KEYMAKER-U01 Substudy 01I: A Phase 2, Randomized, Umbrella Study With Rolling Arms of Investigational Agents in Participants With Previously Treated Stage IV Squamous Non-small Cell Lung Cancer (NSCLC)

Researchers are looking for other ways to treat metastatic squamous non-small cell lung cancer (NSCLC). Squamous NSCLC is cancer that starts in squamous cells, which are flat cells that line the inside of the airways in the lungs. Metastatic means the cancer has spread to other parts of the body.
Standard treatment (usual treatment) for metastatic squamous NSCLC is immunotherapy with or without chemotherapy. Immunotherapy is a treatment that helps the immune system fight cancer. Chemotherapy is medicine that destroys cancer cells or stops them from growing. However, standard treatment may not work or may stop working to treat metastatic squamous NSCLC.
Researchers want to learn if study treatments that are antibody drug conjugates (ADCs) can treat metastatic squamous NSCLC that did not respond (get smaller or go away) to standard treatment. An ADC attaches to a protein on cancer cells and delivers treatment to destroy those cells.
The main goals of this study are to learn about:
* The cancer response to the study treatments compared to chemotherapy
* The safety of the study treatments and if people tolerate them
This study is one of the substudies being conducted under one pembrolizumab umbrella master protocol (MK-3475-U01/KEYMAKER-U01).

Start Date28 May 2025

Sponsor / Collaborator

Merck Sharp & Dohme LLC

[+1]

NCT06780085

/ RecruitingPhase 2

KEYMAKER-U01 Substudy 01H: A Phase 2, Randomized, Umbrella Study With Rolling Arms of Investigational Agents in Participants With Previously Treated Stage IV Nonsquamous Non-small Cell Lung Cancer (NSCLC)

Researchers are looking for new ways to treat metastatic nonsquamous non-small cell lung cancer (NSCLC) that has been treated before. Metastatic means the cancer has spread to other parts of the body. Nonsquamous means the cancer did not start in squamous cells, which are flat cells that line the inside of the lungs.
Standard treatment (usual treatment) for NSCLC is surgery, then immunotherapy with or without chemotherapy after surgery. Immunotherapy is a treatment that helps the immune system fight cancer. Chemotherapy is a medicine that works to destroy cancer cells or stop them from growing.
However, standard treatment may not work or may stop working for some people. Researchers want to know if 2 antibody drug conjugates (ADCs) can help treat metastatic nonsquamous NSCLC that did not respond (get smaller or go away) to treatment. An ADC attaches to specific targets on cancers cells and delivers treatment to destroy those cells.
Researchers will compare 2 different ADCs (the study treatments) to chemotherapy in this study. The goals of this study are to learn:
* About the safety of the study treatments and if people tolerate them
* How many people have the cancer respond to the study treatments

Start Date13 May 2025

Sponsor / Collaborator

Merck Sharp & Dohme LLC

[+1]

NCT06843447

/ RecruitingPhase 1/2

A Phase 1b/2 Open-label, Multicenter Study to Evaluate the Safety and Efficacy of Raludotatug Deruxtecan With or Without Other Anticancer Investigational Agents in Participants With High-grade Serous Epithelial Ovarian, Primary Peritoneal, or Fallopian Tube Cancer Who Have Relapsed After Prior Platinum-based Chemotherapy

Researchers are looking for other ways to treat relapsed high-grade serous ovarian cancer. Relapsed means the cancer came back after treatment. High-grade means the cancer cells grow and spread quickly. Serous means the cancer started in the cells that cover the ovaries, the lining of the belly, or in the fallopian tubes.
Standard treatment (usual treatment) for people with relapsed high-grade serous ovarian cancer may include:
* Chemotherapy, which is a treatment that uses medicine to destroy cancer cells or stop them from growing
* Targeted therapy, which is a treatment that works to control how specific types of cancer cells grow and spread
Raludotatug deruxtecan (R-DXd) is a study treatment that is an antibody drug conjugate (ADC). An ADC attaches to a protein on cancer cells and delivers treatment to destroy those cells. Researchers want to know if R-DXd is safe to take with other treatments and if people tolerate them together. They also want to learn how many people have the cancer respond (gets smaller or goes away) to the treatments.

Start Date15 Apr 2025

Sponsor / Collaborator

Merck Sharp & Dohme LLC

[+1]

100 Clinical Results associated with Raludotatug deruxtecan

100 Translational Medicine associated with Raludotatug deruxtecan

100 Patents (Medical) associated with Raludotatug deruxtecan

Literatures (Medical) associated with Raludotatug deruxtecan

14 Nov 2024·JOURNAL OF MEDICINAL CHEMISTRY

Evaluation of Double Self-Immolative Linker-Based Antibody–Drug Conjugate FDA022-BB05 with Enhanced Therapeutic Potential

Article

Author: Liu, Shuangxi ; Yin, Sicheng ; Zhang, Yifan ; Yang, Tong ; Zhang, Wenbo ; Shen, Keyu ; Zhu, Shulei ; Xie, Qian ; Gao, Bei ; Wu, Yinghan ; Song, Ruiwen ; Cao, Xuemei ; Qiu, Xuefei ; Cheng, Zhiyang ; Wang, Baoxia ; Zhao, Teng ; Xu, Jun ; Wu, Jingsong ; Li, Weinan ; Guo, Qingsong ; Wang, Lei ; Lu, Wei

Typical antibody-drug conjugates (ADCs) with valine-alanine linkage, often conjugated with the amino group in payloads, face challenges when interacting with hydroxyl group-containing payloads. Herein, we introduced a transformative Val-Ala-based double self-immolative linker-payload platform, reshaping ADCs by optimizing hydroxyl group-containing payload integration. Utilizing this platform, FDA022-BB05 was successfully conjugated with the hydroxyl group-containing payload DXd using trastuzumab (FDA022) as the monoclonal antibody (mAb). FDA022-BB05 demonstrated enhanced stability, effective cathepsin B sensitivity, reduced cell proliferation, increased bystander killing, and targeted delivery. Notably, acute toxicity evaluations in diverse preclinical models indicated favorable safety profiles and tolerability, with a broad therapeutic index in HER2-positive and -negative xenografts. Overall, these compelling findings support the promising therapeutic potential of FDA022-BB05, emphasizing the significance of diverse linker-payload platform strategies. This ADC is a valuable addition to targeted cancer therapy development, currently advancing through phase I clinical trials.

01 Oct 2024·BIOORGANIC CHEMISTRY

Novel antibody-drug conjugates based on DXd-ADC technology

Review

Author: Chen, Yuchen ; Ye, Qiang ; Hu, Xuefang ; Bai, Lan ; Shi, Jianyou ; Ren, Zhiwen ; Hu, Yuan ; Chen, Rong

In recent years, antibody-drug conjugate (ADC) technology, which uses monoclonal antibodies (mAbs) to specifically deliver effective cytotoxic payloads to tumor cells, has become a promising method of tumor targeted therapy. ADCs are a powerful class of biopharmaceuticals that link antibodies targeting specific antigens and small molecule drugs with potent cytotoxicity via a linker, thus enabling selective destruction of cancer cells while minimizing systemic toxicity. DXd is a topoisomerase I inhibitor that induces DNA damage leading to cell cycle arrest, making it an option for ADC payloads. The DXd-ADC technology, developed by Daiichi Sankyo, is a cutting-edge platform that produces a new generation of ADCs with improved therapeutic metrics and has shown significant therapeutic potential in various types of cancer. This review provides a comprehensive assessment of drugs developed with DXd-ADC technology, with a focus on mechanisms of action, pharmacokinetics studies, preclinical data, and clinical outcomes for DS-8201a, U3-1402, DS-1062a, DS-7300a, DS-6157a, and DS-6000a. By integrating existing data, we aim to provide valuable insights into the current therapeutic status and future prospects of these novel agents.

