EGFR antagonists(Epidermal growth factor receptor erbB1 antagonists), HER2 antagonists(Receptor protein-tyrosine kinase erbB-2 antagonists), HER4 antagonists(Receptor protein-tyrosine 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+ [21]

Inactive Indication

Advanced Malignant Solid NeoplasmEstrogen receptor positive breast cancerHER2 Positive Cancer+ [1]

Originator Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Active Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Dr. Reddy's Laboratories Ltd.

Inactive Organization

Hengrui Therapeutics, Inc.

Drug Highest PhaseApproved

First Approval Date

China (12 Aug 2018),

HER2 Positive Breast Cancer

RegulationConditional marketing approval (China), Special Review Project (China), Priority Review (China), Breakthrough Therapy (China)

Structure/Sequence

Molecular FormulaC36H35ClN6O7

InChIKeyZUZJPRMSUMMELD-ZLWATVBPSA-N

CAS Registry1397922-61-0

View All Structures (2)

244

Clinical Trials associated with Pyrotinib Maleate

ChiCTR2500096763

/ SuspendedNot ApplicableIIT

Pyrotinib in T-DXD-treated HER2-positive advanced breast cancer: a prospective, single-arm, multicenter, real-world study

Start Date21 Feb 2025

Sponsor / Collaborator

The First Hospital of Jilin University

ChiCTR2500096074

/ SuspendedPhase 4IIT

Efficacy and Safety Study of Inetetamab and Pyrotinib Combined with Chemotherapy as First-Line Treatment for HER2-Expressing Advanced Cholangiocarcinoma

Start Date20 Jan 2025

Sponsor / Collaborator-

NCT06718933

/ RecruitingPhase 1/2IIT

A Prospective, Single-arm, Exploratory, Phase Ib/II Study of SHR-A1811 Combined with Pyrotinib and Bevacizumab in Advanced Breast Cancer with Brain Metastasis.

In phase Ib, our study is aimed to evaluate the safety and tolerance of SHR-A1811 combined with pyrotinib in breast cancer with brain metastasis, and confirm the recommended phase 2 dose combined with preliminary results of efficacy.
In phase II, our study is aimed to evaluate the efficacy and safety of SHR-A1811 combined with pyrotinib and bevacizumab at RP2D in breast cancer with brain metastasis.

Start Date08 Jan 2025

Sponsor / Collaborator

Fudan University

100 Clinical Results associated with Pyrotinib Maleate

100 Translational Medicine associated with Pyrotinib Maleate

100 Patents (Medical) associated with Pyrotinib Maleate

409

Literatures (Medical) associated with Pyrotinib Maleate

31 Dec 2025·Human Vaccines & Immunotherapeutics

Cost-effectiveness of trastuzumab deruxtecan as a second-line treatment for HER2-mutant advanced non-small cell lung cancer

Article

Author: Zhou, Aiping ; Huang, Jinglong ; Cai, Qi ; Zhang, Wen ; Gong, Caifeng ; You, Shuhui

The study of DESTINY-Lung01 and DESTINY-Lung02 demonstrated the favorable efficacy and optimal dosage of trastuzumab deruxtecan (T-DXd) in managing the human epidermal growth factor receptor 2 (HER2)-mutant non-small cell lung cancer (NSCLC) patients who had received previous treatment. The study sought to assess the cost-effectiveness of T-DXd in both the United States (US) and Chinese healthcare systems. Markov models were developed to evaluate the overall cost, incremental cost-effectiveness ratio (ICER), quality-adjusted life years (QALYs), and life years (LYs) of treatment with T-DXd compared with docetaxel, nivolumab, and pyrotinib for patients in the US and China. The level of willingness-to-pay (WTP) in the US and China is 150,000/QALYs and 32,517/QALYs, respectively. Sensitivity analyses were carried out to ensure the precision of the model. T-DXd yielded additional QALYs of 0.63 and 0.06 with an ICER of $338997.84 and $1437258.33 per QALY, respectively, in the US compared to the docetaxel and nivolumab regimens. And T-DXd yielded additional QALYs of 0.63, 0.06, and 0.13 with an ICER of $137959.45, $623805.93, and $515447.12 per QALY, respectively, in China compared to the docetaxel, nivolumab, and pyrotinib regimens. Sensitivity analysis showed that the cost of drugs is the most influential factor. T-DXd provides substantial therapeutic benefit for NSCLC patients with HER2 mutations who have had previous treatment but is not deemed cost-effective in either the US or China when compared to docetaxel, nivolumab, and pyrotinib. Price reduction is perhaps the main way to make T-DXd cost-effective.

