EGFR antagonists(Epidermal growth factor receptor erbB1 antagonists), HER2 antagonists(Receptor tyrosine-protein kinase erbB-2 antagonists), HER4 antagonists(Receptor tyrosine-protein kinase erbB-4 antagonists)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal DiseasesRespiratory Diseases+ [1]

Active Indication

Advanced HER2-Positive Breast CarcinomaHER2 Positive Breast CancerHER2-Low Breast Carcinoma+ [14]

Inactive Indication

Adenocarcinoma of LungAdvanced biliary tract cancerAdvanced Malignant Solid Neoplasm+ [8]

Originator Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Active Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Dr. Reddy's Laboratories Ltd.

Inactive Organization

Hengrui Therapeutics, Inc.

License Organization

Dr. Reddy's Laboratories Ltd.

HLB Life Science Co., Ltd.

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

China (12 Aug 2018),

HER2 Positive Breast Cancer

RegulationPriority Review (China), Breakthrough Therapy (China), Conditional marketing approval (China), Special Review Project (China)

Structure/Sequence

Molecular FormulaC40H39ClN6O11

InChIKeyKLHFGQSCVQPTIN-XUZAKNADSA-N

CAS Registry1397922-61-0

305

Clinical Trials associated with Pyrotinib Maleate

NCT05745740

/ Not yet recruitingPhase 1/2

An Open-label, Single-center, Phase Ib/II Study to Evaluate the Safety, Efficacy and Pharmacokinetics of RC48-ADC Combined With Pyrotinib in Local Advanced or Metastasis NSCLC With HER2 Mutation

This study will evaluate the efficacy, safety and pharmacokinetics of RC48-ADC for injection combined with pyrotinib in subjects with local advanced or metastatic non-small cell lung cancer with HER2 mutation.

Start Date01 Dec 2027

Sponsor / Collaborator

RemeGen Co., Ltd.

NCT07892274

/ Not yet recruitingPhase 3IIT

An Open-Label, Multicenter Clinical Study of Trastuzumab Rezetecan Followed by Pyrotinib in Combination With Fulvestrant and Dalpiciclib in Patients With HR-Positive, HER2-Positive Advanced Breast Cancer

The purpose of this clinical trial is to evaluate whether, in patients with hormone receptor-positive (HR-positive) and HER2-positive advanced breast cancer whose disease has progressed after trastuzumab-based therapy, switching to pyrotinib, fulvestrant, and dalpiciclib after induction with trastuzumab rezetecan-among those without disease progression-is superior to continued treatment with trastuzumab rezetecan. The three medicines are pyrotinib (a medicine that blocks HER2 and similar signals), fulvestrant (a hormone therapy), and dalpiciclib (a medicine that slows cancer cell division).
The primary question this study aims to answer is:
Does switching to pyrotinib, fulvestrant, and dalpiciclib prolong the time participants live without their cancer worsening compared with continued treatment with trastuzumab rezetecan?
The study will also assess overall survival, tumor response to treatment, and adverse events.
Researchers will compare the three-medicine combination with continued trastuzumab rezetecan.
Participants will:
Receive trastuzumab rezetecan once every 3 weeks for 6 cycles.
If the cancer has not worsened after these 6 cycles, be randomly assigned to receive either the three-medicine combination or continued trastuzumab rezetecan.
Undergo imaging scans every 6 weeks during the first 24 weeks and every 9 weeks thereafter to assess the cancer.
Undergo blood tests, cardiac assessments, and other safety evaluations during treatment and follow-up.

Start Date01 Nov 2026

Sponsor / Collaborator

Sun Yat-Sen Memorial Hospital

NCT07836257

/ Not yet recruitingPhase 2IIT

A Single-arm, Exploratory, Phase II Clinical Study of the Efficacy and Safety of Trastuzumab (T-DXd) in Combination With Pyrotinib in Patients Progressed After T-DXd Treatment for Advanced HER2-positive Breast Cancer

This is a single-arm, exploratory, phase II study evaluating the efficacy and safety of trastuzumab deruxtecan (T-DXd) in combination with pyrotinib in patients with HER2-positive advanced breast cancer whose disease has progressed after prior treatment with T-DXd.T-DXd is the established standard second-line therapy for HER2-positive advanced breast cancer. However, acquired resistance inevitably develops, and there is currently no approved standard treatment for patients progressing after T-DXd. Real-world studies report an objective response rate (ORR) of approximately 14.5% and a median progression-free survival of only 3 to 4 months in this setting, representing a major unmet medical need.Pyrotinib is an oral, irreversible pan-ErbB receptor tyrosine kinase inhibitor that potently inhibits HER1, HER2 and HER4 kinase activity and blocks downstream PI3K/AKT and MAPK signaling. Preclinical and clinical data (including the HER2CLIMB-02 and TROPHY studies) support the synergistic potential of combining an anti-HER2 antibody-drug conjugate with a tyrosine kinase inhibitor.Participants receive T-DXd 5.4 mg/kg intravenously on Day 1 of each 21-day cycle plus pyrotinib 320 mg orally once daily, continuously, until disease progression, unacceptable toxicity, withdrawal of consent, or other protocol-defined discontinuation criteria. Tumor response is assessed using RECIST v1.1.The primary endpoint is objective response rate (ORR). Secondary endpoints include disease control rate (DCR), duration of response (DoR), progression-free survival (PFS), overall survival (OS), and safety/tolerability. Approximately 28 participants will be enrolled.

