Strategies and challenges for the next generation of antibody–drug conjugates

PD-1 Blockade in Tumors with Mismatch-Repair Deficiency

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PD-1 Blockade with Nivolumab in Relapsed or Refractory Hodgkin's Lymphoma

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Microtubule-binding agents: a dynamic field of cancer therapeutics

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Site-specific conjugation of a cytotoxic drug to an antibody improves the therapeutic index

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Effects of Drug Loading on the Antitumor Activity of a Monoclonal Antibody Drug Conjugate

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DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1

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Conjugation site modulates the in vivo stability and therapeutic activity of antibody-drug conjugates

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Antibody–Drug Conjugates: An Emerging Concept in Cancer Therapy

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THE COVALENT STRUCTURE OF AN ENTIRE γG IMMUNOGLOBULIN MOLECULE

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Approval summary: gemtuzumab ozogamicin in relapsed acute myeloid leukemia.

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Strategies and challenges for the next generation of therapeutic antibodies

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Novel antibody-antibiotic conjugate eliminates intracellular S. aureus

Lehar, S. M., Pillow, T., Xu, M., Staben, L., Kajihara, K. K., Vandlen, R., DePalatis, L., Raab, H., Hazenbos, W. L., Hiroshi Morisaki, J., et al. (2015) · Nature · doi:10.1038/nature16057 · Cited by 838 · see citing works

The discovery and development of brentuximab vedotin for use in relapsed Hodgkin lymphoma and systemic anaplastic large cell lymphoma

Senter, P. D., & Sievers, E. L. (2012) · Nature Biotechnology · doi:10.1038/nbt.2289 · Cited by 767 · see citing works

Brentuximab vedotin as consolidation therapy after autologous stem-cell transplantation in patients with Hodgkin's lymphoma at risk of relapse or progression (AETHERA): a randomised, double-blind, placebo-controlled, phase 3 trial

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Site-specific antibody drug conjugates for cancer therapy

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Antibody–drug conjugates: targeted drug delivery for cancer

Alley, S. C., Okeley, N. M., & Senter, P. D. (2010) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2010.06.170 · Cited by 653 · see citing works

A DLL3-targeted antibody-drug conjugate eradicates high-grade pulmonary neuroendocrine tumor-initiating cells in vivo

Saunders, L. R., Bankovich, A. J., Anderson, W. C., Aujay, M. A., Bheddah, S., Black, K., Desai, R. C., Escarpe, P. A., Hampl, J., Laysang, A., et al. (2015) · Science Translational Medicine · doi:10.1126/scitranslmed.aac9459 · Cited by 600 · see citing works

Characterization of Therapeutic Antibodies and Related Products

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Rovalpituzumab tesirine, a DLL3-targeted antibody-drug conjugate, in recurrent small-cell lung cancer: a first-in-human, first-in-class, open-label, phase 1 study

Rudin, C. M., Pietanza, M. C., Bauer, T. M., Ready, N., Morgensztern, D., Glisson, B. S., Byers, L. A., Johnson, M. L., Burris, H. A., Robert, F., et al. (2016) · The Lancet Oncology · doi:10.1016/s1470-2045(16)30565-4 · Cited by 572 · see citing works

Reducing hydrophobicity of homogeneous antibody-drug conjugates improves pharmacokinetics and therapeutic index

Lyon, R. P., Bovee, T. D., Doronina, S. O., Burke, P., Hunter, J. H., Neff‐LaFord, H. D., Jonas, M., Anderson, M. E., Setter, J. R., & Senter, P. D. (2015) · Nature Biotechnology · doi:10.1038/nbt.3212 · Cited by 564 · see citing works

Ado-trastuzumab Emtansine (T-DM1): An Antibody–Drug Conjugate (ADC) for HER2-Positive Breast Cancer

Lambert, J. M., & Chari, R. V. J. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm500766w · Cited by 550 · see citing works

Trastuzumab-DM1 (T-DM1) retains all the mechanisms of action of trastuzumab and efficiently inhibits growth of lapatinib insensitive breast cancer

Junttila, T. T., Li, G., Parsons, K. L., Phillips, G. D. L., & Sliwkowski, M. X. (2010) · Breast Cancer Research and Treatment · doi:10.1007/s10549-010-1090-x · Cited by 539 · see citing works

