Therapeutic bispecific antibodies cross the blood-brain barrier in nonhuman primates

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Boosting Brain Uptake of a Therapeutic Antibody by Reducing Its Affinity for a Transcytosis Target

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Increased Brain Penetration and Potency of a Therapeutic Antibody Using a Monovalent Molecular Shuttle

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Blood–Brain Barrier Transport of Therapeutics via Receptor-Mediation

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Transferrin receptor (TfR) trafficking determines brain uptake of TfR antibody affinity variants

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Addressing Safety Liabilities of TfR Bispecific Antibodies That Cross the Blood-Brain Barrier

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A Therapeutic Antibody Targeting BACE1 Inhibits Amyloid-β Production in Vivo

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Developing Therapeutic Antibodies for Neurodegenerative Disease

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Transport pathways across the blood-brain barrier for waste clearance and drug delivery

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Antibody-Mediated Delivery of BRM/BRG1 Protein Degraders Affords Strong Antitumor Efficacy in Multiple BRM-Dependent Non-Small Cell Lung Cancer Xenograft Models

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Monoclonal Antibodies: From Structure to Therapeutic Application

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Safety Concerns in Neurological Clinical Trials: A Challenge That the FDA Must Resolve

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Prospects and Challenges for Alzheimer Therapeutics

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Site of effect of LY2951742 for migraine prophylaxis–Authors' reply

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Multiplex screening of transferrin receptor-targeted lipid nanoparticles for systemic brain delivery using DNA barcodes

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Antibody drug conjugates in Alzheimer’s disease: emerging strategies and future directions

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Impact of ASO conjugation and receptor binding affinity on intracellular transport of mono- and bispecific TfR- and CD98-Brainshuttle TM variants

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Monoclonal antibody neutralizes Staphylococcus aureus serine protease-like protein B (SplB)-induced pathology

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Longitudinal pharmacokinetic and safety studies of an antibody-erythropoietin fusion protein for Alzheimer's disease

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Motif‐driven protein binder design towards transferrin receptor helical domain

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The Significance of the Choroid Plexus for Cerebral Iron Homeostasis

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Antibody-Based Formats to Target Glioblastoma: Overcoming Barriers to Protein Drug Delivery

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β-Secretase Inhibition

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Two peptides targeting endothelial receptors are internalized into murine brain endothelial cells

Hudecz, D., Sigurdardóttir, S. B., Christensen, S. C., Hempel, C., Urquhart, A. J., Andresen, T. L., & Nielsen, M. S. (2021) · PLoS ONE · doi:10.1371/journal.pone.0249686 · Cited by 3

Monoclonal Antibodies: From Structure to Therapeutic Application

Deng, R., Boswell, C. A., Putnam, W. S., Tang, M. T., Garg, A., Li, C., Chung, S., & Girish, S. (2019) · Springer eBooks · doi:10.1007/978-3-030-00710-2_8 · Cited by 3

Engineering Antibody‐Based Therapeutics: Progress and Opportunities

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Microfluidics for Brain Endothelial-Astrocytic InteractionsPreprint

Sanapathi, J., Vipparthi, P., Sosnik, A., & Kumarasamy, M. (2023) · Preprints.org · doi:10.20944/preprints202306.1121.v1 · Cited by 3

Synthesis of Bispecific Conjugates by ADP‐Ribosyl Cyclases

Kim, S. H., Ansari, A. J., Zhang, L., Kao, G., Hoang, T. M. L., Zhang, Z., Srinivasarao, S., Katz, B. B., & Zhang, Y. (2025) · Advanced Science · doi:10.1002/advs.202518329 · Cited by 2

RNA-based therapeutics for Alzheimer’s disease and related tauopathies: challenges and opportunities

Rajbanshi, B., Brentari, I., Denti, M. A., Cummings, J. L., & Guruacharya, A. (2026) · The Journal of Prevention of Alzheimer s Disease · doi:10.1016/j.tjpad.2026.100585 · Cited by 2

Therapeutic monoclonal antibodies in the central nervous system: Pharmacokinetics, bioanalysis and clinical implications

Onyango, I. G., Woolf, N., Green, J., Stinchcomb, M., & Matveyeva, M. (2026) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2026.104350 · Cited by 2

Process Design for Bispecific Antibodies

Williams, A. J., Giese, G. S., Schaubmar, A. R., & von Hirschheydt, T. (2018) · Elsevier eBooks · doi:10.1016/b978-0-08-100623-8.00042-6 · Cited by 2

Clinical Application of Therapeutic Bispecific Antibodies

Belachew, G. T. (2023) · Biomedical Journal of Scientific & Technical Research · doi:10.26717/bjstr.2023.49.007880 · Cited by 1

Mechanisms and Methods for Evaluating Drug Delivery via Transcytosis to the Brain

Rennie, K., Yogi, Á., & Costain, W. J. (2024) · AAPS introductions in the pharmaceutical sciences · doi:10.1007/978-3-031-62604-3_2 · Cited by 2

