HER2 antagonists(Receptor tyrosine-protein kinase erbB-2 antagonists), TOP1 inhibitors(DNA topoisomerase I inhibitors), ADCC(Antibody-dependent cell-mediated cytotoxicity (ADCC) effects)

Therapeutic Areas

NeoplasmsDigestive System DisordersRespiratory Diseases+ [5]

Active Indication

Metastatic human epidermal growth factor 2 positive carcinoma of breastStomach CancerHER2 Positive Solid Tumors+ [67]

Inactive Indication

HER2 Positive Transitional Cell CarcinomaHER2-expressing Gastroesophageal Junction AdenocarcinomaMeningeal Carcinomatosis+ [1]

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization

Daiichi Sankyo Co., Ltd.

AstraZeneca PLC

Daiichi Sankyo, Inc.

+ [10]

Inactive Organization-

License Organization

Merck & Co., Inc.

AstraZeneca PLC

Daiichi Sankyo Co., Ltd.

+ [2]

Drug Highest PhaseApproved

First Approval Date

United States (20 Dec 2019),

HER2 Positive Breast Cancer

RegulationBreakthrough Therapy (United States), Fast Track (United States), Accelerated Approval (United States), Orphan Drug (United States), Conditional marketing approval (China), Orphan Drug (Japan), Orphan Drug (Australia), Priority Review (Australia), Breakthrough Therapy (China), Priority Review (United States), Priority Review (China), SAKIGAKE (Japan)

Structure/Sequence

Boost your research with our ADC technology data.

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Sequence Code 18481L

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Sequence Code 44772H

Source: *****

201

Clinical Trials associated with Fam-trastuzumab deruxtecan-NXKI

NCT07578116

/ Not yet recruitingPhase 3IIT

Randomized Phase III Trial of Multimodality Therapy Versus Standard of Care Systemic Therapy in HER2 Positive (HER2+) De Novo (AJCC Stage IV) Oligometastatic Breast Cancer With Response to Initial Chemotherapy

This phase III trial evaluates the effect of adding locoregional therapy (surgery and radiation) and metastasis-directed stereotactic body radiation therapy (SBRT) to standard systemic therapy following standard HER2-targeted systemic therapy, compared to standard systemic therapy alone, in treating patients with HER2-positive stage IV breast cancer that has spread from where it first started (primary site) to other places in the body (metastatic) or to a limited number of sites (oligometastatic). The usual approach for patients with (oligo)metastatic HER2-positive breast cancer is systemic drug treatment, which means medicines that travel through the whole body to treat both the breast and any areas where the cancer has spread. There are a number of approved HER2-targeted systemic therapy regimens available to patients. These typically include immunotherapy and/or chemotherapy. Immunotherapy drugs may induce changes in body's immune system and may interfere with the ability of tumor cells to grow and spread. Chemotherapy drugs work in different ways to stop the growth of tumor cells, either by killing the cells, by stopping them from dividing, or by stopping them from spreading. Unlike systemic therapy, locoregional therapies like surgery and radiation are focused treatments at the site of disease, delivered with the intent of sparing healthy tissues. Breast surgeries such as breast conserving therapy or total mastectomy are procedures in which the cancerous breast tissue (and healthy breast tissue in the case of total mastectomy) are surgically removed from the body. Radiation therapy uses high energy x-rays, particles, or radioactive seeds to kill cancer cells and shrink tumors. SBRT is a type of external radiation therapy that uses special equipment to position a patient and precisely deliver radiation to tumors in the body (except the brain). The total dose of radiation is divided into smaller doses given over several days. This type of radiation therapy helps spare normal tissue. Adding locoregional therapy, as well as metastasis-directed SBRT, to standard systemic therapy may help patients with (oligo)metastatic, HER2-positive stage IV breast cancer live longer overall or before their cancer progresses, and may help more patients achieve no evidence of disease, when compared to standard systemic therapy alone.

