Phase Ib IIT of Heat Shock Protein 90 Inhibitor TAS-116 Combined With Cyclin-dependent Kinase 4/6 Inhibitor Palbociclib in Advanced Breast Cancer Progressing on Palbociclib & Treatment-refractory Solid Tumors With Retinoblastoma Deficiency

The purpose of this study is to evaluate the safety and efficacy of TAS-116 with palbociclib in two groups of patients:
Patients with advanced breast cancer that has become worse after taking palbociclib alone
Patients with cancers that have an abnormality in a gene called the "retinoblastoma gene".

开始日期2023-09-12

申办/合作机构

Brown University

CTR20232143 / Recruiting临床1期

一项TAS-116(pimitespib)联合伊马替尼治疗晚期胃肠道间质瘤患者的Ⅰ期研究

这是一项I期、开放性、多国、多中心研究。在中国患者剂量递增部分，将在中国患者中评估pimitespib单药治疗以及与伊马替尼联合治疗的安全性和耐受性。

开始日期2023-09-04

申办/合作机构

Taiho Pharmaceutical Co., Ltd.

[+2]

JPRN-jRCT2031230263 / Recruiting临床2期

Phase 2 platform study evaluating combination therapy with TAS-116 (pimitespib) in patients with malignant tumors - CHAPTER-Platform-201

开始日期2023-08-25

申办/合作机构-

100 项与 Pimitespib 相关的临床结果

登录后查看更多信息

100 项与 Pimitespib 相关的转化医学

登录后查看更多信息

100 项与 Pimitespib 相关的专利（医药）

登录后查看更多信息

项与 Pimitespib 相关的文献（医药）

2023-09-01·The Journal of dermatology

Overexpression of heat shock protein 90 through the downregulation of miR-9-5p in extramammary Paget's disease.

Article

作者: Maeda-Otsuka, Saki ; Sakamoto, Ryoko ; Sawamura, Soichiro ; Kajihara, Ikko ; Yamada-Kanazawa, Saori ; Aoi, Jun ; Ohnuma, Takehiro ; Mijiddorj, Myangat Tselmeg ; Masuguchi, Shinichi ; Makino, Katsunari ; Fukushima, Satoshi

Heat shock protein 90 (HSP90) facilitates diverse cellular processes by interacting process with more than 200 client proteins. Overexpression of HSP90 contributes to the pathogenesis of various malignant tumors, and HSP90 inhibitors attenuate the progression of malignant tumors in vitro/vivo. Numerous clinical trials have used HSP90 inhibitors to treat several cancers, and pimitespib (an HSP90 inhibitor) is covered by insurance for advanced gastrointestinal stromal tumor in Japan. In this study, we investigated the expression pattern of HSP90 and analyzed its clinical significance in extramammary Paget's disease (EMPD). All 77 EMPD tissues investigated were positive for HSP90 expression. The immunoreactivity of HSP90 in fetal cases due to EMPD tended to be highly stained. Although there was no significant difference in HSP90 mRNA levels between 24 paired lesional and nonlesional tissues, microRNA-inhibiting HSP90 levels in tumor tissues were significantly decreased compared with those in normal tissues. Thus, HSP90 may play an important role in the pathogenesis of EMPD and may be a novel therapeutic target for EMPD.

2023-06-15·International Journal of Cancer

Combination of pimitespib (TAS‐116) with sunitinib is an effective therapy for imatinib‐resistant gastrointestinal stromal tumors

Article

作者: Makino, Tomoki ; Takahashi, Tsuyoshi ; Saito, Takuro ; Obata, Yuuki ; Ohkubo, Shuichi ; Yamashita, Kotaro ; Kurokawa, Yukinori ; Nakajima, Kiyokazu ; Yamamoto, Kazuyoshi ; Hirota, Seiichi ; Saito, Yurina ; Teranishi, Ryugo ; Doki, Yuichiro ; Fujimoto, Minoru ; Kazuno, Hiromi ; Tanaka, Koji ; Eguchi, Hidetoshi ; Serada, Satoshi ; Naka, Tetsuji ; Nishida, Toshirou

Abstract:

Despite the effectiveness of imatinib, most gastrointestinal stromal tumors (GISTs) develop resistance to the treatment, mainly due to the reactivation of KIT tyrosine kinase activity. Sunitinib, which inhibits the phosphorylation of KIT and vascular endothelial growth factor (VEGF) receptor, has been established as second‐line therapy for GISTs. The recently‐developed heat shock protein 90 (HSP90) inhibitor pimitespib (PIM; TAS‐116) demonstrated clinical benefits in some clinical trials; however, the effects were limited. The aim of our study was therefore to clarify the effectiveness and mechanism of the combination of PIM with sunitinib for imatinib‐resistant GISTs. We evaluated the efficacy and mechanism of the combination of PIM with sunitinib against imatinib‐resistant GIST using imatinib‐resistant GIST cell lines and murine xenograft models. In vitro analysis demonstrated that PIM and sunitinib combination therapy strongly inhibited growth and induced apoptosis in imatinib‐resistant GIST cell lines by inhibiting KIT signaling and decreasing auto‐phosphorylated KIT in the Golgi apparatus. In addition, PIM and sunitinib combination therapy enhanced antitumor responses in the murine xenograft models compared to individual therapies. Further analysis of the xenograft models showed that the combination therapy not only downregulated the KIT signaling pathway but also decreased the tumor microvessel density. Furthermore, we found that PIM suppressed VEGF expression in GIST cells by suppressing protein kinase D2 and hypoxia‐inducible factor‐1 alpha, which are both HSP90 client proteins. In conclusion, the combination of PIM and sunitinib is effective against imatinib‐resistant GIST via the downregulation of KIT signaling and angiogenic signaling pathways.

2023-06-01·Cancer medicine

Efficacy of post-first-line agents for advanced gastrointestinal stromal tumors following imatinib failure: A network meta-analysis.

Article

作者: Hu, Kehan ; Wang, Xingyue ; Zhang, Hu ; Shu, Mingrong

BACKGROUND:

Imatinib is the standard first-line treatment for advanced gastrointestinal stromal tumors (GISTs); however, most patients eventually develop imatinib resistance, leading to considerable clinical challenges. Few direct comparisons have been made between different post-first-line therapies on clinical efficacy in advanced GIST following imatinib failure.

METHODS:

Databases including PubMed, Embase, Scopus, Google Scholars, and Cochrane Library from inception to February 2023 were retrieved for randomized controlled trials evaluating the clinical efficacy of different post-first-line agents for advanced GIST following imatinib failure. Network and conventional meta-analysis were carried out using Stata/MP 16.0.

