Open-label Phase 1b Study of Ulixertinib and Cetuximab or Ulixertinib in Combination With Cetuximab and Encorafenib in Patients With Unresectable or Metastatic Colorectal Cancer Who Have Previously Received EGFR or BRAF-directed Therapy

To find the recommended dose of ulixertinib that can be given in combination with cetuximab and/or encorafenib to patients with unresectable/metastatic CRC and who have received EGFR or BRAF-directed therapy in the past.

开始日期2024-01-18

申办/合作机构

The University of Texas MD Anderson Cancer Center

[+2]

NCT05804227 / Recruiting早期临床1期IIT

Window-of-Opportunity Trial of Ulixertinib for MAPK-Activated Low-Grade Gliomas in Adults

To learn if the study drug, ulixertinib, can cross over the blood-brain barrier in patients with recurrent brain tumors

开始日期2023-04-20

申办/合作机构

The University of Texas MD Anderson Cancer Center

[+1]

100 项与优立替尼相关的临床结果

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100 项与优立替尼相关的转化医学

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100 项与优立替尼相关的专利（医药）

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项与优立替尼相关的文献（医药）

2023-09-01·Life sciences

Exosomal miR-21 determines lung-to-brain metastasis specificity through the DGKB/ERK axis within the tumor microenvironment

Article

作者: Chan, Mei-Lin ; Kuo, Kuang-Tai ; Pikatan, Narpati Wesa ; Tiong, Tung-Yu ; Yeh, Chi-Tai ; Yadav, Vijesh Kumar ; Wang, Chun-Hua ; Fong, Iat-Hang ; Huang, Wen-Chien

BACKGROUND:

Brain metastasis affects 20-40 % of lung cancer patients, severely diminishing their quality of life. This research focuses on miR-21, overexpressed in these patients and inversely associated with DGKB in the ERK/STAT3 pathway, suggesting a dysregulated pathway with therapeutic potential.

AIMS:

The objective was to investigate miR-21's role in lung cancer patients with brain metastases and whether targeting this pathway could improve treatment outcomes. We also examined the miR-21 content in tumor spheres-derived extracellular vesicles (EVs) and their influence on ERK/STAT3 signaling and metastasis.

MATERIALS AND METHODS:

Tumor spheres were created from metastatic lung cancer cells. We studied miR-21 levels in these spheres, their impact on macrophage polarization, and the transition of nonmetastatic lung cancer cells. Furthermore, we analyzed miR-21 content in EVs derived from these spheres and their effect on ERK/STAT3 signaling and metastasis potential.

KEY FINDINGS:

We found tumor spheres had high miR-21 levels, promoting macrophage polarization and, epithelial-mesenchymal transition. These spheres-derived EVs, enriched with miR-21, accelerated ERK/STAT3 signaling and metastasis. Silencing miR-21 and inhibiting ERK signaling with ulixertinib notably mitigated these effects. Moreover, ulixertinib reduced brain metastasis incidence and increased survival in a mouse model and led to reduced tumor sphere generation and miR-21 levels in EVs.

SIGNIFICANCE:

Our study highlights the exacerbation of lung-to-brain metastasis via miR-21-rich EV secretion. This underlines the therapeutic promise of targeting the miR-21/ERK/STAT3 pathway with ulixertinib for managing brain metastasis from lung cancer.

2023-08-01·Nature nanotechnology

Tailoring renal-clearable zwitterionic cyclodextrin for colorectal cancer-selective drug delivery

Article

作者: Kim, Dahan ; Lee, Jae-Young ; Nguyen, Duy-Thuc ; Yoo, So-Yeol ; Kim, Dae-Duk ; Lee, Sang Min ; Baek, Min-Jun

Although cyclodextrin-based renal-clearable nanocarriers have a high potential for clinical translation in targeted cancer therapy, their designs remain to be optimized for tumour retention. Here we report on the design of a tailored structure for renal-clearable zwitterionic cyclodextrin for colorectal cancer-selective drug delivery. Twenty cyclodextrin derivatives with different charged moieties and spacers are synthesized and screened for colloidal stability. The resulting five candidates are evaluated for biodistribution and an optimized structure is identified. The optimized cyclodextrin shows a high tumour accumulation and is used for delivery of doxorubicin and ulixertinib. Higher tumour accumulation and tumour penetration facilitates tumour elimination. The improved antitumour efficacy is demonstrated in heterotopic and orthotopic colorectal cancer models.