Start Date10 Oct 2026

Sponsor / Collaborator

Fujian Medical University

100 Clinical Results associated with Pyrotinib Maleate

100 Translational Medicine associated with Pyrotinib Maleate

100 Patents (Medical) associated with Pyrotinib Maleate

457

Literatures (Medical) associated with Pyrotinib Maleate

01 Jan 2027·Clinical and Translational Radiation Oncology

Timing of cranial radiotherapy in HER2-positive breast Cancer brain metastases treated with Pyrotinib: a multicentre real-world cohort study

Article

Author: Mao, Dan ; Jing, Hao ; Chen, Zhengting ; Huang, Sheng ; Ma, Yuchao ; Chen, Xuesong ; Li, Lan ; Yi, Junlin ; Bi, Dongyu ; Zhou, Xinyan ; Lu, Shuang ; Zhang, Ye ; Wang, Miao ; Xia, Yaoxiong ; Hou, Yu

BACKGROUND AND PURPOSE:

Cranial radiotherapy (RT) and pyrotinib both demonstrate efficacy in HER2-positive breast cancer brain metastases (BCBM); however, the optimal sequencing of these modalities remains to be established. We evaluated survival across treatment sequences within a real-world cohort.

MATERIALS AND METHODS:

This retrospective, two-centre study included 101 patients with HER2-positive BCBM treated with cranial RT plus pyrotinib (June 2018-July 2025). Based on treatment sequence, patients were categorized into: concurrent RT and pyrotinib (Group A, n = 41); RT after intracranial progression on pyrotinib (Group B, n = 38); and pyrotinib upon progression following RT (Group C, n = 22). The primary endpoint was CNS-PFS. Survival outcomes were assessed via Kaplan-Meier estimation and Cox proportional hazards models.

RESULTS:

At a median follow-up of 43.3 months, 63 patients (62.4%) had died and 70 (69.3%) experienced CNS-PFS events. Median CNS-PFS was 14.8 months (95% CI 10.68-19.92) overall, and 14.3, 15.0, and 21.4 months in groups A, B, and C, respectively (P = 0.252); median OS was 36.0 months (95% CI 28.0-39.7) overall, and 33.0, 35.4, and 42.0 months in groups A, B, and C, respectively (P = 0.281). Focal cranial RT was independently associated with longer OS (HR 0.56, 95% CI 0.34-0.94; P = 0.028). Any-grade adverse events occurred in 100 of 101 patients (99.0%); grade ≥ 3 events occurred in 2.4%, 7.9%, and 4.5% of groups A, B, and C, respectively (all P > 0.05), and radiation necrosis occurred in 7 patients (6.9%). An exploratory threshold of RT initiated >3.9 months before pyrotinib (OS 49.9 vs 29.8 months; HR 0.31, 95% CI 0.11-0.91; P = 0.025) did not withstand internal validation.

CONCLUSIONS:

Treatment sequence did not significantly affect OS or CNS-PFS. Focal cranial RT was independently associated with longer survival, and toxicity was manageable. The proposed timing threshold is hypothesis-generating and warrants prospective validation.

01 Dec 2026·Materials Today Bio

Targeting an ASCL1–WNT11–ERK feed-forward loop to overcome pyrotinib resistance in HER2-positive breast cancer

Article

Author: Liu, Wei ; Li, Yingliang ; Liu, Zide ; Zhang, Zhanglin ; Wang, Yu ; Zeng, Qi ; Zhou, Boxuan ; Yu, Kuai ; Tang, Hong ; Zhu, Chao ; Mao, Xiaocheng ; Le, Aiping ; Gao, Chengqi ; Meng, Chuang ; Fan, Linwei ; Yin, Fang ; Liu, Hongfei ; Jiang, Alan ; Fu, Tianmei

Pyrotinib resistance remains a therapeutic obstacle in human epidermal growth factor receptor 2-positive (HER2⁺) breast cancer (BC), and tumor-selective strategies to restore drug response are lacking. Here, we identify ASCL1 as a mediator of pyrotinib resistance. ASCL1 was elevated in resistant cells and pretreatment tumors from pyrotinib-resistant patients. High ASCL1 expression was associated with shorter overall survival after adjustment for TNM stage. Mechanistically, ASCL1 promotes WNT11 transcription, thereby engaging non-canonical WNT11-ROR2 signaling to sustain ERK phosphorylation under pyrotinib treatment. Persistent ERK activity promotes CREB1 phosphorylation and p-CREB1 binding to the ASCL1 promoter and enhances its transcription, forming an ERK-CREB1-ASCL1-WNT11 feed-forward loop that reinforces resistance. To overcome this resistance program, we develop HApt-PEG-ZIF-8@siASCL1/Pyrotinib, a HER2 aptamer-guided ZIF-8 nanoplatform for tumor-selective co-delivery of ASCL1 siRNA and pyrotinib. This nanoplatform exhibits minimal hemolysis, enhanced uptake in HER2⁺ BC cells, prolonged circulation, and improved tumor delivery efficiency in vivo. Co-delivery suppresses ASCL1/WNT11 signaling and downstream p-ERK and p-CREB1, inhibits proliferation, migration, and invasion, induces apoptosis, and achieves robust antitumor efficacy in pyrotinib-resistant xenografts without detectable systemic toxicity. Together, this study reveals an ASCL1-driven resistance mechanism and establishes a HER2-targeted nanotherapeutic strategy to restore pyrotinib sensitivity, supporting ASCL1 as a therapeutic target in HER2⁺ BC.