01 Oct 2024·MOLECULAR CANCER THERAPEUTICS

FZ-AD005, a Novel DLL3-Targeted Antibody–Drug Conjugate with Topoisomerase I Inhibitor, Shows Potent Antitumor Activity in Preclinical Models

Article

Author: Wu, Jinsong ; Lu, Wei ; Shen, Jiafei ; Zhao, Teng ; Gao, Bei ; Yang, Tong ; Song, Ruiwen ; Guo, Qingsong ; Xie, Qian ; Lou, Sensen ; Li, Weinan ; Zhang, Yifan ; Zhu, Shulei ; Wang, Lei

Abstract:

Delta-like ligand 3 (DLL3) is overexpressed in small cell lung cancer (SCLC) and has been considered an attractive target for SCLC therapy. Rovalpituzumab tesirine was the first DLL3-targeted antibody–drug conjugate (ADC) to enter clinical studies. However, serious adverse events limited progress in the treatment of SCLC with rovalpituzumab tesirine. In this study, we developed a novel DLL3-targeted ADC, FZ-AD005, by using DXd with potent cytotoxicity and a relatively better safety profile to maximize the therapeutic index. FZ-AD005 was generated by a novel anti-DLL3 antibody, FZ-A038, and a valine–alanine (Val–Ala) dipeptide linker to conjugate DXd. Moreover, Fc-silencing technology was introduced in FZ-AD005 to avoid off-target toxicity mediated by FcγRs and showed negligible Fc-mediated effector functions in vitro. In preclinical evaluation, FZ-AD005 exhibited DLL3-specific binding and demonstrated efficient internalization, bystander killing, and excellent in vivo antitumor activities in cell line–derived xenograft and patient-derived xenograft models. FZ-AD005 was stable in circulation with acceptable pharmacokinetic profiles in cynomolgus monkeys. FZ-AD005 was well tolerated in rats and monkeys. The safety profile of FZ-AD005 was favorable, and the highest nonseverely toxic dose was 30 mg/kg in cynomolgus monkeys. In conclusion, FZ-AD005 has the potential to be a superior DLL3-targeted ADC with a wide therapeutic window and is expected to provide clinical benefits for the treatment of patients with SCLC.

166

News (Medical) associated with Raludotatug deruxtecan

02 Jul 2026

·www.biospace.com

Enhertu® Approved in the EU as First Tumor Agnostic HER2 Directed Therapy and Antibody Drug Conjugate for Patients with Previously Treated HER2 Positive Metastatic Solid Tumors

