Although many phase III clinical trials evaluate the quality of life as a secondary endpoint, male sexuality remains a neglected topic in oncology research. In light of the long-term efficacy of new-generation anticancer treatments for ANSCLC (i.e. targeted therapies and immunotherapy), there is a paucity of data about any detrimental effect on fertility and sexuality that could complicate the therapy proposal, especially in young patients.
The aim of this trial is to assess incidence of endocrine toxicity and sexual dysfuction in male patients receiving active treatment for ANSCLC

开始日期2024-08-05

申办/合作机构-

NCT06458036

/ Recruiting临床2期

Selpercatinib to Enhance RAI Avidity in Children, Adolescents, and Young Adults With Newly Diagnosed Differentiated Thyroid Cancers Harboring RET Fusions

Papillary thyroid cancer (PTC) is the most common form of differentiated thyroid cancer (DTC). The traditional first line treatment for patients with advanced DTC after surgical resection is radioactive iodine (RAI) therapy. However, less than a quarter of patients with lung metastases will achieve a complete response to RAI therapy, and this therapy carries the risk of pulmonary fibrosis and an increasingly recognized risk of secondary malignancies.

开始日期2024-07-29

申办/合作机构

The Children's Hospital of Philadelphia

[+2]

CTR20233072

/ RecruitingN/A

一项评价塞普替尼胶囊（Selpercatinib Capsules）治疗晚期或转移性RET基因融合阳性甲状腺癌（成人和儿童）患者有效性和安全性的（前瞻性、非干预性、）上市后观察性研究

主要目的：通过评估中国晚期或转移性RET基因融合阳性甲状腺癌患者的rwORR，评价塞普替尼的有效性。次要目的：通过评估中国晚期或转移性RET基因融合阳性甲状腺癌患者的rwPFS、rwDoR和rwDCR，评价塞普替尼的有效性。探索性目的：描述塞普替尼的安全性特征。考察塞普替尼在真实世界诊疗常规中的治疗模式

开始日期2023-12-25

申办/合作机构

Eli Lilly & Co.

[+2]

100 项与塞普替尼相关的临床结果

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100 项与塞普替尼相关的转化医学

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100 项与塞普替尼相关的专利（医药）

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473

项与塞普替尼相关的文献（医药）

2025-06-01·JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

Separation, characterization and cytotoxicity of unknown forced degradation impurity of selpercatinib using Prep-LC, HRMS and NMR

Article

作者: Sun, Rongwei ; Wu, Wenyi ; Wang, Qin ; Cai, Liangliang

Selpercatinib (LOXO-292) is a newly marketed oral selective receptor tyrosine kinase inhibitor targeting rearranged during transfection (RET), demonstrating precise therapeutic effects against RET-positive non-small cell lung cancer and thyroid cancer. In this study, an unknown acid forced degradation impurity of selpercatinib, designated sel-1, was isolated and purified using semi-preparative liquid chromatography (semi-Prep-LC). The purified sel-1 showed a chromatographic purity of 99.1 % as determined by high-performance liquid chromatography (HPLC). It appeared as a white amorphous powder, with a maximum absorption peak at 235 nm and a chemical formula of C₂₈H₂₉N₇O₃. Its molecular structure was elucidated using high-resolution mass spectrometry (HRMS) and nuclear magnetic resonance (NMR). sel-1 was identified as 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-oxo-1,6-dihydropyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile. In vitro MTT assays revealed that sel-1 exhibited significant antitumor activity, particularly against HepaRG and MKN-1 cell lines, with stronger inhibition than selpercatinib. The study contributes to enhancing the quality control standards for selpercatinib and suggests that sel-1 holds potential for further drug development.

2025-04-01·JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES

Rapid and sensitive HPLC with fluorescence detection method for quantifying selpercatinib in liver microsomes and rat plasma: Implications for drug-drug interaction studies

Article

作者: Alshekhhossin, Aysheh M ; Al Hroot, Jomana ; Zayed, Aref L ; Al Kilani, Omar M ; Jaber, Sana'a A ; Dawood, Leen L ; Alzarieni, Kawthar Z

Selpercatinib (RETEVMO®) is a selective anticancer agent recently approved for thyroid and non-small cell lung cancer. Reliable analytical methods are essential for investigating its potential drug interactions. In this study, the fluorescence properties of selpercatinib were exploited for the first time to develop a sensitive high-performance liquid chromatography with fluorescence detection (HPLC-FLD) method to quantify selpercatinib in human and rat liver microsomes and rat plasma. The method was successfully validated according to M10 guidelines demonstrating excellent accuracy, precision, selectivity, and sensitivity across a concentration range of (50-2000) ng/mL in plasma samples, with a short run time of less than 4 min. The method was applied to metabolic stability studies, where selpercatinib exhibited moderate intrinsic clearance (CL_int) in human liver microsomes (CL_int of 44.9 μL/min/mg), low clearance in female rat liver microsomes (CL_int 10.6 μL/min/mg), and nearly no depletion in male rat liver microsomes. After treatment with dexamethasone, the clearance of selpercatinib was enhanced in both female and male rat liver microsomes, suggesting potential drug-drug interaction. Dexamethasone-treated female rat liver microsomes showed clearance similar to human liver microsomes, indicating their suitability as a surrogate model for studying human metabolism in vitro. Additionally, the inhibitory effect of myricetin on selpercatinib metabolism was comparable in both human and dexamethasone-treated female rat liver microsomes, with IC₅₀ values of 9.3 μM and 10.9 μM, respectively. These findings suggest the need to investigate these potential drug interactions in clinical settings, as they may affect selpercatinib efficacy and toxicity. This HPLC-FLD method offers a rapid, sensitive, and cost-effective alternative to LC-MS/MS for studying pharmacokinetics in various in vitro and in vivo models.