01 Oct 2026·LUNG CANCER

First-line pyrotinib plus apatinib in advanced non-small cell lung cancer harboring HER2 mutations or amplification: a phase II trial

Article

Author: Wei, Fang ; Xing, Puyuan ; Tian, Linyan ; Jiang, Wenxin ; Li, Weihua ; Yang, Yaning ; Hao, Xuezhi ; Yang, Guangjian ; Lei, Siyu ; Li, Junling ; Wang, Yan ; Xu, Haiyan

BACKGROUND:

Although emerging agents have broadened the therapeutic landscape for non-small cell lung cancer (NSCLC) harboring HER2 alterations, effective and accessible first-line therapy remains limited.

METHODS:

In this single-arm, phase II trial, treatment-naïve patients with stage IIIB-IV NSCLC harboring de novo HER2 mutations or amplification were given oral pyrotinib (400 mg) in combination with apatinib (250 mg) once daily until disease progression, intolerable toxicity, or death. The primary endpoint was overall response rate (ORR). Secondary endpoints consisted of disease control rate (DCR), progression-free survival (PFS), and safety.

RESULTS:

Between November 2021 and March 2024, 22 eligible patients were enrolled. The ORR was 72.7 % (95 % CI, 49.8-89.3), and the DCR reached 95.5 % (95 % CI, 77.2-99.9). With a median follow-up of 37.0 months (95 % CI, 36.1-37.9), the median PFS was 10.7 months (95 % CI, 6.6-14.8). Both patients harboring HER2 amplification achieved PFS exceeding 10 months, while the patient harboring HER2 exon 19 L755P mutation achieved a PFS exceeding 24 months. Grade 3-4 treatment-related adverse events occurred in 27.3 % of subjects, with diarrhea being the most prevalent (18.2 %). In the propensity score-matched analysis, pyrotinib plus apatinib prolonged PFS compared with chemotherapy-based regimens (robust standard error HR 0.53, 95 % CI: 0.34-0.81, P = 0.003). Circulating tumor DNA analysis demonstrated decreased HER2 variant allele frequency in 93.3 % of patients with paired baseline and post-C1 samples.

CONCLUSION:

Pyrotinib combined with apatinib demonstrated promising first-line activity, rapid responses, and manageable toxicity in advanced HER2-altered NSCLC, supporting its potential as an accessible chemotherapy-sparing therapy, particularly in resource-constrained settings.

News (Medical) associated with Pyrotinib Maleate

25 Oct 2026

·www.biospace.com

Live from ESMO | Hengrui Debuts Exhibition Booth with Landmark Data Showcasing Pharma’s Emerging Innovation Power