Approval based on three phase 2 trials of Daiichi Sankyo and AstraZeneca’s Enhertu that demonstrated clinically meaningful responses across a broad range of tumors Enhertu now approved for six indications in the EU TOKYO--(BUSINESS WIRE)--Enhertu ® (trastuzumab deruxtecan) has been approved in the European Union (EU) as a monotherapy for the treatment of adult patients with unresectable or metastatic HER2 positive (immunohistochemistry [IHC] 3+) solid tumors who have received prior treatment and who have no satisfactory treatment options. Enhertu is a specifically engineered HER2 directed DXd antibody drug conjugate (ADC) discovered by Daiichi Sankyo (TSE: 4568) and being jointly developed and commercialized by Daiichi Sankyo and AstraZeneca (LSE/STO/NYSE: AZN). The approval by the European Commission follows the positive opinion of the Committee for Medicinal Products for Human Use of the European Medicines Agency and is based on results from subgroups of patients with HER2 positive (IHC 3+) tumors across three phase 2 trials, including DESTINY-PanTumor02 , DESTINY-Lung01 and DESTINY-CRC02 . In DESTINY-PanTumor02, Enhertu demonstrated a confirmed objective response rate (ORR) of 52.3% (95% confidence interval [CI]: 42.6-61.8) and median duration of response (DOR) of 21.1 months (95% CI: 10.6-25.0) in a subgroup of previously treated patients (n=111) with centrally or locally assessed HER2 positive solid tumors, including biliary tract, bladder, cervical, endometrial, ovarian, pancreatic or other tumors. In DESTINY-Lung01, Enhertu demonstrated a confirmed ORR of 52.9% (95% CI: 27.8-77.0) and median DOR of 6.9 months (95% CI: 4.0-9.8) in a subgroup of previously treated patients (n=17) with centrally confirmed HER2 positive non-small cell lung cancer (NSCLC). In DESTINY-CRC02, Enhertu demonstrated a confirmed ORR of 46.9% (95% CI: 34.3-59.8) and median DOR of 5.5 months (95% CI: 4.2-8.1) in a subgroup of previously treated patients (n=64) with centrally confirmed HER2 positive colorectal cancer. “HER2 overexpression occurs across multiple tumor types and is associated with aggressive disease and a poor prognosis. Until now, HER2 directed therapies were only available for specific tumor types," said Benedikt Westphalen, MD, Head of the Precision Oncology Program, Comprehensive Cancer Center of the University of Munich, Germany. “The approval of trastuzumab deruxtecan as a tumor agnostic therapy opens a new treatment option for patients with HER2 positive cancers regardless of where the tumor originated.” In DESTINY-PanTumor02, DESTINY-Lung01 and DESTINY-CRC02, the safety pro Enhertu was consistent with previous clinical trials with no new safety concerns identified. Grade 3 or grade 4 adverse reactions from a pooled safety analysis of patients treated with Enhertu (5.4 mg/kg) across multiple tumor types in clinical studies included neutropenia (18.5%), anemia (9.9%), fatigue (8.2%), leukopenia (5.8%), thrombocytopenia (5.2%), nausea (4.8%), lymphopenia (4.2%), hypokalemia (3.6%), increased transaminases (3.6%), diarrhea (2.5%), vomiting (2.4%), decreased appetite (1.6%), pneumonia (1.4%) and decreased ejection fraction (1.0%). Grade 5 adverse reactions occurred in 1.1% of patients, including interstitial lung disease/pneumonitis (1.0%). “This approval of Enhertu marks a significant milestone in the EU for patients with HER2 positive metastatic solid tumors and establishes the first tumor agnostic indication for a HER2 directed therapy and antibody drug conjugate in the region,” said Ken Keller, Global Head of Oncology Business, and President and CEO, Daiichi Sankyo, Inc. “Enhertu is now approved for six indications in the EU, which demonstrates our commitment to advancing innovative medicines in areas of high unmet need to patients with cancer.” “Precision medicine is reshaping cancer care by helping inform treatment decisions based on the molecular and biological characteristics of a patient’s disease,” said Dave Fredrickson, Executive Vice President, Oncology Hematology Business Unit, AstraZeneca. “Enhertu is already approved in breast, gastric and lung cancers, and with this approval, clinicians may now consider Enhertu for patients with HER2 positive status across multiple additional tumor types. This highlights the importance of biomarker testing to identify eligible patients and ensure that those with HER2 positive disease are considered for targeted treatment.” Enhertu (5.4 mg/kg) is approved in more than 40 countries/regions worldwide for the treatment of adult patients with unresectable or metastatic HER2 positive (IHC 3+) solid tumors who have received prior systemic treatment and/or have no satisfactory alternative treatment options based on efficacy results from the DESTINY-PanTumor02, DESTINY-Lung01, DESTINY-CRC02 and/or HERALD trials. Additional regulatory submissions for Enhertu also are underway in the EU, including in combination with pertuzumab for the first-line treatment of adult patients with unresectable or metastatic HER2 positive breast cancer based on data from the DESTINY-Breast09 trial and for patients with HER2 positive breast cancer with residual invasive disease after neoadjuvant HER2 targeted treatment based on data from the DESTINY-Breast05 trial. Financial Considerations Following this approval in the EU, an amount of $25 million is due from AstraZeneca to Daiichi Sankyo as a milestone payment for the HER2 positive metastatic solid tumor indication. Sales of Enhertu in most EU territories are recognized by Daiichi Sankyo. For further details on the financial arrangements, please consult the collaboration agreement from March 2019 . About DESTINY-PanTumor02 DESTINY-PanTumor02 is a global, multicenter, multi-cohort, open-label, phase 2 trial evaluating the efficacy and safety of Enhertu (5.4 mg/kg) for the treatment of previously treated HER2 expressing tumors, including biliary tract, bladder, cervical, endometrial, ovarian, pancreatic cancer or other tumors. The primary endpoint of DESTINY-PanTumor02 is confirmed ORR as assessed by investigator. Secondary endpoints include DOR, disease control rate (DCR), progression-free survival (PFS), overall survival (OS), safety, tolerability and pharmacokinetics. Results from DESTINY-PanTumor02 were published in the Journal of Clinical Oncology . DESTINY-PanTumor02 enrolled 267 patients, including 111 HER2 positive (IHC 3+) adult patients at multiple sites in Asia, Europe, North America, South America and Oceania. For more information about the trial, visit ClinicalTrials.gov . About DESTINY-Lung01 DESTINY-Lung01 is a global, open-label, two-cohort, phase 2 trial evaluating the efficacy and safety of Enhertu (5.4 mg/kg or 6.4 mg/kg) in patients with HER2 mutant (Cohort 2, n=91) or HER2 overexpressing (defined as IHC 3+ or IHC 2+) (Cohort 1 and 1a, n=90) unresectable or metastatic NSCLC who had progressed after one or more systemic therapies. The primary endpoint of DESTINY-Lung01 is confirmed ORR by independent central review. Key secondary endpoints include DOR, DCR, PFS, OS and safety. Results from the HER2 mutant cohort were published in The New England Journal of Medicine and results from the HER2 overexpressing cohort were published in The Lancet Oncology . DESTINY-Lung01 enrolled 181 patients, including 17 HER2 positive (IHC 3+) adult patients at multiple sites in Asia, Europe and North America. For more information about the trial, visit ClinicalTrials.gov . About DESTINY-CRC02 DESTINY-CRC02 is a global, randomized, two arm, parallel, multicenter, phase 2 trial evaluating the efficacy and safety of two doses (5.4 mg/kg or 6.4 mg/kg) of Enhertu in patients with locally advanced, unresectable or metastatic HER2 positive colorectal cancer of BRAF wild-type, RAS wild-type or RAS mutant tumor types previously treated with standard therapy. The trial was conducted in two stages. In the first stage, patients (n=80) were randomized 1:1 to receive either 5.4 mg/kg or 6.4 mg/kg of Enhertu. In the second stage, additional patients (n=42) were enrolled in the 5.4 mg/kg arm. The primary endpoint in DESTINY-CRC02 is confirmed ORR as assessed by blinded independent central review. Secondary endpoints include DOR, DCR, investigator-assessed confirmed ORR, clinical benefit ratio, PFS, OS and safety. Results from DESTINY-CRC02 were published in The Lancet Oncology. DESTINY-CRC02 enrolled 122 patients, including 64 HER2 positive (IHC 3+) adult patients at multiple sites in Asia, Europe, North America and Oceania. For more information about the trial, visit ClinicalTrials.gov . About HER2 Expression in Solid Tumors HER2 is a tyrosine kinase receptor growth-promoting protein expressed on the surface of various tissue cells throughout the body and is involved in normal cell growth. 