01 Apr 2025·Clinical Breast Cancer

Real-World Outcomes of Pyrotinib-Based Therapy for HER2-Positive Breast Cancer With Brain Metastases: A Multicentre, Retrospective Analysis

Article

Author: Zhang, Jian ; Lei, Sen ; Tang, Yijing ; Xie, Weimin ; He, Chengzu ; Wu, Muxin ; Tan, Aihua ; Lu, Xin'an ; Wang, Hongxue

OBJECTIVEThis study was designed to investigate the efficacy and safety of pyrotinib-based therapy for HER2-positive breast cancer with brain metastases (BM) in the real-world setting.METHODSData of HER2-positive breast cancer patients with BM treated with pyrotinib-based therapy from a multicetre, registered, real-world study were analyzed.RESULTSAmong 45 female patients, the overall objective response rate (ORR) was 62.2%, higher in 1st/2nd-line than ≥ 3rd-line (71.0% vs. 42.9%, P = .072). The objective response rate of intracranial lesions (CNS-ORR) was 71.1 %, with a significantly higher CNS-ORR observed in the 1st or 2nd-line subgroup compared to that of ≥ 3rd-line subgroup (83.9% vs. 42.9%, P < .05). By the end of follow-up, 20 patients (44.4%) died, and the 1-year survival rate was 73.3%. The median progression-free survival (PFS) was 9.1 months (95% CI 6.7-11.5). Patients with 1 or 2 BM had a longer median PFS of 12.0 months compared to 7.7 months for those with ≥ 3 BM (P = .01). In addition, 1- or 2-line therapy and full dose exposure of pyrotinib of 320mg-400mg/day were associated with improved median PFS (all P > .05). The median intracranial PFS (CNS-PFS) was 11.4 months (95% CI 7.5-15.3). However, local intervention plus systemic treatment seemed to prolong CNS-PFS compared with systemic treatment alone (13.7 vs. 9.1 months, P = .128). Diarrhea was most common (88.9%), 24.4% grade 3.CONCLUSIONSThe pyrotinib-based therapy is effective for HER-2 positive breast cancer with BM, especially in 1st- or 2nd-line treatment, with tolerable adverse events. However, insufficient dosing of pyrotinib may impair efficacy outcomes.

01 Apr 2025·Anti-Cancer Drugs

Clinical efficacy of pyrotinib combined with chemotherapy for neoadjuvant treatment in HER2-positive breast cancer: a single-center study

Article

Author: Li, Fan ; Wei, Benkai ; Yan, Huanhuan ; Shen, Jun

This study aimed to evaluate the efficacy of pyrotinib, an orally administered small molecule tyrosine kinase inhibitor, combined with neoadjuvant chemotherapy in treating patients with human epidermal growth factor receptor 2 (HER2)-positive breast cancer. Pyrotinib works by inhibiting the HER2 signaling pathway, thereby preventing tumor cell growth. This single-arm clinical trial aimed to assess the total pathological complete response (tpCR; ypT0/is and ypN0) rate as the primary endpoint. A total of 27 patients were enrolled, each receiving 4–8 cycles of pyrotinib in combination with neoadjuvant chemotherapy. Pyrotinib combined with neoadjuvant chemotherapy demonstrated notable antitumor activity in patients with HER2-positive breast cancer. Among 26 patients, the tpCR rate was 26% (7/26), while the breast pathological complete response rate was 30% (8/26), indicating complete inhibition of the primary tumor in some cases. Notably, patients with HR-negative breast cancer demonstrated a higher tpCR rate compared with those with HR-positive breast cancer. The treatment regimen was well-tolerated. Diarrhea was the most common adverse event, occurring in 92.3% of patients, with 46.2% experiencing grade 3 or higher diarrhea. No severe adverse events or treatment-related fatalities were reported.

News (Medical) associated with Pyrotinib Maleate

06 Mar 2025

·www.prnewswire.com

TEPMETKO Continues to Strengthens its Position as a Leading METex14 Skipping NSCLC Therapy | DelveInsight