BERLIN , Oct. 20, 2025 /PRNewswire/ -- From October 17 to 21, the European Society for Medical Oncology (ESMO) Annual Congress convened in Berlin, bringing together global leaders in oncology and pharmaceutical innovation. Representing China's advancing biopharmaceutical landscape, Hengrui Pharma not only returned with a comprehensive portfolio of oncology research but also debuted as an exhibitor, marking a new milestone in its global academic engagement. Since 2016, Hengrui has presented pioneering research at the ESMO Annual Congress for ten consecutive years. This year, the company unveiled 46 studies across 14 innovative therapeutic programs, including nine oral presentations, two mini oral sessions, and four late-breaking abstracts (LBAs), underscoring its global R&D strength. These data highlight the company's commitment to multi-cancer coverage and multi-mechanism innovation in oncology. In parallel, Hengrui scheduled a series of academic events, fostering in-depth dialogue with leading global experts and clinical researchers on cutting-edge topics in oncology. These initiatives established a dynamic platform for international academic exchange and infused Chinese innovation into the global landscape of cancer diagnosis and treatment – marking a new chapter in Hengrui's journey of international scientific engagement. As one of the world's premier oncology platforms, the ESMO Annual Congress attracts more than ten thousand experts and hundreds of leading international pharmaceutical companies each year. The meeting showcases the latest advances in cancer research and therapeutics, serving as a high-level hub for academic exchange and collaboration. It continues to catalyze innovation and clinical translation across the oncology community, aligning with the 2025 Congress vision: "Standing by those who care about cancer." Global Vision: China Innovation Going Global At the ESMO 2025 Annual Congress, Hengrui co-hosted the roundtable "China Innovation Going Global," bringing together leading Chinese and international experts to discuss strategic pathways and future prospects for the globalization of China-origin innovations. During the global launch of the CARES-009 study, featuring Hengrui's innovative therapeutic combination of camrelizumab and rivoceranib, Academician Jia Fan of the Chinese Academy of Sciences and Professor Jian Zhou of Zhongshan Hospital, Fudan University, jointly presented the latest global data from the study, garnering widespread attention from the international oncology community. Ms. Jo Feng, President and Chief Operating Officer of Hengrui Pharma, led the company's delegation at this year's Congress. She stated, "ESMO serves as a premier global platform for oncology exchange, and this year, Hengrui proudly presented 46 research achievements – highlighting our growing academic presence on the world stage. As an innovation-driven global pharmaceutical company, Hengrui places medical innovation at the heart of its strategic vision, with a steadfast commitment to addressing unmet clinical needs. Looking ahead, we remain firmly patient-centric, continuing to advance groundbreaking therapies to improve the lives of patients worldwide." Breakthroughs Across Multiple Cancer Types At this year's ESMO Annual Congress, Hengrui had 46 oncology research projects accepted, including four LBAs, spanning 14 innovative therapeutic programs. Among these, nine were selected for oral presentations, two for mini oral sessions, 32 as posters, and three as e-posters. Collectively, these studies encompass more than 10 cancer types, including esophagogastric cancer, gynecologic malignancies, liver cancer, breast cancer, pancreatic cancer, lung cancer, sarcoma, biliary tract cancer, head and neck squamous cell carcinoma, prostate cancer, and thyroid cancer. In breast cancer, Hengrui had 11 research studies accepted, comprising one oral presentation, one mini oral, eight posters, and one e-poster. Notably, an LBA featuring Hengrui's antibody-drug conjugate (ADC) trastuzumab rezetecan (SHR-A1811) compared with pyrotinib plus capecitabine for patients with HER2-positive advanced or metastatic breast cancer was selected for presentation. Multiple studies highlighting both established and emerging therapies, including pyrotinib, dalpiciclib, and adebrelimab, demonstrate Hengrui's deep and sustained commitment to advancing breast cancer research. In gastrointestinal cancers, 14 studies were accepted, including two oral presentations, 11 posters, and one e-poster. Alongside flagship therapies such as camrelizumab and rivoceranib, four studies on adebrelimab in the gastrointestinal field were featured. In addition, investigational agents including HRS-4642 (a KRAS G12D inhibitor) and SHR-1701 (a PD-L1/TGF-β bifunctional antibody) were also presented, reflecting the strong momentum of both Hengrui's established portfolio and emerging pipeline in advancing care for patients with gastrointestinal malignancies. In lung cancer, six poster presentations featuring camrelizumab and adebrelimab were accepted, underscoring Hengrui's expanding footprint in this therapeutic area. These studies covered both non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC), further validating the clinical potential and versatility of these regimens. Across additional disease areas, including gynecologic tumors, thymic epithelial tumors, head and neck squamous cell carcinoma, sarcoma, prostate cancer, and thyroid cancer, Hengrui had 13 studies accepted, featuring a diverse range of innovative therapies such as camrelizumab, fuzuloparib, rivoceranib, rezvilutamide, adebrelimab, famitinib, HRS-7058, and HRS-4642. These included six oral presentations, one mini oral, five posters, and one e-poster, highlighting Hengrui's robust and broad-based R&D capabilities. In addition, two posters were accepted on hetrombopag and ondansetron oral soluble films, focusing on the prevention and management of chemotherapy-induced thrombocytopenia, nausea, and vomiting. Dr. Frank Jiang, Executive Vice President and Chief Strategy Officer of Hengrui Pharma, stated: "At this year's ESMO Annual Congress, we unveiled a broader and more impactful portfolio of research findings. The concentrated release of these breakthrough data not only reflects Hengrui's robust R&D capabilities, but also highlights the results of our science-driven, globally oriented innovation R&D strategy. Our pipeline is both deep and forward-looking – while reinforcing our existing product portfolio, we are also actively expanding into cutting-edge therapeutic areas. We firmly believe that through this in-depth engagement with the global oncology community, we can better enable our breakthroughs to benefit more patients worldwide." A Decade of ESMO Participation: China Innovation Going Global Since 2016, Hengrui Oncology has participated in the ESMO Annual Congress for 10 consecutive years, consistently setting new benchmarks for Chinese pharmaceutical companies. Between 2023 and 2025, Hengrui presented a total of 119 research achievements: 2023: 36 studies accepted, including two preferred oral presentations, six mini oral presentations, and 28 posters, covering multiple therapeutic areas such as gastrointestinal cancers, breast cancer, cervical cancer, pancreatic cancer, and melanoma. 2024: 37 studies accepted, spanning 13 innovative therapies and more than 10 cancer types, including esophagogastric cancer, gynecologic malignancies, liver cancer, breast cancer, and lung cancer. 2025: Marking its first-ever exhibition booth at ESMO, Hengrui presented 46 studies across 14 innovative medicines. This milestone represents a significant step forward in Hengrui's internationalization strategy and its commitment to advancing global cancer care. Commitment to Global Impact with the Promise of Patient Focus Hengrui remains steadfast in its commitment to science and innovation driven by the goal of addressing unmet patient needs. Leveraging a global R&D network, the company is advancing innovative medicines onto the international stage. Through a strategically structured pipeline, continuous breakthroughs across multiple cancer types, and active participation in global academic exchange, Hengrui Oncology is accelerating the internationalization and bringing new hope and broader treatment options to patients worldwide. About Hengrui Pharma Hengrui Pharma is an innovative, global pharmaceutical company dedicated to the research, development and commercialization of high-quality medicines to address unmet clinical needs. Its therapeutic areas of focus include oncology, metabolic and cardiovascular diseases, immunological and respiratory diseases, and neuroscience. Founded in 1970 with the core principle of putting patients first, Hengrui Pharma remains committed to advancing human health by striving to conquer diseases, improve health, and extend lives through the power of science and technology. About Hengrui Oncology Hengrui Oncology specializes in the development, production, and global commercialization of innovative cancer therapies. It is the first business unit within Hengrui to achieve technological breakthroughs and successfully enter international markets. Hengrui Oncology has established a robust and diversified oncology pipeline encompassing multiple tumor types, with a comprehensive portfolio that includes immunotherapies, targeted therapies, and ADCs. In key areas such as breast cancer, Hengrui Oncology provides full-course treatment solutions that span multiple lines of therapy. To date, 14 novel oncology agents developed by Hengrui have been approved for marketing in China. View original content: SOURCE Hengrui Pharma