2023-07-15·Journal of translational medicine

Single-cell analysis of white adipose tissue reveals the tumor-promoting adipocyte subtypes.

Article

作者: Gao, Zhi-Jie ; Li, Bei ; Liu, Si-Qing ; Sun, Si ; Chen, Ding-Yuan ; Li, Wen-Ge ; Wu, Qi ; Yu, Xin ; Liu, Zhou ; Wang, Yuan ; Sun, Sheng-Rong ; Feng, Hong-Fang

BACKGROUND:

The tumor-adipose microenvironment (TAME) is characterized by the enrichment of adipocytes, and is considered a special ecosystem that supports cancer progression. However, the heterogeneity and diversity of adipocytes in TAME remains poorly understood.

METHODS:

We conducted a single-cell RNA sequencing analysis of adipocytes in mouse and human white adipose tissue (WAT). We analyzed several adipocyte subtypes to evaluate their relationship and potential as prognostic factors for overall survival (OS). The potential drugs are screened by using bioinformatics methods. The tumor-promoting effects of a typical adipocyte subtype in breast cancer are validated by performing in vitro functional assays and immunohistochemistry (IHC) in clinical samples.

RESULTS:

We profiled a comprehensive single-cell atlas of adipocyte in mouse and human WAT and described their characteristics, origins, development, functions and interactions with immune cells. Several cancer-associated adipocyte subtypes, namely DPP4⁺ adipocytes in visceral adipose and ADIPOQ⁺ adipocytes in subcutaneous adipose, are identified. We found that high levels of these subtypes are associated with unfavorable outcomes in four typical adipose-associated cancers. Some potential drugs including Trametinib, Selumetinib and Ulixertinib are discovered. Emphatically, knockdown of adiponectin receptor 1 (AdipoR1) and AdipoR2 impaired the proliferation and invasion of breast cancer cells. Patients with AdipoR2-high breast cancer display significantly shorter relapse-free survival (RFS) than those with AdipoR2-low breast cancer.

CONCLUSION:

Our results provide a novel understanding of TAME at the single-cell level. Based on our findings, several adipocyte subtypes have negative impact on prognosis. These cancer-associated adipocytes may serve as key prognostic predictor and potential targets for treatment in the future.

项与优立替尼相关的新闻（医药）

2023-03-23

·PRNewswire

Clarivate Announces Gordon Samson as President, Intellectual Property and Nominates Dr. Saurabh Saha as New Independent Director

