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+ [13]

Inactive Indication

Adenocarcinoma of LungAdvanced biliary tract cancerAdvanced breast cancer+ [9]

Originator Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Active Organization

Dr. Reddy's Laboratories Ltd.

Jiangsu Hengrui Pharmaceuticals Co., 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

300

Clinical Trials associated with Pyrotinib Maleate

NCT07766772

/ Not yet recruitingPhase 2IIT

A Single-arm, Exploratory Clinical Study of Sequential Use of Regorafenib in Combination With Pegylated Tyrosine Kinase Inhibitor and Trastuzumab in Combination With Capecitabine as First-line Treatment for Advanced HER2-positive Breast Cancer

This study is a single-arm, exploratory clinical trial, aiming to include patients with HER2-positive advanced breast cancer. It intends to explore the efficacy and safety of trastuzumab combined with pyrotinib, capecitabine ± endocrine therapy as a first-line maintenance treatment for HER2+ advanced breast cancer after induction therapy with rucaparib trastuzumab.
After the subjects meet the screening criteria and are enrolled, they receive induction therapy with rucaparib trastuzumab. Among them, patients without disease progression enter the maintenance treatment period and receive trastuzumab combined with pyrotinib, capecitabine ± endocrine therapy (±OFS) for treatment. Until disease progression, or toxicity becomes intolerable, or withdrawal of informed consent, or the investigator determines that the medication must be discontinued. During the study period, imaging evaluations are conducted according to the RECIST 1.1 standard, and the center assessment results are the final results.
During the study period, the efficacy indicators such as PFS, ORR, DOR, CBR, and safety indicators of the subjects are evaluated according to the established trial standards, and statistical descriptions are conducted.

Start Date30 Sep 2026

Sponsor / Collaborator

Fujian Cancer Hospital

NCT07600164

/ RecruitingPhase 4IIT

Real-world Study of Pyrotinib-containing Regimens in First-line or Second-line Treatment of Advanced HER2-positive Breast Cancer

Given that pyrotinib has been proven to exert significant efficacy against HER2-positive advanced breast cancer in multiple Phase III studies, and the novel ADC drug disitamab vedotin has demonstrated potent anti-tumor activity, there remains insufficient real-world data on their sequential administration. This multicenter, prospective real-world study plans to enroll 500 patients with HER2-positive advanced breast cancer receiving first-line or second-line treatment. It aims to evaluate the efficacy and safety of sequential disitamab vedotin treatment after disease progression or intolerance to pyrotinib-based regimens (first-line: pyrotinib plus trastuzumab combined with chemotherapy; second-line: pyrotinib plus capecitabine). The primary endpoint is real-world second progression-free survival (rwPFS2), while secondary endpoints cover real-world progression-free survival (rwPFS), tumor response, overall survival (OS), time to treatment failure, safety profiles and patient-reported outcomes. It is currently expected to further validate the efficacy and safety of pyrotinib in patients with advanced HER2-positive breast cancer in the real-world setting, and to evaluate the efficacy and safety of recindopril trastuzumab following pyrotinib-containing regimens.

Start Date06 Jul 2026

Sponsor / Collaborator

Peking University People's Hospital

NCT07653451

/ Not yet recruitingPhase 2/3IIT

Precision Medicine Strategies for Advanced Esophageal Cancer Refractory to Immune Checkpoint Inhibitors