Start Date09 Mar 2027

Sponsor / Collaborator

SWOG

[+1]

NCT07126561

/ Not yet recruitingPhase 2IIT

Phase II Open Label Trial of Trastuzumab Deruxtecan (Enhertu, DS-8210) in HER2 Positive Newly Diagnosed Metastatic Esophageal, Gastric, GEJ Cancer Patients With an ECOG Performance Status of 2

Purpose: This clinical trial is designed to evaluate the safety and effectiveness of Trastuzumab Deruxtecan for patients with HER2 Positive Newly Diagnosed Metastatic Esophageal, Gastric, GEJ Cancer. The goal is to determine how well this treatment works and to identify any potential side effects.
Who Can Participate: We are looking for Participants with histologically confirmed HER2 positive locally advanced unresectable and/or metastatic esophageal, gastric or GEJ adenocarcinoma with an ECOG PS of 2 and measurable disease according to RECIST 1.1 within 42 days prior to registration. Participants will be carefully screened to ensure they meet the study requirements.
What to Expect: Participants will undergo 6.4mg/kg, IV infusion of Trastuzumab deruxtucan over the course of the study. They will receive detailed information about the study and will have the opportunity to ask questions before deciding to participate. Informed consent will be obtained to ensure that participants understand the study's purpose, procedures, risks, and benefits.
Safety Monitoring: The health and safety of participants are our top priority. An Independent Data and Safety Monitoring Committee (DSMC) will regularly review the study data to ensure participant safety and to monitor for any adverse events. Any serious side effects will be reported and addressed promptly.
Benefits and Risks: While the study aims to provide potential benefits, such as improved treatment options for HER2 Positive Newly Diagnosed Metastatic Esophageal, Gastric, GEJ Cancer there may also be risks involved. Participants will be informed of all possible risks before enrolling in the study.
Confidentiality: All personal information will be kept confidential, and data will be used only for research purposes.
Contact Information: For more information about this study, please contact PhaseIICRA@medicine.bsd.uchicago.edu

Start Date01 Nov 2026

Sponsor / Collaborator

The University of Chicago

NCT07137416

/ RecruitingPhase 1IIT

Phase 1b Study of Pidnarulex and Trastuzumab Deruxtecan in Patients With HER2 Expressing Solid Tumors

This phase I trial tests the safety, side effects, and best dose of pidnarulex in combination with trastuzumab deruxtecan in treating patients with breast cancer and other solid tumors that express varying levels of a protein called HER2 and that has spread from where it first started (primary site) to other places in the body (metastatic), that cannot be removed by surgery (unresectable), or that has spread to nearby tissue or lymph nodes (locally advanced). Pidnarulex is an enzyme inhibitor that causes cell death and prevents tumor cell growth. Trastuzumab deruxtecan is in a class of medications called antibody-drug conjugates. It is composed of a monoclonal antibody, called trastuzumab, linked to a chemotherapy drug, called deruxtecan. Trastuzumab attaches to HER2 positive tumor cells in a targeted way and delivers deruxtecan to kill them. Giving pidnarulex in combination with trastuzumab deruxtecan may be safe, tolerable and/or effective in treating patients with metastatic, unresectable, or locally advanced HER2-expressing breast cancer or other solid tumors.

Start Date05 Oct 2026

Sponsor / Collaborator

National Cancer Institute

100 Clinical Results associated with Fam-trastuzumab deruxtecan-NXKI

100 Translational Medicine associated with Fam-trastuzumab deruxtecan-NXKI

100 Patents (Medical) associated with Fam-trastuzumab deruxtecan-NXKI

1,167

Literatures (Medical) associated with Fam-trastuzumab deruxtecan-NXKI

01 Oct 2026·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

An intrinsically hydrophilic linker enables a stable, high-DAR exatecan-based HER2 ADC with potent antitumor activity

Article

Author: Feng, Chaoyang ; Ma, Jianglei ; Wu, Chenglong ; Huang, Jinkun ; Bao, Yiwen ; Heng, Xiaojie ; Zeng, Nan ; Yang, Tingting ; Ni, Dechun