RESULTS:

Ripretinib showed significant improvement in progression-free survival (PFS) rates from the 2nd to the 12th month compared to placebo, while there was virtually no evidence that the rest active agents had a significant benefit at the 12th month. Masitinib, ripretinib, sunitinib, regorafenib, and pimitespib exhibited significantly longer median PFS than placebo, and pairwise comparisons indicated there were no significant differences among masitinib, ripretinib, and sunitinib. These post-first-line agents decreased the risk of disease progression or death by 65% (HR = 0.35, 95% CI: 0.26-0.47) compared to placebo. Ripretinib and sunitinib came into effect earlier and exhibited more consistent overall survival (OS) rate improvements than masitinib and pimitespib, while pairwise comparisons revealed no significant differences in these four active agents concerning the improvement in OS rate. These post-first-line agents decreased the risk of death by 39% (HR = 0.61, 95% CI: 0.44-0.83) over placebo for advanced GIST following imatinib failure.

CONCLUSION:

The active agents in our analysis as post-first-line therapies are able to provide superior clinical efficacy, with improved PFS rate and OS rate at certain time points, as well as absolute values of PFS and OS for advanced GIST. Ripretinib might be the optimal recommendation as a post-first-line treatment for advanced GIST following imatinib failure.

项与 Pimitespib 相关的新闻（医药）

2023-05-10

·PRNewswire

Soft Tissue Sarcoma Pipeline Space Brims With Novel Emerging Therapies with Over 125 Key Companies Working in the Domain | DelveInsight