Novel immunotherapy strategies involving matrix metalloproteinase (MMP) family

Garay-Canales, C. A., Díaz-Alvarez, L., & López-Cortés, G. I. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-822028-3.00015-7 · Cited by 2

Natural Antibodies: Protecting Role of IgM in Glioblastoma and Brain Tumours

Semwal, S., Boukherroub, R., Savvides, S. N., & Bouckaert, J. M. J. (2021) · Current Pharmaceutical Design · doi:10.2174/1381612827666210728103524 · Cited by 2

Quantitation of regional distribution of antibodies in rat brain following systemic and intra-CNS administration

Wu, S., Huang, H. W., Panchal, A., Chowdhury, E. A., & Shah, D. K. (2025) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1177/0271678x251333536 · Cited by 1

Rational design of anticancer multidrug nanosystems and their adaptation for glioblastoma treatment

Pacheco, C., Baltazar, F., Costa, B. M., & Sarmento, B. F. C. C. (2025) · Drug Delivery and Translational Research · doi:10.1007/s13346-025-02025-1 · Cited by 1

The Design Strategies and Applications of Engineered Nanoparticles for Traumatic Brain Injury

Xiang, C., Zhu, Y., Gao, X., Guo, F., He, X., Luo, W., Liu, W., & Gu, R. (2026) · International Journal of Nanomedicine · doi:10.2147/ijn.s591179 · Cited by 1

CA-IV-directed small-molecule shuttle enables targeted brain delivery of biologics

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Blood-brain barrier transport kinetics of NOTA-modified proteins: the somatropin case

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Frontiers in Clinical Drug Research - Alzheimer Disorders

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Ex vivo nanoscale abluminal mapping of putative cargo receptors at the blood-brain barrier of expanded brain capillaries

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Quantitative Algorithm-Based Paired Imaging Measurement for Antibody-Triggered Endocytosis in Cultured Cells

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Novel Technologies for Generation of Bispecific Constructs

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Drug Delivery Strategies to Cross, Target, or Bypass the Blood–Brain Barrier

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Harnessing TfR1 for Cross-Species Systemic Delivery of siRNAs to Deep Brain Regions Using Single-Domain AntibodiesPreprint

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Alzheimer's drug sneaks through blood–brain barrier

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Translational Considerations in Developing Bispecific Antibodies: What Can We Learn from Quantitative Pharmacology?

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Biotherapeutics ADME and PK/PD Principles

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Bispecifics

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Faculty Opinions recommendation of Transferrin receptor targeting by de novo sheet extension.

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Research Strategy of Anti-Transferrin Receptor Antibody Targeting Intracerebral Drug Delivery

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Faculty Opinions recommendation of Current progress in innovative engineered antibodies.

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Research Progress of “Iron Gate” Targeting Antibody

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Modification Strategies of Anti-Transferrin Receptor Antibody across the Blood-Brain Barrier

瞿, 成. (2023) · Pharmacy Information · doi:10.12677/pi.2023.123019

Novel Theranostics for Parkinson's Disease

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Transferrin receptor-mediated transport at the blood-brain barrier is elevated during early development but maintained across adult agingPreprint

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Transferrin receptor-binding blood-brain barrier shuttle enhances brain delivery and efficacy of a therapeutic anti-Aβ antibodyPreprint

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The path towards precision medicine: Next generation biotherapeutics and delivery strategies across the blood–brain barrier for the treatment of neurodegenerative diseases

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Immunotherapy and impact on tissue reservoirs

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Additional file 1 of Age, dose, and binding to TfR on blood cells influence brain delivery of a TfR-transported antibody

Faresjö, R., Sehlin, D., & Syvänen, S. (2024) · Figshare · doi:10.6084/m9.figshare.26588739

Additional file 1 of Brain pharmacokinetics of two BBB penetrating bispecific antibodies of different size

Faresjö, R., Bonvicini, G., Fang, X. T., Aguilar, X., Sehlin, D., & Syvänen, S. (2021) · Figshare · doi:10.6084/m9.figshare.14722064

Additional file 1 of ImmunoPET imaging of amyloid-beta in a rat model of Alzheimer’s disease with a bispecific, brain-penetrating fusion protein

Bonvicini, G., Syvänen, S., Andersson, K. G., Haaparanta‐Solin, M., Lopez‐Picon, F. R., & Sehlin, D. (2023) · Figshare · doi:10.6084/m9.figshare.22614299

Additional file 2 of Age, dose, and binding to TfR on blood cells influence brain delivery of a TfR-transported antibody

Faresjö, R., Sehlin, D., & Syvänen, S. (2024) · Figshare · doi:10.6084/m9.figshare.26588742

Accurate quantification of anti-drug antibodies against each unique Fab of a bispecific antibody using an ECL bridging assay

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Bispecifics: The future of therapeutic antibodies

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Trafic intracellulaire de peptide-vecteurs ciblant le récepteur au LDL pour des stratégies de délivrance ciblée d'agents thérapeutiques ou d'imagerie à travers la barrière hémato-encéphalique

