ArticleCell reports2022
Homogeneity of antibody-drug conjugates critically impacts the therapeutic efficacy in brain tumors.
Article in Cell reports, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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.
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Who cites it
32 citing papers in PubMed, 46 citations in OpenAlex.
- Article
- Human Pharmacokinetic Prediction of Antibody-Drug Conjugates Using Human FcRn Transgenic Mice.Clinical and translational science · 2026Article
- From Unmet Medical Need to Drug Candidate: A Translational Therapeutic Development Roadmap Illustrated by Dual-Payload Antibody-Drug Conjugates.Biomolecules · 2026Review
- Drug resistance to antibody-drug conjugates: mechanisms, challenges, and perspectives.Cancer biology & medicine · 2026Review
- Review
- Development of an Active Chimeric IL13Rα2 ADC for Diffuse Intrinsic Pontine Glioma.ImmunoTargets and therapy · 2026Article
- Site-specific ligase-dependent conjugation with ring-opening linker improves safety and stability of HER2-targeting ADCs.Nature communications · 2025Article
- Trastuzumab Deruxtecan for ERBB2-Mutant Metastatic Non-Small Cell Lung Cancer With or Without Brain Metastases: A Secondary Analysis of Randomized Clinical Trials.JAMA network open · 2025Observational
- Antibody drug conjugates in metastatic brain tumors: current landscape, therapeutic potential and challenges.Journal of neuro-oncology · 2025Review
- Microtubule-Targeting Agents: Advances in Tubulin Binding and Small Molecule Therapy for Gliomas and Neurodegenerative Diseases.International journal of molecular sciences · 2025Review
- 177Lu-Labeled Antibody-Drug Conjugate: A Dual-Mechanistic Treatment Modality in Solid Tumors.Molecular cancer therapeutics · 2025Article
- Exploring the Role of ADCs in Brain Metastases and Primary Brain Tumors: Insight and Future Directions.Cancers · 2025Review
- Immune response recalibration using immune therapy and biomimetic nano-therapy against high-grade gliomas and brain metastases.Asian journal of pharmaceutical sciences · 2025Review
- Molecular evolution of central nervous system metastasis and therapeutic implications.Trends in molecular medicine · 2025Review
- Diverse Roles of Antibodies in Antibody-Drug Conjugates.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Branched Linkers for Homogeneous Antibody-Drug Conjugates: How Long Is Long Enough?International journal of molecular sciences · 2024Article
- Generation of binder-format-payload conjugate-matrices by antibody chain-exchange.Nature communications · 2024Article
- Antibody-drug conjugates are active in patients with HER2-positive breast cancer brain metastases: where do we go from here?ESMO open · 2024Article
- Decoding of the surfaceome and endocytome in primary glioblastoma cells identifies potential target antigens in the hypoxic tumor niche.Acta neuropathologica communications · 2024Article
- Recent Technological and Intellectual Property Trends in Antibody-Drug Conjugate Research.Pharmaceutics · 2024Review
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
Glioblastoma multiforme (GBM) is the most aggressive and fatal disease of all brain tumor types. Most therapies rarely provide clinically meaningful outcomes in the treatment of GBM. Although antibody-drug conjugates (ADCs) are promising anticancer drugs, no ADCs have been clinically successful for GBM, primarily because of poor blood-brain barrier (BBB) penetration. Here, we report that ADC homogeneity and payload loading rate are critical parameters contributing to this discrepancy. Although both homogeneous and heterogeneous conjugates exhibit comparable in vitro potency and pharmacokinetic profiles, the former shows enhanced payload delivery to brain tumors. Our homogeneous ADCs provide improved antitumor effects and survival benefits in orthotopic brain tumor models. We also demonstrate that overly drug-loaded species in heterogeneous conjugates are particularly poor at crossing the BBB, leading to deteriorated overall brain tumor targeting. Our findings indicate the importance of homogeneous conjugation with optimal payload loading in generating effective ADCs for intractable brain tumors.
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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.