Site-Specific Antibody–Drug Conjugates: The Nexus of Bioorthogonal Chemistry, Protein Engineering, and Drug Development

Agarwal, P., & Bertozzi, C. (2014) · Bioconjugate chemistry · doi:10.1021/bc5004982 · Cited by 534 · see citing works

Location Matters: Site of Conjugation Modulates Stability and Pharmacokinetics of Antibody Drug Conjugates

Strop, P., Liu, S., Dorywalska, M., Delaria, K., Dushin, R. G., Tran, T.-T., Ho, W.-H., Farias, S., Casas, M. G., Abdiche, Y. N., et al. (2013) · Chemistry & Biology · doi:10.1016/j.chembiol.2013.01.010 · Cited by 507 · see citing works

Trop-2 is a novel target for solid cancer therapy with sacituzumab govitecan (IMMU-132), an antibody-drug conjugate (ADC)*

Goldenberg, D. M., Cardillo, T. M., Govindan, S. V., Rossi, E. A., & Sharkey, R. M. (2015) · Oncotarget · doi:10.18632/oncotarget.4318 · Cited by 500 · see citing works

Effects of antibody, drug and linker on the preclinical and clinical toxicities of antibody-drug conjugates

Donaghy, H. (2016) · mAbs · doi:10.1080/19420862.2016.1156829 · Cited by 499 · see citing works

Novel anti–B-cell maturation antigen antibody-drug conjugate (GSK2857916) selectively induces killing of multiple myeloma

Tai, Y., Mayes, P. A., Acharya, C., Zhong, M. Y., Cea, M., Cagnetta, A., Craigen, J. L., Yates, J. W., Gliddon, L., Fieles, W. E., et al. (2014) · Blood · doi:10.1182/blood-2013-10-535088 · Cited by 485 · see citing works

Antibody-Drug Conjugates Designed to Eradicate Tumors with Homogeneous and Heterogeneous Expression of the Target Antigen

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Antibody–drug conjugates: current status and future directions

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Self-hydrolyzing maleimides improve the stability and pharmacological properties of antibody-drug conjugates

Lyon, R. P., Setter, J. R., Bovee, T. D., Doronina, S. O., Hunter, J. H., Anderson, M. E., Balasubramanian, C., Duniho, S. M., Leiske, C. I., Li, F., et al. (2014) · Nature Biotechnology · doi:10.1038/nbt.2968 · Cited by 465 · see citing works

Long-Term Stabilization of Maleimide–Thiol Conjugates

Fontaine, S. D., Reid, R. R., Robinson, L., Ashley, G. W., & Santi, D. V. (2014) · Bioconjugate Chemistry · doi:10.1021/bc5005262 · Cited by 431 · see citing works

Potent antibody drug conjugates for cancer therapy

Senter, P. D. (2009) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2009.03.023 · Cited by 403 · see citing works

A Biparatopic HER2-Targeting Antibody-Drug Conjugate Induces Tumor Regression in Primary Models Refractory to or Ineligible for HER2-Targeted Therapy

Li, J. Y., Perry, S. R., Muniz-Medina, V. M., Wang, X., Wetzel, L. K., Rebelatto, M. C., Hinrichs, M. J., Bezabeh, B. Z., Fleming, R. L., Dimasi, N., et al. (2016) · Cancer Cell · doi:10.1016/j.ccell.2015.12.008 · Cited by 400 · see citing works

Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate

Okeley, N. M., Miyamoto, J. B., Zhang, X., Sanderson, R. J., Benjamin, D. R., Sievers, E. L., Senter, P. D., & Alley, S. C. (2010) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-09-2069 · Cited by 395 · see citing works

SGN-CD33A: a novel CD33-targeting antibody–drug conjugate using a pyrrolobenzodiazepine dimer is active in models of drug-resistant AML

Sutherland, M. K., Walter, R. B., Jeffrey, S. C., Burke, P., Yu, C., Kostner, H., Stone, I. J., Ryan, M. C., Sussman, D. R., Lyon, R. P., et al. (2013) · Blood · doi:10.1182/blood-2013-03-491506 · Cited by 390 · see citing works

Brentuximab Vedotin (SGN-35)