This study is an open-label, biomarker-integrated umbrella trial designed to evaluate the clinical efficacy of molecular subtype- and genomic biomarker-guided precision therapies in patients with advanced esophageal cancer refractory to prior immunotherapy. Conducted in a two-step process, the study first enrolls patients with locally advanced or metastatic esophageal squamous cell carcinoma (ESCC) who have progressed on prior immunotherapy, performing circulating tumor DNA (ctDNA) sequencing to stratify them into three distinct treatment cohorts, after which patients receive tailored combination regimens matched to their specific molecular profiling in the second step. Specifically, Cohort 1 includes patients with high EGFR expression or activation of EGFR-related signaling pathways, who will receive Afatinib (40 mg, p.o., Q.D.) combined with Toripalimab (240 mg, i.v., Q21D) in a 21-day treatment cycle, continuing until radiographic disease progression (PD), unacceptable toxicity, loss to follow-up, death, or other investigator-determined criteria for discontinuation, with a maximum toripalimab treatment duration of 24 months. Cohort 2 comprises patients harboring genomic alterations directly associated with cell cycle regulation or activation of cell cycle signaling pathways, who will be treated with Dalpiciclib (125 mg, p.o., Q.D. for 21 consecutive days followed by a 7-day off period in a 28-day cycle [Q4W]) combined with Pyrotinib maleate (320 mg, p.o., Q.D., administered within 30 minutes post-meal, Q4W) until disease progression, unacceptable toxicity, initiation of a new anti-tumor therapy, withdrawal of consent, or investigator's decision for treatment discontinuation. Cohort 3 includes patients with other molecular profiles who do not fit Cohorts 1 or 2, who will receive Camrelizumab (200 mg, i.v., Q3W) and Apatinib (250 mg, p.o., Q.D.), with clinical efficacy evaluations performed every 6 weeks, continuing until radiographic PD, unacceptable toxicity, death, or treatment discontinuation, whichever occurs first. The study aims to recruit an estimated maximum of 90 subjects, enrolling up to 30 subjects per cohort, with the final sample size dependent on the observed toxicities and the prevalence of each molecular cohort within the screened population.

Start Date01 Jul 2026

Sponsor / Collaborator-

100 Clinical Results associated with Pyrotinib Maleate

100 Translational Medicine associated with Pyrotinib Maleate

100 Patents (Medical) associated with Pyrotinib Maleate

429

Literatures (Medical) associated with Pyrotinib Maleate

01 Dec 2026·Pharmaceutical Science Advances

Recent advances in HER2-targeted inhibitors for cancer therapy

Review

Author: Zhu, Wenjian ; Lu, Xiaoyun

HER2 (ErbB2), a ligand-independent HER family member, regulates cell growth, differentiation, and survival. Its overexpression, gene amplification, and activating mutations are oncogenic drivers in multiple malignancies. The past two decades have witnessed transformative advances in HER2-targeted therapeutics, exemplified by tyrosine kinase inhibitors (TKIs), including first-generation reversible pan-HER (e.g., lapatinib), second-generation covalent pan-HER (neratinib, pyrotinib), and novel selective HER2 inhibitors (tucatinib, sevabertinib, zongertinib). Nonetheless, the extensive molecular heterogeneity in HER2 activation (e.g., dimerization, amplification) and mutation profiles (e.g., L755S, exon 20 insertions), combined with tumor-type-specific pathogenic mechanisms, poses significant challenges to precision oncology in clinical practice. Currently, numerous promising inhibitors in preclinical and clinical development hold potential for providing more effective treatment options. This review comprehensively summarizes recent advances in HER2-targeted TKIs and their emergent resistance mechanisms, further analyzing strategies to both mitigate off-target toxicity and overcome resistance through rational design of selective HER2 inhibitors. Collectively, these insights provide a roadmap for developing next-generation precision therapies in HER2-driven cancers.

01 Aug 2026·LANCET ONCOLOGY

Trastuzumab rezetecan versus pyrotinib plus capecitabine for patients with HER2-positive metastatic breast cancer (HORIZON-Breast01): interim analysis of a multicentre, open-label, randomised, controlled, phase 3 trial

Article

Author: Fu, Fangmeng ; Zhou, Shoubing ; Niu, Zhaofeng ; Yan, Min ; Yan, Xi ; Zhu, Zhengqiu ; Gao, Jinnan ; Xie, Weimin ; Wang, Biyun ; Li, Wenfeng ; Sun, Tao ; Wang, Shusen ; Yuan, Peng ; Sun, Zhengkui ; Ouyang, Quchang ; Yao, Herui ; Nie, Jianyun ; Zhao, Bing ; Zhang, Ying ; Geng, Cuizhi ; Cheng, Jing ; Cheng, Lin ; Li, Wei ; Sheng, Zhen ; Yin, Yongmei ; Wu, Jingna ; Wang, Xinshuai ; Song, Erwei ; Zhu, Xiaoyu ; Wu, Zhiyong ; Tong, Zhongsheng ; Yi, Tienan ; Zhang, Qingyuan ; Yang, Yaping ; Wang, Xiaojia ; Wei, Wei ; Gan, Lu ; Han, Xinghua ; Zhao, Jianli ; Li, Huiping ; Wang, Yongsheng

