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

A Highly Efficient Recombineering-Based Method for Generating Conditional Knockout MutationsPreprint

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

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Targeting the β secretase BACE1 for Alzheimer's disease therapy

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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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Identification of lamprey variable lymphocyte receptors that target the brain vasculature

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Passive and receptor mediated brain delivery of an anti-GFAP nanobody

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Programmable DNA Nanodevices for Applications in Neuroscience

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Brain-penetrant complement inhibition mitigates neurodegeneration in an Alzheimer’s disease mouse model

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Re-evaluation of the Blood-Brain Barrier in the Presence of Alzheimer’s Disease Pathology

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Tissue Physiology of Cynomolgus Monkeys: Cross-Species Comparison and Implications for Translational Pharmacology

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A microfluidic bone marrow chip for the safety profiling of biologics in pre-clinical drug development

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Antibody-mediated cell depletion therapies in multiple sclerosis

Mariottini, A., Muraro, P. A., & Lünemann, J. D. (2022) · Frontiers in Immunology · doi:10.3389/fimmu.2022.953649 · Cited by 22

Antibody-Based In Vivo Imaging of Central Nervous System Targets—Evaluation of a Pretargeting Approach Utilizing a TCO-Conjugated Brain Shuttle Antibody and Radiolabeled Tetrazines

Bredack, C., Edelmann, M. R., Borroni, E., Gobbi, L. B., & Honer, M. (2022) · Pharmaceuticals · doi:10.3390/ph15121445 · Cited by 21

Drugs and drug delivery systems targeting amyloid-β in Alzheimer's disease

Robinson, M. J., Lee, B. Y., & Leonenko, Z. (2015) · AIMS molecular science · doi:10.3934/molsci.2015.3.332 · Cited by 24

The effects of dose, valency, and affinity on TfR-mediated brain delivery in vivo

Bonvicini, G., Singh, S. G., Sandersjöö, L., Sehlin, D., Syvänen, S., & Andersson, K. G. (2025) · Fluids and Barriers of the CNS · doi:10.1186/s12987-025-00643-y · Cited by 24

Leveraging neonatal Fc receptor (FcRn) to enhance antibody transport across the blood brain barrier

Lafrance‐Vanasse, J., Sadekar, S., Yang, Y., Yadav, D. B., Meilandt, W. J., Wetzel-Smith, M. K., Cai, H., Crowell, S. R., Nguyen, V., Lee, V., et al. (2025) · Nature Communications · doi:10.1038/s41467-025-59447-1 · Cited by 20

Enhanced anti-angiogenetic effect of transferrin receptor-mediated delivery of VEGF-trap in a glioblastoma mouse model

Zhao, P., Anami, Y., Gao, P., Fan, X., Li, L., Tsuchikama, K., Zhang, N., & An, Z. (2022) · mAbs · doi:10.1080/19420862.2022.2057269 · Cited by 20

Novel multispecific heterodimeric antibody format allowing modular assembly of variable domain fragments

Egan, T. J., Diem, D., Weldon, R., Neumann, T., Meyer, S., & Urech, D. (2016) · mAbs · doi:10.1080/19420862.2016.1248012 · Cited by 20

Single domain antibody-based vectors in the delivery of biologics across the blood–brain barrier: a review

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Transferrin Receptor Binding BBB-Shuttle Facilitates Brain Delivery of Anti-Aβ-Affibodies

Faresjö, R., Lindberg, H., Ståhl, S., Löfblom, J., Syvänen, S., & Sehlin, D. (2022) · Pharmaceutical Research · doi:10.1007/s11095-022-03282-2 · Cited by 22

Development of a Bispecific Nanobody Targeting CD20 on B-Cell Lymphoma Cells and CD3 on T Cells

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Improved assembly of bispecific antibodies from knob and hole half‐antibodies

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A D ‐Peptide Ligand of Nicotine Acetylcholine Receptors for Brain‐Targeted Drug Delivery

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Narcolepsy and influenza vaccination—the inappropriate awakening of immunity

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Non-Human Primate Blood–Brain Barrier and In Vitro Brain Endothelium: From Transcriptome to the Establishment of a New Model

Chaves, C., Do, T.-M., Cegarra, C., Roudières, V., Tolou, S., Thill, G., Rocher, C., Didier, M., & Lesuisse, D. (2020) · Pharmaceutics · doi:10.3390/pharmaceutics12100967 · Cited by 18