1 HER2 protein overexpression may occur as a result of HER2 gene amplification and is often associated with aggressive disease and poor prognosis in some cancers. 2 HER2 overexpression occurs in a range of solid tumors with the prevalence varying by tumor type. 3 HER2 directed therapies have been used to treat HER2 overexpression in breast, gastric and biliary tract cancers in the EU. 1,4,5,6 Although HER2 is overexpressed in additional solid tumor types including biliary tract, lung, bladder, cervical, colorectal, endometrial, ovarian, salivary gland and pancreatic cancers, HER2 testing is not routinely performed in these additional tumor types and prior to this approval there were no HER2 directed treatments approved in the EU to treat a broad range of solid tumors. 2,7,8 About Enhertu Enhertu (trastuzumab deruxtecan; fam-trastuzumab deruxtecan-nxki in the U.S. only) is a HER2 directed ADC. Designed using Daiichi Sankyo’s proprietary DXd ADC Technology, Enhertu is the lead ADC in the oncology portfolio of Daiichi Sankyo and the most advanced program in AstraZeneca’s ADC scientific platform. Enhertu consists of a HER2 monoclonal antibody attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers. Enhertu (5.4 mg/kg) is approved in the U.S. for the adjuvant treatment of adult patients with HER2 positive breast cancer who have residual invasive disease following neoadjuvant trastuzumab (with or without pertuzumab) and taxane-based treatment based on the DESTINY-Breast05 trial. Enhertu (5.4 mg/kg) followed by THP is approved in China and the U.S. as a neoadjuvant treatment for adult patients with HER2 positive (IHC 3+ or ISH+) stage 2 or stage 3 breast cancer based on the results from the DESTINY-Breast11 trial. Continued approval in China for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial. Enhertu (5.4 mg/kg) in combination with pertuzumab is approved in Brazil, India, Israel, Saudi Arabia, Switzerland, the United Arab Emirates and the U.S. as a first-line treatment for adult patients with unresectable or metastatic HER2 positive (IHC 3+ or ISH+) breast cancer, as determined by a locally or regionally approved test, based on the results from the DESTINY-Breast09 trial. Enhertu (5.4 mg/kg) is approved in more than 95 countries/regions worldwide for the treatment of adult patients with unresectable or metastatic HER2 positive (IHC 3+ or ISH+) breast cancer who have received a prior anti-HER2-based regimen, either in the metastatic setting or in the neoadjuvant or adjuvant setting, and have developed disease recurrence during or within six months of completing therapy based on the results from the DESTINY-Breast03 trial. Enhertu (5.4 mg/kg) is approved in more than 95 countries/regions worldwide for the treatment of adult patients with unresectable or metastatic HER2 low (IHC 1+ or IHC 2+/ISH-) breast cancer who have received a prior systemic therapy in the metastatic setting or developed disease recurrence during or within six months of completing adjuvant chemotherapy based on the results from the DESTINY-Breast04 trial. Enhertu (5.4 mg/kg) is approved in more than 70 countries/regions worldwide for the treatment of adult patients with unresectable or metastatic hormone receptor (HR) positive, HER2 low (IHC 1+ or IHC 2+/ ISH-) or HER2 ultralow (IHC 0 with membrane staining) breast cancer, as determined by a locally or regionally approved test, that have progressed on one or more endocrine therapies in the metastatic setting based on the results from the DESTINY-Breast06 trial. Enhertu (5.4 mg/kg) is approved in more than 75 countries/regions worldwide for the treatment of adult patients with unresectable or metastatic NSCLC whose tumors have activating HER2 ( ERBB2 ) mutations, as detected by a locally or regionally approved test, and who have received a prior systemic therapy based on the results from the DESTINY-Lung02 and/or DESTINY-Lung05 trials. Continued approval in China and the U.S. for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial. Enhertu (6.4 mg/kg) is approved in more than 90 countries/regions worldwide for the treatment of adult patients with locally advanced or metastatic HER2 positive (IHC 3+ or IHC 2+/ISH+) gastric or gastroesophageal junction (GEJ) adenocarcinoma who have received a prior trastuzumab-based regimen based on the results from the DESTINY-Gastric01 , DESTINY-Gastric02 and/or DESTINY-Gastric04 trials. Enhertu (5.4 mg/kg) is approved in more than 40 countries/regions worldwide for the treatment of adult patients with unresectable or metastatic HER2 positive (IHC 3+) solid tumors who have received prior systemic treatment and/or have no satisfactory alternative treatment options based on efficacy results from the DESTINY-PanTumor02 , DESTINY-Lung01 , DESTINY-CRC02 and/or HERALD trials. Continued approval in the U.S. for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial. About the Enhertu Clinical Development Program A comprehensive global clinical development program is underway evaluating the efficacy and safety of Enhertu as a monotherapy or in combination or sequentially with other cancer medicines across multiple HER2 targetable cancers. About the Daiichi Sankyo and AstraZeneca Collaboration Daiichi Sankyo and AstraZeneca entered into a global collaboration to jointly develop and commercialize Enhertu in March 2019 and Datroway ® in July 2020 , except in Japan where Daiichi Sankyo maintains exclusive rights for each ADC. Daiichi Sankyo is responsible for the manufacturing and supply of Enhertu and Datroway. About the ADC Portfolio of Daiichi Sankyo The Daiichi Sankyo ADC portfolio consists of eight ADCs in clinical development crafted from ADC technology discovered in-house by Daiichi Sankyo. The DXd ADC Technology platform of Daiichi Sankyo consists of seven ADCs in clinical development where each ADC is comprised of a monoclonal antibody attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers. The DXd ADCs include Enhertu and Datroway, which are being jointly developed and commercialized globally with AstraZeneca, and ifinatamab deruxtecan (I-DXd), raludotatug deruxtecan (R-DXd) and patritumab deruxtecan (HER3-DXd), which are being jointly developed and commercialized globally with Merck & Co., Inc, Rahway, NJ, USA. DS-3939 and DS3790 are being developed by Daiichi Sankyo. An additional ADC being developed by Daiichi Sankyo is DS3610, which consists of an antibody attached to a novel payload that acts as an agonist of STING. Ifinatamab deruxtecan, raludotatug deruxtecan, patritumab deruxtecan, DS-3939, DS3610 and DS3790 are investigational medicines that have not been approved for any indication in any country. Safety and efficacy have not been established. About Daiichi Sankyo Daiichi Sankyo (TSE: 4568) is a global healthcare company committed to becoming a trusted healthcare innovator, transforming the lives of people through its strength in science and technology. The company discovers and develops new standards of care to address diverse medical needs to fulfill its purpose of contributing to the enrichment of quality of life around the world. With a strategic focus on oncology, Daiichi Sankyo is advancing an industry-leading antibody drug conjugate portfolio along with identifying new breakthrough generating technologies to deliver practice-changing medicines to patients, healthcare professionals and society. For more information, please visit . ________________________________ REFERENCES: 1 Iqbal N, et al. Mol Biol Int. 2014;852748. 2 Cheng X. Genes (Basel ). 2024;15(7):903. 3 Yan M, et al. Cancer Metastasis Reviews. 2015;34(1):157-164. 4 Benli Y, et al. Clin Transl Oncol . 2025;27(9):3607-3624. 5 Uy NF, et al. Cancers (Basel) . 2022;14(17):4155. 6 Haigh JE, et al. Curr Oncol . 2024;31(9):5652-5661. 7 Omar N, et al. Pathogenesis . 2015;2(3):1-9. 8 Ismail A, et al. Oncologist . 2025;30(9):258. Contacts MEDIA CONTACTS: Global: Jennifer Brennan jennifer.brennan@daiichisankyo.com +1 908 900 3183 (mobile) EU: Simone Jendsch-Dowé simone.jendsch-dowe@daiichisankyo.com +49 (89) 78080 (office) Japan: DS-PR_jp@daiichisankyo.com INVESTOR RELATIONS CONTACT: DaiichiSankyoIR_jp@daiichisankyo.com