2025-04-01·MOLECULAR DIVERSITY

Targeting AFP-RARβ complex formation: a potential strategy for treating AFP-positive hepatocellular carcinoma

Article

作者: Dev, Radul R ; Soman, Sowmya ; Banjan, Bhavya ; Raju, Rajesh ; Vishwakarma, Riya ; Kalath, Haritha ; Rehman, Niyas ; Revikumar, Amjesh ; Kumar, Pankaj ; Abhinand, Chandran S ; Ramakrishnan, Krishnapriya

Alpha-fetoprotein (AFP) is a glycoprotein primarily expressed during embryogenesis, with declining levels postnatally. Elevated AFP levels correlate with pathological conditions such as liver fibrosis, cirrhosis, and hepatocellular carcinoma (HCC). Recent investigations underscore AFP's intracellular role in HCC progression, wherein it forms complexes with proteins like Phosphatase and tensin homolog (PTEN), Caspase 3 (CASP3), and Retinoic acid receptors and Retinoid X receptors (RAR/RXR). RAR and RXR regulate gene expression linked to cell death and tumorigenesis in normal physiology. AFP impedes RAR/RXR dimerization, nuclear translocation, and function, promoting gene expression favoring cancer progression in HCC that provoked us to target AFP as a drug candidate. Despite extensive studies, inhibitors targeting AFP to disrupt complex formation and activities remain scarce. In this study, employing protein-protein docking, amino acid residues involved in AFP-RARβ interaction were identified, guiding the definition of AFP's active site for potential inhibitor screening. Currently, kinase inhibitors play a significant role in cancer treatment and, the present study explores the potential of repurposing FDA-approved protein kinase inhibitors to target AFP. Molecular docking with kinase inhibitors revealed Lapatinib as a candidate drug of the AFP-RARβ complex. Molecular dynamics simulations and binding energy calculations, employing Mechanic/Poisson-Boltzmann Surface Area (MM-PBSA), confirmed Lapatinib's stability with AFP. The study suggests Lapatinib's potential in disrupting the AFP-RARβ complex, providing a promising avenue for treating molecularly stratified AFP-positive HCC or its early stages.

615

项与塞普替尼相关的新闻（医药）

2025-03-27

·PRNewswire

Innovent to Present Preclinical Data of Multiple Novel Molecules at the 2025 AACR Annual Meeting

SAN FRANCISCO and SUZHOU, China, March 26, 2025 /PRNewswire/ -- Innovent Biologics, Inc. ("Innovent") (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high quality medicines for the treatment of oncology, cardiovascular and metabolic, autoimmune, ophthalmology and other major diseases, announces that preclinical data on multiple novel bispecific antibodies as well as antibody-drug-conjugates (ADCs) from its oncology pipeline will be presented at the American Association for Cancer Research (AACR) Annual Meeting 2025. The AACR Annual Meeting will take place from April 25 to April 30, 2025, in Chicago, Illinois. Late-Breaking Research: Immunology 2 Topic: Preclinical Data of IAR037, A Novel CD40/PD-L1 Bispecific Antibody for the Treatment of Advanced Solid Tumors Resistant to Immune Checkpoint Inhibitors Abstract Number: LB139 Presentation Time ：Monday Apr 28, 2025 9:00 AM - 12:00 PM Location: Poster Section 52 Late-Breaking Research: Clinical Research 1 Topic: Preclinical characterization of IBI3010, a FRα targeting biparatopic antibody-drug conjugate (ADC), for the treatment of FRα expressing tumors Abstract Number: LB222 Presentation Time ：Monday Apr 28, 2025 2:00 PM - 5:00 PM Location: Poster Section 53 Poster Session: Experimental and Molecular Therapeutics - New and Emerging Cancer Drug Targets Topic: IBI3019, a first-in-class EGFR/CDH17/CD16A tri-specific antibody, demonstrated potent efficacy against CRC and an excellent safety profile in preclinical studies Abstract Number: 4249 Presentation Time: Tuesday Apr 29, 2025 9:00 AM - 12:00 PM Location: Poster Section 17 Poster Board Number: 6 Poster Session: Experimental and Molecular Therapeutics - Therapeutic Approaches to Attack the Tumor Microenvironment Topic: IBI3026, a first-in-class anti-PD-1/IL-12 fusion protein, demonstrates the potential to be a new immuno-oncology therapy by releasing the break in immune response and strongly activating T and NK cells in the tumor microenvironment Abstract Number: 3118 Presentation Time: Monday Apr 28, 2025 2:00 PM - 5:00 PM Location: Poster Section 24 Poster Board Number: 2 Poster Session: Experimental and Molecular Therapeutics - Biochemical Modulators of Cancer / Differentiation Therapeutic Strategies Topic: IBI3014, a TROP2xPD-L1 bi-specific ADC integrating ADC killing with checkpoint blockade within one molecule, exhibits promising efficacy and safety in preclinical models Abstract Number: 344 Presentation Time: Sunday Apr 27, 2025 2:00 PM - 5:00 PM Location: Poster Section 16 Poster Board Number: 11 Poster Session: Experimental and Molecular Therapeutics - Biochemical Modulators of Cancer / Differentiation Therapeutic Strategies Topic: Trop2 and B7H4 bi-specific ADC with improved efficacy and safety for gynecologic cancers Abstract Number: 345 Presentation Time: Sunday Apr 27, 2025 2:00 PM - 5:00 PM Location: Poster Section 16 Poster Board Number: 12 Poster Session: Immunology - T Cell Engagers Topic: A 2+1 format MUC16 targeting T cell engager induces MUC16-dependent T cell activity and superior anti-tumor efficacy Abstract Number: 3510 Presentation Time: Monday Apr 28, 2025 2:00 PM - 5:00 PM Location: Poster Section 38 Poster Board Number: 18 Poster Session: Immunology - Modulation of Tumor Microenvironment: Modulation of Lymphocyte Influx Topic: A PD1-IFNα fusion protein, composed of an attenuated IFNα fused to a clinically validated PD1 mAb, induced PD1-dependent IFNα signaling and demonstrated superior anti-tumor efficacy Abstract Number: 4881 Presentation Time: Tuesday Apr 29, 2025 9:00 AM - 12:00 PM Location: Poster Section 40 Poster Board Number: 9 Poster Session: Experimental and Molecular Therapeutics - Novel Antitumor Agents 3 Topic: Olverembatinib* (HQP1351) in combination with lisaftoclax (APG-2575) overcomes venetoclax resistance in preclinical models of acute myeloid leukemia (AML) Abstract Number: 5652 Presentation Time: Tuesday Apr 29, 2025 2:00 PM – 5:00 PM Poster Session: Experimental and Molecular Therapeutics - Novel Antitumor Agents 3 Topic: Effects of olverembatinib* (HQP1351) in combination with BCL-2 inhibitor lisaftoclax (APG-2575) in T-cell acute lymphoblastic leukemia (T ALL) Abstract Number: 5648 Presentation Time: Tuesday Apr 29, 2025 2:00 PM – 5:00 PM * In July 2021, Innovent and Ascentage Pharma (6855.HK) reached the agreement regarding the joint development and commercialization of olverembatinib in China. Dr. Kaijie He, Vice President of Innovent, stated: "With the expansion and enhancement of Innovent Academy's technology platforms, our global R&D efforts are taking shape and accelerating global competitiveness, enabling the efficient generation of novel molecules with global potential. We are proud to showcase a batch of preclinical research findings at this year's AACR Annual Meeting, including multiple globally first-in-class bispecific antibodies, multi-specific antibodies, and antibody-drug conjugates (ADCs). These breakthroughs not only demonstrate our growing scientific capabilities but also reaffirm our commitment to delivering transformative therapeutic options for patients worldwide. Moving forward, we remain focused on innovation—optimizing precision targets and exploring novel mechanisms—to provide revolutionary solutions for some of the world's most challenging diseases and enable more patients to benefit from the rapid advancements in cutting-edge science." About Innovent Innovent is a leading biopharmaceutical company founded in 2011 with the mission to empower patients worldwide with affordable, high-quality biopharmaceuticals. The company discovers, develops, manufactures and commercializes innovative medicines that target some of the most intractable diseases. Its pioneering therapies treat cancer, cardiovascular and metabolic, autoimmune and eye diseases. Innovent has launched 15 products in the market. It has 3 new drug applications under regulatory review, 3 assets in Phase III or pivotal clinical trials and 16 more molecules in early clinical stage. Innovent partners with over 30 global healthcare companies, including Eli Lilly, Sanofi, Incyte, Adimab, LG Chem and MD Anderson Cancer Center. Guided by the motto, "Start with Integrity, Succeed through Action," Innovent maintains the highest standard of industry practices and works collaboratively to advance the biopharmaceutical industry so that first-rate pharmaceutical drugs can become widely accessible. For more information, visit , or follow Innovent on Facebook and LinkedIn. Statement: （1）Innovent does not recommend the use of any unapproved drug (s)/indication (s). （2）Ramucirumab (Cyramza®) and Selpercatinib (Retsevmo®) and Pirtobrutinib (Jaypirca®) were developed by Eli Lilly and Company. Forward-looking statement This news release may contain certain forward-looking statements that are, by their nature, subject to significant risks and uncertainties. The words "anticipate", "believe", "estimate", "expect", "intend" and similar expressions, as they relate to Innovent Biologics ("Innovent"), are intended to identify certain of such forward-looking statements. The Company does not intend to update these forward-looking statements regularly. These forward-looking statements are based on the existing beliefs, assumptions, expectations, estimates, projections and understandings of the management of the Company with respect to future events at the time these statements are made. These statements are not a guarantee of future developments and are subject to risks, uncertainties and other factors, some of which are beyond the Company's control and are difficult to predict. Consequently, actual results may differ materially from information contained in the forward-looking statements as a result of future changes or developments in our business, the Company's competitive environment and political, economic, legal and social conditions. The Company, the Directors and the employees of the Company assume (a) no obligation to correct or update the forward-looking statements contained in this site; and (b) no liability in the event that any of the forward-looking statements does not materialise or turn out to be incorrect. SOURCE Innovent Biologics WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