Antibody-drug conjugates (ADCs) combine the targeting specificity of monoclonal antibodies with the potent cytotoxicity of small-molecule drugs. However, ADC development using Exatecan, a potent topoisomerase I inhibitor, has been challenged by its hydrophobicity, leading to aggregation, rapid clearance, and off-target toxicity. Herein, we report the design of an intrinsically hydrophilic drug-linker platform (SMP-70067-L) that enables the construction of a homogeneous Exatecan-based HER2-targeted ADC (SMP-70067-X) with a high drug-to-antibody ratio (DAR of 7.92). Similar to Trastuzumab deruxtecan (DS-8201a), which achieves high DAR without PEG or polysarcosine chains through a hydrophilic self-immolative spacer, SMP-70067-L integrates minimal hydrophilic elements, including a glutamic acid residue and a modified aromatic self-immolative spacer, to balance hydrophilicity, stability, and efficient payload release. The resulting ADC exhibits low aggregation (<1%), favorable plasma and thermal stability, and sustained exatecan release. SMP-70067-X demonstrates potent cytotoxicity in HER2-positive tumor cells (sub-nanomolar IC₅₀ values) and significantly enhanced antitumor efficacy compared to DS-8201a in HER2-moderate and HER2-low xenograft models. These results highlight the critical role of rational linker engineering in expanding the therapeutic window of hydrophobic topoisomerase I inhibitor-based ADCs.

01 Jul 2026·Respiratory Investigation

Response to trastuzumab deruxtecan in postoperative recurrent lung adenocarcinoma harboring concurrent EGFR and HER2 mutations after progression on adjuvant osimertinib

Article

Author: Muramoto, Kei ; Naito, Daiki ; Goebuchi, Kageaki ; Fukushima, Kazuaki ; Furukawa, Tsuguhiro ; Akaike, Kimitaka ; Saruwatari, Koichi ; Tomita, Yusuke ; Sakagami, Takuro ; Nishiyama, Taketaka ; Okabayashi, Hiroko

Epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) mutations are key molecular targets in non-small cell lung cancer (NSCLC). We report a rare case of postoperative recurrent lung adenocarcinoma in an 84-year-old woman harboring EGFR L858R and HER2 S310F mutations after progression on adjuvant osimertinib. After further progression on chemotherapy, she received trastuzumab deruxtecan (T-DXd), which induced metastatic regression and yielded disease control for approximately 6 months. This case highlights a therapeutic approach for NSCLC with multiple driver alterations and demonstrates the clinical activity of T-DXd in osimertinib-refractory EGFR-mutant disease with a concurrent HER2 alteration.

01 Jul 2026·Value in Health Regional Issues

Budget Impact Analysis of Fam-Trastuzumab-Deruxtecan as a Second Line in Patients With HER2-Positive Metastatic Breast Cancer in Oman

Article

Author: Aljaber, Rana ; Al Froukh, Rawan F ; Al Hashar, Amna

OBJECTIVES:

Despite advancements, breast cancer remains a major global health and financial challenge. Trastuzumab-based therapies, particularly Fam-Trastuzumab-Deruxtecan (T-DXd), have shown superior outcomes, leading to its recommendation as a preferred second-line treatment. However, its high cost necessitates a budget impact analysis (BIA) to evaluate financial feasibility. This study assesses the 1-year budget impact of replacing Trastuzumab Emtansine (TDM1) with T-DXd for HER2+ metastatic breast cancer in an Omani cancer center.

METHODS:

A static BIA model was built based on National Institute for Health and Care Excellence template with adaptation as required. The model time horizon was 1 year then projected over another 2 years, using 2022 as the baseline year, adopting Omani healthcare-payer perspective. The analysis considered 2 scenarios: (1) TDM1 as the current formulary drug and (2) T-DXd is introduced instead of TDM1, assuming that treatment share would be 100%. One-way sensitivity analysis is performed to assess the model's robustness.

RESULTS:

The BIA demonstrated that replacing TDM1 with T-DXd for the eligible patients would lead to increase in the budget expenditure. Over a 3-year period, considering the provided assumptions and input data, the cumulative excess amount to €5 909 481.67. The primary contributing factors are the drug acquisition cost and the median treatment duration. The sensitivity analysis results suggest the model is robust to changes in adverse drug reaction costs, unlike changes in treatment duration and drug cost.

CONCLUSIONS:

Although T-DXd improves clinical outcomes, its adoption as a second-line treatment in Oman poses a substantial financial burden, necessitating careful budget planning to ensure long-term affordability.