Clinical ResultPhase 2Drug ApprovalLicense out/inADC

01 Jul 2026

·www.biospace.com

Datroway® Recommended for Approval in the EU by CHMP as First-Line Treatment for Patients with Metastatic Triple Negative Breast Cancer Who Are Not Candidates for Immunotherapy

Recommendation based on TROPION-Breast02 phase 3 trial where Daiichi Sankyo and AstraZeneca’s Datroway showed a statistically significant and clinically meaningful improvement for the dual primary endpoints of overall survival and progression-free survival If approved, Datroway has potential to be the first TROP2 directed antibody drug conjugate for patients in EU with a demonstrated overall survival benefit as first-line treatment TOKYO--(BUSINESS WIRE)--Datroway ® (datopotamab deruxtecan) has been recommended for approval in the European Union (EU) as monotherapy for the first-line treatment of adult patients with unresectable or metastatic triple negative breast cancer (TNBC) who are not candidates for PD-1/PD-L1 inhibitor therapy. Datroway is a specifically engineered TROP2 directed DXd antibody drug conjugate (ADC) discovered by Daiichi Sankyo (TSE: 4568) and being jointly developed and commercialized by Daiichi Sankyo and AstraZeneca (LSE/STO/NYSE: AZN). The Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) based its positive opinion on results from the TROPION-Breast02 phase 3 trial, which were presented at the 2025 European Society for Medical Oncology Congress and published in Annals of Oncology . The recommendation will now be reviewed by the European Commission, which has the authority to grant marketing authorizations for medicines in the EU. In TROPION-Breast02, Datroway demonstrated a statistically significant and clinically meaningful 5.0-month improvement in median overall survival (OS) versus investigator’s choice of chemotherapy (hazard ratio [HR]=0.79; 95% confidence interval [CI]: 0.64-0.98; p=0.0291). Median OS was 23.7 months for patients treated with Datroway versus 18.7 months for those treated with chemotherapy. Datroway reduced the risk of disease progression or death by 43% compared to chemotherapy (HR=0.57; 95% CI: 0.47-0.69; p<0.0001) as assessed by blinded independent central review (BICR). Median progression-free survival (PFS) was 10.8 months for patients treated with Datroway versus 5.6 months for those treated with chemotherapy in patients with metastatic TNBC who are not candidates for PD-1/PD-L1 inhibitor therapy. Datroway was also associated with more robust treatment responses compared to chemotherapy, with an objective response rate (ORR) of 62.5% versus 29.3% for those treated with chemotherapy. “Triple negative breast cancer remains one of the most aggressive types of breast cancer, with limited treatment options for patients with metastatic disease who are not candidates for immunotherapy and are currently treated with traditional chemotherapy,” said John Tsai, MD, Global Head, R&D, Daiichi Sankyo. “This positive recommendation by the CHMP underscores the potential for Datroway to replace traditional chemotherapy in this setting and we look forward to working closely with the EMA to bring this new indication to patients in the EU.” “As one of the hardest cancers to treat, today only 15% of patients with metastatic triple negative breast cancer survive beyond five years,” said Susan Galbraith, MBBChir, PhD, Executive Vice President, Oncology Hematology R&D, AstraZeneca. “This positive opinion from the CHMP marks an important step forward in bringing the potential of Datroway to transform outcomes for patients with this type of cancer in the EU.” The safety pro Datroway (6 mg/kg) was evaluated in 319 patients with TNBC who received Datroway in TROPION-Breast02. The most common (≥20%) adverse reactions, including laboratory abnormalities, were stomatitis, increased amylase, nausea, alopecia, decreased hemoglobin, decreased white blood cells, constipation, decreased calcium, decreased lymphocytes, fatigue, decreased neutrophils, increased alanine aminotransferase, increased aspartate aminotransferase, dry eye, keratitis, decreased albumin, vomiting, musculoskeletal pain, decreased sodium and increased blood alkaline phosphatase. Serious adverse reactions occurred in 17% of patients who received Datroway. Serious adverse reactions in more than 1% of patients who received Datroway included pneumonia, vomiting, COVID-19 and anemia. One patient fatality was attributed to interstitial lung disease/pneumonitis. Datroway was approved in the U.S. in May 2026 for the treatment of adult patients with unresectable or metastatic TNBC who are not candidates for PD-1/PD-L1 inhibitor therapy. Additional reviews are underway in China and Japan, as well as Australia, Canada, Singapore and Switzerland as part of Project Orbis. About TROPION-Breast02 TROPION-Breast02 is a global, multicenter, randomized, open-label phase 3 trial evaluating the efficacy and safety of Datroway versus investigator’s choice of chemotherapy (paclitaxel, nab-paclitaxel, capecitabine, carboplatin or eribulin) in patients with previously untreated locally recurrent inoperable or metastatic TNBC for whom immunotherapy was not an option. This included patients whose tumors did not express PD-L1 as well as patients with PD-L1 expressing tumors who could not receive immunotherapy due to prior exposure in early-stage disease, comorbidities or immunotherapy not being accessible in their geography. Enrollment included patients with de novo or recurrent disease, regardless of disease-free interval, and those with poor prognostic factors such as stable brain metastases. The dual primary endpoints of TROPION-Breast02 are OS and PFS as assessed by BICR. Secondary endpoints include PFS as assessed by investigator, ORR, duration of response, disease control rate, pharmacokinetics and safety. TROPION-Breast02 enrolled 644 patients at sites in Africa, Asia, Europe, North America and South America. For more information visit ClinicalTrials.gov . About Triple Negative Breast Cancer TNBC accounts for approximately 15% of all breast cancer cases, with an estimated 345,000 diagnoses globally each year. 1,2 In Europe, there are an estimated 83,000 diagnoses of TNBC each year. 1,3 TNBC is diagnosed more frequently in younger and premenopausal women, and is more prevalent in Black and Hispanic women. 4,5,6 Metastatic TNBC is the most aggressive type of breast cancer and has one of the worst prognoses, with median OS of just 12 to 18 months and only about 15% of patients living five years following diagnosis. 4,7,8 While some breast cancers may test positive for estrogen receptors, progesterone receptors or overexpression of HER2, TNBC tests negative for all three. 4 Due to its aggressive nature and absence of common breast cancer receptors, TNBC is characteristically difficult to treat. 4 For patients with metastatic disease with PD-L1 expressing tumors, the addition of immunotherapy to chemotherapy has improved outcomes in the first-line setting. 9,10 However, for approximately 70% of patients with metastatic TNBC who are not candidates for immunotherapy, chemotherapy was the standard first-line treatment. 11 TROP2 is a protein broadly expressed in several solid tumors, including TNBC. 12 TROP2 is associated with increased tumor progression and poor survival in patients with breast cancer. 13,14 About Datroway Datroway (datopotamab deruxtecan; datopotamab deruxtecan-dlnk in the U.S. only) is a TROP2 directed ADC. Designed using Daiichi Sankyo’s proprietary DXd ADC Technology, Datroway is one of seven DXd ADCs in the oncology pipeline of Daiichi Sankyo, and one of the most advanced programs in AstraZeneca’s ADC scientific platform. Datroway is comprised of a humanized anti-TROP2 IgG1 monoclonal antibody, developed in collaboration with Sapporo Medical University, attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers. Datroway (6 mg/kg) is approved in Brazil, Russia and the U.S. for the treatment of adult patients with unresectable or metastatic TNBC who are not candidates for PD-1/PD-L1 inhibitor therapy based on the results from the TROPION-Breast02 trial. Datroway (6 mg/kg) is approved in more than 40 countries/regions worldwide for the treatment of adult patients with unresectable or metastatic HR positive, HER2 negative (IHC 0, IHC 1+ or IHC 2+/ISH-) breast cancer who have received prior endocrine-based therapy and chemotherapy for unresectable or metastatic disease based on the results from the TROPION-Breast01 trial. Datroway (6 mg/kg) is approved in Russia and the U.S. for the treatment of adult patients with locally advanced or metastatic EGFR-mutated non-small cell lung cancer (NSCLC) who have received prior EGFR-directed therapy and platinum-based chemotherapy, based on the results from TROPION-Lung05 and TROPION-Lung01 trials. Continued approval for this indication in the U.S. may be contingent upon verification and description of clinical benefit in a confirmatory trial. About the Datroway Clinical Development Program A comprehensive global clinical development program is underway with more than 20 trials evaluating the efficacy and safety of Datroway across multiple cancers, including NSCLC, TNBC and urothelial cancer. The program includes eight phase 3 trials in lung cancer, five phase 3 trials in breast cancer, and one phase 2/3 trial in urothelial cancer evaluating Datroway as a monotherapy and in combination with other cancer treatments in various settings. About the Daiichi Sankyo and AstraZeneca Collaboration Daiichi Sankyo and AstraZeneca entered into a global collaboration to jointly develop and commercialize Enhertu ® in March 2019 and Datroway in July 2020 , except in Japan where Daiichi Sankyo maintains exclusive rights for each ADC. Daiichi Sankyo is responsible for the manufacturing and supply of Enhertu and Datroway. About the ADC Portfolio of Daiichi Sankyo The Daiichi Sankyo ADC portfolio consists of eight ADCs in clinical development crafted from ADC technology discovered in-house by Daiichi Sankyo. The DXd ADC Technology platform of Daiichi Sankyo consists of seven ADCs in clinical development where each ADC is comprised of a monoclonal antibody attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers. The DXd ADCs include Enhertu and Datroway, which are being jointly developed and commercialized globally with AstraZeneca, and ifinatamab deruxtecan (I-DXd), raludotatug deruxtecan (R-DXd) and patritumab deruxtecan (HER3-DXd), which are being jointly developed and commercialized globally with Merck & Co., Inc, Rahway, NJ, USA. DS-3939 and DS3790 are being developed by Daiichi Sankyo. An additional ADC being developed by Daiichi Sankyo is DS3610, which consists of an antibody attached to a novel payload that acts as an agonist of STING. Ifinatamab deruxtecan, raludotatug deruxtecan, patritumab deruxtecan, DS-3939, DS3610 and DS3790 are investigational medicines that have not been approved for any indication in any country. Safety and efficacy have not been established. About Daiichi Sankyo Daiichi Sankyo (TSE: 4568) is a global healthcare company committed to becoming a trusted healthcare innovator, transforming the lives of people through its strength in science and technology. The company discovers and develops new standards of care to address diverse medical needs to fulfill its purpose of contributing to the enrichment of quality of life around the world. With a strategic focus on oncology, Daiichi Sankyo is advancing an industry-leading antibody drug conjugate portfolio along with identifying new breakthrough generating technologies to deliver practice-changing medicines to patients, healthcare professionals and society. For more information, please visit . References: 1 O’Reilly D, et al. World J Clin Oncol 2021;12(3):164-182. 2 World Health Organization. Breast Cancer . Accessed June 2026. 3 World Health Organization. Global Cancer Observatory: Europe . Accessed June 2026. 4 American Cancer Society. Triple-Negative Breast Cancer . Accessed June 2026. 5 Martinez M, et al. Breast Cancer Res Treat . 2017;166(1):185-193. 6 Vargas L, et al. Cancer Epidemiol Biomarkers Prev . 2019;28(11):1771-1783. 7 National Cancer Institute. SEER Cancer Stat Facts: Female Breast Cancer Subtypes . Accessed June 2026. 8 Huppert L, et al. Ther Adv Med Oncol . 2022;14:1-25. 9 Cortes J, et al. N Engl J Med . 2022;387:217-226. 10 Geurts V, et al. Curr Treat Options Oncol . 2023;24:628-643. 11 Punie K, et al. Oncologist . 2025;30(3):oyaf034. 12 Rossi V, et al. Front Immunol . 2024;15:1447280. 13 Lin H, et al. Exp Mol Pathol . 2013:94(1):73-78. 14 Goldenberg D, et al. Oncotarget . 2018;9(48):28989-29006. Contacts MEDIA CONTACTS: Global: Jennifer Brennan jennifer.brennan@daiichisankyo.com + 1 908 900 3183 (mobile) Japan: DS-PR_jp@daiichisankyo.com EU: Simone Jendsch-Dowé simone.jendsch-dowe@daiichisankyo.com +49 (89) 78080 (office) INVESTOR RELATIONS CONTACT: DaiichiSankyoIR_jp@daiichisankyo.com