The prevalence of soft tissue sarcoma has been rising over the past few years, which prompts the growing demand for treatment options. The increasing prevalence of soft tissue sarcoma and the growing research and development activities to develop novel therapies to treat soft tissue sarcoma to drive the market. The companies developing the potential therapies in the last stage of development include Advenchen Laboratories, Philogen, Nanobiotix, and several others. LAS VEGAS, May 10, 2023 /PRNewswire/ -- DelveInsight's ' Soft Tissue Sarcoma Pipeline Insight – 2023 ' report provides comprehensive global coverage of available, marketed, and pipeline soft tissue sarcoma therapies in various stages of clinical development, major pharmaceutical companies are working to advance the pipeline space and future growth potential of the soft tissue sarcoma pipeline domain. Key Takeaways from the Soft Tissue Sarcoma Pipeline Report DelveInsight's soft tissue sarcoma pipeline report depicts a robust space with 125+ active players working to develop 130+ pipeline therapies for soft tissue sarcoma treatment. Key soft tissue sarcoma companies such as Advenchen Laboratories, Philogen, Gradalis, Epizyme, Chugai Pharma France, CytRx, Taiho Pharmaceuticals, KaryoPharm Therapeutics, Nanobiotix, Apexigen, Lytix Biopharma, Incyte Corporation, Iovance Biotherapeutics, Aadi Bioscience, Inc., AVEO Pharmaceuticals, Bayer, VasGene Therapeutics, Mirati Therapeutics, Novartis Pharmaceuticals, Incyte Corporation, Tracon Pharmaceuticals, Jiangsu Hengrui Medicine, Exelixis, Qbiotics, AstraZeneca, Loxo Oncology, ImmunityBio, Monopar Therapeutics, Chipscreen Biosciences, Ltd., Agenus, C4 Therapeutics, Inc., Noxopharm Limited, Moleculin Biotech, Inc., Sunshine Guojian Pharmaceutical (Shanghai) Co., Ltd., Tracon Pharmaceuticals Inc., Guangdong Xiangxue Precision Medical Technology Co., Ltd., Cornerstone Pharmaceuticals, Takara Bio Inc., Jazz Pharmaceuticals, Lyell Immunopharma, Telix Pharmaceuticals, and others are evaluating new soft tissue sarcoma drugs to improve the treatment landscape. Promising soft tissue sarcoma pipeline therapies in various stages of development include AL-3818, Onfekafusp alfa, Vigil, Tazemetostat, Aldoxorubicin, TAS-116, Selinexor, NBTXR3, APX005M, GPX-150, LTX-315, Lenvatinib, Chiauranib, Zalifrelimab, INCB081776, LN-145-S1, ABI-009, Tivozanib, LOXO-101, sEphB4-HSA, Sitravatinib, Envafolimab, Camrelizumab, Tigilanol Tiglate, Durvalumab, Tremelimumab, CFT8634, NOX66, Liposomal Annamycin, 609A, YH001, TAEST16001, CPI-613+Hydroxychloroquine, TBI-1301, Lurbinectedin, LYL132, and others. In October 2022, LIXTE Biotechnology Holdings, Inc. announced that the Spanish Agency for Medicines and Health Products (Agencia Española de Medicamentos y Productos Sanitarios, AEMPS) had authorized a Phase 1b/randomized Phase 2 study of LB-100, the Company's lead clinical compound, plus doxorubicin versus doxorubicin alone, the global standard for initial treatment of advanced soft tissue sarcomas (ASTS). In September 2022, Immutep Limited was pleased to announce it has signed a Material Transfer Agreement ("Agreement") with the Maria Skłodowska-Curie National Research Institute of Oncology in Warsaw, Poland, to enable an investigator-initiated open-label Phase II clinical trial. The trial will evaluate Immutep's lead product candidate, efti in combination with pembrolizumab and radiotherapy in the neoadjuvant setting (prior to surgery) in up to 40 patients with select soft tissue sarcoma (STS). In September 2022, TRACON Pharmaceuticals, Inc. announced that the U.S. Food and Drug Administration (FDA) has granted fast-track designation for the development of envafolimab (KN035) for patients with locally advanced, unresectable or metastatic undifferentiated pleomorphic sarcoma (UPS) and myxofibrosarcoma (MFS) who have progressed on one or two prior lines of chemotherapy. In September 2022, Avacta Group plc announced that the US Food and Drug Administration (FDA) had granted Orphan Drug Designation (ODD) to the company's lead pre|CISION drug candidate, AVA6000, for treatment of soft tissue sarcoma.AVA6000 is a form of the generic chemotherapy doxorubicin that has been modified using the pre|CISION technology so that it is activated predominantly in the tumor with the aim of sparing healthy tissue from exposure and improving the safety, tolerability, and efficacy of the drug. In May 2022, Immix Biopharma, Inc., announced positive interim study data showing that after one cycle of treatment, ImmixBio's lead candidate IMX-110 produced 75% survival vs. 0% survival for Trabectedin (sold as YONDELIS ® by Janssen, a Johnson & Johnson Company, a U.S. FDA approved drug) in a connective tissue cancer Soft Tissue Sarcoma (STS) mice study. In this study, IMX-110 was compared against approved drugs used to treat STS. Trabectedin was dosed according to Meco et al., 2003 (trabectedin monotherapy treatment arm), and IMX-110 was administered at 2.0 mg/kg. In April 2022, Telix Pharmaceuticals Limited announced that it has entered into a license agreement with Eli Lilly and Company ("Lilly") under which Telix is granted exclusive worldwide rights to develop and commercialize radiolabelled forms of Lilly's olaratumab antibody for the diagnosis and treatment of human cancers. Telix's initial development focus will be on a rare type of cancer known as soft tissue sarcoma (STS). Request a sample and discover the recent advances in soft tissue sarcoma drug treatment @ Soft Tissue Sarcoma Pipeline Report The soft tissue sarcoma pipeline report provides detailed profiles of pipeline assets, a comparative analysis of clinical and non-clinical stage soft tissue sarcoma drugs, inactive and dormant assets, a comprehensive assessment of driving and restraining factors, and an assessment of opportunities and risks in the soft tissue sarcoma clinical trial landscape. Soft Tissue Sarcoma Overview Soft-tissue sarcomas (STS) are