AACR会议抗体药物偶联物免疫疗法

2025-03-25

·信达生物

信达生物2024年度业绩亮点

率先实现盈利转正，迈进双轮驱动和全球发展新时期 2025年3月26日，美国旧金山和中国苏州——信达生物制药集团（香港联交所股票代码：01801），一家致力于研发、生产和销售肿瘤、代谢及心血管、自身免疫、眼科等重大疾病领域创新药物的生物制药公司公布2024年度业绩，汇报公司业务进展，财务表现及中长期发展战略。信达生物制药集团创始人、董事长兼CEO俞德超博士表示：“作为中国生物制药行业可持续发展的先行者，2024年我们取得了历史性突破——公司率先实现了Non-IFRS净利润和EBITDA转正。过去一年，公司收入创下新高，商业化产品组合扩充至15款，研发里程碑全面兑现。早期创新管线也频频取得突破，有望迎来全球开发新机遇，全球战略合作加速布局。清晰的战略指引和卓越的执行力为我们奠定了坚实的基础盘，2025年将是公司步入双轮驱动和全球创新的关键一年。我们将保持在肿瘤领域的领先地位，实现慢病商业化的成功启航，并将新一代创新管线推向全球开发。信达将锚定2027年实现200亿产品收入、2030年实现5个管线进入全球三期临床的战略性目标，朝着成长为国际一流的生物制药企业不断努力，为我们的患者、员工、股东及社会持续创造价值。” 率先实现盈利转正，稳步迈向2027年200亿目标首次实现Non-IFRS净利润和EBITDA转正* ⚬ 净利润3.3亿元; EBITDA (息税折旧摊销前利润) 4.1亿元 ⚬ 毛利率84.9%，同比上升2.1个百分点 ⚬ 销售和行政开支比率50.9%，同比下降7.1个百分点 ⚬ 研发投入25.0亿元；现金储备102.2亿元人民币，折合超14亿美元，为公司长期发展提供坚实保障收入再创新高，树立优秀的企业品牌和产品品牌 ⚬ 总收入 94.2亿，同比增长51.8% ⚬ 产品收入 82.3亿，同比增长43.6% ⚬ 成为肿瘤治疗领域领导品牌，持续拓展和医保覆盖 ⚬ 建设慢病全方位商业化平台，致力成为慢病领域创新领先企业 2025年迎来六款新品上市和双轮驱动 ⚬ 肺癌和血液瘤领域新添三款靶向精准疗法：达伯乐® （己二酸他雷替尼胶囊）-潜在同类最佳的ROS1抑制剂；奥壹新® （利厄替尼片）-第三代EGFR TKI 肺癌靶向药；捷帕力® （匹妥布替尼片）-血液瘤首个非共价BTK抑制剂； ⚬ 慢病突破性药物陆续上市，打造第二增长极信必乐® （托莱西单抗注射液）:首个且唯一纳入国家医保的中国原研PCSK9抑制剂；信必敏® (替妥尤单抗N01注射液):中国首个获批的IGF-1R单抗，七十年来治疗甲状腺眼病的突破性创新药；计划新开临床研究，拓展至一线和非活动期甲状腺眼病；玛仕度肽(GCG/GLP-1): 全球首个GCG/GLP-1双重激动剂，两项NDA在NMPA审评中，针对减重及2型糖尿病（T2D）;新III期临床研究将启动，包括青少年肥胖、阻塞性睡眠呼吸暂停（OSA）及头对头司美格鲁肽2.4mg治疗肥胖合并代谢相关性脂肪性肝病(MAFLD)。此外，还将启动代谢相关脂肪性肝炎(MASH)，射血分数保留心力衰竭(HFpEF)和高剂量用药的新临床研究；匹康奇拜单抗 (IL-23p19)：同类最优的银屑病治疗长效生物制剂，用于治疗中重度斑块状银屑病的NDA在NMPA审评中。并计划新开临床研究，探索IL-17响应不佳的银屑病、青少年银屑病和银屑病关节炎（PsA）。稳步迈向2027年200亿收入目标 ⚬ 肿瘤+综合产品线双轮驱动的产品组合持续打开向上空间迈入全球研发新篇章到2030年实现5款创新管线进入全球III期临床研究 ⚬ 国清院聚焦创新技术平台 ⚬ 加速管线全球开发步伐 ⚬ 领航管线亮点频出，陆续步入后期开发 ⚬ IBI363(PD-1/IL-2α-bias)：全球首创下一代IO治疗候选分子肺癌、黑色素瘤、肠癌等均读出亮眼早期数据，挑战免疫治疗失败、PD-L1低表达甚至不表达冷肿瘤等有望取得突破性进展两获FDA快速审评通道（IO经治黑色素瘤和鳞肺癌）启动首个挑战Keytruda头对头关键临床研究，用于IO初治黏膜型和肢端型黑色素瘤全球开发加速进行中 ⚬ IBI343（CLDN18.2 ADC）：具有突破潜力的新一代ADC候选分子启动首个胃癌国际多中心三期临床研究中美开展胰腺癌国际多中心一期临床获CDE突破性疗法、FDA快速审评通道多项资格 ⚬ 推进近10款下一代创新管线进入全球开发：肿瘤：IBI3009(DLL3 ADC)、IBI3001(EGFR/B7H3双抗ADC)、IBI3020 (CEACAM5双载荷ADC) CVM：IBI3016（AGT siRNA）、IBI3032（口服GLP-1小分子）、IBI3012 (GGG抗体多肽偶联物)、IBI3030（GGG-PCSK9抗体多肽偶联物）自身免疫：IBI3002(TSLP/IL-4α双抗)、IBI356 （OX40L） ⚬ 多元化出海模式，加速全球化布局 IBI3009（DLL3 ADC）：授权罗氏全球开发，加速造福全球小细胞肺癌患者 ⚬ 高质量研究结果荣登国际知名学术会议肿瘤管线创新发现：AACR、ASCO、ESMO GI、ESMO Plenary、ESMO、WCLC、SITC、ESMO Asia 综合产品线重磅研究：ADA、APAO、ICE、CSE 拓展全球布局坚守高质量生产标准 ● 研发中心（医学）2024年8月正式启用 ● 2024年3月, 美国研发中心搬迁至更具创新力的加州 ● 截至目前，信达生物已投入使用的产能共14万升，占全国生物药总产能20% ● 第一基地6万升抗体产能和ADC产业化生产线，保障高质量产能供应 ● 第二基地8万升已建成抗体产能，保障全球供应和CDMO业务高质量可持续发展切实践行ESG承诺 ● MSCI ESG评级跃升至AAA，在中国医药行业处于领先水平 ● 推出ESG网站，加强ESG管理实践，践行可持续发展与企业责任承诺 ● 启动“爱心驿站”，让“城市守护者”感受信达温度；发起第三届“童书乐捐”公益活动，“书”送希望与爱心。 ● 发起、参与多项患者援助项目，累计已惠及20余万普通患者，药物捐赠总价值36亿元人民币。 ● 荣获“医疗公益推动者”公益荣誉奖项和 “中国公益企业”称号，来自社会各界的认可，激励着我们持续回馈社会！ ● 再度荣登《2024中国最具吸引力雇主榜单》。信达生物共有7000名员工，累计为应届生提供1800多份就业岗位。 ● 截至目前，信达生物制药集团累计纳各类税费等50多亿人民币。关于信达生物 “始于信，达于行”，开发出老百姓用得起的高质量生物药，是信达生物的使命和目标。信达生物成立于2011年，致力于研发、生产和销售肿瘤、自身免疫、代谢、眼科等重大疾病领域的创新药物，让我们的工作惠及更多的生命。公司已有15个产品获得批准上市，它们分别是信迪利单抗注射液（达伯舒®），贝伐珠单抗注射液（达攸同®），阿达木单抗注射液（苏立信®），利妥昔单抗注射液（达伯华®），佩米替尼片（达伯坦®），奥雷巴替尼片（耐立克®），雷莫西尤单抗注射液（希冉择®），塞普替尼胶囊（睿妥®），伊基奥仑赛注射液（福可苏®），托莱西单抗注射液（信必乐®），氟泽雷塞片（达伯特®），匹妥布替尼片(捷帕力®)，己二酸他雷替尼胶囊（达伯乐®），利厄替尼片（奥壹新®）和替妥尤单抗N01注射液（信必敏®）。目前，同时还有3个品种在NMPA审评中，4个新药分子进入III期或关键性临床研究，另外还有15个新药品种已进入临床研究。公司已与礼来、罗氏、赛诺菲、Adimab、Incyte和MD Anderson 癌症中心等国际合作方达成30多项战略合作。信达生物在不断自研创新药物、谋求自身发展的同时，秉承经济建设以人民为中心的发展思想。多年来，始终心怀科学善念，坚守“以患者为中心”，心系患者并关注患者家庭，积极履行社会责任。公司陆续发起、参与了多项药品公益援助项目，让越来越多的患者能够得益于生命科学的进步，买得到、用得起高质量的生物药。截至目前，信达生物患者援助项目已惠及20余万普通患者，药物捐赠总价值36亿元人民币。信达生物希望和大家一起努力，提高中国生物制药产业的发展水平，以满足百姓用药可及性和人民对生命健康美好愿望的追求。详情请访问公司网站：www.innoventbio.com或公司领英账号 www.linkedin.com/company/innovent-biologics/ 。声明：信达生物不推荐未获批的药品/适应症的使用。前瞻性声明本新闻稿所发布的信息中可能会包含某些前瞻性表述。这些表述本质上具有相当风险和不确定性。在使用“预期”、“相信”、“预测”、“期望”、“打算”及其他类似词语进行表述时，凡与本公司有关的，目的均是要指明其属前瞻性表述。本公司并无义务不断地更新这些预测性陈述。这些前瞻性表述乃基于本公司管理层在做出表述时对未来事务的现有看法、假设、期望、估计、预测和理解。这些表述并非对未来发展的保证，会受到风险、不确性及其他因素的影响，有些乃超出本公司的控制范围，难以预计。因此，受我们的业务、竞争环境、政治、经济、法律和社会情况的未来变化及发展的影响，实际结果可能会与前瞻性表述所含资料有较大差别。如需了解更多信息，敬请联系: 媒体：邮件： pr@innoventbio.com 电话：+86 512-69566088 投资者：邮件： ir@innoventbio.com 电话：+86 512-69566088 * 注：本文提及的财务数据，除非标明，均采用非国际财务报告准则(Non-IFRS)计量，详情请参阅集团业绩公告。