Phase 3ImmunotherapyClinical ResultLicense out/inDrug Approval

28 May 2026

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Daiichi Sankyo Showcases Progress Across Industry-Leading Oncology Portfolio with Latest Research Updates at ASCO

New analyses from five landmark trials of Enhertu® and Datroway® in breast and gastric cancer alongside pipeline data across other tumor types demonstrate continued oncology leadership Early phase trials-in-progress featuring potential medicines with novel mechanisms highlight the company’s commitment to identifying new breakthrough generating technologies for patients with cancer TOKYO--(BUSINESS WIRE)--Daiichi Sankyo (TSE: 4568) will present new clinical research across its oncology portfolio with more than 25 abstracts in multiple cancers at the 2026 American Society of Clinical Oncology Annual Meeting (#ASCO26). Data at ASCO will highlight the company’s progress toward advancing new standards of care for patients with cancer, including new analyses from five landmark trials in breast and gastric cancer, including the DESTINY-Breast05 (# 516 ), DESTINY-Breast06 (# 1063 ), DESTINY-Breast09 (# 1021 ) and DESTINY-Gastric04 (# 4111 ) phase 3 trials of Enhertu ® (trastuzumab deruxtecan), and the TROPION-Breast02 (# 1002 ) phase 3 trial of Datroway ® (datopotamab deruxtecan). Additional results from earlier phase trials as well as trials-in-progress across new medicines being developed through the company’s breakthrough generating technology (BGT), a platform-based drug discovery model designed to deliver innovative medicines to patients faster, will be highlighted. Data from DESTINY-Breast05 formed the basis of one of two new Enhertu indications recently approved in the U.S. for certain patients with early-stage HER2 positive breast cancer and data from DESTINY-Gastric04 was included as part of a label update to expand the use of Enhertu in Japan and China to include the second-line treatment of patients with HER2 positive metastatic gastric cancer. Additionally, results from TROPION-Breast02 formed the basis of the recent U.S. approval of Datroway in patients with metastatic triple negative breast cancer (TNBC) who are not candidates for PD-1/PD-L1 inhibitor therapy, the first antibody drug conjugate (ADC) to be approved in this setting of TNBC. “The approvals received just prior to ASCO for Enhertu and Datroway, two of our leading DXd antibody drug conjugates, together with the strong science being showcased across our pipeline, highlight the momentum of our oncology portfolio,” said John Tsai, MD, Global Head, R&D, Daiichi Sankyo. “Daiichi Sankyo is committed to creating new standards of care for patients with cancer and continues to leverage its scientific and technological expertise to advance innovation.” Additional Enhertu Data Spans Broad Range of HER2 Expressing Cancers Additional research updates across several additional HER2 expressing cancers include oral and poster sessions highlighting the preliminary safety run-in results from the DESTINY-Ovarian01 (# 5554 ) phase 3 trial evaluating Enhertu in combination with bevacizumab compared to bevacizumab monotherapy as a first-line maintenance therapy in patients with HER2 expressing ovarian cancer; the primary analysis from part 1 of the DESTINY-PanTumor03 (# 3026 ) phase 2 trial evaluating Enhertu in pretreated patients in China with HER2 positive (IHC 3+) solid tumors (excluding breast and gastric cancer); and, findings from the MYTHOS (# 6011 ) phase 2 trial evaluating Enhertu in patients with HER2-low recurrent or metastatic salivary gland cancer. Additional breast and gastric cancer data for Enhertu include an oral presentation from one arm of the DESTINY-Breast07 (# 1012 ) phase 1b/2 trial evaluating Enhertu in combination with durvalumab as a first-line treatment in patients with HER2 positive metastatic breast cancer and a poster presentation highlighting a safety analysis from the DESTINY-Gastric03 (# 4022 ) phase 1b/2 trial evaluating Enhertu in combination with chemotherapy and immunotherapy as a first-line treatment in patients with HER2 expressing metastatic gastric cancer, gastroesophageal junction (GEJ) adenocarcinoma or esophageal adenocarcinoma. Results from cohort two of the EPOC2203 (# 4024 ) phase 1b/2 trial evaluating Enhertu in combination with nivolumab and capecitabine and oxaliplatin in patients with HER2 low gastroesophageal adenocarcinoma and an exploratory analysis of translational data from the EPOC2003 (# 3129 ) phase 2 trial evaluating neoadjuvant chemotherapy in combination with Enhertu in patients with HER2 positive gastric cancer will be highlighted as poster presentations. New Data and Trials-in-Progress Presentations Across Oncology Portfolio Poster presentations will include a trial-in-progress update of REJOICE-Ovarian01 ( TPS5637 ) for the phase 3 part of a phase 2/3 trial evaluating raludotatug deruxtecan (R-DXd) compared to treatment of physician’s choice in patients with platinum-resistant ovarian cancer. Two additional poster presentations will highlight an exposure-response analysis (# 5570 ) and a population pharmacokinetic analysis (# 5571 ) of data from both the REJOICE-Ovarian01 phase 2/3 trial and the phase 1 trial evaluating raludotatug deruxtecan in patients with advanced ovarian cancer or renal cell carcinoma. An oral presentation will highlight results from a phase 1/2 trial (# 6504 ) of Vanflyta® (quizartinib) plus decitabine and venetoclax in patients with newly diagnosed or relapsed/refractory FLT3 -ITD acute myeloid leukemia. Trials-in-progress poster presentations across the DXd ADC portfolio include the TROPION-Urothelial03 ( TPS4642 ) phase 2/3 trial evaluating Datroway and platinum chemotherapy compared to gemcitabine plus platinum chemotherapy in patients with locally advanced or metastatic urothelial carcinoma; the HERTHENA-Breast04 ( TPS1149 ) phase 3 trial evaluating patritumab deruxtecan (HER3-DXd) compared to treatment of physician’s choice in patients with HR positive, HER2 negative unresectable locally advanced or metastatic breast cancer; and the DESTINY-PanTumor04 ( TPS11202 ) hybrid observational trial evaluating Enhertu in patients with HER2 positive (IHC 3+) solid tumors. Trials-in-Progress Presentations Highlight Breakthrough Generating Technology Focus Daiichi Sankyo is leveraging its strength in science and technology to create new medicines for patients with cancer through its BGT approach which is designed to deliver innovative medicines to patients faster and with a higher probability of success. Trials-in-progress poster presentations featuring three potential new medicines include DS3610 ( TPS3159 ), a STING (stimulator of interferon genes) ADC, in patients with advanced or metastatic solid tumors; DS5361 ( TPS2680 ), a small-molecule, nonsense-mediated mRNA decay inhibitor, in patients with advanced or metastatic solid tumors; and, DS9051 ( TPS3179 ), a novel targeted protein degradation molecule, in patients with advanced or metastatic adrenocortical carcinoma or metastatic castration-resistant prostate cancer. Overview of clinical data and trials-in-progress from oncology pipeline of Daiichi Sankyo include: Presentation Title Author Abstract Presentation (CDT) Breast A DESTINY-Breast09 analysis of treatment duration and clinical outcomes by best response to trastuzumab deruxtecan (T-DXd) + pertuzumab Y. Park 1021 Rapid Oral Presentation Sunday, May 31 11:30 am – 1:00 pm Secondary safety analysis of trastuzumab deruxtecan (T-DXd) vs trastuzumab emtansine (T-DM1) in DESTINY-Breast05: clinical and demographic risk factors of interstitial lung disease and radiation pneumonitis M. Untch 516 Rapid Oral Presentation Monday, June 1 9:45 – 11:15 am Neoadjuvant rilvegostomig (R) + trastuzumab deruxtecan (T-DXd) in high-risk HER2-negative breast cancer: Results from the I-SPY 2.2 trial C. O’Sullivan LBA514 Rapid Oral Presentation Monday, June 1 9:45 – 11:15 am Trastuzumab