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Production of Site-Specific Antibody–Drug Conjugates Using Optimized Non-Natural Amino Acids in a Cell-Free Expression System

Zimmerman, E. S., Heibeck, T. H., Gill, A., Li, X., Murray, C. J., Madlansacay, M. R., Tran, C., Uter, N. T., Yin, G., Rivers, P. J., et al. (2014) · Bioconjugate Chemistry · doi:10.1021/bc400490z · Cited by 367 · see citing works

Trastuzumab emtansine (T-DM1) renders HER2 + breast cancer highly susceptible to CTLA-4/PD-1 blockade

Müller, P., Kreuzaler, M., Khan, T. A., Thommen, D. S., Martin, K., Glatz, K., Savic, S., Harbeck, N., Nitz, U. A., Gluz, O., et al. (2015) · Science Translational Medicine · doi:10.1126/scitranslmed.aac4925 · Cited by 351 · see citing works

First-in-Human Trial of a Novel Anti-Trop-2 Antibody-SN-38 Conjugate, Sacituzumab Govitecan, for the Treatment of Diverse Metastatic Solid Tumors

Starodub, A., Ocean, A. J., Shah, M. A., Guarino, M. J., Picozzi, V. J., Vahdat, L. T., Thomas, S. S., Govindan, S. V., Maliakal, P. P., Wegener, W. A., et al. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-3321 · Cited by 340 · see citing works

Safety and activity of the anti-CD79B antibody–drug conjugate polatuzumab vedotin in relapsed or refractory B-cell non-Hodgkin lymphoma and chronic lymphocytic leukaemia: a phase 1 study

Palanca-Wessels, M. C., Czuczman, M. S., Salles, G., Assouline, S. E., Sehn, L. H., Flinn, I. W., Patel, M. R., Sangha, R. S., Hagenbeek, A., Advani, R. H., et al. (2015) · The Lancet Oncology · doi:10.1016/s1470-2045(15)70128-2 · Cited by 337 · see citing works

A general approach to site-specific antibody drug conjugates

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Therapeutic IgG4 antibodies engage in Fab-arm exchange with endogenous human IgG4 in vivo

Labrijn, A. F., Buijsse, A. O., van den Bremer, E. T. J., Verwilligen, A., Bleeker, W. K., Thorpe, S. J., Killestein, J., Polman, C. H., Aalberse, R. C., Schuurman, J., et al. (2009) · Nature Biotechnology · doi:10.1038/nbt.1553 · Cited by 297 · see citing works

Maturing antibody–drug conjugate pipeline hits 30

Mullard, A. (2013) · Nature Reviews Drug Discovery · doi:10.1038/nrd4009 · Cited by 295 · see citing works

A new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs

Prota, A. E., Bargsten, K., Díaz, J. F., Marsh, M., Cuevas, C., Liniger, M., Neuhaus, C., Andreu, J. M., Altmann, K., & Steinmetz, M. O. (2014) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1408124111 · Cited by 285 · see citing works

Tumor-Specific Activation of an EGFR-Targeting Probody Enhances Therapeutic Index

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Limitations of radiolabeled monoclonal antibodies for localization of human neoplasms.

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Chemoenzymatic Conjugation of Toxic Payloads to the Globally Conserved N-Glycan of Native mAbs Provides Homogeneous and Highly Efficacious Antibody–Drug Conjugates

Geel, R. V., Wijdeven, M. A., Heesbeen, R., Verkade, J. M. M., Wasiel, A. A., van Berkel, S. S., & van Delft, F. L. (2015) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.5b00224 · Cited by 282 · see citing works

Tumor Cells Chronically Treated with a Trastuzumab–Maytansinoid Antibody–Drug Conjugate Develop Varied Resistance Mechanisms but Respond to Alternate Treatments

Loganzo, F., Tan, X., Sung, M. S., Jin, G., Myers, J. S., Melamud, E., Wang, F., Diesl, V., Follettie, M. T., Musto, S., et al. (2015) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-14-0862 · Cited by 277 · see citing works

From Anthramycin to Pyrrolobenzodiazepine (PBD)‐Containing Antibody–Drug Conjugates (ADCs)

Mantaj, J., Jackson, P. J. M., Rahman, K. M., & Thurston, D. E. (2017) · Angewandte Chemie International Edition · doi:10.1002/anie.201510610 · Cited by 262 · see citing works