财报临床3期突破性疗法

2025-03-24

·信达生物

信达生物IBI354 (创新型HER2 ADC) 治疗铂耐药卵巢癌的III期临床研究完成首例受试者给药

2025年3月24日，美国旧金山和中国苏州——信达生物制药集团（香港联交所股票代码：01801），一家致力于研发、生产和销售肿瘤、自身免疫、代谢、眼科等重大疾病领域创新药物的生物制药公司宣布，IBI354 (HER2单克隆抗体-喜树碱衍生物偶联物，HER2 ADC）治疗HER2表达的铂耐药的卵巢癌、输卵管癌或原发性腹膜癌患者的随机、对照、多中心III期临床研究（HeriCare-Ovarian01）完成中国首例受试者给药。 HeriCare-Ovarian01（NCT06834672）是中国首个针对HER2表达（IHC 1+，2+或3+）的铂耐药卵巢癌的III期临床研究。该研究将对照IBI354与研究者选择的化疗之间的有效性和安全性。研究的主要终点为无进展生存期（PFS）和总生存期（OS）。此前，一项IBI354在晚期实体瘤受试者的多中心1/2期研究中，共入组87例铂耐药卵巢癌受试者，分别接受6~12mg/kg剂量，其中67例（67/87，77.0%）受试者既往接受过至少3种系统性抗肿瘤治疗方案。截至2024年7月24日，总体客观缓解率（ORR）为40.2%，疾病控制率（DCR）为81.6%。其中，在40例接受12mg/kg Q3W IBI354治疗的卵巢癌受试者中，ORR达到52.5%，DCR为90.0%；在HER2 IHC 1+的27例接受12mg/kg Q3W的受试者中，ORR达到55.6%，DCR为88.9%。截至数据截止日期，12mg/kg Q3W剂量组中位随访时间为6.5个月，无进展生存期（PFS）和缓解持续时间（DoR）尚未成熟。该研究数据已在2024年ESMO大会公布。同时在1/2期临床研究中（n=368），IBI354展示出优异的安全性信号。剂量爬坡至18mg/kg, 未发生DLT事件。三级及以上治疗相关不良事件（TRAE）的总体发生率为21.5%，导致剂量暂停的TRAE发生率为12.2%，导致剂量降低的TRAE发生率为2.4%，导致永久停药的TRAE总体发生率为1.6%，无导致死亡的TRAE。最常见的TRAE是恶心、白细胞计数降低和贫血。间质性肺炎发生率仅为1.6%，且均为1级。本项研究的主要研究者、重庆大学附属肿瘤医院周琦教授表示：“延长铂耐药卵巢癌的PFS和OS是亟待解决的临床问题。卵巢癌有反复复发的特点，最终导致铂耐药，非铂单药化疗是目前主要治疗措施，但疗效差，这是卵巢癌死亡率高的主要原因。HER2靶点作为一个成熟靶点，针对HER2的靶向治疗在乳腺癌和胃癌中已被证实具有较好的疗效。IBI354作为创新型抗HER2 ADC，在前期研究中看到其在HER2表达的铂耐药卵巢癌中表现出良好的抗肿瘤活性，尤其是针对HER2 表达较低（IHC 1+）的人群的疗效，与HER2表达较高人群的疗效相当，显示了IBI354独特的疗效，相较同类ADC常见或关注的毒性，具有更好的安全性，如间质性肺疾病、乏力、腹泻、脱发、眼毒性等，IBI354发生风险低。期待HeriCare-Ovarian01研究进展顺利，在3期研究获得积极的结果，希望IBI354可以为更多的不同程度HER2表达铂耐药卵巢癌患者带来生存获益。” 本项研究的主要合作研究者、浙江省肿瘤医院朱滔教授表示：“很高兴HeriCare-Ovarian01研究在我院完成首例入组。虽然卵巢癌的发病率低于宫颈癌和子宫内膜癌，居妇科恶性肿瘤的第三位，但死亡率却超过宫颈癌及子宫内膜癌之和，高居妇科癌症首位，是严重威胁妇女健康的恶性疾病。IBI354作为抗HER2单克隆抗体-喜树碱衍生物偶联物（ADC），初步研究结果提示在HER2表达的铂耐药卵巢癌观察到了令人鼓舞的客观缓解率和疾病控制率。同时，IBI354治疗展现出明显优于其它ADC的优秀临床安全性和治疗耐受性。目前已有的临床数据提示IBI354在铂耐药卵巢癌人群具有良好的开发前景，期待IBI354在HeriCare-Ovarian01研究中取得成功，为铂耐药卵巢癌患者带来新的治疗选择。" 信达生物制药集团高级副总裁周辉博士表示：“很高兴IBI354在HER2表达的铂耐药卵巢癌的临床III期研究完成首例受试者首次给药，也十分期待IBI354获得积极结果，为HER2表达的铂耐药卵巢癌患者提供更理想的治疗选择。ADC是信达生物战略布局的核心技术领域之一，我们结合世界领先的抗体工程和多套差异化的连接子-毒素（linker-payload）技术，打造了具有高度竞争力的创新型TOPO1i ADC技术平台SoloTx®。IBI354在前期研究中展现出了优异的安全和疗效数据，充分证明了信达生物ADC的平台价值与开发实力。我们将深度布局ADC和免疫治疗领域，着眼下一代创新，致力于为肿瘤患者带来更优的获益。” 关于卵巢癌 - 滑动查看更多介绍 - 卵巢癌（Ovarian Cancer, OC）是导致妇科癌症死亡的主要原因之一。根据国际癌症研究机构统计，2022年全球新发卵巢癌病例约为32.4万，死亡人数约20.6万[1]。中国新发约6.1万例，死亡人数约为3.3万例[2]。含铂化疗是进展期卵巢癌系统性治疗的首选。约70%的卵巢癌患者会在接受含铂化疗后复发，并最终发展为铂耐药[3]。铂耐药癌患者目前尚缺乏有效的治疗手段，现有证据为非铂单药化疗联合或不联合抗血管生成治疗，ORR仅约4-13.2%，中位总生存期（OS）仅约10.9-14个月[4-8]。铂耐药后卵巢癌缓存在巨大的未满足的临床需求，国内外指南中均推荐这部分患者参加临床试验。文献报道约38%的卵巢癌患者存在HER2表达[5]。目前国内尚无任何抗HER2治疗获批用于HER2表达的卵巢癌。关于IBI354 - 滑动查看更多介绍 - IBI354是抗HER2单克隆抗体-喜树碱衍生物偶联物，基于信达生物拥有自主知识产权的创新ADC 技术平台。基于此ADC平台，信达生物正在推进多款自研ADC分子的临床试验研究，并展现出优异的安全性和疗效信号。 IBI354药物抗体比（DAR）值为8，能够携带更多的毒素载荷到达肿瘤细胞；ADC分子具有良好的亲水性和优异的体内PK表现；毒素小分子有很强的细胞膜渗透能力，展现出更好的旁观者效应；血浆中游离毒素小分子浓度极低，带来更低的脱靶毒性和更好的安全性。IBI354不仅在多种荷瘤药理学模型中展现出了良好抗肿瘤活性，在HER2靶向治疗耐药和转移模型中也表现出了突出的抑瘤效力。从临床迫切需求出发，除了已经开展的铂耐药卵巢癌III期研究（HeriCare-Ovarian01），信达生物将布局IBI354在多个实体瘤适应症进行开发。