deruxtecan (T-DXd) + durvalumab in patients with previously untreated HER2 positive unresectable/metastatic breast cancer (mBC): final analysis from DESTINY-Breast07 S. Loi 1012 Oral Presentation Sunday, May 31 8:30 – 10:00 am First-line datopotamab deruxtecan (Dato-DXd) vs chemotherapy in patients with locally recurrent inoperable or metastatic triple negative breast cancer for whom immunotherapy was not an option: additional efficacy endpoints from the TROPION-Breast02 study D. Cescon 1002 Oral Presentation Tuesday, June 2 9:45 am – 12:45 pm Impact of adherence to interstitial lung disease (ILD)/pneumonitis toxicity management guidelines on ILD/pneumonitis outcomes: a retrospective analysis of patients treated with trastuzumab deruxtecan (T-DXd) in DESTINY-Breast06 C. Mateo 1063 Poster Session Monday, June 1 1:30 – 4:30 pm HERTHENA-Breast04: a phase 3, randomized, open-label study evaluating the efficacy and safety of patritumab deruxtecan (HER3-DXd) versus treatment of physician’s choice in hormone receptor positive (HR +)/HER2-) unresectable locally advanced or metastatic breast cancer B. Pistilli TPS1149 Poster Session Monday, June 1 1:30 – 4:30 pm Identifying patients with human epidermal growth factor receptor 2 (HER2) low and ultralow breast cancer: use of digital, artificial intelligence-based computational algorithms to assist HER2 scoring by pathologists S. Krishnamurthy 1022 Poster Session Monday, June 1 1:30 – 4:30 pm Gastric Additional health-related quality of life analysis from DESTINY-Gastric04, a randomized phase 3 study of trastuzumab deruxtecan (T-DXd) vs ramucirumab + paclitaxel in patients with HER2 positive unresectable/metastatic gastric cancer/gastroesophageal junction adenocarcinoma K. Shitara 4111 Poster Session Saturday, May 30 9:00 am – 12:00 pm First-line trastuzumab deruxtecan (T-DXd)-based regimens in advanced HER2 expressing gastric cancer, gastroesophageal junction adenocarcinoma, or esophageal adenocarcinoma: safety results from DESTINY-Gastric03 Part 2 arms D and F, and Part 4 Y. Janjigian 4022 Poster Session Saturday, May 30 9:00 am – 12:00 pm An open-label phase 1b/2 study of trastuzumab deruxtecan combined with nivolumab and CAPOX in patients with HER2 low gastroesophageal adenocarcinoma (EPOC2203) Y. Aoki 4024 Poster Session Saturday, May 30 9:00 am – 12:00 pm Tumor and immune microenvironment remodeling with neoadjuvant trastuzumab deruxtecan in HER2 positive gastric cancer: exploratory analyses from the phase 2 EPOC2003 study A. Kawazoe 3129 Poster Session Saturday, May 30 1:30 – 4:30 pm Ovarian Trastuzumab deruxtecan (T-DXd) + bevacizumab (BEV) as first-line (1L) maintenance therapy in patients with HER2 expressing ovarian cancer: results from the DESTINY-Ovarian01 safety run-in A. Gonzalez Martin 5554 Poster Session Monday, June 1 9:00 am – 12:00 pm REJOICE-Ovarian01: phase 3 part of a phase 2/3 study evaluating raludotatug deruxtecan (R-DXd) versus treatment of physician’s choice in patients with platinum-resistant ovarian cancer D. Richardson TPS5637 Poster Session Monday, June 1 9:00 am – 12:00 pm Exposure-response analyses of efficacy and safety with raludotatug deruxtecan (R-DXd), a CDH6-directed ADC, to inform dose selection for phase 3 development in platinum-resistant ovarian cancer F. Hurtado 5570 Poster Session Monday, June 1 9:00 am – 12:00 pm Population pharmacokinetic analysis of raludotatug deruxtecan (R-DXd), a CDH6-directed ADC, in patients with advanced ovarian cancer or renal cell carcinoma F. Hurtado 5571 Poster Session Monday, June 1 9:00 am – 12:00 pm Urothelial TROPION-Urothelial03: a phase 2/3 study of datopotamab deruxtecan (Dato-DXd) + platinum chemotherapy vs gemcitabine + platinum chemotherapy in participants with locally advanced or metastatic urothelial carcinoma with progression on or after enfortumab vedotin + pembrolizumab M. Galsky TPS4642 Poster Session Sunday, May 31 9:00 am – 12:00 pm Salivary Trastuzumab deruxtecan in patients with HER2 low recurrent/metastatic salivary gland carcinoma: results from the phase 2 MYTHOS trial I. Kinoshita 6011 Oral Presentation Monday, June 1 8:00 – 9:30 am AML Quizartinib in combination with decitabine and venetoclax for newly diagnosed and relapsed/refractory FLT3 mutated acute myeloid leukemia M. Yilmaz 6504 Oral Presentation Tuesday, June 2 9:45 am – 12:45 pm Pan Tumor Trastuzumab deruxtecan (T-DXd) for pretreated patients in China with HER2 IHC 3+ solid tumors: DESTINY-PanTumor03 Part 1 primary analysis Y. Zhang 3026 Poster Session Saturday, May 30 1:30 – 4:30 pm A pragmatic, hybrid observational study evaluating the effectiveness of trastuzumab deruxtecan (T-DXd) in patients with HER2 IHC3+ solid tumors: DESTINY-PanTumor04 B. Monk TPS11202 Poster Session Monday, June 1 9:00 am – 12:00 pm HER2 independent antitumor and pharmacodynamic responses to trastuzumab deruxtecan in patients with advanced solid tumors S. Shin 3031 Poster Session Saturday, May 30 1:30 – 4:30 pm Topoisomerase 1 and DNA damage: pharmacodynamic responses and mechanism of trastuzumab deruxtecan in HER2-expressing advanced solid tumors D. Wilsker 3092 Poster Session Saturday, May 30 1:30 – 4:30 pm BGT A phase 1, first-in-human study of DS3610, a stimulator of interferon genes (STING) agonist ADC, in patients with advanced/metastatic solid tumors S. Koganemaru TPS3159 Poster Session Saturday, May 30 1:30 – 4:30 pm A phase 1, first-in-human study of DS5361, a small-molecule, nonsense-mediated mRNA decay inhibitor, in patients with advanced/metastatic solid tumors (Parts 1 and 2) S. Sen TPS2680 Poster Session Saturday, May 30 1:30 – 4:30 pm A phase 1, first-in-human study of DS9051, a novel targeted protein degradation molecule, in patients with advanced/metastatic adrenocortical carcinoma or metastatic castration-resistant prostate cancer M. Patel TPS3179 Poster Session Saturday, May 30 1:30 – 4:30 pm About the ADC Portfolio of Daiichi Sankyo The Daiichi Sankyo ADC portfolio consists of eight ADCs in clinical development crafted from ADC technology discovered in-house by Daiichi Sankyo. The DXd ADC Technology platform of Daiichi Sankyo consists of seven ADCs in clinical development where each ADC is comprised of a monoclonal antibody attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers. The DXd ADCs include Enhertu and Datroway, which are being jointly developed and commercialized globally with AstraZeneca, and ifinatamab deruxtecan (I-DXd), raludotatug deruxtecan (R-DXd) and patritumab deruxtecan (HER3-DXd), which are being jointly developed and commercialized globally with Merck & Co., Inc, Rahway, NJ, USA. DS-3939 and DS3790 are being developed by Daiichi Sankyo. An additional ADC being developed by Daiichi Sankyo is DS3610, which consists of an antibody attached to a novel payload that acts as an agonist of STING. Ifinatamab deruxtecan, raludotatug deruxtecan, patritumab deruxtecan, DS-3939, DS3610 and DS3790 are investigational medicines that have not been approved for any indication in any country. Safety and efficacy have not been established. About Daiichi Sankyo Daiichi Sankyo (TSE: 4568) is a global healthcare company committed to becoming a trusted healthcare innovator, transforming the lives of people through its strength in science and technology. The company discovers and develops new standards of care to address diverse medical needs to fulfill its purpose of contributing to the enrichment of quality of life around the world. With a strategic focus on oncology, Daiichi Sankyo is advancing an industry-leading antibody drug conjugate portfolio along with identifying new breakthrough generating technologies to deliver practice-changing medicines to patients, healthcare professionals and society. For more information, please visit . Contacts MEDIA CONTACTS: Global: Jennifer Brennan jennifer.brennan@daiichisankyo.com +1 908 900 3183 (mobile) Japan: DS-PR_jp@daiichisankyo.com INVESTOR RELATIONS CONTACT: DaiichiSankyoIR_jp@daiichisankyo.com