A plug-and-play approach to antibody-based therapeutics via a chemoselective dual click strategy

Maruani, A., Smith, M. E. B., Miranda, E., Chester, K. A., Chudasama, V., & Caddick, S. (2015) · Nature Communications · doi:10.1038/ncomms7645 · Cited by 256 · see citing works

Tumor Delivery and In Vivo Processing of Disulfide-Linked and Thioether-Linked Antibody−Maytansinoid Conjugates

Erickson, H. K., Widdison, W. C., Mayo, M. F., Whiteman, K., Audette, C., Wilhelm, S. D., & Singh, R. (2010) · Bioconjugate Chemistry · doi:10.1021/bc900315y · Cited by 246 · see citing works

A Potent Anti-CD70 Antibody–Drug Conjugate Combining a Dimeric Pyrrolobenzodiazepine Drug with Site-Specific Conjugation Technology

Jeffrey, S. C., Burke, P., Lyon, R. P., Meyer, D. W., Sussman, D. R., Anderson, M. E., Hunter, J. H., Leiske, C. I., Miyamoto, J. B., Nicholas, N. D., et al. (2013) · Bioconjugate Chemistry · doi:10.1021/bc400217g · Cited by 245 · see citing works

Cell killing by antibody–drug conjugates

Kovtun, Y., & Goldmacher, V. S. (2007) · Cancer Letters · doi:10.1016/j.canlet.2007.04.010 · Cited by 244 · see citing works

Engineered antibody-drug conjugates with defined sites and stoichiometries of drug attachment

McDonagh, C. F., Turcott, E., Westendorf, L., et al. (2006) · Protein Engineering Design and Selection · doi:10.1093/protein/gzl013 · Cited by 243 · see citing works

TP53 loss creates therapeutic vulnerability in colorectal cancer

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IMGN853, a Folate Receptor-α (FRα)–Targeting Antibody–Drug Conjugate, Exhibits Potent Targeted Antitumor Activity against FRα-Expressing Tumors

Ab, O., Whiteman, K. R., Bartle, L. M., Sun, X., Singh, R., Tavares, D., LaBelle, A., Payne, G. M., Lutz, R. J., Pinkas, J., et al. (2015) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-14-1095 · Cited by 239 · see citing works

Mechanisms of Resistance to Antibody–Drug Conjugates

Loganzo, F., Sung, M. S., & Gerber, H. (2016) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-16-0408 · Cited by 237 · see citing works

Anetumab Ravtansine: A Novel Mesothelin-Targeting Antibody–Drug Conjugate Cures Tumors with Heterogeneous Target Expression Favored by Bystander Effect

Golfier, S., Kopitz, C., Kahnert, A., Heisler, I., Schatz, C., Stelte-Ludwig, B., Mayer-Bartschmid, A., Unterschemmann, K., Bruder, S., Linden, L., et al. (2014) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-13-0926 · Cited by 232 · see citing works

Sortase Enzyme-Mediated Generation of Site-Specifically Conjugated Antibody Drug Conjugates with High In Vitro and In Vivo Potency

Beerli, R. R., Hell, T., Merkel, A. S., & Grawunder, U. (2015) · PLoS ONE · doi:10.1371/journal.pone.0131177 · Cited by 227 · see citing works

Design, Synthesis, and Evaluation of Linker-Duocarmycin Payloads: Toward Selection of HER2-Targeting Antibody–Drug Conjugate SYD985

Elgersma, R. C., Coumans, R. G. E., Huijbregts, T., Menge, W. M. P. B., Joosten, J., Spijker, H. J., de Groot, F. M. H., van der Lee, M. M. C., Ubink, R., van den Dobbelsteen, D. J., et al. (2015) · Molecular Pharmaceutics · doi:10.1021/mp500781a · Cited by 223 · see citing works

Site-Specific Antibody–Drug Conjugation through Glycoengineering

Zhou, Q., Stefano, J. E., Manning, C. M., Kyazike, J., Chen, B., Gianolio, D. A., Park, A., Busch, M., Jaworski, J. A., Zheng, X., et al. (2014) · Bioconjugate Chemistry · doi:10.1021/bc400505q · Cited by 223 · see citing works