Naming the first of three business leaders for its newly created market segments and nominating new Independent Director to its Board LONDON, March 23, 2023 /PRNewswire/ -- Clarivate Plc (NYSE: CLVT), a global leader in connecting people and organizations to intelligence they can trust, today announced that Gordon Samson, currently Chief Product Officer, has been appointed President of its Intellectual Property (IP) market segment, effective April 1. The Company also announced that it has nominated Dr. Saurabh Saha to stand for election as a director at its 2023 Annual General Meeting of shareholders on May 4, 2023. Jonathan Gear, Chief Executive Officer, Clarivate said: "I'm very pleased to announce the appointment of Gordon who has been a trusted and valued member of our Executive Leadership Team since he came to Clarivate from CPA Global as part of our acquisition in 2020. In this newly created role, he will be responsible for accelerating the growth of our IP segment empowering customers to establish, protect and manage their IP. Based on my experience working with him over the last eight months and the work we've done this year to align the organization, I'm confident that he will be instrumental to how we capitalize on product and service innovation to deliver organic growth. This is the first of our presidential appointments and we look forward to providing updates on further appointments in due course." Samson joined Clarivate in October 2020 with the acquisition of CPA Global, having joined CPA Global in 2014 as Chief Operating Officer. During the last three years with Clarivate, Samson has made significant contributions, helping transform the Company's APAC region and bringing together the Company's entire product portfolio to offer customers a full range of enriched data, insights, analytics and workflow solutions. He has a long and successful track record of driving organizational transformation and growth in the IP industry and beyond, having held senior executive roles with both operating and P&L accountability for more than 20 years. Andy Snyder, Chairman of the Board, Clarivate commented: "We look forward to Dr. Saha joining our Board. He will bring a great deal of experience in the pharmaceutical and biotech industries and his guidance will provide valuable insights and perspective, especially as we continue to execute on our growth strategy in the Life Sciences & Healthcare segment." Dr. Saha is a physician-scientist, pharmaceutical executive, and biotech entrepreneur dedicated to discovering and developing novel life-changing medicines. He is notable for leading the development and demonstrating human effectiveness of two innovative cancer drugs, an ERK kinase inhibitor (Ulixertinib) and an oncolytic immunotherapy (C. novyi-NT). He is currently CEO of Centessa Pharmaceuticals (NASDAQ: CNTA), a global pharma company. Prior to Centessa, Dr. Saha was a Senior Vice President of R&D and Global Head of Translational Medicine for all disease areas at Bristol Myers Squibb. Other past roles include Venture Partner at Atlas Venture, a VC firm in Cambridge MA, Chief Executive Officer at Delinia, Chief Medical Officer of Synlogic, a management consultant at McKinsey & Company, and head of the New Indications Discovery Unit at Novartis. He is an associate member and Global Clinical Scholar at Harvard Medical School, holds an MD and PhD in medicine and cancer genetics from The Johns Hopkins School of Medicine, an MSc in biophysics from the University of Oxford and a BSc in biochemistry from Caltech. About Clarivate Clarivate™ is a leading global information services provider. We connect people and organizations to intelligence they can trust to transform their perspective, their work and our world. Our subscription and technology-based solutions are coupled with deep domain expertise and cover the areas of Academia & Government, Life Sciences & Healthcare and Intellectual Property. For more information, please visit clarivate.com. Investor Relations Contact Mark Donohue, Head of Investor Relations, [email protected], +1 (215) 243 2202 Media Contact Amy Bourke-Waite, Senior Director, Corporate Communications, [email protected] SOURCE Clarivate Plc

