Unlocking the potential of antibody–drug conjugates for cancer therapy

ANG1005, a brain penetrating peptide-drug conjugate, shows activity in patients with breast cancer with leptomeningeal carcinomatosis and recurrent brain metastases

(2020) Priya Kumthekar et al.   CLINICAL CANCER RESEARCH

Trastuzumab emtansine (T-DM1)-associated cardiotoxicity: Pooled analysis in advanced HER2-positive breast cancer

(2020) Noam Pondé et al.   EUROPEAN JOURNAL OF CANCER

Phase Ib study of mirvetuximab soravtansine, a folate receptor alpha (FRα)-targeting antibody-drug conjugate (ADC), in combination with bevacizumab in patients with platinum-resistant ovarian cancer

(2020) David M. O'Malley et al.   GYNECOLOGIC ONCOLOGY

Study EV-103: Preliminary durability results of enfortumab vedotin plus pembrolizumab for locally advanced or metastatic urothelial carcinoma.

(2020) Jonathan E. Rosenberg et al.   JOURNAL OF CLINICAL ONCOLOGY

Antitumor Activity and Safety of Trastuzumab Deruxtecan in Patients With HER2-Low–Expressing Advanced Breast Cancer: Results From a Phase Ib Study

(2020) Shanu Modi et al.   JOURNAL OF CLINICAL ONCOLOGY

HER2-Low Breast Cancer: Pathological and Clinical Landscape

(2020) Paolo Tarantino et al.   JOURNAL OF CLINICAL ONCOLOGY

How to select IgG subclasses in developing anti-tumor therapeutic antibodies

(2020) Jifeng Yu et al.   Journal of Hematology & Oncology

Targeting apoptosis in cancer therapy

(2020) Benedito A. Carneiro et al.   Nature Reviews Clinical Oncology

Trastuzumab Deruxtecan in Previously Treated HER2-Positive Gastric Cancer

(2020) Kohei Shitara et al.   NEW ENGLAND JOURNAL OF MEDICINE

HER2-Mediated Internalization of Cytotoxic Agents in ERBB2 Amplified or Mutant Lung Cancers

(2020) Bob T. Li et al.   Cancer Discovery

Cancer stromal targeting therapy to overcome the pitfall of EPR effect

(2020) Yasuhiro Matsumura   ADVANCED DRUG DELIVERY REVIEWS

Phase 1b study of anti-NaPi2b antibody-drug conjugate lifastuzumab vedotin (DNIB0600A) in patients with platinum-sensitive recurrent ovarian cancer

(2020) Kathleen N. Moore et al.   GYNECOLOGIC ONCOLOGY

Inferences about drug safety in phase 3 trials in oncology: Examples from advanced prostate cancer

(2020) Joshua Z Drago et al.   JNCI-Journal of the National Cancer Institute

Membrane-Anchored Serine Proteases and Protease-Activated Receptor-2–Mediated Signaling: Co-Conspirators in Cancer Progression

(2019) Nisha R. Pawar et al.   CANCER RESEARCH

Sacituzumab Govitecan-hziy in Refractory Metastatic Triple-Negative Breast Cancer

(2019) Aditya Bardia et al.   NEW ENGLAND JOURNAL OF MEDICINE

HER2 heterogeneity as a predictor of response to neoadjuvant T-DM1 plus pertuzumab: Results from a prospective clinical trial.

(2019) Otto Metzger Filho et al.   JOURNAL OF CLINICAL ONCOLOGY

Engineering a HER2-specific antibody–drug conjugate to increase lysosomal delivery and therapeutic efficacy

(2019) Jeffrey C. Kang et al.   NATURE BIOTECHNOLOGY

Potential mechanisms of target-independent uptake and toxicity of antibody-drug conjugates

(2019) Prathap Kumar Mahalingaiah et al.   PHARMACOLOGY & THERAPEUTICS

Antibody–Oligonucleotide Conjugates as Therapeutic, Imaging, and Detection Agents

(2019) Igor Dovgan et al.   BIOCONJUGATE CHEMISTRY

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

(2019) John Y. Li et al.   CANCER CELL

Pivotal Trial of Enfortumab Vedotin in Urothelial Carcinoma After Platinum and Anti-Programmed Death 1/Programmed Death Ligand 1 Therapy