rare neoplasms that can develop in supporting or connective tissue, such as muscle, nerves, tendons, blood vessels, and fatty and fibrous tissues. They commonly affect the arms, legs, and trunk. They can also be found in the stomach and intestines (GIST), behind the abdomen (retroperitoneal sarcomas), and in the female reproductive system (gynecological sarcomas). Soft tissue sarcomas are classified based on the cell type involved, the nature of the malignancy, and the clinical course of the disease. The signs and soft tissue sarcoma symptoms differ greatly between patients depending on the type of soft tissue sarcoma. It is not associated with any obvious symptoms early in the course of the disease, but affected individuals may notice a slow-growing, painless mass in the affected area. Find out more about drugs for soft tissue sarcoma @ New Soft Tissue Sarcoma Drugs A snapshot of the Soft Tissue Sarcoma Pipeline Drugs mentioned in the report: Learn more about the emerging soft tissue sarcoma pipeline therapies @ Soft Tissue Sarcoma Clinical Trials Soft Tissue Sarcoma Therapeutics Assessment The soft tissue sarcoma pipeline report proffers an integral view of soft tissue sarcoma emerging novel therapies segmented by stage, product type, molecule type, mechanism of action, and route of administration. Scope of the Soft Tissue Sarcoma Pipeline Report Coverage: Global Therapeutic Assessment By Product Type: Mono, Combination, Mono/Combination Therapeutic Assessment By Clinical Stages: Discovery, Pre-clinical, Phase I, Phase II, Phase III Therapeutics Assessment By Route of Administration: Infusion, Intra-arterial, Intradermal, Intralesional, Intratumoral, Intravenous, Oral, Parenteral, Subcutaneous Therapeutics Assessment By Molecule Type: Antibody, Antibody-drug conjugate, Cell therapy, Gene therapy, Immunotherapy, Nanoparticle, Peptide, Recombinant fusion protein, Small molecule Therapeutics Assessment By Mechanism of Action: Fibroblast growth factor receptor antagonists, Platelet-derived growth factor beta receptor antagonists, Proto oncogene protein c-kit inhibitors, Vascular endothelial growth factor receptor 3 antagonists, Vascular endothelial growth factor receptor-1 antagonists, Vascular endothelial growth factor receptor-2 antagonists, Immunostimulants, Free radical stimulants, DNA intercalators, Type II DNA topoisomerase inhibitors, Cell membrane structure modulators, Antibody-dependent cell cytotoxicity, Programmed cell death-1 receptor antagonists, T lymphocyte stimulants, Type 1 fibroblast growth factor receptor antagonists, Type 3 fibroblast growth factor receptor antagonists, Type 4 fibroblast growth factor receptor antagonists, Type-2 fibroblast growth factor receptor antagonists, Fms-like tyrosine kinase 3 inhibitors, Lymphocyte specific protein tyrosine kinase p56(lck) inhibitors; Lyn protein-tyrosine kinase inhibitors, Src-Family kinase inhibitors Key Soft Tissue Sarcoma Companies: Advenchen Laboratories, Philogen, Gradalis, Epizyme, Chugai Pharma France, CytRx, Taiho Pharmaceuticals, KaryoPharm Therapeutics, Nanobiotix, Apexigen, Lytix Biopharma, Incyte Corporation, Iovance Biotherapeutics, Aadi Bioscience, Inc., AVEO Pharmaceuticals, Bayer, VasGene Therapeutics, Mirati Therapeutics, Novartis Pharmaceuticals, Incyte Corporation, Tracon Pharmaceuticals, Jiangsu Hengrui Medicine, Exelixis, Qbiotics, AstraZeneca, Loxo Oncology, ImmunityBio, Monopar Therapeutics, Chipscreen Biosciences, Ltd., Agenus, C4 Therapeutics, Inc., Noxopharm Limited, Moleculin Biotech, Inc., Sunshine Guojian Pharmaceutical (Shanghai) Co., Ltd., Tracon Pharmaceuticals Inc., Guangdong Xiangxue Precision Medical Technology Co., Ltd., Cornerstone Pharmaceuticals, Takara Bio Inc., Jazz Pharmaceuticals, Lyell Immunopharma, Telix Pharmaceuticals, and others. Key Soft Tissue Sarcoma Pipeline Therapies: AL-3818, Onfekafusp alfa, Vigil, Tazemetostat, Aldoxorubicin, TAS-116, Selinexor, NBTXR3, APX005M, GPX-150, LTX-315, Lenvatinib, Chiauranib, Zalifrelimab, INCB081776, LN-145-S1, ABI-009, Tivozanib, LOXO-101, sEphB4-HSA, Sitravatinib, Envafolimab, Camrelizumab, Tigilanol Tiglate, Durvalumab, Tremelimumab, CFT8634, NOX66, Liposomal Annamycin, 609A, YH001, TAEST16001, CPI-613+Hydroxychloroquine, TBI-1301, Lurbinectedin, LYL132, and others. Dive deep into rich insights for new drugs for soft tissue sarcoma treatment; visit @ Soft Tissue Sarcoma Medications Table of Contents For further information on the soft tissue sarcoma pipeline therapeutics, reach out @ Soft Tissue Sarcoma Drug Treatment Related Reports Soft Tissue Sarcoma Market Soft Tissue Sarcoma Market Insights, Epidemiology, and Market Forecast – 2032 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, market share of the individual therapies, and key soft tissue sarcoma companies, including Gem Pharmaceuticals, Lytix Biopharma, Incyte Corporation, Daiichi Sankyo, NantPharma, Iovance Biotherapeutics, Agenus, Eli Lilly and Company, Adaptimmune, Aadi, AVEO Pharmaceuticals, Amgen, among others. Soft Tissue Sarcoma Epidemiology Forecast Soft Tissue Sarcoma Epidemiology Forecast – 2032 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the soft tissue sarcoma epidemiology trends. Clear Cell Sarcoma Pipeline Clear Cell Sarcoma Pipeline Insight – 2023 report provides comprehensive insights about the pipeline landscape, including clinical and non-clinical stage products and the key clear cell sarcoma companies, including Tesaro, NantPharma, Rafael Pharmaceuticals, Pfizer, among others. Ewing Sarcoma Pipeline Ewing Sarcoma Pipeline Insight – 2023 report provides comprehensive insights about the pipeline landscape, including clinical and non-clinical stage products, and the key Ewing sarcoma companies, including Gradalis, Inc., Shanghai Pharmaceuticals Holding Co., Ltd, Tyme, Inc, Pfizer, Hutchison Medipharma Limited, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +1(919)321-6187 Logo: SOURCE DelveInsight Business Research, LLP