关于信达生物 - 滑动查看更多介绍 - “始于信，达于行”，开发出老百姓用得起的高质量生物药，是信达生物的使命和目标。信达生物成立于2011年，致力于研发、生产和销售肿瘤、自身免疫、代谢、眼科等重大疾病领域的创新药物，让我们的工作惠及更多的生命。公司已有15个产品获得批准上市，它们分别是信迪利单抗注射液（达伯舒®），贝伐珠单抗注射液（达攸同®），阿达木单抗注射液（苏立信®），利妥昔单抗注射液（达伯华®），佩米替尼片（达伯坦®），奥雷巴替尼片（耐立克®），雷莫西尤单抗注射液（希冉择®），塞普替尼胶囊（睿妥®），伊基奥仑赛注射液（福可苏®），托莱西单抗注射液（信必乐®），氟泽雷塞片（达伯特®），匹妥布替尼片(捷帕力®)，己二酸他雷替尼胶囊（达伯乐®），利厄替尼片（奥壹新®）和替妥尤单抗N01注射液（信必敏®）。目前，同时还有3个品种在NMPA审评中，3个新药分子进入III期或关键性临床研究，另外还有16个新药品种已进入临床研究。公司已与礼来、罗氏、赛诺菲、Adimab、Incyte和MD Anderson 癌症中心等国际合作方达成30多项战略合作。信达生物在不断自研创新药物、谋求自身发展的同时，秉承经济建设以人民为中心的发展思想。多年来，始终心怀科学善念，坚守“以患者为中心”，心系患者并关注患者家庭，积极履行社会责任。公司陆续发起、参与了多项药品公益援助项目，让越来越多的患者能够得益于生命科学的进步，买得到、用得起高质量的生物药。截至目前，信达生物患者援助项目已惠及20余万普通患者，药物捐赠总价值36亿元人民币。信达生物希望和大家一起努力，提高中国生物制药产业的发展水平，以满足百姓用药可及性和人民对生命健康美好愿望的追求。详情请访问公司网站：www.innoventbio.com或公司领英账号：Innovent Biologics。声明： 1.信达生物不推荐未获批的药品/适应症的使用。 2.雷莫西尤单抗注射液（希冉择®）、塞普替尼胶囊（睿妥®）和匹妥布替尼片（捷帕力®）由礼来公司研发。参考文献 1.Bray, F., et al., Global cancer statistics 2022: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin, 2024. 74(3): p. 229-263. 2.Han, B., et al., Cancer incidence and mortality in China, 2022. J Natl Cancer Cent, 2024. 4(1): p. 47-53. 3.Armstrong, D.K., et al., NCCN Guidelines Insights: Ovarian Cancer, Version 1.2019. J Natl Compr Canc Netw, 2019. 17(8): p. 896-909. 4.Gaillard S, Oaknin A, Ray-Coquard I, et al. Lurbinectedin versus pegylated liposomal doxorubicin or topotecan in patients with platinum-resistant ovarian cancer: A multicenter, randomized, controlled, open-label phase 3 study (CORAIL). Gynecol Oncol. 2021;163(2):237-245. 5.Pujade-Lauraine E, Hilpert F, Weber B, et al. Bevacizumab combined with chemotherapy for platinum-resistant recurrent ovarian cancer: The AURELIA open-label randomized phase III trial [published correction appears in J Clin Oncol. 2014 Dec 10;32(35):4025]. J Clin Oncol. 2014;32(13):1302-1308. 6.Pujade-Lauraine E, Fujiwara K, Ledermann JA, et al. Avelumab alone or in combination with chemotherapy versus chemotherapy alone in platinum-resistant or platinum-refractory ovarian cancer (JAVELIN Ovarian 200): an open-label, three-arm, randomised, phase 3 study. Lancet Oncol. 2021;22(7):1034-1046. 7.Cannistra SA. Evaluating new regimens in recurrent ovarian cancer: how much evidence is good enough?. J Clin Oncol. 2010;28(19):3101-3103. 8.Naumann RW, Coleman RL. Management strategies for recurrent platinum-resistant ovarian cancer. Drugs. 2011;71(11):1397-1412. 9.Yoon, J. and D.Y. Oh, HER2-targeted therapies beyond breast cancer - an update. Nat Rev Clin Oncol, 2024. 21(9): p. 675-700. 前瞻性声明本新闻稿所发布的信息中可能会包含某些前瞻性表述。这些表述本质上具有相当风险和不确定性。在使用“预期”、“相信”、“预测”、“期望”、“打算”及其他类似词语进行表述时，凡与本公司有关的，目的均是要指明其属前瞻性表述。本公司并无义务不断地更新这些预测性陈述。这些前瞻性表述乃基于本公司管理层在做出表述时对未来事务的现有看法、假设、期望、估计、预测和理解。这些表述并非对未来发展的保证，会受到风险、不确性及其他因素的影响，有些乃超出本公司的控制范围，难以预计。因此，受我们的业务、竞争环境、政治、经济、法律和社会情况的未来变化及发展的影响，实际结果可能会与前瞻性表述所含资料有较大差别。