With increasing biomarker-driven cancer treatments, TEPMETKO benefits from growing adoption in precision oncology. Competition from other MET inhibitors like TABRECTA (capmatinib) exists, but TEPMETKO's once-daily dosing and efficacy profile offer differentiation. LAS VEGAS, March 6, 2025 /PRNewswire/ -- DelveInsight's " TEPMETKO Market Size, Forecast, and Market Insight Report" highlights the details around TEPMETKO, a kinase inhibitor indicated for the treatment of adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of TEPMETKO. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan]. EMD Serono's TEPMETKO (tepotinib) Overview TEPMETKO is a kinase inhibitor prescribed for adult patients with metastatic non-small cell lung cancer (NSCLC) carrying MET exon 14 skipping alterations. The active component is Tepotinib (as hydrochloride monohydrate), administered orally. Patients should be cautioned about the heightened risk of severe or fatal interstitial lung disease/pneumonitis, liver toxicity, and potential embryo-fetal toxicity, necessitating effective contraception during and shortly after treatment. Tepotinib specifically targets MET, including variants with exon 14 skipping mutations. It blocks HGF-dependent and independent MET phosphorylation, disrupting MET-driven signaling pathways. Additionally, at clinically relevant concentrations, Tepotinib inhibits melatonin 2 and imidazoline 1 receptors. In vitro studies show that it suppresses tumor cell proliferation, anchorage-independent growth, and migration of MET-dependent cancer cells. In mouse models with MET-driven tumors, including those with MET exon 14 skipping alterations, Tepotinib reduced tumor growth, sustained MET phosphorylation inhibition, and, in one case, decreased metastasis formation. The recommended dose of TEPMETKO is 450 mg taken orally once daily until disease progression or intolerable toxicity occurs. Patients should take it at the same time each day, swallowing tablets whole without chewing, crushing, or splitting them. If a dose is missed and less than eight hours remain until the next scheduled dose, patients should skip it. In cases of vomiting after taking TEPMETKO, the next dose should be taken at the usual time. Learn more about TEPMETKO projected market size for NSCLC @ TEPMETKO Market Potential Non-small cell lung cancer (NSCLC) is the most common type of lung cancer, accounting for 81% of all diagnosed cases. Early detection greatly improves outcomes, but diagnosing NSCLC and other lung cancers is challenging because their symptoms are often mistaken for common illnesses or the long-term effects of smoking. Consequently, 80% of NSCLC cases are already at advanced stages by the time they are identified, making treatment more difficult. Around 80% of EGFR mutations in NSCLC involve either exon 19 deletions or the exon 21 L858R substitution, both of which are classified as sensitizing mutations. Until the last decade, chemotherapy was the primary treatment for advanced and metastatic lung cancer. However, this changed in 2015 with the approval of the first immune checkpoint inhibitor (ICI), KEYTRUDA (pembrolizumab), as a second-line therapy for advanced cases. This was followed by TECENTRIQ (atezolizumab) in 2016. Both therapies were later approved for first-line treatment, broadening their use to a larger patient population. In 2020, the combination of OPDIVO (nivolumab) and ipilimumab also received approval as a first-line treatment for metastatic NSCLC. According to DelveInsight, the NSCLC market size across the 7MM is projected to grow from USD 30 billion in 2024, with a substantial CAGR through 2034. This growth is largely driven by the introduction of emerging therapies during the forecast period (2025–2034). Discover more about the NSCLC market in detail @ Non-small Cell Lung Cancer Market Report Emerging Competitors of TEPMETKO The NSCLC pipeline is very robust with the promising therapies such as Telisotuzumab vedotin (AbbVie), Patritumab deruxtecan (Daiichi Sankyo/AstraZeneca), Datopotamab deruxtecan (Daiichi Sankyo/AstraZeneca), Eftilagimod alpha (Immutep), BNT311/GEN1046 (acasunlimab) (Genmab), V940 (mRNA-4157) + Pembrolizumab (Moderna Therapeutics/Merck), Plinabulin + Docetaxel (BeyondSpring), Olomorasib (LY3537982) (Eli Lilly and Company), Zipalertinib (Cullinan Oncology/Taiho Pharma), Ceralasertib (AZD6738) (AstraZeneca), TEDOPI (EP-2101; IDM 2101; OSE-2101) (OSE