ASCOImmunotherapyDrug Approval

20 Oct 2025

·www.prnewswire.com

Live from ESMO | Hengrui Debuts Exhibition Booth with Landmark Data Showcasing Pharma's Emerging Innovation Power

BERLIN, Oct. 20, 2025 /PRNewswire/ -- From October 17 to 21, the European Society for Medical Oncology (ESMO) Annual Congress convened in Berlin, bringing together global leaders in oncology and pharmaceutical innovation. Representing China's advancing biopharmaceutical landscape, Hengrui Pharma not only returned with a comprehensive portfolio of oncology research but also debuted as an exhibitor, marking a new milestone in its global academic engagement. Since 2016, Hengrui has presented pioneering research at the ESMO Annual Congress for ten consecutive years. This year, the company unveiled 46 studies across 14 innovative therapeutic programs, including nine oral presentations, two mini oral sessions, and four late-breaking abstracts (LBAs), underscoring its global R&D strength. These data highlight the company's commitment to multi-cancer coverage and multi-mechanism innovation in oncology. In parallel, Hengrui scheduled a series of academic events, fostering in-depth dialogue with leading global experts and clinical researchers on cutting-edge topics in oncology. These initiatives established a dynamic platform for international academic exchange and infused Chinese innovation into the global landscape of cancer diagnosis and treatment – marking a new chapter in Hengrui's journey of international scientific engagement. As one of the world's premier oncology platforms, the ESMO Annual Congress attracts more than ten thousand experts and hundreds of leading international pharmaceutical companies each year. The meeting showcases the latest advances in cancer research and therapeutics, serving as a high-level hub for academic exchange and collaboration. It continues to catalyze innovation and clinical translation across the oncology community, aligning with the 2025 Congress vision: "Standing by those who care about cancer." Global Vision: China Innovation Going Global At the ESMO 2025 Annual Congress, Hengrui co-hosted the roundtable "China Innovation Going Global," bringing together leading Chinese and international experts to discuss strategic pathways and future prospects for the globalization of China-origin innovations. During the global launch of the CARES-009 study, featuring Hengrui's innovative therapeutic combination of camrelizumab and rivoceranib, Academician Jia Fan of the Chinese Academy of Sciences and Professor Jian Zhou of Zhongshan Hospital, Fudan University, jointly presented the latest global data from the study, garnering widespread attention from the international oncology community. Ms. Jo Feng, President and Chief Operating Officer of Hengrui Pharma, led the company's delegation at this year's Congress. She stated, "ESMO serves as a premier global platform for oncology exchange, and this year, Hengrui proudly presented 46 research achievements – highlighting our growing academic presence on the world stage. As an innovation-driven global pharmaceutical company, Hengrui places medical innovation at the heart of its strategic vision, with a steadfast commitment to addressing unmet clinical needs. Looking ahead, we remain firmly patient-centric, continuing to advance groundbreaking therapies to improve the lives of patients worldwide." Breakthroughs Across Multiple Cancer Types At this year's ESMO Annual Congress, Hengrui had 46 oncology research projects accepted, including four LBAs, spanning 14 innovative therapeutic programs. Among these, nine were selected for oral presentations, two for mini oral sessions, 32 as posters, and three as e-posters. Collectively, these studies encompass more than 10 cancer types, including esophagogastric cancer, gynecologic malignancies, liver cancer, breast cancer, pancreatic cancer, lung cancer, sarcoma, biliary tract cancer, head and neck squamous cell carcinoma, prostate cancer, and thyroid cancer. In breast cancer, Hengrui had 11 research studies accepted, comprising one oral presentation, one mini oral, eight posters, and one e-poster. Notably, an LBA featuring Hengrui's antibody-drug conjugate (ADC) trastuzumab rezetecan (SHR-A1811) compared with pyrotinib plus capecitabine for patients with HER2-positive advanced or metastatic breast cancer was selected for presentation. Multiple studies highlighting both established and emerging therapies, including pyrotinib, dalpiciclib, and adebrelimab, demonstrate Hengrui's deep and sustained commitment to advancing breast cancer research. In gastrointestinal cancers, 14 studies were accepted, including two oral presentations, 11 posters, and one e-poster. Alongside flagship therapies such as camrelizumab and rivoceranib, four studies on adebrelimab in the gastrointestinal field were featured. In addition, investigational agents including HRS-4642 (a KRAS G12D inhibitor) and SHR-1701 (a PD-L1/TGF-β bifunctional antibody) were also presented, reflecting the strong momentum of both