Aldehyde Tag Coupled with HIPS Chemistry Enables the Production of ADCs Conjugated Site-Specifically to Different Antibody Regions with Distinct in Vivo Efficacy and PK Outcomes

Drake, P. M., Albers, A. E., Baker, J., Bañas, S., Barfield, R. M., Bhat, A., de Hart, G. W., Garofalo, A. W., Holder, P. G., Jones, L. C., et al. (2014) · Bioconjugate Chemistry · doi:10.1021/bc500189z · Cited by 214 · see citing works

Marketing approval of mogamulizumab

Beck, A., & Reichert, J. M. (2012) · mAbs · doi:10.4161/mabs.20996 · Cited by 211 · see citing works

Microtubule-Depolymerizing Agents Used in Antibody–Drug Conjugates Induce Antitumor Immunity by Stimulation of Dendritic Cells

Müller, P., Martin, K., Theurich, S., Schreiner, J., Savic, S., Terszowski, G., Lardinois, D., Heinzelmann-Schwarz, V. A., Schlaak, M. S., Kvasnicka, H. M., et al. (2014) · Cancer Immunology Research · doi:10.1158/2326-6066.cir-13-0198 · Cited by 206 · see citing works

The Monoclonal Antibody nBT062 Conjugated to Cytotoxic Maytansinoids Has Selective Cytotoxicity Against CD138-Positive Multiple Myeloma Cells In vitro and In vivo

Ikeda, H., Hideshima, T., Fulciniti, M., Lutz, R. J., Yasui, H., Okawa, Y., Kiziltepe, T., Vallet, S., Pozzi, S., Santo, L., et al. (2009) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-08-2867 · Cited by 203 · see citing works

The Preclinical Profile of the Duocarmycin-Based HER2-Targeting ADC SYD985 Predicts for Clinical Benefit in Low HER2-Expressing Breast Cancers

van der Lee, M. M. C., Groothuis, P. G., Ubink, R., van der Vleuten, M. A. J., van Achterberg, T. A. E., Loosveld, E. M., Damming, D., Jacobs, D. C. H., Rouwette, M., Egging, D. F., et al. (2015) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-14-0881-t · Cited by 201 · see citing works

Mild Method for Succinimide Hydrolysis on ADCs: Impact on ADC Potency, Stability, Exposure, and Efficacy

Tumey, L. N., Charati, M. B., He, T., et al. (2014) · Bioconjugate Chemistry · doi:10.1021/bc500357n · Cited by 193 · see citing works

EMERGE: A Randomized Phase II Study of the Antibody-Drug Conjugate Glembatumumab Vedotin in Advanced Glycoprotein NMB–Expressing Breast Cancer

Yardley, D. A., Weaver, R., Melisko, M., Saleh, M. N., Arena, F. P., Forero, A., Cigler, T., Stopeck, A., Citrin, D. L., Oliff, I. A., et al. (2015) · Journal of Clinical Oncology · doi:10.1200/jco.2014.56.2959 · Cited by 190 · see citing works

Combining antibody–drug conjugates and immune-mediated cancer therapy: What to expect?

Gerber, H., Sapra, P., Loganzo, F., & May, C. (2015) · Biochemical Pharmacology · doi:10.1016/j.bcp.2015.12.008 · Cited by 186 · see citing works

Site-specific conjugation improves therapeutic index of antibody drug conjugates with high drug loading

Strop, P., Delaria, K., Foletti, D. L., et al. (2015) · Nature Biotechnology · doi:10.1038/nbt.3274 · Cited by 184 · see citing works

Innovative Native MS Methodologies for Antibody Drug Conjugate Characterization: High Resolution Native MS and IM-MS for Average DAR and DAR Distribution Assessment

Debaene, F., Bœuf, A., Wagner‐Rousset, E., Colas, O., Ayoub, D., Corvaı̈a, N., DORSSELAER, A. V., Beck, A., & Cianférani, S. (2014) · Analytical Chemistry · doi:10.1021/ac502593n · Cited by 182 · see citing works

Enhanced Delivery of SN-38 to Human Tumor Xenografts with an Anti-Trop-2–SN-38 Antibody Conjugate (Sacituzumab Govitecan)