Immuno-therapeutics), Sigvotatug vedotin (PF08046047) (Pfizer), ANKTIVA (N-803) (ImmunityBio), Aumolertinib/Almonertinib/HS-10206 (Jiangsu Hansoh Pharmaceutical), Niraparib (GSK), Savolitinib (AstraZeneca/Hutchison MediPharma), TRODELVY (Gilead Sciences), Pyrotinib (Jiangsu HengRui Medicine), Ociperlimab (BGB-A1217) (BieGene), Volrustomig (AstraZeneca), Gotistobart (BNT316/ONC-392) (OncoC4/BioNTech), Ivonescimab (AK112/SMT112) (Akeso Biopharma/Summit Therapeutics), ZYNYZ (retifanlimab/INCMGA00012) (Incyte/Macrogenics), Divarasib (GDC-6036) (Roche/Genentech), Tiragolumab (RG6058) (Roche), Sacituzumab Tirumotecan (Merck and Kelun-Biotech), JEMPERLI (dostarlimab/TSR-042) (GSK and AnaptysBio), Zongertinib (BI-1810631) (Boehringer Ingelheim), BAY 2927088 (Bayer), Serplulimab (HLX10) (Shanghai Henlius Biotech), Rilvegostomig (AZD2936) (AstraZeneca), MK-1084 (Merck, Taiho Pharmaceutical, and Astex), Domvanalimab (Arcus Biosciences and Gilead Sciences), OPDUALAG (nivolumab and relatlimab) (Bristol-Myers Squibb), Belrestotug + JEMPERLI (iTeos Therapeutics and GSK), Firmonertinib (ArriVent BioPharma), Sunvozertinib (DZD9008) (Dizal Pharmaceutical), Cobolimab (GSK), Livmoniplimab (AbbVie), Fianlimab (REGN3767) (Regeneron Pharmaceuticals), BNT327/PM8002 (Biotheus/BioNTech), HS-20117 (Hansoh BioMedical), IO102-IO103 + Pembrolizumab (IO Biotech), Naptumomab estafenatox (NeoTX Therapeutics/Active Biotech), FF-10832 (FUJIFILM Corporation), BNT116 (BioNTechSE/Regeneron Pharmaceuticals), CAN-2409 (Candel Therapeutics), Mecbotamab Vedotin (BA3011/CAB-AXL-ADC) (BioAtla), Bemcentinib (BGB 324/BGB-3234/R-428) (BerGenBio/Rigel Pharmaceuticals), DOVBLERON (taletrectinib/AB-106/IBI-344) (Nuvation Bio/Innovent Biologics/Daiichi Sankyo/Nippon Kayaku), Lifileucel (Iovance Biotherapeutics), IBI363 (Innovent Biologics), Sotevtamab (AB-16B5) (Alethia Biotherapeutics), Avutometinib (VS6766) (Verastem Oncology), Vebreltinib (APL-101) (Apollomics), LP-300 (Lantern Pharma), JNJ-90301900 (Johnson & Johnson Innovative Medicine), AMG 193 (Amgen), Luveltamab tazevibulin (Sutro Biopharma), PRT3789 (Prelude Therapeutics), Disitamab vedotin (Seagen), PADCEV (enfortumab vedotin) (Astellas Pharma), RP1 (Replimune), TIVDAK (tisotumab vedotin) (Seagen), Zanidatamab (Jazz Pharmaceuticals), Utidelone injectable (UTD1) (Beijing Biostar Pharmaceuticals), REGN5093-M114 (Regeneron Pharmaceuticals), SLC-391 (SignalChem Lifesciences), fulzerasib (GenFleet), Davutamig (REGN5093) (Regeneron Pharmaceuticals), TAS3351 (Taiho Oncology), H002 (RedCloud Bio), JIN-A02 (J INTS BIO), FWD1509 (Forward Pharma), Sabestomig (AZD7789) (AstraZeneca), Sasanlimab (Pfizer), Selvigaltin (GB1211) (Galecto Biotech), Vepafestinib Helsinn (Healthcare/Taiho Pharmaceutical), EP0031 (A400/ KL590586) (Ellipses Pharma/Kelun-Biotech), Pamvatamig (MCLA-129) (Merus), Zidesamtinib (NVL-520) (Nuvalent), NVL-655 (Nuvalent), RMC-4630 (Revolution Medicines), REQORSA (quaratusugene ozeplasmid) (Genprex), PDC*lung01 (PDC*line Pharma), Evalstotug (BA3071) (BioAtla and BeiGene), PT-112 (Promontory Therapeutics), MRT-2359 (Monte Rosa Therapeutics), GAIA-102 (GAIA BioMedicine), Rigosertib (Traws Pharma), HMBD-001 (Hummingbird Bioscience), PLB1004 (Avistone Biotechnology), ANS03 (Avistone Biotechnology), MYTX-011 (Mythic Therapeutics), A166 (Sichuan Kelun-Biotech Bio-pharmaceutical), Atamparib (BN-2397) (Ribon Therapeutics), DELTACEL (KB-GDT-01) (Kiromic BioPharma), Carotuximab (ENV-105) (Kairos Pharma), YL202 (MediLink Therapeutics), and others. To know more about the number of competing drugs in development, visit @ TEPMETKO Market Positioning Compared to Other Drugs Key Milestones of TEPMETKO In February 2024, the FDA granted traditional approval to TEPMETKO for adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. In February 2022, the EC approved TEPMETKO as monotherapy for the treatment of adult patients with advanced NSCLC harboring alterations leading to METex14 skipping who require systemic therapy following prior treatment with immunotherapy and/or platinum-based chemotherapy. In February 2021, Merck announced that the US FDA has approved TEPMETKO following priority review for the treatment of adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. This indication was approved under accelerated approval based on ORR and DOR. In October 2020, TEPMETKO received ODD for treating NSCLC with MET genomic tumor aberrations In March 2020, EMD Serono (the