1,161

News (Medical) associated with Fam-trastuzumab deruxtecan-NXKI

06 Jul 2026

·www.fiercebiotech.com

Novartis to pay $1.1B upfront for UK biotech Myricx to expand the pharma's ADC pipeline

Novartis is pushing deeper into antibody-drug conjugate (ADC) development, paying $1.1 billion upfront to buy Myricx Bio for a pipeline based on a novel payload. Switzerland’s Novartis largely stayed on the sidelines as its peers plowed into the ADC space. Talking to investors in recent years, Novartis executives explained that they have internal ADC projects and keep tabs on external developments. But the company made targeted radioligand therapies (RLTs), not ADCs, the cornerstone of its oncology business. Now, Novartis has found a platform compelling enough to get more actively involved in ADCs. Myricx, a London-based biotech, is developing ADCs that deliver N-myristoyltransferase inhibitor (NMTi) payloads. The FDA has approved ADCs using a range of payloads. Drugs including AstraZeneca and Daiichi Sankyo’s Enhertu deliver topoisomerase I (TOPO-1) inhibitors, while ADCs such as Astellas and Pfizer’s Padcev use microtubule inhibitors. NMTis are a different approach that Novartis predicts could tackle resistance and other limitations of existing payloads, broadening the use of ADCs across multiple tumor types. Myricx and its collaborators found NMTis selectively eliminate senescent cells, which can facilitate tumor progression. In solid cancer models, NMTi-ADCs aimed at HER2, TROP2 and B7-H3 matched (PDF) or beat the efficacy of TOPO-1 treatments aimed at the same targets. The biotech picked the B7-H3 and HER2 ADCs as its lead candidates. Pursuing the targets puts Myricx in competition with multiple other ADCs, including approved assets. The FDA approved the HER2-directed ADC Enhertu in 2019, with AstraZeneca reporting (PDF) sales of $2.8 billion last year. Daiichi and Merck & Co.’s B7-H3-directed ADC ifinatamab deruxtecan is undergoing priority review at the FDA. With rivals showing B7-H3 and HER2 are viable ADC targets, Myricx’s programs are partly derisked. The biotech knows ADCs against B7-H3 and HER2 can improve outcomes in solid tumor patients. The critical outstanding question is whether Myricx’s technology can improve on the incumbent drugs, potentially by treating TOPO-1-resistant patients or unlocking settings where existing payloads have limitations. The B7-H3 and HER2 programs could serve as a proving ground for NMTis. If it clinically validates the technology, Novartis sees opportunities to establish NMTis as a new class of ADC payload for use across more targets and platforms. Up to $400 million in milestones are tied to the success of Myricx’s assets. The acquisition aligns with comments Shiva Malek, Ph.D., global head, oncology disease area at Novartis Institutes for BioMedical Research, made at the company’s “meet the management” day in November. The pharma is focused on selectively delivering “biology-matched payloads” to tumors, Malek said at the time. Within that work, Novartis was considering where pan-cytotoxic ADCs may complement its work on RLTs.

ADCDrug ApprovalPriority ReviewAcquisition

06 Jul 2026

·www.biopharmadive.com

Novartis to acquire ADC developer in a deal worth up to $1.5B

Novartis, aiming to bolster its oncology portfolio, will acquire the privately held Myricx Bio and gain its pipeline of differentiated antibody drug conjugates for up to $1.5 billion.The Swiss pharmaceutical giant said Monday it will pay $1.1 billion up front and potentially as much as $400 million in milestone payments to the U.K.-based biotech, with the transaction expected to close before the end of the year. The deal hands over Myricxs two leading ADC assets designed to deliver cancer-killing treatments directly to tumor cells and address limitations of current ADCs.This proposed acquisition reflects our strategy to scale innovative platforms, as we have with radioligand therapies, to deliver more durable, transformative treatments for patients, said Fiona Marshall, president of biomedical research at Novartis, in a statement.ADCs have exploded in popularity in recent years for their ability to replace certain standard cancer treatments. The drugs are a form of precision chemotherapy that targets malignant cells directly while sparing surrounding healthy cells, with several approved to treat a range of tumors. AstraZeneca and Daiichi Sankyos Enhertu has become a top seller, and several pharmas such as Eli Lilly, AbbVie and Merck & Co. have inked deals aimed at bringing differentiated ADCs to market or to expand their use.Novartis, meanwhile, had not joined its peers in the ADC gold rush.The company, which markets lucrative radiopharmaceuticals like Lutathera and Pluvicto, has bet billions on multiple experimental cancer drugs in the past couple of years. The latest deal with Myricx marks its entry into the world of differentiated ADCs for cancer.Myricx brings two lead candidates targeting tumors that are positive for HER2- and B7-H3 proteins commonly found in breast and lung cancers. The biotechs platform is built around a next-generation inhibitor of the enzyme N-myristoyltransferase, or NMTi, which plays a key role in cancer cell growth, as well as the drug resistance that has become an increasing challenge for ADCs. Blocking the enzymes activity should disrupt the development of cancer cells.Myricx, with support of Cancer Research UK, was spun out of Imperial College London and the Francis Crick Institute. The company received seed investment from Brandon Capital and Sofinnova Partners in 2019, with investors such as Lilly and Novo Holdings backing later financing rounds. '