临床结果临床3期抗体药物偶联物临床2期

100 项与塞普替尼相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11713	塞普替尼	L01XE	DB15685

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
RET融合阳性实体瘤	美国	Eli Lilly & Co.	2024-04-10
转移性非小细胞肺癌	美国	Eli Lilly & Co.	2022-09-21
转移性实体瘤	美国	Eli Lilly & Co.	2022-09-21
甲状腺髓样癌	美国	Eli Lilly & Co.	2022-09-21
RET融合阳性非小细胞肺癌	欧盟	Eli Lilly Nederland BV	2021-02-11
RET融合阳性非小细胞肺癌	冰岛	Eli Lilly Nederland BV	2021-02-11
RET融合阳性非小细胞肺癌	列支敦士登	Eli Lilly Nederland BV	2021-02-11
RET融合阳性非小细胞肺癌	挪威	Eli Lilly Nederland BV	2021-02-11
RET融合阳性甲状腺癌	欧盟	Eli Lilly Nederland BV	2021-02-11
RET融合阳性甲状腺癌	冰岛	Eli Lilly Nederland BV	2021-02-11
RET融合阳性甲状腺癌	列支敦士登	Eli Lilly Nederland BV	2021-02-11
RET融合阳性甲状腺癌	挪威	Eli Lilly Nederland BV	2021-02-11
非小细胞肺癌	美国	Eli Lilly & Co.	2020-05-08
RET突变阳性甲状腺髓样癌	美国	Eli Lilly & Co.	2020-05-08
甲状腺癌	美国	Eli Lilly & Co.	2020-05-08

未上市

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
RET融合阳性肺腺癌	临床3期	美国	Eli Lilly & Co.	2021-12-20
RET融合阳性肺腺癌	临床3期	中国	Eli Lilly & Co.	2021-12-20
RET融合阳性肺腺癌	临床3期	日本	Eli Lilly & Co.	2021-12-20
RET融合阳性肺腺癌	临床3期	澳大利亚	Eli Lilly & Co.	2021-12-20
RET融合阳性肺腺癌	临床3期	奥地利	Eli Lilly & Co.	2021-12-20
RET融合阳性肺腺癌	临床3期	比利时	Eli Lilly & Co.	2021-12-20
RET融合阳性肺腺癌	临床3期	巴西	Eli Lilly & Co.	2021-12-20
RET融合阳性肺腺癌	临床3期	加拿大	Eli Lilly & Co.	2021-12-20
RET融合阳性肺腺癌	临床3期	捷克	Eli Lilly & Co.	2021-12-20
RET融合阳性肺腺癌	临床3期	丹麦	Eli Lilly & Co.	2021-12-20

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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