Enabling the next steps in cancer immunotherapy: from antibody-based bispecifics to multispecifics, with an evolving role for bioconjugation chemistry

Thoreau, F., & Chudasama, V. (2021) · RSC Chemical Biology · doi:10.1039/d1cb00082a · Cited by 17

Ion Mobility-Mass Spectrometry and Collision-Induced Unfolding of Designed Bispecific Antibody Therapeutics

Villafuerte-Vega, R. C., Li, H. W., Slaney, T. R., Chennamsetty, N., Chen, G., Tao, L., & Ruotolo, B. T. (2023) · Analytical Chemistry · doi:10.1021/acs.analchem.3c00344 · Cited by 19

Host receptor-targeted therapeutic approach to counter pathogenic New World mammarenavirus infections

Hickerson, B. T., Daniels‐Wells, T. R., Payés, C., Clark, L. E., Candelaria, P. V., Bailey, K. W., Sefing, E. J., Zink, S., Ziegenbein, J. C., Abraham, J., et al. (2022) · Nature Communications · doi:10.1038/s41467-021-27949-3 · Cited by 17

Reducing neonatal Fc receptor binding enhances clearance and brain-to-blood ratio of TfR-delivered bispecific amyloid-β antibody

Schlein, E., Andersson, K. G., Dallas, T. D., Syvänen, S., & Sehlin, D. (2024) · mAbs · doi:10.1080/19420862.2024.2339337 · Cited by 18

Engineered Antibodies to Improve Efficacy against Neurodegenerative Disorders

Niazi, S. K., Mariam, Z., & Magoola, M. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25126683 · Cited by 16

Transferrin' bispecific antibodies across the blood–brain barrier

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

Assessing central nervous system drug delivery

Hammarlund‐Udenaes, M., & Loryan, I. (2025) · Expert Opinion on Drug Delivery · doi:10.1080/17425247.2025.2462767 · Cited by 17

Ligand-cascading nano-delivery devices to enable multiscale targeting of anti-neurodegenerative therapeutics

Mullis, A. S., Schlichtmann, B. W., Narasimhan, B., Cademartiri, R., & Mallapragada, S. K. (2018) · Biomedical Materials · doi:10.1088/1748-605x/aaa778 · Cited by 15

Treating brain diseases using systemic parenterally-administered protein therapeutics: Dysfunction of the brain barriers and potential strategies

Zaghmi, A., Drouin‐Ouellet, J., Brambilla, D., & Gauthier, M. A. (2020) · Biomaterials · doi:10.1016/j.biomaterials.2020.120461 · Cited by 17

Towards a translational physiologically-based pharmacokinetic (PBPK) model for receptor-mediated transcytosis of anti-transferrin receptor monoclonal antibodies in the central nervous system

Chang, H.-Y., Wu, S., Chowdhury, E. A., & Shah, D. K. (2022) · Journal of Pharmacokinetics and Pharmacodynamics · doi:10.1007/s10928-021-09800-w · Cited by 16

Mucopolysaccharidoses and the blood–brain barrier

Sahin, O., Thompson, H. P., Goodman, G. W., Li, J., & Urayama, A. (2022) · Fluids and Barriers of the CNS · doi:10.1186/s12987-022-00373-5 · Cited by 16

Homogeneously modified immunoglobulin domains for therapeutic application

Liu, T., Du, J., Luo, X., Schultz, P. G., & Wang, F. (2015) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2015.06.007 · Cited by 15

A novel function of N-linked glycoproteins, alpha-2-HS-glycoprotein and hemopexin: Implications for small molecule compound-mediated neuroprotection

Kanno, T., Yasutake, K., Tanaka, K., Hadano, S., & Ikeda, J. (2017) · PLoS ONE · doi:10.1371/journal.pone.0186227 · Cited by 15

Camelid heavy chain only antibody fragment domain against β‐site of amyloid precursor protein cleaving enzyme 1 inhibits β‐secretase activity in vitro and in vivo

Dorresteijn, B., Rotman, M., Faber, D., Schravesande, R., Suidgeest, E., van der Weerd, L., van der Maarel, S. M., Verrips, C. T., & Khattabi, M. E. (2015) · FEBS Journal · doi:10.1111/febs.13367 · Cited by 15