biopharmaceutical business of Merck KGaA), announced that the MHLW approved TEPMETKO for the treatment of patients with unresectable, advanced, or recurrent NSCLC with METex14 skipping alterations. In September 2019, the US FDA granted BTD for tepotinib in patients with metastatic NSCLC harboring METex14 skipping alterations who progressed following platinum-based cancer therapy Discover how TEPMETKO is shaping the NSCLC treatment landscape @ TEPMETKO NSCLC TEPMETKO Market Dynamics TEPMETKO competes in a growing but highly specialized market where MET-targeted therapies are gaining traction due to their efficacy in addressing MET-altered tumors. The market for MET inhibitors is expanding as precision oncology advances and molecular diagnostics become more widely available, enabling better identification of patients who would benefit from targeted treatments like TEPMETKO. A key factor shaping TEPMETKO's market dynamics is competition. It directly competes with Novartis' TABRECTA (capmatinib), another MET inhibitor approved for the same indication. While TEPMETKO offers the advantage of once-daily dosing compared to TABRECTA's twice-daily regimen, both drugs have similar efficacy profiles, making physician and patient preference an important differentiator. Additionally, broader competition from next-generation MET inhibitors and combination therapies in clinical trials could impact TEPMETKO's long-term market position. Regulatory approvals and market access play a crucial role in TEPMETKO's adoption. The drug has been approved in multiple regions, including the U.S., Europe, and Japan, but reimbursement and pricing strategies vary by market. Payer policies, along with the cost-benefit analysis of MET inhibitors compared to other targeted therapies, influence prescription trends. Furthermore, real-world evidence and post-marketing studies will be critical in demonstrating TEPMETKO's sustained effectiveness and safety, which could support expanded indications and increased market penetration. Looking ahead, the MET inhibitor market is expected to grow with advances in biomarker-driven therapy, further refining patient selection. TEPMETKO's success will depend on continued clinical development, potential label expansions, and strategic partnerships to strengthen its competitive edge. As new entrants emerge, Merck KGaA's ability to differentiate TEPMETKO through combination strategies or enhanced formulations may determine its long-term sustainability in this evolving landscape. Dive deeper to get more insight into TEPMETKO's strengths & weaknesses relative to competitors @ TEPMETKO Market Drug Report Table of Contents Related Reports Non-small Cell Lung Cancer Market Non-small Cell Lung Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key NSCLC companies including Daiichi Sankyo, AstraZeneca, Gilead Sciences, BieGene, AbbVie, Roche, Merck, Novartis, Pfizer, Takeda Pharmaceuticals, Eli Lilly, BerGenBio, GlaxoSmithKline, Duality biologics, among others. Non-small Cell Lung Cancer Pipeline Non-small Cell Lung Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key non-small cell lung cancer companies, including BridgeBio Pharma, Daiichi Sankyo, EMD Serono, Merck, BridgeBio Pharma, Abbvie, Pfizer, Eli Lilly and Company BioNTech SE, Shenzhen TargetRx, Taiho Pharmaceutical, Chong Kun Dang, Bristol Myers Squibb, Innovent Biologics, Xuanzhu Biopharmaceutical, Bayer, GeneScience Pharmaceuticals, InventisBio, Apollomics, Imugene, Ono Pharmaceutical, Pierre Fabre, Jiangsu Hengrui Medicine Co., Bristol-Myers Squibb, Surface Oncology, Inhibrx, Sinocelltech, Mirati Therapeutics, REVOLUTION Medicines, Yong Shun Technology Development, Iovance Biotherapeutics, Galecto Biotech, among others. C-MET Metastatic Non-small Cell Lung Cancer Market C-MET Metastatic Non-small Cell Lung Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key C-MET mNSCLC companies, including Novartis, Merck, EMD Serono, AbbVie, Regeneron Pharmaceuticals, Mythic Therapeutics, Apollomics, Johnson & Johnson Innovation, Haihe Biopharma, among others. C-MET Non-small Cell Lung Cancer Pipeline C-MET Non-small Cell Lung Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key C-MET non-small cell lung cancer companies, including AbbVie, Janssen Research & Development, Beijing Pearl Biotechnology Limited Liability Company, Novartis, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Drug ApprovalImmunotherapyPriority Review