ADCAcquisition

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

100 Deals associated with Fam-trastuzumab deruxtecan-NXKI

External Link

KEGG	Wiki	ATC	Drug Bank
-	Fam-trastuzumab deruxtecan-NXKI	L01XC	DB14962

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Metastatic human epidermal growth factor 2 positive carcinoma of breast	United States	Daiichi Sankyo, Inc.	15 May 2026
Stomach Cancer	India	AstraZeneca PLC	07 Oct 2025
HER2 Positive Solid Tumors	United Kingdom	Daiichi Sankyo UK Ltd.	09 Apr 2025
HR-positive/HER2-low Breast Carcinoma	United States	Daiichi Sankyo Co., Ltd.	28 Jan 2025
Hormone receptor positive HER2 positive breast cancer	South Korea	Daiichi Sankyo Co., Ltd.	19 Sep 2022
HER2 mutant non-small cell lung cancer	United States	Daiichi Sankyo, Inc.	11 Aug 2022
HER2 Positive Stomach Adenocarcinoma	Australia	AstraZeneca Pty Ltd.	08 Oct 2021
HER2-Low Breast Carcinoma	Australia	AstraZeneca Pty Ltd.	08 Oct 2021
Metastatic breast cancer	Canada	AstraZeneca Canada, Inc.	15 Apr 2021
HER2 positive Gastroesophageal Junction Adenocarcinoma	United States	Daiichi Sankyo, Inc.	15 Jan 2021
HER2-positive gastric cancer	Japan	Daiichi Sankyo Co., Ltd.	25 Sep 2020
HER2 Positive Breast Cancer	United States	Daiichi Sankyo, Inc.	20 Dec 2019

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Solid tumor	Phase 3	United States	Daiichi Sankyo, Inc.	23 Dec 2025
Solid tumor	Phase 3	China	Daiichi Sankyo, Inc.	23 Dec 2025
Solid tumor	Phase 3	Japan	Daiichi Sankyo, Inc.	23 Dec 2025
Solid tumor	Phase 3	Australia	Daiichi Sankyo, Inc.	23 Dec 2025
Solid tumor	Phase 3	Brazil	Daiichi Sankyo, Inc.	23 Dec 2025
Solid tumor	Phase 3	France	Daiichi Sankyo, Inc.	23 Dec 2025
Solid tumor	Phase 3	Israel	Daiichi Sankyo, Inc.	23 Dec 2025
Solid tumor	Phase 3	Italy	Daiichi Sankyo, Inc.	23 Dec 2025
Solid tumor	Phase 3	South Korea	Daiichi Sankyo, Inc.	23 Dec 2025
Solid tumor	Phase 3	Spain	Daiichi Sankyo, Inc.	23 Dec 2025

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2026	Not Applicable	Metastatic human epidermal growth factor 2 positive carcinoma of breast HER2-positive \| HER2-low	87	Trastuzumab deruxtecan	ixydhniwob(taqlmzktbg) = glnbvrzvmq edcsmbyuvb (oxbcmdmfbb, 55 - 66) View more	Positive	29 May 2026
NCT04294628 (ASCO2026)	Phase 1	Advanced Malignant Solid Neoplasm HER2 Expression	61	Trastuzumab deruxtecan	hjccnnxvol(agvhiodrri) = kkrbagxryp wembooozwm (yhjvvbdfbh ) View more	Positive	29 May 2026
NCT06271837 (DESTINY-PanTumor03, ASCO2026)	Phase 2	HER2 Positive Solid Tumors Last line HER2 IHC 3+	50	Trastuzumab deruxtecan (T-DXd) 5.4 mg/kg IV Q3W	peqfhokard(woswypcdvu) = ncdomsgjkb lzqhqexyfd (cvgnfcvcvy, 43.2 - 71.8) View more	Positive	29 May 2026
NCT04704934 (DESTINY-Gastric04, ASCO2026)	Phase 3	HER2-positive gastric cancer \| Gastroesophageal junction adenocarcinoma Second line HER2+	494	trastuzumab deruxtecan (T-DXd) 6.4 mg/kg	wqcjniixuo(iunpfrdvyv) = hyufeuixnf umzxkgobrb (bukwrjbnhh, 2.7 - 5.0) View more	Positive	29 May 2026
				ramucirumab + paclitaxel	wqcjniixuo(iunpfrdvyv) = iclnxngxiv umzxkgobrb (bukwrjbnhh, 2.1 - 3.5) View more
ASCO2026	Not Applicable	Advanced breast cancer HER2-positive \| HER2-low	119	Trastuzumab deruxtecan (BMI < 24 kg/m2)	bzexrpuyos(ltrlrvhkel) = cytknkdzla pzafofxyte (pjxgndpnua ) View more	Positive	29 May 2026
				Trastuzumab deruxtecan (BMI ≥24 kg/m2)	bzexrpuyos(ltrlrvhkel) = xcywwwmjfo pzafofxyte (pjxgndpnua ) View more
ASCO2026	Not Applicable	Non-Small Cell Lung Cancer First line HER2-exon 20 insertion mutations \| HER2 mutations \| HER2 amplification	404	Trastuzumab deruxtecan (T-DXd) monotherapy	kidpqxkejv(hkhtirnbuq) = ebabwcwqzz nerrkrxvbe (hehvjrewtl )	Positive	29 May 2026
				Chemotherapy	kidpqxkejv(hkhtirnbuq) = ktuyxprkue nerrkrxvbe (hehvjrewtl )
ASCO2026	Not Applicable	Metastatic breast cancer HER2-positive \| HER2-low	406	Trastuzumab deruxtecan	afuuybmeck(egrpvzamvf) = qwzknhfehy kzegxhbzxj (oqperkeqqn ) View more	Positive	29 May 2026
ASCO2026	Not Applicable	HER2 Positive Solid Tumors HER2-positive	235	Trastuzumab deruxtecan	kxjbyeevjd(vrdmkvxiqk) = jpanitybuw qbaatxdwqi (uwbvcgnrsl ) View more	Positive	29 May 2026
NCT04379596 (DESTINY-Gastric03 (DG-03), ASCO2026)	Phase 1/2	Adenocarcinoma of Esophagus \| HER2-expressing Gastric Adenocarcinoma \| Gastroesophageal junction adenocarcinoma First line HER2-expressing	137	T-DXd 6.4 mg/kg + pembrolizumab + fluoropyrimidine	xadbnadvpr(undpcqesus) = zukzhlriyc rfmugqxdll (lnjmibjyqg ) View more	Positive	29 May 2026
				T-DXd 5.4 mg/kg + pembrolizumab + fluoropyrimidine	xadbnadvpr(undpcqesus) = pbvohubipb rfmugqxdll (lnjmibjyqg ) View more
JPRN-jRCT2011210017 (MYTHOS, ASCO2026)	Phase 2	Salivary gland cancer recurrent HER2-low	36	Trastuzumab deruxtecan 5.4 mg/kg	tawomifxcf(ozwhhahupb) = jauldlgskj gippbfpdsu (kjkkqpekoc, 23.1 - 56.5) View more	Negative	29 May 2026
				Trastuzumab deruxtecan 5.4 mg/kg (salivary duct carcinoma)	tawomifxcf(ozwhhahupb) = demxzbkctv gippbfpdsu (kjkkqpekoc, 28.3 - 65.7)

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