Immunity in Alzheimer’s disease: From mechanisms to therapies

Chen, X., Holtzman, D. M., & Colonna, M. (2026) · Immunity · doi:10.1016/j.immuni.2026.02.004 · Cited by 18

Increasing brain half-life of antibodies by additional binding to myelin oligodendrocyte glycoprotein, a CNS specific protein

Cuypers, M., Jaspers, T., Clerckx, J., Leekens, S., Cawthorne, C., Bormans, G. M., Cleeren, F., Geukens, N., Strooper, B. D., & Dewilde, M. (2025) · Fluids and Barriers of the CNS · doi:10.1186/s12987-025-00624-1 · Cited by 15

Receptor-mediated transportation through BBB

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A new technology for increasing therapeutic protein levels in the brain over extended periods

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Anti-α-synuclein c-terminal antibodies block PFF uptake and accumulation of phospho-synuclein in preclinical models of Parkinson's disease

Brendza, R. P., Gao, X., Stark, K. L., Lin, H., Lee, S.-H., Hu, C., Cai, H., DiCara, D. M., Hsiao, Y.-C., Ngu, H., et al. (2022) · Neurobiology of Disease · doi:10.1016/j.nbd.2022.105969 · Cited by 14

Monoclonal Antibodies: From Structure to Therapeutic Application

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Fine-tuning bispecific therapeutics

Lim, S. I. (2020) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2020.107582 · Cited by 14

The Evolving Applications of Bispecific Antibodies: Reaping the Harvest of Early Sowing and Planting New Seeds

Ellerman, D. A. (2024) · BioDrugs · doi:10.1007/s40259-024-00691-0 · Cited by 13

Targeting β-Secretase (BACE) for the Treatment of Alzheimer’s Disease

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An explicitly designed paratope of amyloid-β prevents neuronal apoptosis in vitro and hippocampal damage in rat brain

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Developing Trojan horses to induce, diagnose and suppress Alzheimer’s pathology

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Small-Sized Co-Polymers for Targeted Delivery of Multiple Imaging and Therapeutic Agents

Ljubimova, J. Y., Ramesh, A., Israel, L. L., & Holler, E. (2021) · Nanomaterials · doi:10.3390/nano11112996 · Cited by 13

Engineering anti-amyloid antibodies with transferrin receptor targeting improves brain biodistribution and mitigates ARIAPreprint

Pizzo, M. E., Plowey, E. D., Khoury, N., Kwan, W., Abettan, J., DeVos, S. L., Discenza, C. B., Earr, T., Joy, D. A., Lye‐Barthel, M., et al. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.07.26.604664 · Cited by 13

Balancing brain exposure, pharmacokinetics and safety of transferrin receptor antibodies for delivery of neuro-therapeutics

Smith, B. A., Meeks, C., Murray-Brown, I., McCarthy, E. A., Julian, M. C., Arndt, J. W., Stewart, M., Spilker, K. A., D’Lima, N., Dolníková, J., et al. (2025) · mAbs · doi:10.1080/19420862.2025.2592422 · Cited by 16

Visualizing advances in the future of primate neuroscience research

Janssen, P., Isa, T., Lanciego, J. L., Leech, K., Logothetis, N. K., Poo, M., & Mitchell, A. S. (2022) · Current Research in Neurobiology · doi:10.1016/j.crneur.2022.100064 · Cited by 12

Lowering the affinity of single-chain monovalent BBB shuttle scFc-scFv8D3 prolongs its half-life and increases brain concentration

de la Rosa, A., Metzendorf, N. G., Efverström, J., Godec, A., Sehlin, D., Morrison, J. I., & Hultqvist, G. (2024) · Neurotherapeutics · doi:10.1016/j.neurot.2024.e00492 · Cited by 16

Viral Infection of the Central Nervous System Exacerbates Interleukin-10 Receptor Deficiency-Mediated Colitis in SJL Mice

Uhde, A., Herder, V., Khan, M. A., Ciurkiewicz, M., Schaudien, D., Teich, R., Floess, S., Baumgärtner, W., Huehn, J., & Beineke, A. (2016) · PLoS ONE · doi:10.1371/journal.pone.0161883 · Cited by 13