Hengrui's established portfolio and emerging pipeline in advancing care for patients with gastrointestinal malignancies. In lung cancer, six poster presentations featuring camrelizumab and adebrelimab were accepted, underscoring Hengrui's expanding footprint in this therapeutic area. These studies covered both non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC), further validating the clinical potential and versatility of these regimens. Across additional disease areas, including gynecologic tumors, thymic epithelial tumors, head and neck squamous cell carcinoma, sarcoma, prostate cancer, and thyroid cancer, Hengrui had 13 studies accepted, featuring a diverse range of innovative therapies such as camrelizumab, fuzuloparib, rivoceranib, rezvilutamide, adebrelimab, famitinib, HRS-7058, and HRS-4642. These included six oral presentations, one mini oral, five posters, and one e-poster, highlighting Hengrui's robust and broad-based R&D capabilities. In addition, two posters were accepted on hetrombopag and ondansetron oral soluble films, focusing on the prevention and management of chemotherapy-induced thrombocytopenia, nausea, and vomiting. Dr. Frank Jiang, Executive Vice President and Chief Strategy Officer of Hengrui Pharma, stated: "At this year's ESMO Annual Congress, we unveiled a broader and more impactful portfolio of research findings. The concentrated release of these breakthrough data not only reflects Hengrui's robust R&D capabilities, but also highlights the results of our science-driven, globally oriented innovation R&D strategy. Our pipeline is both deep and forward-looking – while reinforcing our existing product portfolio, we are also actively expanding into cutting-edge therapeutic areas. We firmly believe that through this in-depth engagement with the global oncology community, we can better enable our breakthroughs to benefit more patients worldwide." A Decade of ESMO Participation: China Innovation Going Global Since 2016, Hengrui Oncology has participated in the ESMO Annual Congress for 10 consecutive years, consistently setting new benchmarks for Chinese pharmaceutical companies. Between 2023 and 2025, Hengrui presented a total of 119 research achievements: 2023: 36 studies accepted, including two preferred oral presentations, six mini oral presentations, and 28 posters, covering multiple therapeutic areas such as gastrointestinal cancers, breast cancer, cervical cancer, pancreatic cancer, and melanoma. 2024: 37 studies accepted, spanning 13 innovative therapies and more than 10 cancer types, including esophagogastric cancer, gynecologic malignancies, liver cancer, breast cancer, and lung cancer. 2025: Marking its first-ever exhibition booth at ESMO, Hengrui presented 46 studies across 14 innovative medicines. This milestone represents a significant step forward in Hengrui's internationalization strategy and its commitment to advancing global cancer care. Commitment to Global Impact with the Promise of Patient Focus Hengrui remains steadfast in its commitment to science and innovation driven by the goal of addressing unmet patient needs. Leveraging a global R&D network, the company is advancing innovative medicines onto the international stage. Through a strategically structured pipeline, continuous breakthroughs across multiple cancer types, and active participation in global academic exchange, Hengrui Oncology is accelerating the internationalization and bringing new hope and broader treatment options to patients worldwide. About Hengrui Pharma Hengrui Pharma is an innovative, global pharmaceutical company dedicated to the research, development and commercialization of high-quality medicines to address unmet clinical needs. Its therapeutic areas of focus include oncology, metabolic and cardiovascular diseases, immunological and respiratory diseases, and neuroscience. Founded in 1970 with the core principle of putting patients first, Hengrui Pharma remains committed to advancing human health by striving to conquer diseases, improve health, and extend lives through the power of science and technology. About Hengrui Oncology Hengrui Oncology specializes in the development, production, and global commercialization of innovative cancer therapies. It is the first business unit within Hengrui to achieve technological breakthroughs and successfully enter international markets. Hengrui Oncology has established a robust and diversified oncology pipeline encompassing multiple tumor types, with a comprehensive portfolio that includes immunotherapies, targeted therapies, and ADCs. In key areas such as breast cancer, Hengrui Oncology provides full-course treatment solutions that span multiple lines of therapy. To date, 14 novel oncology agents developed by Hengrui have been approved for marketing in China. SOURCE Hengrui Pharma WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

ASCOImmunotherapyDrug Approval

17 Oct 2025

·www.prnewswire.com

Kelun-Biotech's Core product Trastuzumab Botidotin Approved for Marketing by NMPA for HER2-positive BC