高管变更

2022-11-02

·药渡Daily

德琪医药ATG-017获FDA批准I期临床，治疗晚期实体瘤！

2022年11月1日，德琪医药宣布，ERK1/2小分子抑制剂ATG-017的1期临床试验申请（IND）已获美国食品药品监督管理局（FDA）批准，用于治疗晚期实体瘤。随后，德琪医药将在美国启动1期ERASER研究的联合治疗部分，以评估ATG-017联合纳武利尤单抗用于治疗晚期实体瘤的安全性、药代动力学和初步疗效。来源：德琪医药官网该项由德琪医药与百时美施贵宝合作的旨在评估ATG-017联合纳武利尤单抗的临床合作是基于已有的临床前数据，其中部分数据已于2021年11月在第36届肿瘤免疫治疗学会（SITC）年会及会前环节中公布。数据显示，ERK1/2抑制剂（ATG-017）联合免疫检查点抑制剂（ICI，PD-L1单抗，阿特朱单抗）发挥了协同作用，在ICI耐药的小鼠体内模型中产生了更好的疗效，达到肿瘤由“冷”至“热”的转化。此外，据Clinicaltrails.gov网站信息显示，2020年3月12日德琪医药登记了一项临床研究（NCT04305249），这是一项开放、多中心I期研究（代号：ERASER），主要评估ATG-107单药治疗晚期实体瘤和恶性血液瘤患者的安全性、药代动力学和初步疗效。目前该单药治疗爬坡正在澳大利亚顺利开展，并将继续参与联合治疗部分的研究。除澳大利亚和美国外，德琪医药还计划在中国开展这项国际多中心研究。目前在药物临床试验登记与信息公示平台暂未检索到ATG-017的临床试验登记号。关于ERK1/2细胞外信号调节蛋白激酶1/2（ERK1/2）是一类丝氨酸/苏氨酸蛋白激酶，是MEK1/2唯一已知的底物，位于RAS-RAF-MEK-ERK（MAPK）通路的下游，其作用是作为RAS-MAPK信号转导级联通路的终端激酶。该级联通路调节细胞增殖等多种细胞进程。RAS-MAPK通路失调发于30%以上的癌症患者，最为常见的变化为多个肿瘤类型的RAS或BRAF基因突变。ERK抑制剂可同时靶向RAS和BRAF突变疾病。目前，已有多种靶向RAS、RAF和MEK的小分子抑制剂被批准用于癌症治疗，然后，长期治疗中产生的获得性耐药降低了这些药物的疗效。近年来，选择性抑制ERK1/2被认为是一种潜在的癌症治疗策略，它不仅可以有效阻断MAPK通路，还可以克服RAS、RAF和MEK上游突变引起的耐药性。ERK1/2的关键调控通路来源：Fu et al. J Med Chem. 2022, 65(20): 13561-13573关于ATG-017ATG-017（AZD0364，Tizaterkib）是一款作用于细胞外信号调节激酶1和2（ERK1/2）的可逆型、ATP竞争性的强效、选择性口服小分子抑制剂，是以阿斯利康已有的先导化合物7为基础，进行构效关系（SAR）优化后得到的激酶选择性更强、药代动力学性质更佳的ATG-107。ATG-107对ERK2的IC50值为0.6 nM，水溶性468 uM，在体外大鼠和人肝细胞中均较稳定，渗透性（Caco-2 Papp）为26.7*10-6 cm/s，是高渗化合物，大鼠和犬灌胃给药后的生物利用度分别为30%和100%，具有较好的药代动力学性质。据文献报道，基于临床前试验数据推测的人体清除率范围是0.5-6 ml/min/kg，预测人体首次给药剂量为20-110 mg，一天两次。根据此前研究报道，在多个体内异种移植瘤模型中，ATG-017展现了对ERK1/2依赖性信号生物标志物的剂量和时间依赖性调节，从而使得BRAF敏感型和KRAS突变敏感型异种移植瘤的肿瘤消退。此外，ATG-01与MEK1/2抑制剂selumetinib (AZD6244和ARRY142886)的联合给药可以更深入、更持久地抑制RAS/MAPK信号通路，这是单药治疗无法实现的。