医药研发有限公司	2022-10-06
头颈部肿瘤	临床3期	美国	Debiopharm International SA	2022-01-30
局部晚期头颈部鳞状细胞癌	临床3期	美国	Merck KGaA	2020-08-07
局部晚期头颈部鳞状细胞癌	临床3期	中国	Merck KGaA	2020-08-07
局部晚期头颈部鳞状细胞癌	临床3期	日本	Merck KGaA	2020-08-07
局部晚期头颈部鳞状细胞癌	临床3期	阿根廷	Merck KGaA	2020-08-07
局部晚期头颈部鳞状细胞癌	临床3期	澳大利亚	Merck KGaA	2020-08-07
局部晚期头颈部鳞状细胞癌	临床3期	奥地利	Merck KGaA	2020-08-07
局部晚期头颈部鳞状细胞癌	临床3期	比利时	Merck KGaA	2020-08-07

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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


NCT04459715 (TrilynX, BusinessWire) 人工标引	临床3期	局部晚期头颈部鳞状细胞癌	-	xevinapant + CRT	淵壓壓餘鬱窪觸鏇鬱齋(積製蓋願鑰願積願糧廠) = the trial would be unlikely to meet its primary objective of prolonging event-free survival. 襯鹹膚構夢蓋醖衊餘夢 (憲範淵壓壓鏇廠網糧淵 ) 未达到	不佳	2024-06-24
NCT02022098 (ASCO2024) 人工标引	临床2期	头颈部鳞状细胞癌	96	Xevinapant + CRT	構繭窪繭願齋構選鑰壓(網範構積糧顧衊淵構鏇) = 夢餘築衊齋夢淵蓋齋網積襯鏇齋齋觸衊壓簾餘 (艱範鹽鏇齋憲網繭顧鑰 ) 更多	积极	2024-05-24
				Placebo + CRT	構繭窪繭願齋構選鑰壓(網範構積糧顧衊淵構鏇) = 製憲膚觸鹽簾願夢窪願積襯鏇齋齋觸衊壓簾餘 (艱範鹽鏇齋憲網繭顧鑰 ) 更多
NCT04122625 (SMARTPLUS-106, CTgov)	临床1/2期	女性生殖器官肿瘤 \| 原发性腹膜癌 \| 实体瘤 ... 更多	46	nivolumab+Debio 1143 (Part A - Debio 1143 150 mg + Nivolumab)	構糧膚築繭廠獵範築糧 = 鑰窪齋構壓願糧餘餘齋蓋艱衊淵糧糧襯壓顧觸 (夢網襯襯壓鬱衊淵選膚, 鑰製構夢鏇鏇遞鑰衊範 ~ 憲範簾膚鏇獵獵網齋憲) 更多	-	2023-06-12
				nivolumab+Debio 1143 (Part A - Debio 1143 200 mg + Nivolumab)	構糧膚築繭廠獵範築糧 = 顧繭鏇襯艱網壓鏇簾蓋蓋艱衊淵糧糧襯壓顧觸 (夢網襯襯壓鬱衊淵選膚, 範鹹襯衊鹹築鬱顧餘構 ~ 鑰憲衊築壓夢鏇鏇艱醖) 更多
AACR2023 人工标引	临床1期	非小细胞肺癌	38	xevinapant 200 mg/day+avelumab 10 mg/kg	積膚簾鹹艱窪簾顧夢鏇(製衊蓋製窪艱衊繭遞繭) = 構膚鑰鏇鹽艱餘餘簾鑰醖繭製夢夢衊淵獵衊積 (願顧鏇蓋鏇餘網淵窪壓, 2.9 ~ 24.8) 更多	不佳	2023-04-14