CHENGDU, China, Oct. 17, 2025 /PRNewswire/ -- Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. (the "Company") announced that the Company's human epidermal growth factor receptor 2 (HER2)-directed antibody-drug conjugate (ADC) trastuzumab botidotin (also known as A166) was approved for marketing by the National Medical Products Administration (NMPA) for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer (BC) who have received one or more prior anti-HER2 therapy. The approval is based on a multi-center, randomized, open-label, controlled, Phase 3 KL166-III-06 study that evaluates the efficacy and safety profile of trastuzumab botidotin versus T-DM1 in patients with HER2-positive unresectable or metastatic BC who have received prior trastuzumab and taxane-containing regimens. At a pre-specified interim analysis, trastuzumab botidotin monotherapy demonstrated a statistically significant and clinically meaningful improvement in the primary endpoint of progression-free survival (PFS) as assessed by the blinded independent central review (BICR) compared with T-DM1; the beneficial trend for overall survival (OS) of trastuzumab botidotin was also observed. Results from this study will be presented as an oral report at the 2025 European Society for Medical Oncology (ESMO) Congress held in Berlin, Germany (Presentation # LBA24, Proffered paper session 1: Breast cancer, metastatic). The Company has initiated an open, multi-center Phase 2 clinical study of trastuzumab botidotin in the treatment of HER2+ unresectable or metastatic BC that previously received a topoisomerase inhibitor ADC. Dr. Michael Ge, CEO of Kelun-Biotech said, "We are thrilled to see our first HER2 ADC drug, trastuzumab botidotin, successfully approved for market. This marks a significant advancement in the treatment of HER2-positive breast cancer. As China's first domestically developed HER2 ADC capable of broadly covering 2L+ HER2 BC patients, trastuzumab botidotin leverages its differentiated structural design to deliver superior efficacy while addressing unmet clinical needs in this population." About HER2+ BC Breast cancer, as the most common malignant tumor, poses a serious threat to women's health. Among its subtypes, HER2-positive breast cancer accounts for approximately 15%–20% of all breast cancer cases[1], and is characterized by its aggressiveness and high malignancy. According to the 2025 CSCO guidelines, first-line treatment for HER2-positive breast cancer primarily consists of trastuzumab and pertuzumab in combination with taxane-based chemotherapeutic agents. Second-line treatment regimens comprise tyrosine kinase inhibitors (TKIs, such as pyrotinib) and antibody-drug conjugates (ADCs, such as T-DM1 and T-DXd). Following disease progression on second-line therapy, subsequent treatment strategies are determined based on prior second-line regimens, the patient's tolerance to therapy, tumor burden, and other relevant factors. Despite recent advances in anti-HER2 therapeutics, a significant number of patients still experience drug resistance or severe adverse effects, highlighting an urgent need for agents with improved safety profiles to address the treatment requirements of patients with recurrent or drug-resistant HER2-positive breast cancer. A bout trastuzumab botidotin Trastuzumab botidotin is a differentiated HER2 ADC to treat advanced HER2+ solid tumors. As an innovative HER2 ADC developed by the Company, it conjugates a novel, monomethyl auristatin F (MMAF) derivative (a highly cytotoxic tubulin inhibitor, Duo-5) via a stable, enzyme-cleavable linker to a HER2 monoclonal antibody with a drug-to-antibody-ratio (DAR) of 2. Trastuzumab botidotin specifically binds to HER2 on the surface of tumor cells and is internalized by tumor cells, releasing the toxin molecule Duo-5 inside the cell. Duo-5 induces tumor cell cycle arrest in the G2/M phase, leading to tumor cell apoptosis. After targeting HER2, trastuzumab botidotin can also inhibit the HER2 signaling pathway; it has antibody-dependent cell-mediated cytotoxicity (ADCC) activity. About Kelun-Biotech Kelun-Biotech (6990.HK) is a holding subsidiary of Kelun Pharmaceutical (002422.SZ), which focuses on the R&D, manufacturing, commercialization and global collaboration of innovative biological drugs and small molecule drugs. The company focuses on major disease areas such as solid tumors, autoimmune, inflammatory, and metabolic diseases, and in establishing a globalized drug development and industrialization platform to address the unmet medical needs in China and the rest of world. The Company is committed to becoming a leading global enterprise in the field of innovative drugs. At present, the Company has more than 30 ongoing key innovative drug projects, of which 4 projects have been approved for marketing, and more than 10 projects are in the clinical stage. The company has established one of the world's leading proprietary ADC and novel DC platforms, OptiDC™, and has 2 ADC projects approved for marketing, and multiple ADC and novel DC assets in clinical or preclinical research stage. For more information, please visit SOURCE Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Drug ApprovalADCPhase 3Phase 2Clinical Result

100 Deals associated with Pyrotinib Maleate

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KEGG	Wiki	ATC	Drug Bank
-	-	L01XE L01E	DB14993

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Advanced HER2-Positive Breast Carcinoma	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	17 Apr 2023
HER2 Positive Breast Cancer	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	12 Aug 2018