ATG-017和selumetinib联合给药也会在KRAS突变的异种移植瘤模型中出现显著的肿瘤消退。因此，ERK1/2抑制剂和MEK1/2抑制剂的联合给药是靶向KRAS突变肿瘤的一种可行的临床方法。体外研究中，ATG-017对MAPK信号通路的直接下游底物具有高细胞活性（如在BRAFV600E突变的A375细胞中，抑制phospho-p90RSK，IC50= 5.73 nM）。ATG-107浓度为1 uM时，在包含353种激酶的激酶库中对其中9种激酶（MEK1, COT, BRAF, MEK2, c-RAF, ERK7, CDK2, CDK5 and ARK5）的抑制作用大于50%。A: AZD0364（ATG-017）的结构式B: AZD0364（ATG-017）与ERK2的结合位点来源：Vikki Flemington. et al. Mol Cancer Ther. 2021, 20(2): 238-249.“RAS/MAPK通路是癌症发生的一个重要驱动因素。ATG-017靶向ERK1/2不仅能阻止肿瘤细胞的生长，还能与其他MAPK激酶抑制剂协同作用，更有效地阻断RAS-MAPK信号传导，同时克服患者对RAF及MEK抑制剂产生耐药。”德琪医药创始人、董事长兼首席执行官梅建明博士说，“我们认为ATG-017拥有强大的临床潜力和广阔的应用前景。不单是针对实体瘤与血液瘤的单药疗法，德琪团队也正深入挖掘ATG-017与公司其他在研产品的协同性，以期获得更好的抗癌效果。”权益合作ATG-017由阿斯利康公司发现及早期研究，德琪医药拥有开发、生产及商业化该产品的全球独家权益。2019年11月6日，德琪医药宣布与英国阿斯利康公司达成一项全球性的独家授权协议，推进创新药物ATG-017（AZD0364）在全球的临床开发，生产和商业化。阿斯利康公司在此次交易前已终止了全球范围内其他关于ATG-017的授权协议，包括与辅仁药业的授权协议。2021年12月13日，德琪医药宣布与百时美施贵宝公司达成了一项临床合作协议，将共同开展一项旨在评估ATG-017联合百时美施贵宝的PD-1检查点抑制剂欧狄沃®（纳武利尤单抗）用于治疗晚期实体瘤的安全性、药代动力学和初步疗效的开放性1/2期临床研究。根据该协议，德琪医药将负责该临床试验的开展，并提供资金支持。百时美施贵宝公司将提供联合疗法的剂量爬坡和剂量扩展研究中所需的欧狄沃®。竞争格局目前关于靶向ERK药物的研究尚处在早期临床阶段，全球范围内仅有BioMed Valley Discoveries公司的BVD-523、Merck公司的MK-8353与Genentech的GDC-0994披露临床数据。全球范围内到目前为止没尚无任何一款已获批上市的ERK1/2抑制剂。BVD-523BVD-523（Ulixertinib，VRT752271）是由BioMed Valley Discoveries公司研发的可逆型、ATP竞争性ERK1/2抑制剂，其对ERK1的Ki < 0. 3 nM，对ERK2的Ki = 0. 04 nM。2017年12月15日，Cancer Discov杂志公布了ERK1/2抑制剂BVD-523的I期临床试验（NCT01781429）数据。结果提示2期临床试验推荐剂量为600 mg BID给药，最常见治疗相关不良反应包括腹泻(48%)、疲劳(42%)、恶心(41%)和痤疮性皮炎(31%)。在部分患者中，BVD-523治疗确实获得了部分缓解或疾病稳定状态，且疗效似不受肿瘤类型的影响。BVD-523具有可接受的安全性和良好的药代动力学性质。MK-8353MK-8353是通过改善SCH772984的PK 而优化得到的（ERK1：IC50= 20 nM；ERK2：IC50 = 7 nM）。SCH772984是由Merck公司通过基于亲和力的质谱高通量平台筛选、鉴定并通过结构优化得到的ATP 竞争性的ERK1/2抑制剂。