Sharkey, R. M., McBride, W. J., Cardillo, T. M., Govindan, S. V., Wang, Y., Rossi, E. A., Chang, C., & Goldenberg, D. M. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-15-0670 · Cited by 173 · see citing works

Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads

Nakada, T., Masuda, T., Naito, H., Yoshida, M., Ashida, S., Morita, K., Miyazaki, H., Kasuya, Y., Ogitani, Y., Yamaguchi, J., et al. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.02.020 · Cited by 172 · see citing works

Brentuximab vedotin

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A Novel Anti-CD22 Anthracycline-Based Antibody–Drug Conjugate (ADC) That Overcomes Resistance to Auristatin-Based ADCs

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A Chemically Defined Trifunctional Antibody–Cytokine–Drug Conjugate with Potent Antitumor Activity

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Editorial [Hot Topic: Therapeutic Antibodies and Derivatives: From the Bench to the Clinic(Guest Editor: Alain Beck)]

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Sensitive ELISA Method for the Measurement of Catabolites of Antibody–Drug Conjugates (ADCs) in Target Cancer Cells

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RP-HPLC DAR Characterization of Site-Specific Antibody Drug Conjugates Produced in a Cell-Free Expression System

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Targeted therapy for Hodgkin lymphoma and systemic anaplastic large cell lymphoma: focus on brentuximab vedotin

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The biology of MDR1-P-glycoprotein (MDR1-Pgp) in designing functional antibody drug conjugates (ADCs): the experience of gemtuzumab ozogamicin.

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Monoclonal antibodies in myeloma.

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Prognostic value of S‐phase cells in AML patients

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Hydrolytically Stable Site-Specific Conjugation at the N-Terminus of an Engineered Antibody

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Enhanced Antitumor Activity of an Anti-5T4 Antibody–Drug Conjugate in Combination with PI3K/mTOR inhibitors or Taxanes

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Computational selection of antibody-drug conjugate targets for breast cancer

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Synthesis of a C2-aryl-pyrrolo[2,1-c][1,4]benzodiazepine monomer enabling the convergent construction of symmetrical and non-symmetrical dimeric analogs

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Covalent Chemical Ligation Strategy for Mono- and Polyclonal Immunoglobulins at Their Nucleotide Binding Sites

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Introducing Glycolinkers for the Functionalization of Cytotoxic Drugs and Applications in Antibody–Drug Conjugation Chemistry

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Rethinking the INN system for therapeutic antibodies

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A novel antibody–drug conjugate targeting SAIL for the treatment of hematologic malignancies

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8thAnnual European Antibody Congress 2012

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A new anti-human Fc method to capture and analyze ADCs for characterization of drug distribution and the drug-to-antibody ratio in serum from pre-clinical species

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Why is it so difficult to use gemtuzumab ozogamicin?

Castaigné, S. (2013) · Blood · doi:10.1182/blood-2013-05-498683 · Cited by 10 · see citing works

Abstract 647: SeriMabs: N-terminal serine modification enables modular, site-specific payload incorporation into antibody-drug conjugates (ADCs)

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Abstract DDT02-04: SGN-CD33A: Preclinical and phase 1 interim clinical trial results of a CD33-directed PBD dimer antibody-drug conjugate for the treatment of acute myeloid leukemia (AML)

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A view on drug resistance in cancer

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Antibody drug conjugate: the “biological missile” for targeted cancer therapy

Fu, Z., Li, S., Han, S., Shi, C., & Zhang, Y. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-00947-7 · Cited by 1,643 · see citing works

The evolution of commercial drug delivery technologies

Vargason, A. M., Anselmo, A. C., & Mitragotri, S. (2021) · Nature Biomedical Engineering · doi:10.1038/s41551-021-00698-w · Cited by 1,361 · see citing works

Exploring the next generation of antibody–drug conjugates

Tsuchikama, K., Anami, Y., Ha, S. Y. Y., & Yamazaki, C. M. (2024) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-023-00850-2 · Cited by 659 · see citing works

Mechanisms of ADC Toxicity and Strategies to Increase ADC Tolerability

Nguyen, T. D., Bordeau, B. M., & Balthasar, J. P. (2023) · Cancers · doi:10.3390/cancers15030713 · Cited by 441 · see citing works

The Journey of Antibody–Drug Conjugates: Lessons Learned from 40 Years of Development