22 May 2024

·www.biospace.com

Breast Cancer Antibodies Combinations Therapy Clinical Trials Insight

One of the most frequently diagnosed cancers worldwide accounts for breast cancer with respect to its high prevalence and fatalities gaits. Hitherto, the management of breast cancer remains a hassle to healthcare professionals. Breast Cancer, a heterogeneous and complex disease, demands innovative treatment strategies to confront its varied manifestations. In recent years, the spotlight has turned towards a promising field the synergy of combining different types of antibodies, which will aid to offer a potential breakthrough in the battle against the formidable adversary, breast cancer. The realm of combinational antibodies has emerged as an innovative treatment regimens in which by harnessing the potential of different types of antibodies with therapeutic agents aid to treat breast cancer. Conventionally, traditional therapies like hormone therapy, chemotherapy or immunotherapy were utilized which exhibited good efficacy and tolerability to breast cancer. However, there exist numerous patients who don’t respond to conventional treatment, creating a major room for improvement. As a result, there is an urgent need of combinational antibodies for the treatment of multiple patients suffering from breast cancer malignancies. Download Antibodies Combinations Therapy Research Insight: The notion of combining antibodies with other therapeutic agents clenches long chronicle which can be backtracked to the late 1990s in which the first monoclonal antibody, Trastuzumab, sold under the brand name Herceptin, was approved by FDA in 1998. Since then, numerous researches for combining different types of monoclonal antibodies like Trastuzumab are being ongoing in the domain with the key objective of developing advanced and innovative antibody combination in order to provide treatment for breast cancer indications. Following that, antibody combinations such as pertuzumab (Perjeta) in conjugation with trastuzumab (Herceptin) and Phesgo (combination of Herceptin, Perjeta along with enzyme Hyaluronidase) are being approved in the year 2012 and 2020 for the management of breast cancer malignancies. Apart from that, numerous combination of antibodies with chemotherapy are enduring that evaluates the role of antibodies with immune checkpoint inhibitors, like PD-1, and HER2 which have already been approved for the management of breast cancer. For instance, Trastuzumab in combination with Pyrotinib, dual inhibitor of EGFR/HER2, is currently in the clinical research for the treatment of breast cancer. The treatment regimen is lately in the phase III stage of development which is sponsored by Shengjing Hospital. With ceaseless advancement and progress in antibody combinations along with molecular biology techniques, helps in managing breast cancer. Preliminary data exhibits remarkable heterogeneity of breast cancer at the molecular level. Utilizing the realm of antibody combinations offers multifaceted approaches, addressing diverse molecular pathways and subtypes. This strategy seeks to overcome the limitations of the single agent therapies by comprehensively targeting different aspects of the disease. The clinical pipeline in the sphere of antibody combination consists of multitudinous combinations of antibodies with chemotherapies, immunomodulatory drugs, vaccines, together with immune checkpoint inhibitors, such as CTLA-4, PD-1 and PD-L1, PARP inhibitors, CDK4/6 inhibitors, bispecific antibodies, CAR T cell therapies, antibody drug conjugates, and others. Besides, the market for antibody combinations also includes the presences of Herceptin bio similar in the clinical pipeline. The aim of these studies is to increase the efficiency and safety of treatment regimen. For instance, Institut fuer Frauengesundheit and Samsung Bioepis initiated a clinical investigation in which a combination of Pertuzumab with Herceptin bio similar medication, Ontruzant that is lately in the phase IV clinical studies for the treatment of HER2 positive breast cancer. Furthermore, due to the presence of the key players along with rising clinical trials will help to launch novel antibody combinations in the commercial market. Giant pharmaceutical companies such as Pfizer, Bristol-Myers Squibb, AstraZeneca, Daiichi Sankyo, Taizhou EOC Pharma, Agenus, Novartis, Celldex Therapeutics and Merck are currently shepherding the clinical trials and studies in order to launch an innovative antibody combination for breast cancer. It is expected that the sphere of antibody combinations will expand in the forthcoming years on account of aspects like agreement, rise in clinical research along with collaborations. For instance, in March 2023, acquisition agreement was settled amongst Pfizer and Seagen with the purpose of combining Seagen’s antibody-drug conjugate (ADC) candidates with Pfizer's antibody candidates to develop a novel antibody combination treatment for breast cancer. This will further provide thrust to the market growth of combination antibodies. As breast cancer incidences, advancement in technology along with research and development expands; the market of antibody combination for the treatment of breast cancer will multiply further in the imminent years.