Construction of a novel bispecific fusion protein to enhance targeting for pancreatic cancer imaging

Wang, Q., Yan, H., Wang, Z., Li, Z., Li, D., Li, Z., Wang, K., Tian, J., & Zhao, X. (2020) · Biomaterials · doi:10.1016/j.biomaterials.2020.120161 · Cited by 11

Translational roadmap of BBB-targeted nanoparticle strategies for neuroregenerative therapy in neurodegenerative diseases

Lee, S., Lee, J., & Lee, K. (2026) · Biomaterials Science · doi:10.1039/d5bm01582k · Cited by 11

Systemic Treatment with siRNA Targeting Gamma-Secretase Activating Protein Inhibits Amyloid-β Accumulation in Alzheimer’s Disease

Kim, S., Ullah, I., Beloor, J., Chung, K., Kim, J.-K., Yi, Y., Kang, E., Yun, G., Heo, S., Pyun, S.-H., et al. (2024) · Biomaterials Research · doi:10.34133/bmr.0027 · Cited by 11

High-resolution Confocal Imaging of the Blood-brain Barrier: Imaging, 3D Reconstruction, and Quantification of Transcytosis

Villaseñor, R., & Collin, L. (2017) · Journal of Visualized Experiments · doi:10.3791/56407 · Cited by 15

IgG-like Bispecific Antibody CD3×EpCAM Generated by Split Intein Against Colorectal Cancer

Wang, L., Qiao, Y., Zong, H., Han, L., Ke, Y., Pan, Z., Chen, J., Lu, J., Li, J., Ying, T., et al. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.803059 · Cited by 11

Modelling a Human Blood-Brain Barrier Co-Culture Using an Ultrathin Silicon Nitride Membrane-Based Microfluidic Device

Hudecz, D., McCloskey, M. C., Vergo, S. B., Christensen, S., McGrath, J. L., & Nielsen, M. S. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24065624 · Cited by 12

Circumventing the blood–brain barrier

Shen, H. H. (2017) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1716187114 · Cited by 12

Transferrin receptor-mediated transport at the blood-brain barrier is elevated during early development and maintained across aging and in an Alzheimer’s mouse model

Torres, V. O., Pizzo, M. E., Chan, D., Dugas, J. C., Huynh, D., Joy, D. A., Liang, E., Sarrafha, L., Becerra, I. A., Chau, R., et al. (2025) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1177/0271678x251361997 · Cited by 13

A brain-penetrant bispecific antibody lowers oligomeric alpha-synuclein and activates microglia in a mouse model of alpha-synuclein pathology

Sehlin, D., Roshanbin, S., Zachrisson, O., Ingelsson, M., & Syvänen, S. (2024) · Neurotherapeutics · doi:10.1016/j.neurot.2024.e00510 · Cited by 11

Immunotherapeutics to Treat HIV in the Central Nervous System

Kapoor, A. K., & Tan, C. S. (2020) · Current HIV/AIDS Reports · doi:10.1007/s11904-020-00519-w · Cited by 10

Subcellular trafficking and transcytosis efficacy of different receptor types for therapeutic antibody delivery at the blood‒brain barrier

Holst, M. R., de Wit, N. M., Ozgür, B., Brachner, A., Hyldig, K., Appelt‐Menzel, A., Sleven, H., Cader, M. Z., de Vries, H. E., Neuhaus, W., et al. (2023) · Fluids and Barriers of the CNS · doi:10.1186/s12987-023-00480-x · Cited by 12

Microfluidics for brain endothelial cell-astrocyte interactions

Sanapathi, J., Vipparthi, P., Mishra, S., Sosnik, A., & Kumarasamy, M. (2023) · Organs-on-a-Chip · doi:10.1016/j.ooc.2023.100033 · Cited by 11

Amyloid-Directed Antibodies: Past, Present, and Future

Noorda, K., Noorda, K. J., Sabbagh, M. N., Bertelson, J. A., Singer, J., & Decourt, B. (2024) · Journal of Alzheimer s Disease · doi:10.3233/jad-240189 · Cited by 9

Evaluation of Tetrazine Tracers for Pretargeted Imaging within the Central Nervous System