BACKGROUND:

Trastuzumab rezetecan has shown antitumour activity in a phase 1 trial. Pyrotinib plus capecitabine is the current standard treatment for patients with HER2-positive advanced or metastatic breast cancer after trastuzumab and chemotherapy (taxane or anthracycline). We aimed to evaluate the efficacy and safety of trastuzumab rezetecan versus pyrotinib plus capecitabine in this patient population.

METHODS:

This interim analysis of a multicentre, open-label, randomised, controlled, phase 3 trial was conducted at 50 hospitals in China. Eligible patients were aged 18-75 years with histologically confirmed HER2-positive unresectable or metastatic breast cancer; previously received a taxane and trastuzumab at the advanced stage or had disease progression within 12 months after (neo)adjuvant treatment with an anti-HER2 monoclonal antibody and taxane-based regimen; had measurable lesions; and an Eastern Cooperative Oncology Group performance status of 0 or 1. Patients were randomly assigned (1:1; stratified by hormone receptor status and previous lines of chemotherapy for metastatic disease), using permuted blocks to intravenous trastuzumab rezetecan (4·8 mg/kg) on day 1 of each 21-day cycle or oral pyrotinib 400 mg once per day continuously plus oral capecitabine 1000 mg/m² twice per day on days 1-14 of each 21-day cycle. Protocol amendments led to a temporary modification (between Nov 29, 2022, and July 12, 2023) of trastuzumab rezetecan dose to 6·4 mg/kg; primary evaluation focuses on the 4·8 mg/kg group. The primary endpoint was progression-free survival per blinded independent central review in the modified intention-to-treat population 1 (defined as all patients randomly assigned to the trastuzumab rezetecan 4·8 mg/kg or control groups). Results presented here are from a prespecified interim analysis. This study was registered with ClinicalTrials.gov, NCT05424835 (active, not recruiting).

FINDINGS:

From Aug 4, 2022, to Aug 9, 2024, 414 patients with HER2-positive metastatic breast cancer were assessed for eligibility, 127 were ineligible and 287 were randomly assigned to trastuzumab rezetecan (n=142) or pyrotinib plus capecitabine (control group; n=145) in the modified intention-to-treat population 1. All 287 patients were female and the median age was 55·0 years (IQR 49·0-60·0). 268 (93%) patients self-reported as Han Chinese and 19 (7%) as other Chinese ethnicity. At data cutoff of the interim analysis on June 30, 2025, after a median follow-up of 15·0 months (IQR 12·9-18·5) for the trastuzumab rezetecan group versus 13·9 months (11·4-17·8) for the control group, 124 progression-free survival events had occurred (37 [26%] vs 87 [60%]). The median progression-free survival was 30·6 months (95% CI 16·8-not reached [NR]) with trastuzumab rezetecan and 8·3 months (6·9-11·0) with pyrotinib plus capecitabine (HR 0·22 [0·15-0·34]; p<0·0001). The 12-month progression-free survival rate was 84·7% (77·0-90·0) in the trastuzumab rezetecan group versus 35·5% (26·8-44·2) in the control group. The most common (grade ≥3) treatment-related adverse events were decreased neutrophil count (77 [54%] with trastuzumab rezetecan vs 13 [9%] with the control), decreased white blood cell count (29 [20%] vs four [3%]), and decreased platelet count (15 [11%] vs two [1%]); whereas treatment-related serious adverse events occurred in 19 (13%) versus 17 (12%). Two adverse events led to death (one [1%] septic shock unrelated to trastuzumab rezetecan treatment and one [1%] unknown reason related to pyrotinib plus capecitabine treatment). Interstitial lung disease occurred in four (3%) patients in the trastuzumab rezetecan group.