引进/卖出孤儿药快速通道临床2期

2023-05-06

·药明康德

2022年有哪些创新靶点涌现？《自然》深度盘点

▎药明康德内容团队编辑2022年，美国、欧盟和日本批准的新药数量略有下滑，从前几年的约60种下降到只有48种，其中有35种药物的靶点拥有明确的作用机理（MOA）。日前，《自然》杂志子刊Nature Reviews Drug Discovery发表了一篇文章，围绕2022年获批的12种拥有全新MOA的新药展开了分析，此前没有任何一款上市药物能够对这些靶点发挥作用。从分子类型上看，这12款药物包括了5款小分子抑制剂、4款单克隆抗体、2款双特异性抗体以及1款多肽药物，其适应症主要集中在罕见性血液和心脏疾病、皮肤和眼睛疾病、糖尿病及相关病变、以及肿瘤。Mavacamten（Camzyos）Mavacamten（商品名：Camzyos）是一种口服、选择性的心肌肌球蛋白小分子别构调节剂。该分子最初由Myokadia公司开发，百时美施贵宝（BMS）于2020年以高达131亿美元对其进行收购并将mavacamten纳入其产品管线。Mavacamten的靶点是β-心肌肌球蛋白7（β-cardiac myosin-7），它能够将整体肌球蛋白群转变到节能、可募集的超松弛状态，因此能够减少症状性梗阻性肥厚型心肌病患者的心脏过度收缩症状。在临床期和临床前研究中，mavacamten可以降低心壁应激的生物标志物，减轻过度的心肌收缩力，减少左心室流出道梯度和增加舒张顺应性。▲Mavacamten结构式（图片来源：PubChem）2022年，mavacamten被FDA批准用于治疗成人梗阻性肥厚型心肌病，成为了FDA批准的首款心肌肌球蛋白别构可逆性抑制剂。Pimitespib（Jeselhy）Pimitespib是由日本大鹏药品（Taiho Pharmaceutical）开发的一种口服小分子抑制剂，可特异性地抑制热休克蛋白90（HSP90）。细胞中的分子伴侣蛋白通过与底物蛋白结合，在蛋白质折叠中扮演着重要角色。HSP90正是一种分子伴侣蛋白，它对于维持与其结合蛋白的构象成熟、稳定性和功能起着关键作用。与HSP90结合的蛋白中，包括了许多参与信号转导、细胞周期调控和凋亡过程的激酶、细胞周期调控因子、转录因子和激素受体。HSP90在各种实体瘤中高度活化，但在正常组织中仍处于相对休眠状态，因此被认为是肿瘤药物开发的潜力靶点。据研究报道，HSP90在胃肠道间质瘤、膀胱癌、急性髓细胞白血病、乳腺癌、非小细胞肺癌、结直肠癌和黑色素瘤中的表达与癌症进展和患者预后相关。此外，HSP90还是肿瘤坏死因子-α（TNF-α）和白细胞介素-17A（IL-17A）信号传导的下游调节剂。▲Pimitespib结构式（图片来源：PubChem）Pimitespib通过靶向作用于HSP90来破坏和减少参与癌症生长和存活过程的蛋白质（如KIT、PDGFRA、HER2和EGFR），继而发挥抗癌作用。2022年6月，日本厚生劳动省（MHLW）批准pimitespib片（商品名：Jeselhy）上市，用于治疗化疗后进展的胃肠道间质瘤。Gefapixant（Lyfnua）Gefapixant是默沙东（MSD）旗下一款口服选择性P2X3受体拮抗剂，用于治疗难治性或不明原因的慢性咳嗽。▲Gefapixant结构式（图片来源：PubChem）P2X3受体是位于呼吸道内衬的感觉神经纤维（主要是C纤维）上发现的受体类型之一。由于气道炎症、外部刺激和机械应力/损伤等过程，包括三磷酸腺苷（ATP）在内的化学刺激物从呼吸道内衬细胞中释放出来。细胞外ATP与呼吸道C纤维上P2X3受体的结合可以被感知为潜在损伤的信号，从而产生动作电位，这可能会引发咳嗽。因此，阻断细胞外ATP与P2X3受体的结合有望减少感觉C纤维的激活，从而缓解咳嗽。去年年初，日本厚生劳动省批准了gefapixant（商品名：Lyfnua）45 mg片剂的上市申请，用于治疗患有难治性或不明原因的慢性咳嗽的成年患者。Lenacapavir（Sunlenca）Sunlenca是吉利德科学（Gilead Sciences）开发的一种具有多阶段作用机制的病毒衣壳抑制剂，对现有的其他药物类别没有已知的交叉耐药性，为不再对其当前疗法显示有效应答的人类免疫缺陷病毒（HIV）感染的患者提供了一种新的治疗选择。Sunlenca的优势还在于患者可能只需每隔6个月接受一次注射，就可以维持它的效力。▲Lenacapavir结构式（图片来源：PubChem）大多数抗病毒药物只作用于病毒复制的一个阶段，但lenacapavir被设计用于在其生命周期的多个阶段中抑制HIV。Lenacapavir通过与衣壳蛋白单体结合，让生成的衣壳成为功能失常的“伪劣产品”，从而阻断病毒的增殖过程。Lenacapavir于2019年5月获得美国FDA授予的突破性疗法认定（BTD），并在2022年8月获全球首次批准，用于联合其他抗逆转录病毒药物治疗多重耐药HIV感染的成人患者。随后，在2022年的12月，lenacapavir也被美国FDA批准上市，用于联合其他抗逆转录病毒药物治疗多重耐药HIV感染的成人患者。此外，日本药品和医疗器械管理局（PMDA）也批准了该药物在日本的上市申请。Mitapivat（Pyrukynd）Mitapivat是一款口服丙酮酸激酶-R（PKR）小分子别构激活剂，它可以激活野生型PKR和一系列PKR突变体，改善血红细胞的能量供应，提高血红细胞的健康水平，从而治疗丙酮酸激酶缺乏症成人患者的溶血性贫血。它为丙酮酸激酶缺乏症患者群体带来了全新的治疗希望。在临床试验中，固定剂量mitapivat治疗24周期后，37%丙酮酸激酶缺乏症患者的输血负荷降低≥33%，22%患者无需接受输血治疗。此外，与安慰剂相比，接受mitapivat治疗的患者血红蛋白水平得到统计显著并持久的增加。▲Mitapivat结构式（图片来源：PubChem）2022年11月，欧盟委员会批准了mitapivat用于治疗丙酮酸激酶缺乏症成年患者。一个月后，美国FDA也批准了mitapivat的上市申请，以治疗患有丙酮酸激酶缺乏症、且出现溶血性贫血的成人患者。Sutimlimab（Enjaymo）Sutimlimab是一款特异性靶向补体C1s蛋白的单克隆抗体，由赛诺菲（Sanofi）开发。补体系统级联介导了多种自身免疫性疾病，通过阻断经典补体通路中的C1s蛋白的功能，sutimlimab有望治疗多种自身免疫性疾病。Sutimlimab曾经获得美国FDA授予的突破性疗法认定、孤儿药资格和优先审评资格。2022年2月，这款疗法被美国FDA批准用于治疗冷凝集素病（CAD）患者。新闻稿指出，这是首款FDA批准用于冷凝集素病患者的疗法，能够抑制患者因为补体蛋白激活导致的溶血。此外，这款疗法还获得了欧洲药品管理局（EMA）和PMDA的批准上市。Spesolimab（Spevigo）Spesolimab是一种人源化拮抗性单克隆IgG1抗体，可与白介素-36受体（IL-36R）结合并阻断人IL-36α、IL-36β和IL-36γ诱导的IL-36R活化，从而抑制炎症性皮肤病中的促炎和促纤维化通路。IL-36是树突细胞和T细胞的强效调节剂，参与树突细胞与辅助性T细胞的激活、抗原呈递和刺激促炎因子产生。研究表明，IL-36在皮肤中大量表达，并在银屑病等皮肤病发病机制中扮演重要角色。2022年9月，该产品获美国FDA批准上市，用于治疗泛发性脓疱型银屑病（GPP）发作。同年12月，该产品在中国获批，用于治疗成人GPP发作。Nemolizumab（Mitchga）Nemolizumab是Galderma公司开发的一种研究性单克隆抗体，它主要靶向白介素31（IL-31）受体，继而阻断IL-31的相关信号转导。IL-31在包括过敏性皮炎和结节性痒疹在内的多种皮肤疾病的病理机制中起着重要作用。由于IL-31可以直接刺激与瘙痒相关的感觉神经元、导致炎症和皮肤屏障功能受损，因此IL-31成为连接免疫和中枢神经系统的“桥梁”，而上述特征也使得IL-31成为了治疗炎症性皮肤病的靶点。2022年3月，nemolizumab获得了日本PMDA的批准上市，用于治疗13岁以上的成人和儿童与特应性皮炎相关的瘙痒（仅在现有治疗不够有效的情况下使用）。Faricimab（Vabysmo）Faricimab是罗氏（Roche）旗下基因泰克（Genentech）公司开发的一款双特异性抗体，它可以同时靶向阻断两条致病关键通路——血管生成素-2（Ang-2）和血管内皮生长因子-A（VEGF-A），这两种通路都能破坏血管的稳定性，使血管发生渗漏，增加炎症的发生，从而驱动许多可导致视力丧失的视网膜疾病。同时靶向这两条通路可以起到一定的互补作用，因此faricimab有望稳定血管，改善患者的视力。在临床研究中，faricimab治疗显著改善了湿性老年黄斑变性患者和糖尿病性黄斑水肿患者的视力，并且疗效可以长期维持下去（治疗间隔延长到4个月一次）。2022年年初，美国FDA批准了faricimab（商品名：Vabysmo）的上市申请，以治疗湿性年龄相关性黄斑变性和糖尿病性黄斑水肿。新闻稿指出，这是首款获FDA批准治疗这两种眼科疾病的双特异性抗体。同年9月，这款疗法又获得了欧盟委员会的批准，用于治疗新生血管性或湿性年龄相关性黄斑变性以及由糖尿病性黄斑水肿导致的视力障碍。此外，faricimab也在日本获批上市。RelatlimabRelatlimab是百时美施贵宝（Bristol Myers Squibb）旗下一款靶向淋巴细胞活化基因3（LAG-3）的抗体药物。LAG-3是一种在效应T细胞和调节性T细胞（Tregs）上表达的免疫检查点蛋白，具有控制T细胞应答、活化和生长的功能。图片来源：123RF临床前研究表明，抑制LAG-3可能恢复耗竭T细胞的效应功能，并可能促进抗肿瘤反应。早期研究证明，靶向LAG-3联合其他潜在互补的免疫检查点可能是更有效增强抗肿瘤免疫活性的关键策略。在一项2期临床试验中，在手术前让晚期黑色素瘤患者接受relatlimab和纳武利尤单抗联合治疗，可以使57%患者体内的肿瘤被彻底清除，并且该治疗方案的安全性良好。2021年9月，美国FDA授予relatlimab和纳武利尤单抗构成的固定剂量组合的生物制品许可申请（BLA）优先审评资格。2022年3月，这款联合疗法获FDA批准上市，治疗罹患不可切除或转移性黑色素瘤的成人和儿童（12岁及以上）患者。