Drug ApprovalPhase 3ImmunotherapyAcquisitionADC

08 Nov 2023

·synapse.patsnap.com

Patent Analysis of Jiangsu Hengrui's PARP1 Inhibitor HRS-1167

At the end of October, Hengrui and Merck reached a transaction cooperation totaling 1.4 billion Euros, with an initial payment of 160 million Euros. The transaction mainly includes Hengrui's independently developed PARP1 inhibitor HRS-1167 and Claudin-18.2 antibody-drug conjugate (ADC) SHR-A1904. The distribution ratio of the initial payment between small molecules and large molecules was not disclosed in the transaction. Considering the current research popularity of ADC, SHR-A1904 should have a higher proportion. Search for the transaction record of HRS-1167 in the Synapse databasePrior to this, Hengrui's overseas cooperation projects included SHR0302, SHR1459, Apatinib, Carrelizumab, Pyrotinib, and SHR1701, among others. The small molecule with the highest upfront payment was EZH2 inhibitor SHR2254, which Hengrui licensed out in February of this year for an upfront payment of $11 million. After all, SHR2254 is already in Phase I/II clinical trials, so the upfront payment naturally wouldn't be low. SHR2254 is indicated for the treatment of conditions including B-cell lymphoma, peripheral T-cell lymphoma, prostate cancer, and solid tumors, among others. This time raising the upfront payment record to 160 million Euros is of milestone significance for Hengrui. What insights can we gain from this? HRS-1167 is a small molecule drug, with PARP1 as its target. PARP1 is a protein associated with DNA repair and cell apoptosis, playing a crucial role in tumor development. Therefore, HRS-1167 is widely used in the field of tumor treatment. At present, HRS-1167 is undergoing phase 1 clinical trials for solid tumors. Solid tumors are a common type of tumor, including lung cancer, breast cancer, colorectal cancer, and so on. By targeting PARP1, HRS-1167 may be able to interfere with the DNA repair mechanisms of tumor cells, leading to the death or inhibition of tumor cell growth. With further research and clinical trials, HRS-1167 is hoped to provide a new treatment option for cancer patients. Search for patents associated with HRS-1167 in the Synapse databaseIn the Synapse database, search for HRS-1167 and find two groups of patents applied for by Hengrui, which are CN115403595A and WO2022247816A1. The WO patent also has a Taiwanese homologous patent, TW202313630A. The drugs protected by these patents may all contain HRS-1167. On May 24 and 27, 2021, Hengrui respectively initiated temporary applications for two patents, and obtained the corresponding patents for molecular formulas and compounds. It is clear which patent is more important. It is considered by the author that HRS-1167 is more likely to be the structure of Example 2 in WO2022247816A1. In the WO patent, the Compound of Example 2 significantly inhibits recombinant PARP1 activity (IC50 = 11 nM), which is more selective than recombinant PARP2 (IC50= 1779 nM). In the Cell Titer-Glo assay, it showed anti-proliferative activity against human breast cancer MDA-MB-436 and colon cancer DLD-1 cells with knocked out BRCA2 (IC50 values of 1 and 2.5 nM respectively), and no significant activity against wild-type DLD-1 cancer cells (IC50>250 nM). WO2022247816A1 includes 10 examples and corresponding isomers. CN115403595A includes 4 examples and related isomers. Timeline of Two Hengrui Patents and Possible Lead Molecule StructuresThese two patents are both fast follows on AstraZeneca's PARP1 inhibitor AZD5305. Hengrui has once again maximized benefits by minimizing costs (with the synthesis of 14 examples). It is also worth admiring AstraZeneca's strong research and development prowess in PARP inhibitors. Additionally, AstraZeneca also has another brain-penetrating PARP1 selective inhibitor AZD9574, the structure of which was first revealed at the 2022 ACS Spring Meeting. It is believed that Hengrui should also have a strategic layout in the same field. The structure of AZD9574The preclinical in vivo pharmacokinetic (PK) characteristics of AZD5305 were measured in mice, rats, dogs, and cynomolgus monkeys. The compound AZD5305 has a very low plasma clearance (CLp) of 0.23, 1.1, 0.33, and 0.84 mL/min/kg respectively in mice, rats, dogs, and monkeys, while the steady-state volume of distribution (Vss) is 0.17, 0.38, 0.30, 0.38 L/kg. The plasma half-life is 8.0, 4.6, 10, and 7.1 hours respectively. The oral bioavailability of AZD5305 is very high in all species, consistent with low hepatic clearance and high absorption rates. With a relatively low unbound clearance rate, coupled with high potency, it is expected that the effective in vivo doses can be reduced. Optimization and partial in vivo data of AZD5305However, the current clinical trials have not revealed the dosage of AZD5305. The clinical registration information updated in July 2023 only includes two items: NCT05938270 and NCT05797168. Among them, NCT05797168 is a phase I/IIa study of AZD5335 as a monotherapy and in combination with anti-cancer drugs for the treatment of solid tumor patients. AZD5335 is AstraZeneca's FRα ADC drug, with AZD5305 being used as a combination drug. NCT05938270 also involves combination use with darolutamide. Moreover, the patent WO2023089527 includes an embodiment of the anti-tumor effect of AZD5305 combined with the TROP-2 ADC drug DS-1062. Patent WO2022074617 introduces the combination use of AZD5305 and DS8201. In AstraZeneca's public pipeline, AZD5305 does not seem to be given enough attention. Based on the previous analysis, the likely structure of HRS-1167 is the molecular structure presented in Embodiment 2 of WO2022247816A1. The difference between this molecule and AZD5305 is merely the attachment of a 6-membered oxygen ring, and derivation of one of its isomers. Some preclinical data disclosed in the patent suggest that this series likely holds potential benefits over AZD5305. This strategy of design is not uncommon, as evidenced by the KRAS inhibitor that Jinfang Pharmaceuticals transferred to Cinda. However, whether the advantages displayed in preclinical stages can effectively translate into clinical benefits is always filled with unknowns.

100 Deals associated with Pyrotinib Maleate

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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
Squamous non-small cell lung cancer	Phase 3	Russia	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Squamous non-small cell lung cancer	Phase 3	Belgium	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Squamous non-small cell lung cancer	Phase 3	South Korea	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Squamous non-small cell lung cancer	Phase 3	Italy	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Squamous non-small cell lung cancer	Phase 3	Spain	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Squamous non-small cell lung cancer	Phase 3	Turkey	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	11 Sep 2020
Early Stage Breast Carcinoma	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	12 Jul 2019
Metastatic human epidermal growth factor 2 positive carcinoma of breast	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	20 Jul 2016
HER2 Positive Cancer	Preclinical	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	22 Apr 2019
Locally advanced breast cancer	Preclinical	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	24 Jul 2018