2018年2月22日，JCI Insight杂志公布了ERK1/2抑制剂MK-8353的I期临床试验（NCT01358331）数据。在所有剂量中MK-8353总体安全性和耐受性良好，并且未发生严重不良事件（SAE）。在400毫克和800毫克剂量组中观察到剂量限制性毒性。在可评价治疗缓解的15名晚期实体瘤患者中，3名患者具有部分缓解，他们全部患有BRAFV600突变型黑色素瘤。GDC-0994GDC-0994是由Genentech公司研发的口服的选择性ERK1/2抑制剂，其对ERK1和ERK2的IC50分别为6. 1和3. 1 nmol/L。2020年3月15日，CCR杂志公布了新型ERK1/2抑制剂GDC-0994的I期临床试验（NCT01875705）数据。47名跨癌种的难治性晚期实体瘤患者，接受了该药物治疗。20名患者在接受治疗前后，均进行PET-CT检测，从PET-CT上可以反应肿瘤的代谢活性，其中11名患者肿瘤代谢活性明显下降，其中就包括4名胰腺癌患者。而从普通CT上看，45名患者中有15人肿瘤控制稳定。最难能可贵的是：2名BRAF突变的难治性肠癌患者，接受该药物治疗后，肿瘤明显缩小，缩小幅度超过30%，给这种极端难治的晚期肠癌患者带来了新的希望。CC-90003CC-90003是不可逆的共价结合的选择性ERK1/2 抑制剂，主要用于治疗KRAS突变的肿瘤，2015年进入1期临床研究。但是由于在1期临床试验中，其最大耐受剂量（MTD）结果不令人满意，目前已经暂停了其临床试验（NCT02313012）。此外，据药渡数据的不完全统计，目前临床阶段上二十多款ERK1/2抑制剂药物正在推进中，进展最快的项目也仅处于2期阶段。国内进展最快的是海和医药的BPI-27336、和记黄埔的HMPL-295S1和捷思英达的JSI-1187，相关ERK1/2抑制剂所处临床阶段多为1期。德琪医药的ATG-017因拥有同类最佳的潜力，且该品种还与免疫检查点抑制剂和其它靶向 RAS/MAPK通路的抑制剂具有很高的联用潜力，有望在竞争中先拔头筹。参考来源各公司官网；Leilei Fu. et al. Targeting Extracellular Signal-Regulated Protein Kinase 1/2 (ERK1/2) in Cancer: An Update on Pharmacological Small-Molecule Inhibitors [J]. J Med Chem. 2022, 65(20): 13561-13573.Richard A. Ward. et al. Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC) [J]. J Med Chem. 2019 62(24):11004-11018.Vikki Flemington. et al. AZD0364 is a potent and selective ERK1/2 inhibitor which enhances anti-tumour activity in KRAS mutant tumour models when combined with the MEK inhibitorSelumetinib [J]. Mol Cancer Ther. 2021, 20(2): 238-249.Andrea Varga. et al. A First-in-Human Phase I Study to Evaluate the ERK1/2 Inhibitor GDC-0994 in Patients with Advanced Solid Tumors [J]. Clin Cancer Res. 2020, 26(6):1229-1236.