新闻稿中指出，relatlimab是美国FDA批准的首款LAG-3抗体，也是近10年来针对全新免疫检查点获批的首款创新癌症免疫疗法。此外，这款组合疗法也获得了EMA的批准。Tebentafusp（Kimmtrak）Tebentafusp是由Immunocore公司开发的创新双特异性蛋白疗法，由两部分融合而成：一端是具有高亲和力的可溶性T细胞受体（TCR），另一端是靶向CD3的免疫效应结构域。这款疗法能特异性地靶向gp100，一种在黑色素细胞和黑色素瘤中表达的抗原。依照设计，tebentafusp能引导和激活T细胞，让它们识别和杀死癌细胞。Tebentafusp先前已被美国FDA授予突破性疗法认定、快速通道资格和孤儿药资格、以及优先审评资格。2022年1月，该疗法获得了FDA的批准，治疗特定的葡萄膜黑色素瘤。新闻稿指出，这项批准创下了多个第一：它是FDA批准的首款治疗不可切除或转移性葡萄膜黑色素瘤的疗法。它同样是首款获得监管批准的T细胞受体（TCR）疗法，以及首款获FDA批准治疗实体肿瘤的双特异性T细胞接头（T cell engager）。Tirzepatide（Mounjaro）Tirzepatide是礼来（Eli Lilly）公司研发的一款葡萄糖依赖性促胰岛素多肽（GIP）和胰高血糖素样肽-1（GLP-1）受体双重激动剂，GIP和GLP-1是调控血糖的天然的肠促胰岛素激素，可以有效改善糖尿病患者的血糖控制。此外，这款药物在减轻体重方面有着不俗的表现，经过72周的tirzepatide治疗，肥胖个体的体重平均减少了16%至22.5%，而对照组成员的成员减重比例仅为2.4%。图片来源：123RF2022年5月，tirzepatide被美国FDA批准上市，用于与控制饮食和锻炼联用，改善成人2型糖尿病患者的血糖控制。近日，礼来公布了tirzepatide在治疗肥胖症或超重、且患有2型糖尿病患者群体中的3期临床数据，并计划在接下来的几周内完成tirzepatide用于治疗肥胖、过重成人（伴有体重相关并发症）的滚动新药申请（NDA）。2022年的获批新药靶点展现出了作用机制和靶点的多样性。虽然获批药物的总体数量有所下降，但在以往停滞不前的领域出现了创新靶点，这表明药理学研究正在不断拓展和前进。值得注意的是，新靶点中有一半针对罕见性疾病，标志着在解决未竟医疗需求方面所取得的巨大突破。回顾过去的一年，对新药靶点的探索仍然是疗法创新的关键驱动力，这些创新疗法的问世不仅改变了众多患者的生活，也为我们揭示了以前未知的药理学领域。我们期待在未来有更多全新MOA靶点被发现，并最终成功转化为临床疗法，造福患者。大家都在看▲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] Novel drug targets in 2022，Retrieved May 4th，2023, From https://www.nature.com/articles/d41573-023-00068-y[2] Ho, Carolyn Y et al. “Evaluation of Mavacamten in Symptomatic Patients With Nonobstructive Hypertrophic Cardiomyopathy.” Journal of the American College of Cardiology vol. 75,21 (2020): 2649-2660. doi:10.1016/j.jacc.2020.03.064[3] Taiho Pharmaceutical Submits New Drug Application for its HSP90 Inhibitor Pimitespib (TAS-116) for GIST，Retrieved May 4th，2023, From https://www.taiho.co.jp/en/release/2021/20210914.html[4] Merck Provides U.S. and Japan Regulatory Update for Gefapixant，Retrieved May 4th，2023, From https://www.merck.com/news/merck-provides-u-s-and-japan-regulatory-update-for-gefapixant/[5] Agios Announces Phase 3 ACTIVATE-T Trial of Mitapivat Achieved Primary Endpoint in Adults with Pyruvate Kinase Deficiency Who Are Regularly Transfused. Retrieved May 4th, 2023, from https://www.globenewswire.com/news-release/2021/01/26/2164670/0/en/Agios-Announces-Phase-3-ACTIVATE-T-Trial-of-Mitapivat-Achieved-Primary-Endpoint-in-Adults-with-Pyruvate-Kinase-Deficiency-Who-Are-Regularly-Transfused.html[6] PYRUKYND® (mitapivat) Approved in the EU for the Treatment of Pyruvate Kinase (PK) Deficiency in Adult Patients，Retrieved May 4th, 2023, from https://investor.agios.com/news-releases/news-release-details/pyrukyndr-mitapivat-approved-eu-treatment-pyruvate-kinase-pk[7] FDA approves the first treatment option for generalized pustular psoriasis flares in adults. Retrieved May 4th, 2023, from https://www.prnewswire.com/news-releases/fda-approves-the-first-treatment-option-for-generalized-pustular-psoriasis-flares-in-adults-301616844.html[8] Keam, Susan J. “Nemolizumab: First Approval.” Drugs vol. 82,10 (2022): 1143-1150. doi:10.1007/s40265-022-01741-z[9] U.S. Food and Drug Administration Approves First LAG-3-Blocking Antibody Combination, Opdualag™ (nivolumab and relatlimab-rmbw), as Treatment for Patients with Unresectable or Metastatic Melanoma, Retrieved May 4th，2023, From https://news.bms.com/news/details/2022/U.S.-Food-and-Drug-Administration-Approves-First-LAG-3-Blocking-Antibody-Combination-Opdualag-nivolumab-and-relatlimab-rmbw-as-Treatment-for-Patients-with-Unresectable-or-Metastatic-Melanoma/default.aspx[10] Immunocore announces FDA approval of KIMMTRAK® (tebentafusp-tebn) for the treatment of unresectable or metastatic uveal melanoma, Retrieved May 4th，2023, From https://www.globenewswire.com/news-release/2022/01/26/2373344/0/en/Immunocore-announces-FDA-approval-of-KIMMTRAK-tebentafusp-tebn-for-the-treatment-of-unresectable-or-metastatic-uveal-melanoma.html[11] Lilly receives U.S. FDA Fast Track designation for tirzepatide for the treatment of adults with obesity, or overweight with weight-related comorbidities. Retrieved May 4th，2023, From https://investor.lilly.com/news-releases/news-release-details/lilly-receives-us-fda-fast-track-designation-tirzepatide[12] Eli Lilly showcases PhIII weight loss data for type 2 diabetes patients taking tirzepatide. Retrieved May 4th，2023, From https://endpts.com/lillys-tirzepatide-helps-patients-with-obesity-and-type-2-diabetes-lose-15-of-body-weight/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