(2019) Jonathan E. Rosenberg et al.   JOURNAL OF CLINICAL ONCOLOGY

Trastuzumab duocarmazine in locally advanced and metastatic solid tumours and HER2-expressing breast cancer: a phase 1 dose-escalation and dose-expansion study

(2019) Udai Banerji et al.   LANCET ONCOLOGY

Targeting the Somatostatin Receptor 2 with the Miniaturized Drug Conjugate, PEN-221: A Potent and Novel Therapeutic for the Treatment of Small Cell Lung Cancer

(2019) Kerry A. Whalen et al.   MOLECULAR CANCER THERAPEUTICS

A view on drug resistance in cancer

(2019) Neil Vasan et al.   NATURE

An FDA oncology analysis of toxicities associated with PBD-containing antibody-drug conjugates

(2019) Haleh Saber et al.   REGULATORY TOXICOLOGY AND PHARMACOLOGY

Trastuzumab Deruxtecan in Previously Treated HER2-Positive Breast Cancer

(2019) Shanu Modi et al.   NEW ENGLAND JOURNAL OF MEDICINE

Human Epidermal Growth Factor Receptor 2 Testing in Breast Cancer: American Society of Clinical Oncology/College of American Pathologists Clinical Practice Guideline Focused Update

(2018) Antonio C. Wolff et al.   ARCHIVES OF PATHOLOGY & LABORATORY MEDICINE

Modulation of Macropinocytosis-Mediated Internalization Decreases Ocular Toxicity of Antibody–Drug Conjugates

(2018) Hui Zhao et al.   CANCER RESEARCH

Docetaxel with or without ramucirumab after immune checkpoint inhibition in platinum-refractory metastatic urothelial carcinoma (mUC): Prespecified subgroup analysis from the phase 3 RANGE trial.

(2018) Alexandra Drakaki et al.   JOURNAL OF CLINICAL ONCOLOGY

Ado-Trastuzumab Emtansine for Patients With HER2-Mutant Lung Cancers: Results From a Phase II Basket Trial

(2018) Bob T. Li et al.   JOURNAL OF CLINICAL ONCOLOGY

Mechanisms of Acquired Resistance to Trastuzumab Emtansine in Breast Cancer Cells

(2018) Guangmin Li et al.   MOLECULAR CANCER THERAPEUTICS

Cooperative targeting of melanoma heterogeneity with an AXL antibody-drug conjugate and BRAF/MEK inhibitors

(2018) Julia Boshuizen et al.   NATURE MEDICINE

Targeting PLK1 overcomes T-DM1 resistance via CDK1-dependent phosphorylation and inactivation of Bcl-2/xL in HER2-positive breast cancer

(2018) Özge Saatci et al.   ONCOGENE

Improved Therapeutic Window in BRCA-mutant Tumors with Antibody-linked Pyrrolobenzodiazepine Dimers with and without PARP Inhibition

(2018) Haihong Zhong et al.   MOLECULAR CANCER THERAPEUTICS

Trastuzumab Emtansine for Residual Invasive HER2-Positive Breast Cancer

(2018) Gunter von Minckwitz et al.   NEW ENGLAND JOURNAL OF MEDICINE

An HER3-targeting antibody–drug conjugate incorporating a DNA topoisomerase I inhibitor U3-1402 conquers EGFR tyrosine kinase inhibitor-resistant NSCLC

(2018) Kimio Yonesaka et al.   ONCOGENE

Small molecule-drug conjugates: A novel strategy for cancer-targeted treatment

(2018) Chunlin Zhuang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

DS-8201a, a new HER2-targeting antibody-drug conjugate incorporating a novel DNA topoisomerase I inhibitor, overcomes HER2-positive gastric cancer T-DM1 resistance

(2017) Naoki Takegawa et al.   INTERNATIONAL JOURNAL OF CANCER

Clinical toxicity of antibody drug conjugates: a meta-analysis of payloads

(2017) Joanna C. Masters et al.   INVESTIGATIONAL NEW DRUGS

Efficacy and Safety of Anti-Trop-2 Antibody Drug Conjugate Sacituzumab Govitecan (IMMU-132) in Heavily Pretreated Patients With Metastatic Triple-Negative Breast Cancer

(2017) Aditya Bardia et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeted radionuclide therapy in combined-modality regimens

(2017) Martin R Gill et al.   LANCET ONCOLOGY

Bispecific Antibodies and Antibody–Drug Conjugates (ADCs) Bridging HER2 and Prolactin Receptor Improve Efficacy of HER2 ADCs