INTERPRETATION:

Trastuzumab rezetecan improved progression-free survival versus pyrotinib plus capecitabine and showed a distinct safety profile in patients with HER2-positive breast cancer, presenting as a potential new treatment option.

FUNDING:

Jiangsu Hengrui Pharmaceuticals.

TRANSLATION:

For the Chinese translation of the abstract see Supplementary Materials section.

01 Jun 2026·BREAST

Association between diarrhea and survival in patients with HER2-positive advanced breast cancer treated with pyrotinib-based therapy: A landmark analysis from the real-world PRETTY study

Article

Author: Xu, Binghe ; Wu, Xinhong ; Li, Wei ; Wang, Wenna ; Wang, Xiaojia ; Cai, Li ; Wang, Haibo ; Li, Man ; Yu, Zhiyong ; Tong, Zhongsheng ; Li, Li ; Yang, Jin ; Ouyang, Quchang ; Han, Zhengxiang ; Li, Yiqun

BACKGROUND:

Diarrhea is the most common adverse event of pyrotinib. This study analyzed the association between diarrhea and survival in patients with HER2-positive advanced breast cancer treated with pyrotinib-based therapy.

METHODS:

A secondary analysis was performed using the individual patient data from the nationwide, prospective real-world PRETTY study. Baseline and treatment characteristics were summarized in groups by severity of diarrhea. Multivariable Cox regression analysis was used to analyze the association of diarrhea with real-world progression-free survival (rwPFS) and overall survival (OS), respectively. Immortal-time bias was adjusted using the landmark analysis and time-dependent Cox model. Multiple imputation was performed for missing data, and pooling ln(hazard ratio [HR]) estimations on the association between diarrhea and survival were reported.

RESULTS:

Of 1129 patients, 826 (73.2%) had any-grade treatment-related diarrhea (including 174 [15.4%] with grade ≥3 diarrhea). After multiple imputation, the multivariable Cox regression analysis showed that diarrhea was independently associated with longer OS (grade 1-2 diarrhea vs. none: HR = 0.57 [95% CI, 0.38-0.86], P = 0.007; grade ≥3 diarrhea vs. none: HR = 0.56 [95% CI, 0.31-0.99], P = 0.047) but was not associated with rwPFS. Significant association between diarrhea and OS was also observed in the 1-month landmark analysis (grade 1-2 diarrhea vs. none: HR = 0.59 [95% CI, 0.39-0.89], P = 0.012; grade ≥3 diarrhea vs. none: HR = 0.54 [95% CI, 0.30-0.98], P = 0.043). Time-dependent Cox model indicated the trend on better OS when diarrhea occurred, but without statistical significance.

CONCLUSION:

For patients with HER2-positive advanced breast cancer, diarrhea that occurs during pyrotinib-based therapy maybe a prognostic marker of longer OS.

News (Medical) associated with Pyrotinib Maleate

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

05 Jun 2025

·www.prnewswire.com

Hengrui Pharma Showcases Global Impact at the 2025 ASCO: 72 Study Results Highlight Chinese Cancer Innovation