并购申请上市

2023-02-06

·药研发

【药研发0207】海创URAT1抑制剂报联合用药IND | 远大医药引进RDC报胶质瘤IND...

「本文共：15条资讯，阅读时长约：3分钟」今日头条海创URAT1抑制剂报联合用药IND。海创药业1类化药HP501缓释片的临床试验申请获CDE受理，拟联合黄嘌呤氧化酶（XO）抑制剂用于原发性高尿酸血症患者的长期治疗。HP501是一款高活性、高选择性URAT1抑制剂，目前已完成多项单药治疗高尿酸血症/痛风的Ⅰ/Ⅱ期试验。现有的临床数据显示，HP501在治疗高尿酸血症/痛风方面具有良好的疗效及安全性。‍国‍‍‍‍内‍药讯‍‍1.日本大鹏HSP90抑制剂在华获批临床。日本大鹏制药2.4类新药pimitespib片获国家药监局临床试验默示许可，拟用于伊马替尼耐药的胃肠道间质瘤（GIST）的治疗。pimitespib（TAS-116）是一款口服热休克蛋白90（HSP90）抑制剂，通过破坏和还原参与癌症生长和生存的蛋白质（如KIT、PDGFRA、HER2和EGFR），进而发挥抗肿瘤作用。2022年6月，日本厚生劳动省（MHLW）已批准pimitespib用于治疗化疗后进展的GIST，商品名为Jeselhy。2.迈威新一代ADC报实体瘤IND。迈威生物抗体偶联药物（ADC）1类新药9MW2921的临床试验申请获CDE受理，拟开发用于实体瘤的治疗。9MW2921可与肿瘤细胞表面的抗原结合并进入肿瘤细胞，通过特定酶解作用，定向释放小分子，从而实现对肿瘤的精准杀伤。在临床前研究中，9MW2921显示出积极的肿瘤杀伤作用；并能有效控制靶向相关毒性以及脱靶毒性，具有良好的药物安全性。3.远大医药引进RDC报胶质瘤IND。远大医药与Telix International 公司合作开发的放射性核素偶联药物(RDC) TLX101(131I-IPA)的新药临床试验(IND)申请获CDE受理，拟开发用于治疗多形性胶质母细胞瘤(GBM)。TLX101 (131I-IPA)可自由通过血脑屏障进入大脑，并靶向胶质母细胞瘤过度表达的L型氨基酸转运蛋白1（LAT-1）精准辐射癌细胞，促使其凋亡以达到治疗效果。此前，TLX101已在美国及欧洲获得孤儿药认定。4.天泽云泰基因疗法报IND。上海天泽云泰开发的基因替代疗法“VGT-I01”新药临床试验申请获CDE受理（受理号：CXSL2300080）。VGR-R01旨在通过回补正确拷贝的CYP4V2基因，介导RPE细胞表达CYP4V2蛋白。CYP4V2蛋白为P450酶家族成员，在视网膜色素上皮细胞（RPE）中高度表达，具有脂肪酸羟化酶活性，与脂肪代谢相关。这也是天泽云泰申报的第三款基因治疗药物。5.创盛桥康引进一款IPF药物。创盛桥康（CS Pharmaceuticals）与Daewoong公司达成独家许可协议，获得后者临床早期口服小分子脯氨酰-tRNA合成酶（PRS）抑制剂抗纤维化药物bersiporocin在大中华区开发和商业化授权。Bersiporocin已获得FDA授予治疗特发性肺纤维化的孤儿药资格以及快速通道资格。根据协议，Daewoong将获得高达7600万美元的预付款和开发里程碑付款以及两位数的净销售额分成，项目交易金额高达3.36亿美元。‍‍‍‍国‍‍‍‍‍‍‍‍‍‍际‍‍‍‍药‍讯‍‍1.Mesoblast公司干细胞疗法再报NDA。Mesoblast公司同种异体间充质干细胞疗法Remestemcel-L重新向FDA提交上市许可申请，用于治疗类固醇难治性急性移植物抗宿主病（SR-aGVHD）儿童患者。新的临床数据显示，与西奈山医院数据库中未接受remestemcel-L治疗的儿科患者相比，接受remestemcel治疗的患儿六个月生存率更高（67%vs10%）。在日本，remestemcel-L已获批用于治疗患有SR-aGVHD的儿童和成人患者。2.创新TCR-T疗法向FDA滚动递交NDA。Adaptimmune公司靶向MAGE-A4抗原的TCR-T细胞疗法Afami-cel滚动向FDA提交上市申请，用于治疗晚期滑膜肉瘤。Afami-cel能够有效地激活和促进增殖性细胞毒性T细胞浸润到肿瘤中，有助于抗肿瘤反应。公布在CTOS2022年会上的关键临床数据显示，afami-cel在滑膜肉瘤患者中的缓解率达到38.6%，中位缓解持续时间为50.3周。如果获批，Afami-cel有望成为首款针对实体瘤的TCR-T疗法。3.Karuna公司囊获多款精神病候选疗法。Karuna Therapeutics宣布，从Goldfinch Bio获得多款拟用于治疗多种精神病和神经疾病的TRPC4/5（瞬时受体电位通道4和5）靶向候选疗法，其中先导候选疗法GFB-887已处于Ⅱ期临床开发阶段。TRPC4/5在先天恐惧功能方面起到重要作用，是动物对环境应急因子的关键反应。在临床前研究中，GFB-887已在情绪和焦虑障碍的临床前模型中显示出显著益处。4.Alto Neuroscience融资推进四项Ⅱ期临床。精神病学药物公司Alto Neuroscience宣布完成约6000万美元B轮融资，以用于支持其创新药物候选疗法开展四项Ⅱ期临床试验。该公司靶向环磷酸腺苷（cAMP）信号通路的创新药物组合（ALTO-103和ALTO-104）已在去年12月获得Ⅰ期研究积极结果；靶向脑源性神经营养因子（BDNF）在研疗法ALTO-100也在治疗抑郁症（MDD）的Ⅱa期临床达到主要研究终点，显著降低带有生物标志物MDD患者的MADRS抑郁量表评分（降低15.5分）。5.默沙东2022年K药收入超200亿美元。2月2日，默沙东公布2022年业绩报告，全年超预期营收592.83亿美元，同比增长22%，扣除新冠口服药Lagevrio（莫诺拉韦，56.84亿美元）影响后，同比增长12%。默沙东制药业务收入520.05亿美元，同比增长22%；其中PD-1抑制剂Keytruda全年销售209.37亿美元，同比增长22%；HPV疫苗Gardasil/Gardasil 9销售额约70亿美元，同比增长22%。6.BioNTech首个质粒DNA制造工厂建成。BioNTech公司宣布，已在德国马尔堡建设完成首个专有质粒DNA生产工厂，预计新的生产设施的总投资约为4000万欧元。质粒DNA制造工厂的建成旨在提高BioNTech在其肿瘤学和COVID-19疫苗管线生产起始材料的灵活性和自主性，以及公司因本地生产而在大流行病防范方面的独立性。质粒DNA是制造基于mRNA的疫苗和疗法以及细胞疗法的重要材料。‍‍‍‍‍‍‍‍医‍‍‍‍‍药‍‍‍‍‍‍‍‍热‍‍‍‍‍点‍‍‍‍‍‍‍‍1.贾伟平院士加盟昆明医科大学。2月3日，贾伟平院士授聘为昆明医科大学名誉教授、昆明医科大学第一附属医院临床医学研究中心主任，授聘仪式在昆医大附一院报告厅举行。根据公开信息，贾伟平，女，1956年11月出生，江苏镇江人。1993年毕业于西安医科大学，获硕士学位，2003年获上海第二医科大学博士学位。上海交通大学特聘教授，博士生导师，现任上海市糖尿病研究所所长，国家基层糖尿病防治管理办公室主任。2.北京市疾控局成立。日前，北京市卫健委在其官方网站更新领导信息。信息显示，曾晓芃任北京市卫生健康委党委委员、副主任（兼），市疾控局局长，市疾控中心党委副书记、主任。这意味着北京市疾控局已组建成立。官方公布的简历显示，曾晓芃专业背景深厚，曾主持多项科技部“十五”和“十一五”国家科技攻关和支撑计划等课题研究与国家标准的制定，参与多项国家推荐性标准、行业标准的起草工作。3.山西增福利减负担鼓励生育。近日，山西省政府印发《关于优化生育政策促进人口长期均衡发展的实施方案》指出，严格落实产假、护理假、育儿假、哺乳假等制度，符合政策规定生育子女的，女方在国家及该省规定产假的基础上，奖励延长产假60日，男方有护理假15日。推动实行父母育儿假制度，符合政策规定生育且子女不满3周岁的，夫妻双方所在单位分别给予每年不少于15日的育儿假，并可分别每月发放不低于200元的婴幼儿保教费。‍‍‍‍‍‍评‍‍‍审‍‍动态‍‍‍‍‍‍ 1. CDE新药受理情况（02月04日) 2. FDA新药获批情况（北美02月03日）股市资讯上个交易日 A 股医药板块 -0.64%涨幅前三跌幅前三济民医疗+10.02% 神州细胞 -7.10%赛科希德 +9.40% 华兰疫苗 -6.84%万孚生物 +6.59% 金迪克 -6.77%【戴维医疗】全资子公司维尔凯迪的产品“鼻氧管”获得第一类医疗器械备案凭证。【上海医药】全资子公司上海第一生化的产品“注射用比伐芦定”获得批准生产。【广生堂】乙肝治疗创新药GST-HG141片II期多中心临床试验首例受试者成功入组。- The End -戳“阅读原文”，了解更多医药研发及股市资讯。