(2017) Julian Andreev et al.   MOLECULAR CANCER THERAPEUTICS

Next generation antibody drugs: pursuit of the 'high-hanging fruit'

(2017) Paul J. Carter et al.   NATURE REVIEWS DRUG DISCOVERY

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

(2017) Alain Beck et al.   NATURE REVIEWS DRUG DISCOVERY

Understanding CD30 biology and therapeutic targeting: a historical perspective providing insight into future directions

(2017) C A van der Weyden et al.   Blood Cancer Journal

Long-Term Effects, Pathophysiological Mechanisms, and Risk Factors of Chemotherapy-Induced Peripheral Neuropathies: A Comprehensive Literature Review

(2017) Nicolas Kerckhove et al.   Frontiers in Pharmacology

Antibody structure and engineering considerations for the design and function of Antibody Drug Conjugates (ADCs)

(2017) Ricarda M. Hoffmann et al.   OncoImmunology

Antibody drug conjugates: lessons from 20 years of clinical experience

(2016) A. W. Tolcher   ANNALS OF ONCOLOGY

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

(2016) Hans-Peter Gerber et al.   BIOCHEMICAL PHARMACOLOGY

Intracellular Released Payload Influences Potency and Bystander-Killing Effects of Antibody-Drug Conjugates in Preclinical Models

(2016) F. Li et al.   CANCER RESEARCH

Enfortumab Vedotin Antibody-Drug Conjugate Targeting Nectin-4 Is a Highly Potent Therapeutic Agent in Multiple Preclinical Cancer Models

(2016) P. M. Challita-Eid et al.   CANCER RESEARCH

Bystander killing effect of DS-8201a, a novel anti-human epidermal growth factor receptor 2 antibody-drug conjugate, in tumors with human epidermal growth factor receptor 2 heterogeneity

(2016) Yusuke Ogitani et al.   CANCER SCIENCE

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

(2016) Y. Ogitani et al.   CLINICAL CANCER RESEARCH

New developments for antibody-drug conjugate-based therapeutic approaches

(2016) Bart ECG de Goeij et al.   CURRENT OPINION IN IMMUNOLOGY

Editorial overview: Special section: New concepts in antibody therapeutics: What's in store for antibody therapy?

(2016) Janine Schuurman et al.   CURRENT OPINION IN IMMUNOLOGY

Non-internalizing antibody-drug conjugates display potent anti-cancer activity upon proteolytic release of monomethyl auristatin E in the subendothelial extracellular matrix

(2016) Rémy Gébleux et al.   INTERNATIONAL JOURNAL OF CANCER

Quantitative characterization of in vitro bystander effect of antibody-drug conjugates

(2016) Aman P. Singh et al.   JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS

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

(2016) Heather Donaghy   mAbs

Biodistribution and Targeting of Anti-5T4 Antibody-Drug Conjugate Using Fluorescence Molecular Tomography

(2016) A. Giddabasappa et al.   MOLECULAR CANCER THERAPEUTICS

Efficient Payload Delivery by a Bispecific Antibody-Drug Conjugate Targeting HER2 and CD63

(2016) B. E. C. G. de Goeij et al.   MOLECULAR CANCER THERAPEUTICS

Mechanisms of Resistance to Antibody–Drug Conjugates

(2016) Frank Loganzo et al.   MOLECULAR CANCER THERAPEUTICS

Antibody-drug conjugates: recent advances in conjugation and linker chemistries

(2016) Kyoji Tsuchikama et al.   Protein & Cell

Mirvetuximab Soravtansine (IMGN853), a Folate Receptor Alpha–Targeting Antibody-Drug Conjugate, Potentiates the Activity of Standard of Care Therapeutics in Ovarian Cancer Models

(2016) Jose F. Ponte et al.   NEOPLASIA

Structural Basis of Microtubule Destabilization by Potent Auristatin Anti-Mitotics

(2016) Andrew B. Waight et al.   PLoS One

Molecular imaging as a tool to investigate heterogeneity of advanced HER2-positive breast cancer and to predict patient outcome under trastuzumab emtansine (T-DM1): the ZEPHIR trial