免疫疗法小分子药物抗体合作

2022-09-12

·PRNewswire

BioMed Valley Discoveries Announces First Patient Dosed in Phase II Combination Trial with Ulixertinib (BVD-523), its First-in-Class and Best-in-Class ERK Inhibitor, in Combination with Hydroxychloroquine

KANSAS CITY, Mo., Sept. 12, 2022 /PRNewswire/ -- BioMed Valley Discoveries (BVD) announced that the first patient has been dosed in a phase II clinical trial of ulixertinib (BVD-523) in combination with hydroxychloroquine (HCQ). Ulixertinib is a first-in-class and best-in-class ERK inhibitor, with this clinical trial focusing on patients with advanced gastrointestinal malignancies and mutations in the MAPK pathway. This study builds upon the finding of the phase I study of the combination, which was completed at Huntsman Cancer Institute at the University of Utah. "Combining an ERK inhibitor with an autophagy inhibitor is anticipated to take advantage of the finding that tumors may become addicted to autophagy for survival in context of MAPK inhibition" said Brent Kreider, Ph.D., President of BioMed Valley Discoveries. "Given the favorable safety profile and efficacy seen with ulixertinib monotherapy, we believe that the combination with hydroxychloroquine has the potential to provide significant benefit to patients with advanced gastrointestinal malignancies." The Phase II efforts build on a successful Phase Ib evaluating ulixertinib monotherapy as a novel targeted cancer treatment in cohorts of patients with genetic alterations that result in aberrant MAPK pathway signaling. Results from phase Ib demonstrated ulixertinib has an acceptable safety profile and early evidence of clinical activity against a wide range of RAS/MAPK pathway-driven cancers, including atypical alterations in BRAF. In addition to targeting the terminal node of the RAS/MAPK pathway, ulixertinib's highly selective kinase inhibition profile is expected to provide potential impact across a number of tumor types in both monotherapy and combination. Previous efforts have also established a recommended phase 2 dose in combination with palbociclib, with additional combination efforts ongoing. About ulixertinib (BVD-523): Ulixertinib is a first-in class and best-in class small molecule inhibitor of extracellular signal-regulated kinase (ERK) family kinases (ERK1 and ERK2) that is being developed as a novel anti-cancer drug. ERK kinases are downstream components of the mitogen-activated protein kinase (MAPK) signaling cascade (RAS-RAF-MEK-ERK). Ulixertinib has demonstrated promising early efficacy for patients with tumors harboring alterations in the MAPK pathway. About the study: This is an open-label, multicenter, prospective phase II basket trial assessing the efficacy of ulixertinib in combination with hydroxychloroquine in patients with advanced gastrointestinal malignancies. All patients recruited must have a mitogen-activated protein kinase (MAPK) activating mutation to be deemed eligible for trial participation. Each disease-based basket will open to enrollment in two-stages and includes pancreatic, colorectal, esophageal, gastric and cholangiocarcinomas . (Clinicaltrials.gov Number NCT05221320). About BioMed Valley Discoveries (BVD): BioMed Valley Discoveries is a clinical stage biotechnology company focused on addressing unmet medical needs in a variety of therapeutic and diagnostic areas. In addition to the ERK inhibitor, BVD's portfolio includes an oncolytic bacteria that has completed enrollment for a Phase I study, and two early-stage antibodies targeting the tumor microenvironment. Operating since 2007, BioMed Valley Discoveries was established by Jim Stowers Jr., founder of the asset management firm American Century Investments, and his wife Virginia, to advance new medical innovations to improve the lives of patients with difficult-to-treat diseases. BVD is owned by a supporting organization of the Stowers Institute for Medical Research, a non-profit, basic biomedical research organization. Since 2000, the endowment of the Stowers Institute has received over $1.7 billion in dividend payments from American Century. The Institute has invested a portion of its endowment in BVD, whose profits accrue to the benefit of the Institute. For more information, visit . Media Contact Joe Chiodo, Head of Media Relations 724-462-8529 [email protected] SOURCE BioMed Valley Discoveries