SHANGHAI, June 5, 2025 /PRNewswire/ -- The 2025 ASCO Annual Meeting successfully concluded in Chicago on June 3 (local time). Hengrui Pharma delivered a strong international presence, featuring 15 innovative drugs and 72 research outcomes. These included 4 oral presentations, 5 rapid oral presentations, 27 poster presentations, and 36 online publications. Multiple groundbreaking research advances has elicited widespread discussion among global experts. In the field of breast cancer, results from 19 studies evaluating the company's innovative drugs—pyrotinib, dalpiciclib, camrelizumab, apatinib, adebrelimab, Trastuzumab rezetecan (SHR-A1811), and SHR-2017, either in combination with each other or with chemotherapies, were presented at ASCO 2025. Notably, 7 studies involving pyrotinib and 6 studies involving dalpiciclib were selected, with both agents consistently demonstrating promising efficacy, reinforcing their established roles in breast cancer treatment. Furthermore, studies evaluating SHR-A1811 and adebrelimab were selected for rapid oral presentations, attracting considerable attention from the industry. In the field of gastrointestinal cancers, drugs such as camrelizumab, apatinib, adebrelimab, and SHR-8068 were featured in a total of 30 accepted studies. Notably, camrelizumab was included in 21 of these studies, demonstrating its broad therapeutic profile and potential while reinforcing its position as a key focus at ASCO. This further solidifies the achievements of China-developed PD-1 inhibitors on the global stage. Additionally, adebrelimab, which has achieved significant breakthroughs in lung cancer in recent years, is actively expanding into new indications. At this year's ASCO, five related studies exploring adebrelimab's efficacy in indications such as hepatocellular carcinoma (HCC), cholangiocarcinoma (CCA) , and pancreatic cancer were presented. The ongoing emergence of cutting-edge research on both established and emerging agents holds promise for improving clinical outcomes for patients with gastrointestinal tumors. Across a wide range of disease areas—including lung cancer, gynecologic cancers, lymphoma, bladder cancer, head and neck cancer, melanoma, sarcoma, nasopharyngeal carcinoma, chordoma, salivary gland cancer, thymic cancer, desmoid tumors, and salivary duct carcinoma—Hengrui Pharma's innovative oncology portfolio (camrelizumab, apatinib, adebrelimab, pyrotinib, dalpiciclib, fluzoparib, famitinib, SHR-A1811, SHR-1501, SHR-1701, SHR-1826, SHR-A1912, and SHR-A2102) was featured in 22 research presentations at ASCO 2025. These comprised 4 oral presentations, 2 rapid oral presentations, 12 poster presentations, and 4 online publications, collectively demonstrating the company's robust R&D capabilities. Additionally, one online publication highlighted ondansetron oral soluble film, underscoring its favorable efficacy in preventing and treating chemotherapy-induced nausea and vomiting (CINV). For 15 consecutive years, Hengrui Pharma has consistently presented its cutting-edge research at the ASCO Annual Meeting, highlighting the company's global leadership in oncology drug research and development while showcasing China's robust pharmaceutical innovation capabilities to the international academic community. The inclusion of 70 Hengrui-sponsored studies at this year's meeting reflects the strong foundation laid by the company's portfolio of 23 marketed innovative drugs and a robust pipeline of over 90 candidates currently in development. Looking ahead, Hengrui will remain committed to its patient-centric approach, striving to develop advanced therapeutics that support the "Healthy China" initiative and enhance clinical outcomes for patients globally. 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

ASCOClinical ResultCSCO

100 Deals associated with Pyrotinib Maleate

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	L01XE	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