Phase 3Clinical ResultPhase 1ASCOPhase 2

100 Deals associated with Raludotatug deruxtecan

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Indication	Highest Phase	Country/Location	Organization	Date
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	United States	Daiichi Sankyo Co., Ltd.	27 Feb 2024
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	United States	Merck Sharp & Dohme LLC	27 Feb 2024
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	China	Merck Sharp & Dohme LLC	27 Feb 2024
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	China	Daiichi Sankyo Co., Ltd.	27 Feb 2024
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Japan	Daiichi Sankyo Co., Ltd.	27 Feb 2024
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Japan	Merck Sharp & Dohme LLC	27 Feb 2024
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Australia	Merck Sharp & Dohme LLC	27 Feb 2024
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Australia	Daiichi Sankyo Co., Ltd.	27 Feb 2024
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Brazil	Merck Sharp & Dohme LLC	27 Feb 2024
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Brazil	Daiichi Sankyo Co., Ltd.	27 Feb 2024

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT06161025 (REJOICE-Ovarian01, ASCO2026)	Phase 3	Platinum-Resistant Ovarian Carcinoma CDH6 expression	600	R-DXd 5.6 mg/kg	ehrmzgphbo(wajgxocsnd) = hmestcsmwd dfqmkkvcxl (gqnjrvzyqf, 42.9 - 57.1) View more	Positive	29 May 2026
NCT04707248 (REJOICE-Ovarian01, ASCO2026)	Phase 1/2	Platinum-Resistant Ovarian Carcinoma CDH6 expression	286	Raludotatug deruxtecan 5.6 mg/kg Q3W	wtebzqzevc(fmtqcwpdys) = Higher R-DXd or DXd payload exposure was associated with an increase in drug-related TEAEs, including Grade ≥3 (G3+) AEs, any-grade ILD, G2+ gastrointestinal AEs (nausea/vomiting), G3+ cytopenias (anemia, neutropenia, thrombocytopenia), and AEs leading to dose reduction. xwqscrrjwn (hqibkpzhgk ) View more	Positive	29 May 2026
NCT04707248 (REJOICE-PanTumor01, ASCO_GU2026)	Phase 2	Urogenital Neoplasms \| Genital Diseases, Female CDH6	40	R-DXd 5.6 mg/kg (Cervical Cancer)	xaboattgxm(sidhrxgisl) = kwieovebbx plskoyjqvv (jrfimovqaq )	Positive	26 Feb 2026
				R-DXd 5.6 mg/kg (Non-HGSOC)	xaboattgxm(sidhrxgisl) = dlepciikpg plskoyjqvv (jrfimovqaq )
NCT06161025 (REJOICE-Ovarian01, ESMO 12025 \| ESMO 22025) Manual	Phase 2	Platinum-Resistant Fallopian Tube Carcinoma \| Platinum-Resistant Primary Peritoneal Carcinoma \| Platinum-Resistant Ovarian Carcinoma	107	R-DXd (4.8 mg/kg)	gdarsvnjbf(yjssktfobn) = tpjwablkbu joxodqeqrl (tqipbbrqvi, 27.9 - 61.9) View more	Positive	17 Oct 2025
				R-DXd (5.6 mg/kg)	gdarsvnjbf(yjssktfobn) = wssdqszcac joxodqeqrl (tqipbbrqvi, 32.9 - 67.1) View more
NCT06780085 (KEYMAKER-U01, ESMO2025)	Phase 2	metastatic non-small cell lung cancer	240	R-DXd 5.6 mg/kg Q3W	ewkynqfgqt(utadpliren) = gqvmaulrbx oiirmjmddl (qpyxqgdpcv )	Positive	17 Oct 2025
				I-DXd 12 mg/kg Q3W	ewkynqfgqt(xjbweccjic) = itrrxgdslb pmwvolcutv (mbtnxjbdqo ) View more
NCT04707248 (Corporate Publications) Manual	Phase 1	Ovarian Cancer	50	Raludotatug deruxtecan	bncplcowrc(lwkhbmnhzs) = rcqfqcaroi tqzrdzqulu (nurworhjrq, 32 - 61) View more	Positive	22 Oct 2023
NCT04707248 (ESMO 12023 \| ESMO 22023) Manual	Phase 1	Ovarian Cancer	42	R-DXd at 4.8 mg/kg	uuurdkhyya(wxblnlfxmy) = osbzachwiz ksaokjfscm (iuwewhfxwm ) View more	Positive	22 Oct 2023
				R-DXd at 6.4 mg/kg	uuurdkhyya(wxblnlfxmy) = bzdbgzjyva ksaokjfscm (iuwewhfxwm ) View more
NCT04707248 (ASCO2022) Manual	Phase 1	Ovarian Cancer \| Advanced Renal Cell Carcinoma	22	DS-6000a	wwtsvnmsso(ccelhxhmms) = vikpkvoayj vejsbrussr (imjimwkyku ) View more	Positive	02 Jun 2022

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