ArticleAntibody therapeutics2021
Preclinical evaluation of MRG002, a novel HER2-targeting antibody-drug conjugate with potent antitumor activity against HER2-positive solid tumors.
Article in Antibody therapeutics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers, 2 of them syntheses that pooled it.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
33 citing papers in PubMed, 2 syntheses or guidelines pooled it, 46 citations in OpenAlex.
- Efficacy and safety of antibody-drug conjugates in HER2-positive and HER2-low advanced gastric cancer: a systematic review and update.Journal of the Egyptian National Cancer Institute · 2026Pooled it
- Efficacy and safety of antibody-drug conjugate based therapy in locally advanced or metastatic urothelial carcinoma: a systematic review and network meta-analysis of emerging clinical evidence.Frontiers in immunology · 2026Pooled it
- Targeting Biliary Tract Cancers with Antibody-Drug Conjugates: Advances in Molecular Targets and Rational Combinations.Cancers · 2026Review
- Antibody-drug conjugates in gastric cancer: from targeted cytotoxicity to immune modulation.Frontiers in immunology · 2026Review
- Research on Targeted Therapy for Malignant Tumors of the Biliary Tract.OncoTargets and therapy · 2026Review
- The Therapeutic Potential of Photoimmunotherapy as a Safe, Effective and Non-Toxic Treatment Option for Superficial Triple Negative Breast Cancer.Cancer medicine · 2025Review
- Navigating the future of gastric cancer treatment: a review on the impact of antibody-drug conjugates.Cell death discovery · 2025Review
- Recent advances of antibody-drug conjugates in treating breast cancer with different HER2 status.Therapeutic advances in medical oncology · 2025Review
- Unveiling the future of breast cancer therapy: Cutting-edge antibody-drug conjugate strategies and clinical outcomes.Breast (Edinburgh, Scotland) · 2024Review
- Antibody-drug conjugates in gastric cancer: from molecular landscape to clinical strategies.Gastric cancer : official journal of the International Gastric Cancer Association and the Japanese Gastric Cancer Association · 2024Review
- HER2-low gastric cancer: is the subgroup targetable?ESMO open · 2024Review
- The Evolving Paradigm of Antibody-Drug Conjugates Targeting the ErbB/HER Family of Receptor Tyrosine Kinases.Pharmaceutics · 2024Review
- Preclinical studies of BB-1701, a HER2-targeting eribulin-containing ADC with potent bystander effect and ICD activity.Antibody therapeutics · 2024Article
- Novel HER-2 Targeted Therapies in Breast Cancer.Cancers · 2023Review
- Shifting the Antibody-Drug Conjugate Paradigm: A Trastuzumab-Gold-Based Conjugate Demonstrates High Efficacy against Human Epidermal Growth Factor Receptor 2-Positive Breast Cancer Mouse Model.ACS pharmacology & translational science · 2023Article
- Novel Anti-HER2 Antibody-Drug Conjugates Versus T-DM1 for HER2-Positive Metastatic Breast Cancer After Tyrosine Kinase Inhibitors Treatment.The oncologist · 2023Article
- Antibody-Drug Conjugates in Solid Tumor Oncology: An Effectiveness Payday with a Targeted Payload.Pharmaceutics · 2023Review
- Observational
- Clinical perspective: Antibody-drug conjugates for the treatment of HER2-positive breast cancer.Molecular therapy : the journal of the American Society of Gene Therapy · 2023Review
- Tumor Site-Specific Cleavage Improves the Antitumor Efficacy of Antibody-Drug Conjugates.International journal of molecular sciences · 2023Article
Corrections and comments
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Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundERBB2 is a proto-oncogene of multiple cancers including breast and gastric cancers with HER2 protein overexpression or gene amplification and has been proven clinically as a valid target for these cancers. HER2-targeting agents such as Herceptin®, Kadcyla® and ENHERTU® have been approved by the FDA for the treatment of breast cancer, but these drugs still face the challenge of acquired resistance and/or severe adverse reactions in clinical use. Therefore, there is significant unmet medical need for developing new agents that are more effective and safer for patients with advanced HER2-positive solid tumors including breast and gastric cancers.
methodsWe report here the making of MRG002, a novel HER2-targeted antibody drug conjugate (ADC), and preclinical characterization including pharmacology, pharmacodynamics and toxicology and discuss its potential as a novel agent for treating patients with HER2-positive solid tumors.
resultsMRG002 exhibited similar antigen binding affinity but much reduced antibody-dependent cellular cytotoxicity (ADCC) activity compared to trastuzumab. In addition to potent
conclusionMRG002 has demonstrated a favorable toxicity profile and potent antitumor activities in the breast and gastric PDX models with varying levels of HER2 expression, and/or resistance to trastuzumab or T-DM1. A phase I clinical study of MRG002 in patients with HER2-positive solid tumors is ongoing (CTR20181778).
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.