抗体合作First in Class小分子药物

100 项与优立替尼相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11038	-	-	DB13930

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
血液肿瘤	临床2期	美国	BioMed Valley Discoveries, Inc.	2024-05-07
胃肠道肿瘤	临床2期	美国	BioMed Valley Discoveries, Inc.	2022-05-26
晚期淋巴瘤	临床2期	美国	National Cancer Institute	2019-07-24
多发性骨髓瘤	临床2期	美国	National Cancer Institute	2019-07-24
难治性淋巴瘤	临床2期	美国	National Cancer Institute	2019-07-24
晚期恶性实体瘤	临床2期	美国	National Cancer Institute	2018-11-14
晚期恶性实体瘤	临床2期	波多黎各	National Cancer Institute	2018-11-14
室管膜瘤	临床2期	美国	National Cancer Institute	2018-11-14
室管膜瘤	临床2期	波多黎各	National Cancer Institute	2018-11-14
肝母细胞瘤	临床2期	美国	National Cancer Institute	2018-11-14

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临床结果

适应症

分期

评价

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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


NCT04488003 (CTgov)	临床2期	晚期恶性实体瘤	104	Ulixertinib	鏇獵齋齋鏇壓淵願範膚(夢鑰壓壓夢構夢壓鬱醖) = 網繭廠襯繭鏇製夢艱顧壓醖構築膚衊糧糧範願 (積鹽夢淵齋齋範襯蓋選, 憲膚齋觸襯遞蓋齋鬱積 ~ 壓築選窪製鑰鏇鏇鹽範) 更多	-	2024-06-04
NCT03698994 (CTgov)	临床2期	难治性软组织肉瘤 \| 复发性中枢神经系统淋巴瘤 \| 难治性中枢神经系统淋巴瘤 ... 更多	20	Pharmacokinetic Study+Ulixertinib	窪願繭淵製鹽築觸構製(網襯製鹽壓衊繭艱夢鹽) = 蓋繭廠淵艱鑰願膚餘衊網獵獵淵鹽網遞簾鹽壓 (遞簾醖築製鑰築窪網製, 簾繭衊蓋製範鹽獵糧積 ~ 積夢網獵壓繭廠獵顧蓋) 更多	-	2023-05-16
NCT02608229 (Pubmed) 人工标引	临床1期	转移性胰腺腺癌	18	Albumin-Bound Paclitaxel+Gemcitabine+Ulixertinib	餘夢願夢鬱範積襯網選(鏇範鏇膚艱鬱簾獵窪選) = ulixertinib 450 mg BID 餘齋獵糧積築鬱齋夢淵 (選獵壓鏇蓋憲壓鏇鑰積 )	积极	2022-11-25
NCT02465060 (EAY131-Z1L, AACR2022) 人工标引	临床1期	癌症 BRAF Fusion	35	BVD-523FB	製繭簾膚蓋觸繭廠製遞(觸範鏇蓋遞壓鑰觸醖襯) = 願膚遞簾簾觸鏇顧製壓淵廠範襯積遞齋醖鹹鏇 (獵願選願網簾鑰壓醖衊 ) 更多	积极	2022-06-15
NCT04566393 (ULI-EAP-100, ASCO2022) 人工标引	N/A	HR阳性/HER2低表达实体瘤 MAPK Mutation	48	ulixertinib	構廠窪築夢淵壓鹹壓鬱(願鬱獵構選選壓積鬱淵) = 淵醖淵餘簾觸壓顧鹹積獵構遞糧醖艱衊範範窪 (顧簾糧壓構窪繭顧蓋構 ) 更多	积极	2022-06-02
NCT03698994 (ASCO2022) 人工标引	临床2期	癌症 MAPK Mutation	20	overall	選構衊憲壓鹽憲願網鑰(衊窪選鏇遞願餘鑰蓋積) = 鑰範齋醖窪憲繭夢範網膚構醖憲壓壓糧衊製鬱 (鏇積築鑰簾襯獵網鬱夢, 17 ~ 58) 更多	积极	2022-06-02
NCT03698994 (ASCO2022) 人工标引	临床2期	癌症 MAPK Mutation	20	Ulixertinib 260 mg/m2 (DL1)	鏇窪築獵範遞廠膚醖構(壓糧窪鬱窪積襯艱網簾) = 襯築憲鑰齋選遞構餘鹹製鹽獵網蓋觸夢遞構憲 (構願鬱願獵廠遞襯醖積 )	积极	2022-06-02
NCT03417739 (CTgov)	临床2期	葡萄膜黑色素瘤	13	BVD-523	膚獵鑰願蓋憲遞繭鹽獵(鹽襯鹽選鑰憲窪襯齋鹽) = 鹽鏇夢鑰構窪餘憲鑰繭顧鏇獵網觸蓋鏇範淵夢 (鏇選築襯膚選鹽壓鹽觸, 衊構糧選構築遞夢糧範 ~ 憲觸獵鹽鏇鹹簾窪網獵) 更多	-	2021-11-11
NCT03454035 (ASCO2021)	临床1期	HR阳性/HER2低表达实体瘤	26	Ulixertinib 300mg BID + Palbociclib 75mg daily	顧鹽廠範艱襯夢膚鏇簾(壓範廠餘膚醖餘餘遞製) = 選製齋遞鏇積憲網糧鬱顧選糧獵鏇窪夢顧糧醖 (構衊襯獵獵鏇艱簾積選, 1.87, not determined)	-	2021-05-28
NCT01781429 (Pubmed \| Invest New Drugs)	临床1期	晚期癌症	135	Ulixertinib	淵衊淵廠齋膚壓範選繭(製膚遞蓋憲衊糧觸簾製) = The most common dAEs included acneiform rash (45/135, 33%), maculopapular rash (36/135, 27%), and pruritus (34/135, 25%). Grade 3 dAEs were observed in 19% (25/135) of patients; no grade 4 or 5 dAEs were seen. 齋憲艱齋觸壓壓鬱製選 (艱襯窪壓網簾蓋鏇淵鬱 )	-	2021-01-03
NCT03417739 (ASCO2020)	临床2期	葡萄膜黑色素瘤	25	Ulixertinib (BVD-523)	築鬱觸構蓋餘蓋繭淵簾(齋網觸簾網襯範鬱繭構) = Grade 3 and 4 toxicities associated with therapy were consistent with BVD-523 and other ERK inhibitors and included LFT elevation, hyponatremia, pruritis, amylase elevation, anemia and rash. 衊網憲蓋選願衊鑰餘襯 (壓廠壓觸廠蓋鬱鑰淵窪 )	不佳	2020-05-25