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05659056 (SABCS2024) Manual	Phase 2	HER2 Positive Breast Cancer Neoadjuvant	52	pyrotinib + trastuzumab + nab-paclitaxel	lucbkqpcsr(owpxvceoin) = yghybjltoc ehaqovgdux (jbnoohcmhk, 29.0 - 56.7) View more	Positive	10 Dec 2024
				pyrotinib + trastuzumab + nab-paclitaxel (HER2-enriched subtype)	lucbkqpcsr(owpxvceoin) = tydwbyrvuk ehaqovgdux (jbnoohcmhk, 37.9 - 73.2)
NCT05582499 (SABCS2024) Manual	Phase 2	HER2 Positive Breast Cancer	265	PCbHP (nab-paclitaxel, carboplatin, trastuzumab, pertuzumab)	(wedicgmsme) = lprhypgtnn qrisyijeed (dxopwfhgvi ) View more	Positive	26 Nov 2024
				Mono-SHR-A1811	(wedicgmsme) = rhdawjxzym qrisyijeed (dxopwfhgvi ) View more
NCT06245824 (TROPHY, SABCS2024) Manual	Phase 1/2	Metastatic human epidermal growth factor 2 positive carcinoma of breast First line	5	Trastuzumab deruxtecan 5.4 mg/kg + Pyrotinib 400 mg	(ubfqrqrmcx) = The only DLT was grade 3 anorexia, which occurred during the first cycle in 1 patient who received 400 mg of pyrotinib. ihdsnsxwpi (zdvhiygxdm ) View more	Positive	26 Nov 2024
				Trastuzumab deruxtecan 5.4 mg/kg + Pyrotinib 320 mg
DDDR-20 (SNO2024)	Not Applicable	HER2 Positive Breast Cancer	52	Pyrotinib + Stereotactic Radiosurgery	(ogxjezmzlt) = nnfmcuwtls hitbeyfakn (rhbcjiyesa, 17.5 - 27.6) View more	Positive	11 Nov 2024
NCT03691051 (PERMEATE, Pubmed \| EClinicalMedicine) Manual	Phase 2	HER2 Positive Breast Cancer	78	Pyrotinib plus capecitabine	(kbjxrrowgv) = ikbvrugrmh cfafzraelx (ljtgzhvzwj, 24.4 - not reached) View more	Positive	01 Oct 2024
				Pyrotinibcapecitabine (Radiotherapy-naïve brain metastases)	(kbjxrrowgv) = idmhtbccby cfafzraelx (ljtgzhvzwj, 12.6 - 33.3) View more
NCT02614794 \| NCT04367090 \| NCT05346861 \| NCT04582968 \| NCT05042791 \| NCT03876587 (Pubmed \| Neoplasia) Manual	Not Applicable	Metastatic human epidermal growth factor 2 positive carcinoma of breast	137	Pyrotinib-based regimen as first-line therapy	(gxhmgfhabv) = dhlerypdcg rbozkiunfz (fgmxiwkuwe ) View more	Positive	01 Oct 2024
				Pyrotinib-based regimen as second-line therapy	(nkbwgtfbpn) = vbvubyhnjr fyuazqnmsx (tyrskthslw, 7.815 - 20.925)
NCT03923179 (ESMO2024) Manual	Phase 2	Metastatic human epidermal growth factor 2 positive carcinoma of breast	22	Pyrotinib 400mg per dayetoposide	(yxufwpxqvp) = inxrpmrwgm eqnftrglzs (bhaufijuzx, 7.6 - 10.4) View more	Positive	16 Sep 2024
NCT04917900 (not available, ESMO2024) Manual	Phase 2	HER2 Positive Breast Cancer Neoadjuvant	214	Pyrotinib plus albumin-bound paclitaxel and trastuzumab (HLX02)	(eujfbofcuf) = krymkgzrvi drqhsghhjx (orhqnoajbl, 55.65 - 69.86) View more	Positive	16 Sep 2024
NCT05635487 (MUKDEN 07, ESMO2024) Manual	Phase 2	HER2 Positive Breast Cancer Neoadjuvant HR+	29	SHR-A1811 + Pyrotinib	(spyestuyee) = gxxxzuhqim jowryortdi (btyzlpotwc, 59.1 - 91.7) View more	Positive	16 Sep 2024
				SHR-A1811SHR-A1811 4.8 mg/kg+ PyrotinibPyrotinib 240 mg/day	(spyestuyee) = onblwvhdij jowryortdi (btyzlpotwc ) View more
ChiCTR1900021684 (PATHER2, ESMO2024)	Phase 2	Advanced Lung Non-Small Cell Carcinoma TP53 \| DNMT3A \| ARID1B ... View more	27	Pyrotinib plus apatinib	(khlkswjvuy) = jpoljujxjr wtsmwanvow (swefbkkdql )	Positive	15 Sep 2024

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