Edelmann, M. R., Bredack, C., Belli, S., Mohr, P., Imhoff, M., Reggiani, F., Kusznir, E. A., Rufer, A. C., Holt, D. P., Valentine, H., et al. (2023) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.3c00385 · Cited by 9

Brain Delivery of Therapeutics via Transcytosis: Types and Mechanisms of Vesicle-Mediated Transport Across the BBB

Haqqani, A. S., & Stanimirovic, D. B. (2022) · AAPS advances in the pharmaceutical sciences series · doi:10.1007/978-3-030-88773-5_3 · Cited by 9

Targeting cerebral diseases with enhanced delivery of therapeutic proteins across the blood-brain barrier

Bao, Y., & Lu, W. (2023) · Expert Opinion on Drug Delivery · doi:10.1080/17425247.2023.2193390 · Cited by 10

An allosteric antibody to the leptin receptor reduces body weight and reverses the diabetic phenotype in the Lepob/Lepob mouse

Bhaskar, V., Goldfine, I. D., Gerstner, R. B., Michelson, K. S., Tran, C., Nonet, G. H., Bohmann, D. J., Pongo, E., Zhao, J., Horwitz, A. H., et al. (2016) · Obesity · doi:10.1002/oby.21539 · Cited by 9

Blood-brain barrier transport using a high-affinity, brain-selective VNAR (Variable Domain of New Antigen Receptor) antibody targeting transferrin receptor 1Preprint

Stocki, P., Szary, J., Rasmussen, C. L. M., Demydchuk, M., Northall, L., Logan, D. B., Gauhar, A., Thei, L., Moos, T., Walsh, F. S., et al. (2019) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/816900 · Cited by 9

Mechanism-based pharmacokinetic and pharmacodynamic modeling for bispecific antibodies: challenges and opportunities

Niu, J., Wang, W., & Ouellet, D. (2023) · Expert Review of Clinical Pharmacology · doi:10.1080/17512433.2023.2257136 · Cited by 8

Restoration of virulence in the attenuated Candid#1 vaccine virus requires reversion at both positions 168 and 427 in the envelope glycoprotein GPC

Nunberg, J. H., Westover, J. B., York, J., Jung, K., Bailey, K. W., Boardman, K. M., Li, M., Furnell, R. S., Wasson, S. R., Murray, J. S., et al. (2024) · Journal of Virology · doi:10.1128/jvi.00112-24 · Cited by 8

Functionalized Nanoparticles: A Promising Approach for Effective Management of Alzheimer’s Disease

Bogadi, S., Bhaskaran, M., Ravichandran, V., Nesamony, J., Selvam, C., Kuppusamy, G., Prakash, G., Karri, V. V. S. R., Mallick, S., Farahim, F., et al. (2025) · Molecular Neurobiology · doi:10.1007/s12035-025-04917-2 · Cited by 10

Translational minimal physiologically based pharmacokinetic model for transferrin receptor-mediated brain delivery of antibodies

Muliaditan, M., van Steeg, T. J., Avery, L. B., Sun, W., Hammond, T. R., Hijdra, D., Choi, S.-L., Pillai, N., Leksa, N. C., & Mavroudis, P. D. (2025) · mAbs · doi:10.1080/19420862.2025.2515414 · Cited by 8

Novel single-domain antibodies targeting a unique transferrin receptor 1 epitope for cross-species delivery of drugs in the central nervous system

David, M., Cohen, R., Beuzelin, D., Ferracci, G., Cresci, M., Faucon, A., Abouzid, K., Godefroy, G., Masse, M., Mechioukhi, Y., et al. (2025) · Journal of Controlled Release · doi:10.1016/j.jconrel.2025.114344 · Cited by 9

Progress in novel delivery technologies to improve efficacy of therapeutic antibodies

Sun, W., Wu, Y., & Ying, T. (2024) · Antiviral Research · doi:10.1016/j.antiviral.2024.105867 · Cited by 8

Plasma membrane damage limits cytoplasmic delivery by conventional cell penetrating peptides

Polderdijk, S. G. I., Limzerwala, J. F., & Spiess, C. (2024) · PLoS ONE · doi:10.1371/journal.pone.0305848 · Cited by 7

High-affinity transferrin receptor binding improves brain delivery of bispecific antibodies at tracer dose

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Antibody Engineering for Receptor-Mediated Transcytosis Across the Blood–Brain Barrier

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