ASCO2026	Phase 2	Metastatic human epidermal growth factor 2 positive carcinoma of breast First line \| Second line HER2-positive	94	Inetetamab + Pyrotinib + Utidelone	idrdrioxsm(zxticpufks) = khlzzegqim eeupjlyxuv (kokavmlthi, 72.6 - 89.8) View more	Positive	29 May 2026
NCT06495541 (ASCO2026)	Not Applicable	Advanced HER2-Positive Breast Carcinoma First line HER2-positive	156	Pyrotinib (trastuzumab-naïve)	zhwhybshhf(doxasjqpgh) = ytlwaajeoi mehgrbswvp (kvyvzixqpc, 63.1 - 96.5) View more	Positive	29 May 2026
				Pyrotinib (trastuzumab-sensitive)	zhwhybshhf(doxasjqpgh) = fuaoaueqys mehgrbswvp (kvyvzixqpc, 78.5 - 100) View more
NCT06483386 (ASCO2026)	Phase 2	HER2 Positive Breast Cancer Neoadjuvant HER2-positive	47	Pyrotinib+SC trastuzumab+capecitabine (HER2-positive early breast cancer)	tyzaevrmwl(lggdckqxou) = ayawjbddyq glmrpbwmgt (bdtmzbpjdc ) View more	Positive	29 May 2026
				Pyrotinib+SC trastuzumab+capecitabine (ER negative, HER2 positive)	tyzaevrmwl(lggdckqxou) = heexwcptny glmrpbwmgt (bdtmzbpjdc )
NCT07335081 (ESMO_BC2026)	Phase 2	HER2 Positive Breast Cancer Neoadjuvant HER2-positive	60	Sequential: Docetaxel, Trastuzumab, Pyrotinib followed by Docetaxel, Trastuzumab, Pertuzumab	csghmtkzhs(fsucxpvzdi) = lfqjzzxwnl pppieznhed (zlwuwxgxdd ) View more	Positive	07 May 2026
				Docetaxel, Trastuzumab, and Pertuzumab	csghmtkzhs(fsucxpvzdi) = fctggsvipj pppieznhed (zlwuwxgxdd ) View more
NCT03863223 (PHILA, Pubmed) Manual	Phase 3	Metastatic human epidermal growth factor 2 positive carcinoma of breast HER2 Positive	590	Pyrotinib + Trastuzumab + Docetaxel	ajospyrcnx(ceneavybco) = sihchhmqvc wkrqhhfuyk (ntezsmcnsv, 19.3 - 27.8) View more	Superior	16 Mar 2026
				Placebo + Trastuzumab + Docetaxel	ajospyrcnx(ceneavybco) = vpcqiilxtp wkrqhhfuyk (ntezsmcnsv, 9.5 - 12.4) View more
NCT03863223 (PHILA, Pubmed \| BMJ)	Phase 3	Metastatic human epidermal growth factor 2 positive carcinoma of breast First line	590	Pyrotinib + Trastuzumab + Docetaxel	djdvzkthhr(uodjdsvfvz) = ewmrfholff sntpgniqju (ctxjgcbyfk, 19.3 - 27.8) View more	Superior	16 Mar 2026
				Placebo + Trastuzumab + Docetaxel	djdvzkthhr(uodjdsvfvz) = ytkjyablkw sntpgniqju (ctxjgcbyfk, 9.5 - 12.4) View more
NCT03863223 (PHILA, SABCS2025) Manual	Phase 3	Metastatic human epidermal growth factor 2 positive carcinoma of breast First line HER2 Positive	590	Pyrotinib + Trastuzumab + Docetaxel	pzbeibfpyy(ubeyfbbqyf) = pibtngjbjz jytlzhlaoe (ywjqapcksx, 19.2 - NE) View more	Positive	12 Dec 2025
				Placebo + Trastuzumab + Docetaxel	pzbeibfpyy(ubeyfbbqyf) = kxzlhlsnmq jytlzhlaoe (ywjqapcksx, 6.4 - 13.2) View more
NCT07014410 (SYSUCC-002, SABCS2025)	Phase 2	Metastatic human epidermal growth factor 2 positive carcinoma of breast First line HER2-Positive \| Estrogen Receptor-Positive	16	PyrotinibDalpiciclibLetrozoleib + PyrotinibDalpiciclibLetrozole + PyrotinibDalpiciclibLetrozole (Estrogen Receptor-Positive and HER2-Positive Metastatic Breast Cancer)	mssjzltynn(hpckmxltpd) = hafsubxiwd wthxqhykme (fguuumqscn, 41 - 88)	Positive	12 Dec 2025
SABCS2025	Not Applicable	HER2 Positive Breast Cancer Consolidation HER2-Positive	104	Pyrotinib 400 mg/day	znciqtntmq(fkdrfsqntl) = xrietbbufb lmihjggbrd (vgghozgawv ) View more	Positive	11 Dec 2025
SABCS2025	Not Applicable	HER2 Positive Breast Cancer Neoadjuvant HR+ \| HER2-positive	104	Pyrotinib-containing regimen	fouetzaohd(koyqsufsaq) = mirfkzehvg wpzasmcudv (hltkvslmom ) View more	Positive	11 Dec 2025

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