Colombo, R., Tarantino, P., Rich, J. R., LoRusso, P. M., & de Vries, E. G. E. (2024) · Cancer Discovery · doi:10.1158/2159-8290.cd-24-0708 · Cited by 254 · see citing works

Antibody Conjugation of a Chimeric BET Degrader Enables <i>in vivo</i> Activity

Pillow, T. H., Adhikari, P., Blake, R. A., Chen, J., Del Rosario, G., Deshmukh, G., Figueroa, I., Gascoigne, K. E., Kamath, A. V., Kaufman, S., et al. (2020) · ChemMedChem · doi:10.1002/cmdc.201900497 · Cited by 216 · see citing works

Thera-SAbDab: the therapeutic structural antibody database

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A review of the clinical efficacy of FDA-approved antibody‒drug conjugates in human cancers

Liu, K., Li, M., Li, Y., Li, Y., Chen, Z., Tang, Y., Yang, M., Deng, G., & Liu, H. (2024) · Molecular Cancer · doi:10.1186/s12943-024-01963-7 · Cited by 196 · see citing works

Treatment‐related adverse events of antibody–drug conjugates in clinical trials: A systematic review and meta‐analysis

Zhu, Y., Liu, K., Wang, K., & Zhu, H. (2023) · Cancer · doi:10.1002/cncr.34507 · Cited by 192 · see citing works

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy

Dragovich, P. S., Pillow, T. H., Blake, R. A., Sadowsky, J. D., Adaligil, E., Adhikari, P., Chen, J., Corr, N., dela Cruz-Chuh, J., Del Rosario, G., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01846 · Cited by 174 · see citing works

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

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Targeted clearance of senescent cells using an antibody-drug conjugate against a specific membrane marker

Poblocka, M., Bassey, A. L., Smith, V. M., Falcicchio, M., Manso, A. S., Althubiti, M., Sheng, X., Kyle, A., Barber, R., Frigerio, M., et al. (2021) · Scientific Reports · doi:10.1038/s41598-021-99852-2 · Cited by 137 · see citing works

The B7-H3–Targeting Antibody–Drug Conjugate m276-SL-PBD Is Potently Effective Against Pediatric Cancer Preclinical Solid Tumor Models

Kendsersky, N. M., Lindsay, J., Kolb, E. A., Smith, M. A., Teicher, B. A., Erickson, S. W., Earley, E. J., Mosse, Y. P., Martinez, D., Pogoriler, J., et al. (2021) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-20-4221 · Cited by 120 · see citing works

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

Dragovich, P. S., Adhikari, P., Blake, R. A., Blaquiere, N., Chen, J., Cheng, Y.-X., den Besten, W., Han, J., Hartman, S. J., He, J., et al. (2020) · Bioorganic &amp; Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2019.126907 · Cited by 120 · see citing works

Antibody interface prediction with 3D Zernike descriptors and SVM

Daberdaku, S., & Ferrari, C. (2019) · Bioinformatics · doi:10.1093/bioinformatics/bty918 · Cited by 88 · see citing works

Tandem-Cleavage Linkers Improve the In Vivo Stability and Tolerability of Antibody–Drug Conjugates

Chuprakov, S., Ogunkoya, A. O., Barfield, R. M., Bauzon, M., Hickle, C., Kim, Y. C., Yeo, D., Zhang, F., Rabuka, D., & Drake, P. M. (2021) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.1c00029 · Cited by 80 · see citing works

GEF-H1 Signaling upon Microtubule Destabilization Is Required for Dendritic Cell Activation and Specific Anti-tumor Responses

Kashyap, A. S., Fernandez-Rodriguez, L., Zhao, Y., Monaco, G., Trefny, M. P., Yoshida, N., Martin, K., Sharma, A., Olieric, N., Shah, P., et al. (2019) · Cell Reports · doi:10.1016/j.celrep.2019.08.057 · Cited by 76 · see citing works

Targeting mutant p53-expressing tumours with a T cell receptor-like antibody specific for a wild-type antigen

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Ion mobility in the pharmaceutical industry: an established biophysical technique or still niche?