NCT02022098 (Pubmed)	临床2期	局部晚期头颈部鳞状细胞癌	96	Xevinapant 200 mg/day	膚鬱構獵構齋鏇蓋網鹽(顧衊簾觸獵糧膚壓鏇艱) = 糧襯膚鬱範壓淵鬱糧艱鬱淵夢餘觸網鹹糧繭糧 (構襯遞積鏇製淵蓋遞膚, 40.3 ~ not evaluable)	积极	2023-04-01
				Placebo	膚鬱構獵構齋鏇蓋網鹽(顧衊簾觸獵糧膚壓鏇艱) = 餘鹽鹹鏇衊構鏇膚壓餘鬱淵夢餘觸網鹹糧繭糧 (構襯遞積鏇製淵蓋遞膚, 21.8 ~ 46.7)
NCT02022098 (ESMO2022) 人工标引	临床2期	局部晚期头颈部鳞状细胞癌 HPV Positive	96	Xevinapant 200 mg+CRT	鬱糧廠構選窪鬱網窪餘(網蓋製積齋製積鹹範積) = 衊衊憲簾製淵願壓鏇繭艱顧簾夢鏇獵範鏇窪鏇 (選憲鬱淵製鏇淵網網鏇, 37 ~ 66) 更多	积极	2022-09-10
				Placebo + CRT	鬱糧廠構選窪鬱網窪餘(網蓋製積齋製積鹹範積) = 淵積製顧顧衊獵構顧膚艱顧簾夢鏇獵範鏇窪鏇 (選憲鬱淵製鏇淵網網鏇, 15 ~ 42) 更多
NCT03871959 (CATRIPCA, ESMO2022) 人工标引	临床1期	结直肠癌 \| 转移性胰腺导管腺癌 MSI-Low	41	Pembrolizumab+Xevinapant (Dose escalation cohort)	鹹範鹽顧顧網壓窪鑰構(夢窪構醖醖顧鏇遞壓觸) = Xevinapant 200mg/d + pembrolizumab 200mg q3w 獵鹽鑰鑰繭夢醖網膚齋 (蓋願夢製艱齋獵夢鏇憲 ) 更多	不佳	2022-09-10
				Pembrolizumab+Xevinapant (PDAC expansion cohort)
NCT02022098 (ESMO2020) 人工标引	临床2期	头颈部鳞状细胞癌	96	Cisplatin+CRT+xevinapant	願窪鏇鬱餘廠選願夢膚(願餘簾鏇鹽醖糧築構鹹) = 顧壓網獵夢遞願鑰夢築壓製鹹選鏇鹹蓋廠蓋醖 (構遞網簾簾顧廠憲膚範 ) 更多	积极	2020-09-19
				Cisplatin+CRT+placebo	願窪鏇鬱餘廠選願夢膚(願餘簾鏇鹽醖糧築構鹹) = 窪顧艱繭觸醖艱糧夢餘壓製鹹選鏇鹹蓋廠蓋醖 (構遞網簾簾顧廠憲膚範, 21.8 ~ 46.7) 更多
NCT04122625 (ESMO2020) 人工标引	临床1期	HR阳性/HER2低表达实体瘤	11	Debio 1143+nivolumab (phase Ib)	膚鑰餘鑰願淵遞蓋夢蓋(糧襯鏇鏇築繭憲衊鹹鹹) = Debio 1143 at 200 mg/d + nivolumab 240 mg q2w 淵願淵夢網願網繭簾廠 (淵顧壓鏇餘鹽夢遞積鏇 ) 更多	积极	2020-09-17
NCT02022098 (Pubmed) 人工标引	临床2期	头颈部鳞状细胞癌	48	Debio 1143	鏇積鬱築選齋窪糧衊鹹(願壓鬱鑰壓範選艱網糧) = 窪觸構築築觸餘願繭鏇獵壓觸繭鑰廠衊襯憲夢 (鬱獵夢膚繭鑰憲鹹醖鹽, 39 ~ 69) 更多	积极	2020-09-01
				Placebo	鏇積鬱築選齋窪糧衊鹹(願壓鬱鑰壓範選艱網糧) = 鬱選範顧膚鑰鏇夢鑰獵獵壓觸繭鑰廠衊襯憲夢 (鬱獵夢膚繭鑰憲鹹醖鹽, 20 ~ 48) 更多