Mobocertinib Succinate

近日，由四川科伦博泰生物医药股份有限公司（下称“科伦博泰”或“公司”，6990.HK）自主研发的创新TROP2 ADC芦康沙妥珠单抗（sac-TMT）单药治疗标准疗法难治性的不可切除的局部晚期或转移性实体瘤的Ⅰ/Ⅱ期研究结果（KL264-01/MK-2870-001）成功发表在国际医学期刊《Journal of Hematology& Oncology》（血液学与肿瘤学杂志，影响因子IF=29.9）上，研究结果展现出芦康沙妥珠单抗（sac-TMT）在该类患者中的治疗潜力。本文通讯作者为殷咏梅教授（简介：江苏省人民医院副院长;教授，主任医师，博士生导师;中国临床肿瘤学会(CSCO)副理事长;CSCO乳腺癌专家委员会书长;CSCO患者教育专家委员会主任委员;CSCO智慧医疗专家委员会副主任委员;中国抗癌协会乳腺癌专业委员会常务委员）研究成果KL264-01/MK-2870-001是一项芦康沙妥珠单抗（sac-TMT）单药治疗标准疗法难治性的不可切除的局部晚期或转移性实体瘤患者的Ⅰ/Ⅱ期首次人体试验，该研究是一项国际多中心研究。本次发表的文章报告了KL264-01研究的Ⅰ期剂量递增结果，及其中三阴性乳腺癌（TNBC）和 激素受体阳性/HER2阴性（HR+/HER2-）乳腺癌两个队列Ⅱ期扩展研究结果。研究结果显示，芦康沙妥珠单抗（sac-TMT）在不可切除的局部晚期或转移性实体瘤患者中表现出可控的安全性，在转移性TNBC和HR+/HER2-乳腺癌中具有良好的抗肿瘤活性。目前，由公司主导的针对sac-TMT的多项3期临床研究正在中国开展。同时，默沙东（美国新泽西州罗威市默克公司的商号）也在拥有独家权利的地区开展全球试验。2022年5月，公司授予默沙东在大中华区(包括中国内地、香港、澳门及台湾)以外的所有地区开发、使用、制造及商业化芦康沙妥珠单抗(sac-TMT)的独家权利。关于芦康沙妥珠单抗（sac-TMT)作为本公司的核心产品，芦康沙妥珠单抗(sac-TMT)是一款本公司拥有自主知识产权的新型TROP2 ADC，针对非小细胞肺癌（NSCLC）、乳腺癌（BC）、胃癌(GC)、妇科肿瘤等晚期实体瘤。芦康沙妥珠单抗(sac-TMT)采用新型连接子进行开发，其通过偶联一种贝洛替康衍生的拓扑异构酶I抑制剂作为有效载荷，药物抗体比(DAR)达到7.4。芦康沙妥珠单抗(sac-TMT)通过重组抗TROP2人源化单克隆抗体特异性识别肿瘤细胞表面的TROP2，其后被肿瘤细胞内吞并于细胞内释放KL610023。KL610023作为拓扑异构酶I抑制剂，可诱导肿瘤细胞DNA损伤，进而导致细胞周期阻滞及细胞凋亡。此外，其亦于肿瘤微环境中释放KL610023。鉴于KL610023具有细胞膜渗透性，其可实现旁观者效应，即杀死邻近的肿瘤细胞。于2022年5月，本公司授予默沙东(美国新泽西州罗威市默克公司的商号)在大中华区(包括中国内地、香港、澳门及台湾)以外的所有地区开发、使用、制造及商业化芦康沙妥珠单抗(sac-TMT)的独家权利。截止目前，芦康沙妥珠单抗(sac-TMT)的2项适应症已于中国获批上市，基于OptiTROP-Breast01研究获批治疗既往至少接受过 2 种系统治疗（其中至少1种治疗针对晚期或转移性阶段）的不可切除的局部晚期或转移性三阴性乳腺癌(TNBC)以及基于OptiTROP-Lung03研究获批治疗经表皮生长因子受体酪氨酸激酶抑制剂(EGFR-TKI)和含铂化疗治疗后进展的EGFR突变阳性的局部晚期或转移性非鳞状非小细胞肺癌。芦康沙妥珠单抗(sac-TMT)成为国内首个获得完全批准上市的具有全球知识产权的国产ADC；也是全球首个在肺癌适应症获批上市的TROP2 ADC。此外，芦康沙妥珠单抗(sac-TMT)用于治疗经EGFR-TKI治疗后进展的EGFR突变局部晚期或转移性非小细胞肺癌及既往接受过内分泌治疗且在晚期或转移性阶段接受过其他系统治疗的不可切除的局部晚期或转移HR+/HER2-BC的2项新增适应症上市申请已获CDE受理，并已纳入优先审评审批程序。截止目前，科伦博泰已在中国开展8项注册性临床研究。默沙东已启动14项正在进行的芦康沙妥珠单抗(sac-TMT)作为单药疗法或联合帕博利珠单抗或其他药物用于多种类型癌症的全球性3期临床研究（这些研究由默沙东申办并主导)。关于科伦博泰四川科伦博泰生物医药股份有限公司（简称“科伦博泰生物”，股票代码：6990.HK）是科伦药业控股子公司，专注于创新生物技术药物及小分子药物的研发、生产、商业化及国际合作。公司围绕全球和中国未满足的临床需求，重点布局肿瘤、自身免疫、炎症和代谢等重大疾病领域，建设国际化药物研发与产业化平台，致力于成为在创新药物领域国际领先的企业。公司目前拥有30余个重点创新药项目，其中3个项目已获批上市，1个项目处于NDA阶段，10余个项目正处于临床阶段。公司成功构建了享誉国际的专有ADC开发平台OptiDCTM，已有1个ADC项目获批上市，1个ADC项目处于NDA阶段，多个ADC或新型偶联药物产品处于临床或临床前研究阶段。更多信息请访问官网https://kelun-biotech.com/。

CHENGDU, China, June 10, 2025 /PRNewswire/ -- Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. (the "Company") today announced that results from the Phase 1/2 study (KL264-01/MK-2870-001) evaluating the novel TROP2 antibody drug conjugate (ADC) sacituzumab tirumotecan (sac-TMT) as monotherapy were published in the international medical journal, Journal of Hematology & Oncology (Impact Factor (IF) = 29.9). Published results include those from the Phase 1 dose-escalation part of the study which evaluated sac-TMT in advanced solid tumors, and those from the Phase 2 expansion cohorts of the study, evaluating sac-TMT in metastatic triple-negative breast . The results of the study demonstrated the therapeutic potential of sac-TMT in this patient population. Results KL264-01/MK-2870-001 is a Phase 1/2 first-in-human trial of sac-TMT as monotherapy in patients who have an unresectable locally advanced or metastatic solid tumor which is refractory to standard therapies, which is a global multi-centre study. Presented results include those from the Phase 1 portion of this study, and the Phase 2 expansion cohorts for TNBC and HR+/HER2– breast cancer. The results of the study showed that sac-TMT demonstrated a manageable safety profile in patients with unresectable locally advanced/metastatic solid tumors and promising antitumor activity in metastatic TNBC and HR+/HER2− breast cancer. Currently, sac-TMT is being investigated in several Phase 3 studies in China, led by the Company, as well as globally, where MSD (the tradename of Merck & Co., Inc., Rahway, NJ, USA) holds the exclusive rights. In May 2022, the Company licensed the exclusive rights to MSD to develop, use, manufacture and commercialize