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Développement d'anticorps à domaine unique comme vecteurs ciblant des récepteurs impliqués dans la transcytose et traversant la barrière hémato-encéphalique pour l'adressage d'agents d'imagerie et thérapeutiques vers le cerveau

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SIRPA suppresses integrin-dependent virus endocytosisPreprint

Yan, Z., Iyer, K. R., Li, M., Jung, K., Hu, C. T., Ansin, N., Sarute, N., Gowen, B. B., & Ross, S. R. (2026) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.64898/2026.04.17.719277

Efficacy of an Fc-silent antibody targeting the apical domain of human transferrin receptor 1 in transgenic mouse models of Junín virus infection

Li, M., Wasson, S. R., Daniels‐Wells, T. R., Westover, J. B., Candelaria, P. V., Bailey, K. W., Penichet, M. L., & Gowen, B. B. (2026) · Antiviral Research · doi:10.1016/j.antiviral.2026.106423

H-ferritin nanoparticle-mediated antibody delivery across the blood-brain barrier

Yuan, Z., Rué, L., Jaspers, T., Cuypers, M., & Dewilde, M. (2026) · Frontiers in Aging Neuroscience · doi:10.3389/fnagi.2026.1839772

Next generation medicines: Emerging approaches to drug ‘difficult to drug’ targets

Owen, D., Chaparro‐Riggers, J. F., Levengood, M. R., & Tadin‐Strapps, M. (2026) · Disease and Therapeutics · doi:10.1016/j.dist.2026.100016

pH-dependent anti-TfR1 NANOBODY® molecules deliver efficacious oligonucleotide payloads to muscle and CNS tissuesPreprint

Hoyt, E. A., Moonens, K., Rapisarda, C., Salvador, A. M., Hammond, T. R., Kharade, S. V., Mondragón-González, R., Moran, F. E. Y., Ramkumar, S., Thummapudi, J., et al. (2026) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.64898/2026.07.29.741483

Cell-to-Cell Signaling Networks at the Blood-Brain Barrier in Health and Disease

McCarty, J. H. (2026) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/atvbaha.126.324590 · Cited by 1

Modulating brain immunity with recombinant proteins

Pathikonda, S., & Arava, C. (2026) · Elsevier eBooks · doi:10.1016/b978-0-443-44631-3.00009-3

Bispecific antibodies that engage pIgR enrich in mucosa in cynomolgus monkeys

Marks, K., Shah, N., Pham, L., Chen, J., White, I., Burke, K., Garrett, P., Marella, M., Shastri, P. N., Brian, G., et al. (2026) · mAbs · doi:10.1080/19420862.2026.2743413

Translational Challenges and Strategies for Antibody Therapeutics in Glioblastoma

Zhou, Y., Li, Y., Chen, Y., Zhao, P., Wang, B., Zhu, H., Sun, H., Zhang, T., Zhang, A., Pan, Y., et al. (2026) · Current Oncology · doi:10.3390/curroncol33100619

Harnessing Functionalized Nano Lipid Carriers for Cardioprotection: Dual Drug Delivery in Focus for Precision Therapeutics

Quadri, N., Khan, I., Qadir, A., Aqil, M., & Najmi, A. K. (2026) · Drug Development and Industrial Pharmacy · doi:10.1080/03639045.2026.2751049

Transferrin' bispecific antibodies across the blood–brain barrier

Bray, N. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4522 · Cited by 16

Boosting Brain Uptake of a Therapeutic Antibody by Reducing Its Affinity for a Transcytosis Target

Yu, Y. J., Zhang, Y., Kenrick, M., Hoyte, K., Luk, W., Lu, Y., Atwal, J., Elliott, J. M., Prabhu, S., Watts, R. J., et al. (2011) · Science Translational Medicine · doi:10.1126/scitranslmed.3002230 · Cited by 794

Novel Human/Non-Human Primate Cross-Reactive Anti-Transferrin Receptor Nanobodies for Brain Delivery of Biologics

Rué, L., Jaspers, T., Degors, I. M. S., Noppen, S., Schols, D., Strooper, B. D., & Dewilde, M. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics15061748 · Cited by 32

O1‐06‐02: Enhancing antibody uptake in brain to target BACE1

Atwal, J., Yu, J., Zhang, Y., Chen, Y., Chiu, C., Meilandt, W. J., Scearce-Levie, K. A., Lu, Y., Kenrick, M., Prabhu, S., et al. (2012) · Alzheimer s & Dementia · doi:10.1016/j.jalz.2012.05.234

Transferrin receptor (TfR) trafficking determines brain uptake of TfR antibody affinity variants

Bien‐Ly, N., Yu, Y. J., Bumbaca, D., Elstrott, J., Boswell, C. A., Zhang, Y., Luk, W., Lu, Y., Dennis, M. S., Weimer, R. M., et al. (2014) · The Journal of Experimental Medicine · doi:10.1084/jem.20131660 · Cited by 356