Campuzano, I. D., & Lippens, J. L. (2018) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2017.11.008 · Cited by 42 · see citing works

Importance and Considerations of Antibody Engineering in Antibody-Drug Conjugates Development from a Clinical Pharmacologist’s Perspective

Lucas, A. T., Moody, A., Schorzman, A. N., & Zamboni, W. C. (2021) · Antibodies · doi:10.3390/antib10030030 · Cited by 40 · see citing works

Nonclinical Efficacy and Safety of CX-2029, an Anti-CD71 Probody–Drug Conjugate

Singh, S., Serwer, L., DuPage, A., Elkins, K., Chauhan, N., Ravn, M., Buchanan, F., Wang, L., Krimm, M., Wong, K., et al. (2022) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-21-0193 · Cited by 41 · see citing works

Current and emerging concepts for systemic treatment of metastatic colorectal cancer

Steup, C., Kennel, K. B., Neurath, M. F., Fichtner-Feigl, S., & Greten, F. R. (2025) · Gut · doi:10.1136/gutjnl-2025-335412 · Cited by 39 · see citing works

Middle-Down Multi-Attribute Analysis of Antibody-Drug Conjugates with Electron Transfer Dissociation

Chen, B., Lin, Z., Zhu, Y., Jin, Y., Larson, E., Xu, Q., Fu, C., Zhang, Z., Zhang, Q., Pritts, W. A., et al. (2019) · Analytical Chemistry · doi:10.1021/acs.analchem.9b02194 · Cited by 38 · see citing works

Clinical translation of nanomedicines for brain diseases: Current challenges and future directions

Wang, G., Wang, N., Xia, X., Ismail, M., & Shi, B. (2026) · Journal of Controlled Release · doi:10.1016/j.jconrel.2025.114426 · Cited by 33 · see citing works

Effect of a MUC5AC Antibody (NPC-1C) Administered With Second-Line Gemcitabine and Nab-Paclitaxel on the Survival of Patients With Advanced Pancreatic Ductal Adenocarcinoma: A Randomized Clinical Trial

Huffman, B. M., Basu Mallick, A., Horick, N. K., Wang-Gillam, A., Hosein, P. J., Morse, M. A., Beg, M. S., Murphy, J. E., Mavroukakis, S., Zaki, A., et al. (2023) · JAMA Network Open · doi:10.1001/jamanetworkopen.2022.49720 · Cited by 25 · see citing works

HER3 Alterations in Cancer and Potential Clinical Implications

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Rapid Analysis of Reduced Antibody Drug Conjugate by Online LC-MS/MS with Fourier Transform Ion Cyclotron Resonance Mass Spectrometry

Larson, E. J., Zhu, Y., Wu, Z., Chen, B., Zhang, Z., Zhou, S., Han, L., Zhang, Q., & Ge, Y. (2020) · Analytical Chemistry · doi:10.1021/acs.analchem.0c03152 · Cited by 21 · see citing works

The evolving landscape of antibody-drug conjugates (ADCs) for treatment of prostate cancer

Lin, C., Hadfield, M. J., Santopietro, A., Lagos, G., Cheng, L., El-Deiry, W. S., Aggarwal, R., Mega, A., Hyams, E., & Carneiro, B. A. (2025) · npj Precision Oncology · doi:10.1038/s41698-025-01131-0 · Cited by 20 · see citing works

Designing poly-agonists for treatment of metabolic diseases: challenges and opportunities

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Brentuximab vedotin. an antibody-drug conjugate targeting CD30

Yanai, T. (2017) · Drug Delivery System · doi:10.2745/dds.32.126

Brentuximab vedotin

Younes, A., Yasothan, U., & Kirkpatrick, P. N. (2012) · Nature Reviews Drug Discovery · doi:10.1038/nrd3629 · Cited by 170 · see citing works

Population PK and Exposure–Response Relationships for the Antibody–Drug Conjugate Brentuximab Vedotin in CTCL Patients in the Phase III ALCANZA Study

Suri, A., Mould, D. R., Liu, Y., Jang, G. R., & Venkatakrishnan, K. (2018) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.1037 · Cited by 33 · see citing works

The discovery and development of brentuximab vedotin for use in relapsed Hodgkin lymphoma and systemic anaplastic large cell lymphoma

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696 Brentuximab vedotin, a CD30-directed antibody-drug conjugate, selectively depletes activated Tregs in vitro and in vivo

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