sac-TMT in all territories outside of Greater China (includes Mainland China, Hong Kong, Macau, and Taiwan). About sac-TMT Sac-TMT, a core product of the Company, is a novel human TROP2 ADC in which the Company has proprietary intellectual property rights, targeting advanced solid tumors such as NSCLC, breast cancer (BC), gastric cancer (GC), gynecological tumors, among others. Sac-TMT is developed with a novel linker to conjugate the payload, a belotecan-derivative topoisomerase I inhibitor with a drug-to-antibody-ratio (DAR) of 7.4. Sac-TMT specifically recognizes TROP2 on the surface of tumor cells by recombinant anti-TROP2 humanized monoclonal antibodies, which is then endocytosed by tumor cells and releases KL610023 intracellularly. KL610023, as a topoisomerase I inhibitor, induces DNA damage to tumor cells, which in turn leads to cell-cycle arrest and apoptosis. In addition, it also releases KL610023 in the tumor microenvironment. Given that KL610023 is membrane permeable, it can enable a bystander effect, or in other words kill adjacent tumor cells. In May 2022, the Company licensed the exclusive rights to MSD to develop, use, manufacture and commercialize sac-TMT in all territories outside of Greater China (includes Mainland China, Hong Kong, Macau, and Taiwan). To date, two indications for sac-TMT have been approved and marketed in China for the treatment of adult patients with unresectable locally advanced or metastatic TNBC who have received at least two prior systemic therapies (at least one of them for advanced or metastatic setting) and EGFR mutation-positive locally advanced or metastatic non-squamous NSCLC following progression on EGFR-TKI therapy and platinum-based chemotherapy. Sac-TMT became the first domestically developed and fully approved-for-marketing ADC in China with global intellectual property rights. It is also the world's first TROP2 ADC to be approved for marketing in a lung cancer indication. In addition, two new indication applications for sac-TMT for the treatment of adult patients with EGFR-mutant locally advanced or metastatic NSCLC who progressed after treatment with EGFR-TKI therapy and with unresectable locally advanced, metastatic HR+/HER2- BC who have received prior endocrine therapy and other systemic treatments in the advanced or metastatic setting were accepted by the NMPA, and were included in the priority review and approval process. As of today, Kelun-Biotech has initiated 8 registrational clinical studies in China. MSD has initiated 14 ongoing Phase 3 global clinical studies of sac-TMT as a monotherapy or with pembrolizumab or other agents for several types of cancer. These studies are sponsored and led by MSD. About Kelun-Biotech Kelun-Biotech（6990.HK）is a holding subsidiary of Kelun Pharmaceutical (002422.SZ), which focuses on the R&D, manufacturing, commercialization and global collaboration of innovative biological drugs and small molecule drugs. The company focuses on major disease areas such as solid tumors, autoimmune, inflammatory, and metabolic diseases, and in establishing a globalized drug development and industrialization platform to address the unmet medical needs in China and the rest of world. The Company is committed to becoming a leading global enterprise in the field of innovative drugs. At present, the Company has more than 30 ongoing key innovative drug projects, of which 3 projects have been approved for marketing, 1 project is in the NDA stage, and more than 10 projects are in the clinical stage. The company has established one of the world's leading proprietary ADC platforms, OptiDC™, and has 1 ADC project approved for marketing, 1 ADC project in NDA stage, and multiple ADC or novel DC aseets in clinical or preclinical research stage. For more information, please visit . Media: [email protected] SOURCE Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED