The first patient has been dosed in the IDeate-Esophageal01 Phase 3 trial evaluating the efficacy and safety of investigational ifinatamab deruxtecan (I-DXd) versus investigator’s choice of chemotherapy in patients with unresectable advanced or metastatic esophageal squamous cell carcinoma (ESCC) with disease progression following treatment with a platinum-containing systemic therapy and an immune checkpoint inhibitor.

IDeate-Esophageal01三期试验已对首位患者进行给药，该试验旨在评估研究性伊菲那塔单抗德鲁斯特坎 (I-DXd) 与研究者选择的化疗方案相比，对患有不可切除的晚期或转移性食管鳞状细胞癌 (ESCC) 且在接受含铂全身疗法和免疫检查点抑制剂治疗后病情出现进展的患者进行的疗效和安全性。

Ifinatamab deruxtecan is a specifically engineered, potential first-in-class B7-H3 directed DXd antibody drug conjugate (ADC) discovered by Daiichi Sankyo (TSE: 4568) and being jointly developed with Merck (NYSE: MRK), known as MSD outside of the United States and Canada.

Ifinatamab deruxtecan 是一种特别设计的、潜在的首创新药 B7-H3 导向的 DXd 抗体药物偶联物 (ADC)，由第一三共（TSE：4568）发现，并与默克公司（纽约证券交易所代码：MRK，美国和加拿大以外地区称为 MSD）共同开发。

ESCC accounts for nearly 90% of esophageal cancers globally with a five-year overall survival rate around 15% to 20% and has a worse prognosis for those diagnosed at an advanced stage of the disease. While the evolved landscape in the first-line metastatic setting of ESCC has helped to improve outcomes for patients, treatment options are limited for patients progressing after first-line therapy, reinforcing the need for new approaches. .

食管鳞状细胞癌 (ESCC) 占全球食管癌的近 90%，其五年总生存率约为 15% 至 20%，对于晚期确诊的患者预后更差。虽然在 ESCC 一线转移性治疗领域的进展有助于改善患者的治疗效果，但对于一线治疗后进展的患者，治疗选择仍然有限，这进一步凸显了对新治疗方法的需求。

“Patients with metastatic esophageal squamous cell carcinoma continue to experience poor outcomes despite currently available treatments,” said Mark Rutstein, MD, head, therapeutic area oncology development, Daiichi Sankyo. “The encouraging clinical activity seen in our early-phase signal finding trial supports further evaluation of ifinatamab deruxtecan as a potential treatment strategy for these patients.” .

“尽管目前已有治疗方法，但转移性食管鳞状细胞癌患者的预后仍然不佳，”第一三共肿瘤学开发治疗领域负责人Mark Rutstein博士表示。“我们在早期信号发现试验中看到的令人鼓舞的临床活性支持进一步评估ifinatamab deruxtecan作为这些患者的潜在治疗策略。”

“Advanced esophageal squamous cell carcinoma is a difficult-to-treat disease, and unfortunately overall survival remains low,” said Marjorie Green, MD, senior vice president and head of oncology, global clinical development, Merck Research Laboratories. “The initiation of the pivotal Phase 3 IDeate-Esophageal01 clinical trial demonstrates our shared commitment with Daiichi Sankyo to further expand our clinical development program evaluating this potentially first-in-class ADC across multiple solid tumors where there are unmet needs for new treatment options.” .

“晚期食管鳞状细胞癌是一种难以治疗的疾病，不幸的是总体生存率仍然很低，”默克研究实验室肿瘤学高级副总裁兼全球临床开发主管Marjorie Green博士说道。“关键性III期IDeate-Esophageal01临床试验的启动表明了我们与第一三共共同致力于进一步扩展我们的临床开发计划，在多个存在未满足治疗需求的实体瘤中评估这款潜在的首创ADC。”

The initiation of IDeate-Esophageal01 is based on results from the

IDeate-Esophageal01 的启动是基于以下结果

IDeate-PanTumor01

泛肿瘤01

Phase 1/2 trial

1/2期试验

presented

呈现

at both the 2022 and 2023 European Society of Medical Oncology (ESMO) where ifinatamab deruxtecan showed promising responses in heavily pretreated patients with ESCC.

在2022年和2023年欧洲肿瘤内科学会（ESMO）上，ifinatamab deruxtecan 在经过多线治疗的食管鳞状细胞癌（ESCC）患者中显示出良好的反应。

About the IDeate-Esophageal01 trial

关于IDeate-Esophageal01试验

IDeate-Esophageal01

食道01

is a global, multicenter, open-label, randomized Phase 3 trial evaluating the safety and efficacy of ifinatamab deruxtecan (12 mg/kg) versus treatment of physician’s choice of chemotherapy (paclitaxel, docetaxel or irinotecan hydrochloride) in patients with advanced or metastatic ESCC with disease progression following treatment with platinum-based chemotherapy therapy and an immune checkpoint inhibitor.

是一项全球性、多中心、开放标签、随机的 III 期试验，评估 ifinatamab deruxtecan（12 mg/kg）与医生选择的化疗（紫杉醇、多西他赛或盐酸伊立替康）在晚期或转移性 ESCC 患者中的安全性和有效性，这些患者在接受铂类化疗和免疫检查点抑制剂治疗后出现疾病进展。

Eligible patients must have received no more than one prior line of systemic therapy in the advanced or metastatic setting. .

符合条件的患者在晚期或转移性环境中接受的既往系统治疗不得超过一线。

The primary endpoint of the trial is overall survival. Secondary endpoints include progression-free survival and objective response rate as assessed by blinded independent central review, and safety.

该试验的主要终点是总生存期。次要终点包括由盲态独立中心审查评估的无进展生存期和客观缓解率，以及安全性。

IDeate-Esophageal01 will enroll approximately 510 patients across Asia, Europe and North America. For more information, please visit

IDeate-Esophageal01 将在亚洲、欧洲和北美招募大约 510 名患者。欲了解更多信息，请访问

About esophageal squamous cell carcinoma

关于食管鳞状细胞癌

More than half a million esophageal cancer cases were diagnosed in 2022, with nearly half a million deaths globally.ESCC accounts for nearly 90% of esophageal cancers globally with a five-year overall survival rate around 15% to 20% and has a worse prognosis for those diagnosed at an advanced stage of the disease.

2022年诊断出超过50万例食管癌病例，全球近50万人死亡。ESCC占全球食管癌病例的近90%，五年总生存率约为15%至20%，对于晚期诊断的患者预后更差。

ESCC is most prevalent in Eastern Asia where mortality rates are also the highest..

食管鳞状细胞癌在东亚地区最为普遍，且死亡率也最高。

While the evolved landscape in the first-line metastatic setting of ESCC has helped to improve outcomes for patients, treatment options are limited for patients progressing after first-line therapy, reinforcing the need for new approaches.

虽然食管鳞状细胞癌一线转移性治疗的进展帮助改善了患者的预后，但对于一线治疗后进展的患者，治疗选择有限，这进一步强调了新方法的必要性。

About B7-H3

关于B7-H3

B7-H3 is a transmembrane protein that belongs to the B7 family of proteins which bind to the CD28 family of receptors that includes PD-1. B7-H3 is overexpressed in a wide range of cancer types, including ESCC, and its overexpression has been shown to correlate with poor prognosis, making B7-H3 a promising therapeutic target.

B7-H3是一种跨膜蛋白，属于B7家族蛋白，该家族蛋白与包括PD-1在内的CD28家族受体结合。B7-H3在多种癌症类型中过表达，包括食管鳞状细胞癌（ESCC），其过表达已被证明与不良预后相关，使B7-H3成为一个有前景的治疗靶点。

There are currently no B7-H3 directed medicines approved for the treatment of any cancer..

目前没有任何针对B7-H3的药物被批准用于治疗任何癌症。

About ifinatamab deruxtecan

关于ifinatamab deruxtecan

Ifinatamab deruxtecan is an investigational potential first-in-class B7-H3 directed ADC. Designed using Daiichi Sankyo’s proprietary DXd ADC Technology, ifinatamab deruxtecan is comprised of a humanized anti-B7-H3 IgG1 monoclonal antibody attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers. .

Ifinatamab deruxtecan 是一种研究性的潜在首创 B7-H3导向的抗体药物偶联物（ADC）。该药物采用第一三共公司的专有 DXd ADC 技术设计，由一种人源化的抗 B7-H3 IgG1 单克隆抗体组成，通过基于四肽的可裂解连接子连接多个拓扑异构酶I抑制剂载荷（一种艾沙替康衍生物，DXd）。

In addition to

此外，除了

IDeate-Esophageal01

食道01

, ifinatamab deruxtecan is being evaluated in a global development program that includes

如果ifinatamab deruxtecan正在一个包括全球开发计划中进行评估，该计划包括

IDeate-Lung01

肺部创意01

, a Phase 2 monotherapy trial in patients with previously treated extensive-stage small cell lung cancer (ES-SCLC);

，一项针对先前治疗过的广泛期小细胞肺癌（ES-SCLC）患者的二期单药治疗试验；

IDeate-Lung02

IDEate-Lung02

, a

，一个

Phase 3 trial

三期临床试验

in patients with relapsed SCLC versus investigator’s choice of chemotherapy;

在复发性小细胞肺癌患者中，与研究者选择的化疗方案相比；

IDeate-Lung03

IDEate-Lung03

, a Phase 1b/2 trial in patients with ES-SCLC in combination with atezolizumab with or without carboplatin as first-line induction or maintenance therapy;

, 一项针对广泛期小细胞肺癌（ES-SCLC）患者的1b/2期试验，与阿特珠单抗联合使用，伴或不伴卡铂作为一线诱导或维持治疗；

IDeate-PanTumor02

IDEate-PanTumor02

, a Phase 2 monotherapy trial in patients with recurrent or metastatic solid tumors; and,

，一项针对复发或转移性实体瘤患者的二期单药治疗试验；以及，

IDeate-PanTumor01

IDEate-PanTumor01

, a Phase 1/2 first-in-human monotherapy trial in patients with advanced solid malignant tumors in collaboration with Sarah Cannon Research Institute (SCRI) with study operational oversight and delivery provided through SCRI’s early phase oncology clinical research organization, SCRI Development Innovations in Nashville, TN. .

，一项与Sarah Cannon研究所（SCRI）合作的针对晚期实体恶性肿瘤患者的1/2期首次人体单药治疗试验，研究的操作监督和实施由SCRI位于田纳西州纳什维尔的早期肿瘤临床研究组织SCRI Development Innovations提供。

Ifinatamab deruxtecan has been granted orphan drug designation in the EU, Japan, Taiwan, and U.S. for the treatment of SCLC.

Ifinatamab deruxtecan 已在欧盟、日本、台湾和美国获得治疗小细胞肺癌（SCLC）的孤儿药资格认定。

About the Daiichi Sankyo and Merck collaboration

关于第一三共和默克的合作

Daiichi Sankyo and Merck entered into a global collaboration in

第一三共和默克公司建立了全球合作关系

October 2023

2023年10月

to jointly develop and commercialize patritumab deruxtecan (HER3-DXd), ifinatamab deruxtecan (I-DXd) and raludotatug deruxtecan (R-DXd), except in Japan where Daiichi Sankyo will maintain exclusive rights. Daiichi Sankyo will be solely responsible for manufacturing and supply. In

共同开发和商业化 patritumab deruxtecan（HER3-DXd）、ifinatamab deruxtecan（I-DXd）和 raludotatug deruxtecan（R-DXd），但在日本除外，第一三共将保留独家权利。第一三共将全权负责制造和供应。在

August 2024

2024年8月

, the global co-development and co-commercialization agreement was expanded to include gocatamig (MK-6070/DS3280), which the companies will jointly develop and commercialize worldwide, except in Japan where Merck will maintain exclusive rights. Merck will be solely responsible for manufacturing and supply for gocatamig..

全球共同开发和共同商业化协议已扩展到包括戈卡替尼（MK-6070/DS3280），两家公司将在全球范围内联合开发和商业化该药物，但在日本默克公司将保留独家权利。默克将单独负责戈卡替尼的生产和供应。

About the ADC portfolio of Daiichi Sankyo

关于第一三共的ADC产品组合

The Daiichi Sankyo ADC portfolio consists of seven ADCs in clinical development crafted from two distinct ADC technology platforms discovered in-house by Daiichi Sankyo.

第一三共的ADC产品组合包括七个处于临床开发阶段的ADC，这些ADC由第一三共内部发现的两个不同的ADC技术平台打造。

The ADC platform furthest in clinical development is Daiichi Sankyo’s DXd ADC Technology where each ADC consists of a monoclonal antibody attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers. The DXd ADC portfolio currently consists of ENHERTU®, a HER2 directed ADC, and DATROWAY®, a TROP2 directed ADC, which are being jointly developed and commercialized globally with AstraZeneca.

临床开发进展最快的ADC平台是第一三共的DXd ADC技术，其中每个ADC由单克隆抗体通过四肽可裂解连接子连接多个拓扑异构酶I抑制剂载荷（艾沙替康衍生物，DXd）组成。DXd ADC产品组合目前包括ENHERTU®（一种HER2导向的ADC）和DATROWAY®（一种TROP2导向的ADC），它们正与阿斯利康合作进行全球共同开发和商业化。

Patritumab deruxtecan (HER3-DXd), a HER3 directed ADC, ifinatamab deruxtecan (I-DXd), a B7-H3 directed ADC, and raludotatug deruxtecan (R-DXd), a CDH6 directed ADC, are being jointly developed and commercialized globally with Merck. DS-3939, a TA-MUC1 directed ADC, is being developed by Daiichi Sankyo. .

Patritumab deruxtecan（HER3-DXd），一种靶向HER3的ADC，Ifinatamab deruxtecan（I-DXd），一种靶向B7-H3的ADC，以及Raludotatug deruxtecan（R-DXd），一种靶向CDH6的ADC，正与默克公司合作进行全球开发和商业化。DS-3939，一种靶向TA-MUC1的ADC，由第一三共开发。

The second Daiichi Sankyo ADC platform consists of a monoclonal antibody attached to a modified pyrrolobenzodiazepine (PBD) payload. DS-9606, a CLDN6 directed PBD ADC, is the first of several planned ADCs in clinical development utilizing this platform.

第二个第一三共ADC平台由连接到修饰的吡咯并苯二氮杂卓（PBD）有效载荷的单克隆抗体组成。DS-9606是一种针对CLDN6的PBD ADC，是利用该平台进行临床开发的计划中的首个ADC。

Ifinatamab deruxtecan, patritumab deruxtecan, raludotatug deruxtecan, DS-3939 and DS-9606 are investigational medicines that have not been approved for any indication in any country. Safety and efficacy have not been established.

Ifinatamab deruxtecan、patritumab deruxtecan、raludotatug deruxtecan、DS-3939 和 DS-9606 是尚未在任何国家获批用于任何适应症的在研药物，其安全性和有效性尚未确立。

About Daiichi Sankyo

关于第一三共

Daiichi Sankyo is an innovative global healthcare company contributing to the sustainable development of society that discovers, develops and delivers new standards of care to enrich the quality of life around the world. With more than 120 years of experience, Daiichi Sankyo leverages its world-class science and technology to create new modalities and innovative medicines for people with cancer, cardiovascular and other diseases with high unmet medical needs.

第一三共是一家创新的全球医疗保健公司，致力于为社会的可持续发展做出贡献，通过发现、开发和提供新的护理标准来提升世界各地的生活质量。凭借120多年的经验，第一三共利用其世界级的科学和技术，为癌症、心血管疾病及其他存在高度未满足医疗需求的疾病患者创造新的治疗模式和创新药物。

Merck’s focus on cancer

默克公司对癌症的关注

Every day, we follow the science as we work to discover innovations that can help patients, no matter what stage of cancer they have. As a leading oncology company, we are pursuing research where scientific opportunity and medical need converge, underpinned by our diverse pipeline of more than 25 novel mechanisms.

每天，我们在努力发现可以帮助患者的创新疗法时都遵循科学，无论患者处于癌症的哪个阶段。作为领先的肿瘤公司，我们在科学机遇与医疗需求交汇的领域开展研究，依托我们多样化的研发管线，其中包含25种以上的新机制。

With one of the largest clinical development programs across more than 30 tumor types, we strive to advance breakthrough science that will shape the future of oncology. By addressing barriers to clinical trial participation, screening and treatment, we work with urgency to reduce disparities and help ensure patients have access to high-quality cancer care.

通过在超过30种肿瘤类型中开展规模最大的临床开发项目之一，我们致力于推动突破性科学发展，塑造肿瘤学的未来。通过解决参与临床试验、筛查和治疗的障碍，我们紧急行动以减少差异，帮助确保患者获得高质量的癌症治疗。

Our unwavering commitment is what will bring us closer to our goal of bringing life to more patients with cancer. For more information, visit .

我们坚定不移的承诺将使我们更接近为更多癌症患者带来生命的目标。欲了解更多信息，请访问。

About Merck

关于默克

At Merck, known as MSD outside of the United States and Canada, we are unified around our purpose: We use the power of leading-edge science to save and improve lives around the world. For more than 130 years, we have brought hope to humanity through the development of important medicines and vaccines.

在默克（在美国和加拿大以外地区称为MSD），我们围绕一个使命团结一致：我们利用前沿科学的力量拯救生命并改善世界各地人们的生活。130多年来，我们通过研发重要的药物和疫苗，为人类带来了希望。

We aspire to be the premier research-intensive biopharmaceutical company in the world – and today, we are at the forefront of research to deliver innovative health solutions that advance the prevention and treatment of diseases in people and animals. We foster a diverse and inclusive global workforce and operate responsibly every day to enable a safe, sustainable and healthy future for all people and communities.

我们立志成为全球首屈一指的研究密集型生物制药公司——今天，我们站在研究的最前沿，提供创新的健康解决方案，推动人类和动物疾病预防与治疗的进步。我们培养多元化和包容性的全球员工队伍，并每天负责任地运营，以确保为所有人和社区创造一个安全、可持续和健康的未来。