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
HER2-Low Breast Carcinoma	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	17 Jan 2024
Hormone receptor positive breast cancer	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	17 Jan 2024
HR-positive/HER2-low Breast Carcinoma	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	17 Jan 2024
Invasive Mammary Carcinoma	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	17 Jan 2024
Advanced Lung Non-Small Cell Carcinoma	Phase 3	United States	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Advanced Lung Non-Small Cell Carcinoma	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Advanced Lung Non-Small Cell Carcinoma	Phase 3	Australia	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Advanced Lung Non-Small Cell Carcinoma	Phase 3	Belgium	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Advanced Lung Non-Small Cell Carcinoma	Phase 3	France	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Advanced Lung Non-Small Cell Carcinoma	Phase 3	Germany	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT06832904 (NEOTORCH-BREAST05, ESMO2026)	Phase 2	HER2 Positive Breast Cancer Neoadjuvant HER2-positive	38	Neoadjuvant chemotherapy + Pyrotinib + trastuzumab	jjznwqxyrl(zoodcizmkz) = diarrhea (29, 76.3%) tgqtdcccto (smyhsndbhi ) View more	Positive	23 Oct 2026
ESMO2026	Not Applicable	Advanced HER2-Positive Breast Carcinoma HER2-positive	67	Inetetamab combined with Pyrotinib	qgvrwaltok(wmebfdscem) = uqsozobkuh danrgweaya (sqtxwhczur, 16.05 - 29.53) View more	Positive	23 Oct 2026
				Inetetamab combined with Pyrotinib (first- or second-line therapy)	qgvrwaltok(wmebfdscem) = pipjctwluk danrgweaya (sqtxwhczur, 21.5 - 34.5)
ESMO2026	Not Applicable	Advanced HER2-Positive Breast Carcinoma First line HER2-positive	9,187	THPyro	aptnmwyeqq(kecpemmsvp) = zomguqemvi lgvepncffw (xoxuuepwhs )	Positive	23 Oct 2026
				T-DXd+P	aptnmwyeqq(kecpemmsvp) = ezkjtjrhex lgvepncffw (xoxuuepwhs )
CSCO2026	Not Applicable	HER2 Positive Breast Cancer Neoadjuvant HER2 positive	63	Pyrotinib + Trastuzumab + liposomal doxorubicin + cyclophosphamide + nab-paclitaxel	vbntpsaqqo(jzrurvlmug) = diarrhea (1.6%) and neutropenia (1.6%). hilyuakvij (spicpegznb ) View more	Positive	11 Sep 2026
				Pyrotinib + Trastuzumab + liposomal doxorubicin + cyclophosphamide + nab-paclitaxel (hormone receptor-negative)
CSCO2026	Not Applicable	HER2 Positive Breast Cancer HER2-positive	251	Pyrotinib plus upfront RT	nzpcjbkzoj(kpgthwzdji): HR = 0.6 (95.0% CI, 0.41 - 0.86), P-Value = 0.006 View more	Positive	11 Sep 2026
				Pyrotinib monotherapy
CSCO2026	Not Applicable	Advanced HER2-Positive Breast Carcinoma First line HER2-positive	143	Pyrotinib plus Trastuzumab and a taxane (PyHT)	ujibdhnybk(rhigtthmdu) = lpphxxxfbc pxtcnfwzuq (lfoitkfdkv ) View more	Positive	11 Sep 2026
				Pertuzumab plus Trastuzumab and a taxane (THP)	ujibdhnybk(rhigtthmdu) = ouqqvstjrq pxtcnfwzuq (lfoitkfdkv ) View more
NCT06234137 (neoPICD, ASCO_Breakthrough2026)	Phase 2	Locally advanced breast cancer Neoadjuvant HER2-positive	124	Inetetamab + Pyrotinib + Chemotherapy	tcshcdiziz(usnedrjurj) = zinzzzpkgt shxyocoboa (mgjdfxpjnm, 87.6 - 97.6) View more	Positive	25 Jun 2026
				Inetetamab + Pyrotinib + Chemotherapy (HR-negative)	xmsfrchqdx(uzxkohzdxa) = mnnqfhdxff jvdfbmhujj (odjgnfscsf ) View more
ASCO2026	Phase 2	Metastatic human epidermal growth factor 2 positive carcinoma of breast First line \| Second line HER2-positive	94	Inetetamab + Pyrotinib + Utidelone	feyufwzglc(bazkagjhzz) = tfzvasynlz onmgevcdrh (cdedsabtbz, 72.6 - 89.8) View more	Positive	29 May 2026
NCT06483386 (ASCO2026)	Phase 2	HER2 Positive Breast Cancer Neoadjuvant HER2-positive	47	Pyrotinib+SC trastuzumab+capecitabine (HER2-positive early breast cancer)	kygflpextw(mhiayfoptn) = mrzdulenqb ieofnfxfer (aazgsfrxko ) View more	Positive	29 May 2026
				Pyrotinib+SC trastuzumab+capecitabine (ER negative, HER2 positive)	kygflpextw(mhiayfoptn) = qxdxjnxhjn ieofnfxfer (aazgsfrxko )
NCT06495541 (ASCO2026)	Not Applicable	Advanced HER2-Positive Breast Carcinoma First line HER2-positive	156	Pyrotinib (trastuzumab-naïve)	gfdzanqrdk(ooalqedbed) = yqtdahdney dyswicjqtx (wjcqeeaixg, 63.1 - 96.5) View more	Positive	29 May 2026
				Pyrotinib (trastuzumab-sensitive)	gfdzanqrdk(ooalqedbed) = yrwjdxbvfl dyswicjqtx (wjcqeeaixg, 78.5 - 100) View more

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