NCT05136404 (CTgov)	临床1期	-	42	Selpercatinib	築壓繭簾網製積衊艱襯(構製顧鹹製選廠簾憲襯) = 鹹壓鏇構鏇選鬱廠積餘夢衊選獵鏇鑰鏇觸艱襯 (簾簾鏇鏇築網窪觸廠廠, 艱壓製網築窪鏇壓糧獵 ~ 艱鹽顧窪願糧網繭製築) 更多	-	2025-03-25
NCT05324124 (CTgov)	临床1期	-	46	Selpercatinib (Selpercatinib Fasted (Reference))	繭鏇衊鬱襯齋夢獵鏇膚(淵齋獵餘鏇膚壓顧衊蓋) = 夢餘壓蓋積遞獵顧製網廠衊淵顧壓繭醖遞鑰膚 (觸鹹壓積醖膚襯鏇廠範, 32) 更多	-	2025-03-21
				Selpercatinib (Selpercatinib Fed (Test))	繭鏇衊鬱襯齋夢獵鏇膚(淵齋獵餘鏇膚壓顧衊蓋) = 鹽衊遞獵獵選築鏇製膚廠衊淵顧壓繭醖遞鑰膚 (觸鹹壓積醖膚襯鏇廠範, 44) 更多
NCT05089019 (CTgov)	临床1期	-	224	Selpercatinib (160 mg Selpercatinib (Reference))	醖膚鏇鹽鬱顧範餘願壓(範積構鹹窪蓋淵選積憲) = 餘築衊餘願餘願願糧繭製蓋顧繭醖觸淵艱簾窪 (夢蓋鹽獵餘憲簾壓願憲, 61) 更多	-	2025-03-17
				Selpercatinib (160 mg Selpercatinib (Test))	醖膚鏇鹽鬱顧範餘願壓(範積構鹹窪蓋淵選積憲) = 鹹醖獵襯選衊鹹醖網夢製蓋顧繭醖觸淵艱簾窪 (夢蓋鹽獵餘憲簾壓願憲, 91) 更多
NCT04280081 (LIBRETTO-321, Pubmed \| Ther Adv Med Oncol) 人工标引	临床2期	RET融合阳性非小细胞肺癌 RET Positive	47	Selpercatinib	鏇醖艱襯窪獵壓鬱簾繭(構構鹽願艱願餘廠遞鹹) = 膚鏇鏇醖繭顧廠廠鑰衊壓衊製遞築繭壓選衊衊 (鬱衊窪願艱餘夢築繭簾, 57.4 ~ 84.4) 更多	积极	2025-01-01
				Selpercatinib (treatment-naïve)	鏇醖艱襯窪獵壓鬱簾繭(構構鹽願艱願餘廠遞鹹) = 鹽艱憲觸糧選艱鹹製鏇壓衊製遞築繭壓選衊衊 (鬱衊窪願艱餘夢築繭簾, 71.5 ~ 100.0) 更多
NCT05338502 (CTgov)	临床1期	-	20	Selpercatinib+Ranitidine (150 mg Ranitidine Dosed With 160 mg Selpercatinib)	築鹽艱衊餘齋願選鬱蓋(壓築窪鬱淵蓋蓋鹹蓋壓) = 獵餘網齋蓋窪窪淵糧淵願願淵構繭選膚鏇簾廠 (鑰鬱鑰夢選醖觸構製糧, 31.9) 更多	-	2024-10-30
				Selpercatinib+Omeprazole (40 mg Omeprazole Dosed With 160 mg Selpercatinib)	築鹽艱衊餘齋願選鬱蓋(壓築窪鬱淵蓋蓋鹹蓋壓) = 顧鏇鬱膚齋鏇衊遞範醖願願淵構繭選膚鏇簾廠 (鑰鬱鑰夢選醖觸構製糧, 27.4) 更多
NCT03157128 (LIBRETTO-001, ESMO2024)	临床1/2期	非小细胞肺癌 \| 甲状腺髓样癌	115	Selpercatinib	簾衊廠鬱窪構窪繭遞醖(膚憲築夢憲網繭膚齋遞) = 艱淵鬱選餘獵夢遞簾襯鏇鏇壓糧簾憲餘積艱廠 (積壓觸遞鏇願齋膚壓獵, 4 ~ 40)	积极	2024-09-14
				Placebo	簾衊廠鬱窪構窪繭遞醖(膚憲築夢憲網繭膚齋遞) = 製齋鏇觸窪選醖製膚鑰鏇鏇壓糧簾憲餘積艱廠 (積壓觸遞鏇願齋膚壓獵 )
NCT04194944 \| NCT03157128 (LIBRETTO-431, WCLC2024) 人工标引	N/A	RET融合阳性非小细胞肺癌 RET+	415	Selpercatinib (KIF5B-RET)	鑰窪積鹽鏇糧獵鏇艱膚(衊夢願窪糧製築廠願選) = 廠醖觸鑰窪顧壓襯襯鹽獵鬱積製齋選糧網構鏇 (餘壓選範遞廠醖觸憲顧, 59.6 ~ 70.7) 更多	积极	2024-09-08
				Selpercatinib (KIF5B-RET + Prior Treatment)	鑰窪積鹽鏇糧獵鏇艱膚(衊夢願窪糧製築廠願選) = 壓鹹構齋夢鹽顧鹽鹹鏇獵鬱積製齋選糧網構鏇 (餘壓選範遞廠醖觸憲顧, 46.0 ~ 61.1)
WCLC2024	N/A	非小细胞肺癌一线 RET fusion-positive	504	Selpercatinib 160 mg twice daily	衊膚獵遞壓範鬱壓齋築(淵鏇淵顧醖製鹽廠簾觸) = Aspartate and alanine aminotransferase elevation were the most common adverse events leading to dose adjustments 築網鹹憲憲襯憲網選糧 (構膚鹹網廠構衊選遞鏇 ) 更多	积极	2024-09-08
NCT03157128 (LIBRETTO-001, Pubmed) 人工标引	临床1/2期	RET融合阳性甲状腺癌 \| RET突变阳性甲状腺髓样癌 RET Fusion \| RET Mutation	390	Selpercatinib (medullary thyroid cancer + cabozantinib/vandetanib-naïve)	蓋構窪齋窪繭顧顧蓋糧(遞醖製繭蓋選淵築願鬱) = 顧獵願觸廠醖襯餘鏇糧繭淵網顧鏇簾鬱築衊繭 (觸夢選淵鏇齋鹹淵淵簾 ) 更多	积极	2024-08-02
				Selpercatinib (thyroid cancer + treatment-naïve)	蓋構窪齋窪繭顧顧蓋糧(遞醖製繭蓋選淵築願鬱) = 艱窪醖憲繭淵膚鹽窪鹹繭淵網顧鏇簾鬱築衊繭 (觸夢選淵鏇齋鹹淵淵簾 ) 更多
NCT03899792 (LIBRETTO-121, FDA) 人工标引	临床1/2期	甲状腺癌转移 \| 实体瘤 \| 甲状腺癌 RET Fusion \| RET Mutation	25	Selpercatinib 92 mg/m2	膚製範繭鑰製衊網憲襯(鏇憲襯鏇窪夢範襯壓繭) = 願窪繭糧憲膚廠遞夢窪襯餘齋鹹鹽壓鑰鏇願鑰 (鏇繭醖鏇遞鑰願觸鏇鑰, 28 ~ 69) 更多	积极	2024-06-29
				Selpercatinib 92 mg/m2 (MTC)	膚製範繭鑰製衊網憲襯(鏇憲襯鏇窪夢範襯壓繭) = 觸製顧壓鏇壓築積衊遞襯餘齋鹹鹽壓鑰鏇願鑰 (鏇繭醖鏇遞鑰願觸鏇鑰, 18 ~ 71) 更多