临床申请孤儿药抗体药物偶联物信使RNA基因疗法

100 项与 Pimitespib 相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14876

研发状态

适应症	最高研发状态	国家/地区	公司
胃肠道间质瘤	批准上市	日本更多	Taiho Pharmaceutical Co., Ltd. 更多
实体瘤	无进展	日本更多	-
晚期恶性实体瘤	无进展	英国更多	Taiho Oncology, Inc. 更多

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05245968 (CHAPTER-GIST-101, ESMO2023) 人工标引	临床1期	胃肠道间质瘤二线	12	Pimitespib + Imatinib	積構壓鏇築觸醖壓獵積(積衊鏇廠糧製選選構淵) = 鹹遞憲網簾襯繭齋鹽簾積膚壓鬱繭鹹廠醖醖鹹 (蓋鏇淵糧積鏇襯觸夢選 ) 更多	积极	2023-10-21
ERS2022	N/A	肺纤维化 HSP90	-	TAS-116	獵夢鏇襯繭遞淵憲願獵(鹽鑰憲醖選憲顧鏇糧選) = Mice treated with TAS-116, starting either 24h or 96h after HCl exposure, demonstrated downregulation of TGFβ signaling 淵鏇簾獵鏇獵簾夢簾獵 (積夢壓蓋製壓艱製鑰鑰 ) 更多	-	2022-09-04
JPRN-JapicCTI-184094 (ASCO2021)	临床3期	胃肠道间质瘤	86	Pimitespib 160 mg	鬱顧網糧鹽獵夢壓觸醖(夢鹽齋鏇鹹鏇壓製衊遞) = 壓憲築憲顧鬱糧糧遞蓋觸夢觸遞鬱艱齋蓋夢網 (顧顧衊簾鹹範構蓋壓衊, 9.2–not reached) 更多	积极	2021-05-28
JPRN-JapicCTI-184094 (ASCO2021)	临床3期	胃肠道间质瘤	86	Placebo	鬱顧網糧鹽獵夢壓觸醖(夢鹽齋鏇鹹鏇壓製衊遞) = 積鬱網鏇醖艱鑰醖壓餘觸夢觸遞鬱艱齋蓋夢網 (顧顧衊簾鹹範構蓋壓衊, 5.5–not reached) 更多	积极	2021-05-28
JPRN-UMIN000032801 (EPOC1704, ASCO2020)	临床1期	实体瘤 \| 结直肠癌	44	TAS-116 plus nivolumabTAS-116 plus nivolumab	鏇衊範鑰積獵蓋鑰衊鏇(製鑰齋築鑰鏇繭淵艱齋) = 築餘繭鑰繭齋築艱夢繭選願繭襯積鑰獵製網衊 (繭衊鬱襯夢繭繭齋觸繭 ) 更多	积极	2020-05-25
NCT02965885 (ASCO2017) 人工标引	临床1期	晚期恶性实体瘤	52	Pimitespib	淵鹽遞鬱繭鑰遞願衊築(遞醖憲鑰觸齋遞夢衊積) = gastrointestinal disorders and increased creatinine 願衊壓網衊鹽膚壓顧衊 (壓鏇構糧醖淵願衊蓋鑰 )	积极	2017-06-05
NCT02965885 (ASCO2017) 人工标引	临床1期	晚期恶性实体瘤	52	Pimitespib (QD)		积极	2017-06-05