(2015) G. Gebhart et al.   ANNALS OF ONCOLOGY

Advances in Antibody Design

(2015) Kathryn E. Tiller et al.   Annual Review of Biomedical Engineering

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

(2015) Paresh Agarwal et al.   BIOCONJUGATE CHEMISTRY

An emerging playbook for antibody–drug conjugates: lessons from the laboratory and clinic suggest a strategy for improving efficacy and safety

(2015) Penelope M Drake et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Emerging formats for next-generation antibody drug conjugates

(2015) Mahendra P Deonarain et al.   Expert Opinion on Drug Discovery

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

(2015) Denise A. Yardley et al.   JOURNAL OF CLINICAL ONCOLOGY

Antibody–Drug Conjugates and Small Molecule–Drug Conjugates: Opportunities and Challenges for the Development of Selective Anticancer Cytotoxic Agents

(2015) Giulio Casi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ocular Adverse Events Associated with Antibody–Drug Conjugates in Human Clinical Trials

(2015) Joshua Seth Eaton et al.   JOURNAL OF OCULAR PHARMACOLOGY AND THERAPEUTICS

Anti-CD22 and anti-CD79B antibody drug conjugates are active in different molecular diffuse large B-cell lymphoma subtypes

(2015) M Pfeifer et al.   LEUKEMIA

AMG 595, an Anti-EGFRvIII Antibody-Drug Conjugate, Induces Potent Antitumor Activity against EGFRvIII-Expressing Glioblastoma

(2015) K. J. Hamblett et al.   MOLECULAR CANCER THERAPEUTICS

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

(2015) F. Loganzo et al.   MOLECULAR CANCER THERAPEUTICS

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

(2015) M. M. C. van der Lee et al.   MOLECULAR CANCER THERAPEUTICS

High Turnover of Tissue Factor Enables Efficient Intracellular Delivery of Antibody-Drug Conjugates

(2015) B. E. C. G. de Goeij et al.   MOLECULAR CANCER THERAPEUTICS

CD30 Downregulation, MMAE Resistance, and MDR1 Upregulation Are All Associated with Resistance to Brentuximab Vedotin

(2015) R. Chen et al.   MOLECULAR CANCER THERAPEUTICS

Mechanisms of action of therapeutic antibodies for cancer

(2015) J.M. Redman et al.   MOLECULAR IMMUNOLOGY

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

(2015) Robert P Lyon et al.   NATURE BIOTECHNOLOGY

Evolving Strategies for Target Selection for Antibody-Drug Conjugates

(2015) Marc Damelin et al.   PHARMACEUTICAL RESEARCH

Current ADC Linker Chemistry

(2015) Nareshkumar Jain et al.   PHARMACEUTICAL RESEARCH

An FDA oncology analysis of antibody-drug conjugates

(2015) Haleh Saber et al.   REGULATORY TOXICOLOGY AND PHARMACOLOGY

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

(2015) David M. Goldenberg et al.   Oncotarget

Immunogenicity of Antibody Drug Conjugates: Bioanalytical Methods and Monitoring Strategy for a Novel Therapeutic Modality

(2014) M. Benjamin Hock et al.   AAPS Journal

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

(2014) Y.-T. Tai et al.   BLOOD

Potential Mechanisms for Thrombocytopenia Development with Trastuzumab Emtansine (T-DM1)

(2014) H. Uppal et al.   CLINICAL CANCER RESEARCH

Phase I/II Study of the Antibody-Drug Conjugate Glembatumumab Vedotin in Patients With Advanced Melanoma

(2014) Patrick A. Ott et al.   JOURNAL OF CLINICAL ONCOLOGY

Using the Lessons Learned From the Clinic to Improve the Preclinical Development of Antibody Drug Conjugates

(2014) Dowdy Jackson et al.   PHARMACEUTICAL RESEARCH

IgG Subclasses and Allotypes: From Structure to Effector Functions

(2014) Gestur Vidarsson et al.   Frontiers in Immunology

5-fluorouracil induced cardiotoxicity: Review of the literature

(2013) Michael F. Sorrentino et al.   Cardiology Journal

Cardiotoxicity of novel HER2-targeted therapies

(2013) Mehmet A.N. Sendur et al.   CURRENT MEDICAL RESEARCH AND OPINION

Antibody–drug conjugates: current status and future directions

(2013) Heidi L. Perez et al.   DRUG DISCOVERY TODAY

Emerging Paradigms in the Development of Resistance to Tyrosine Kinase Inhibitors in Lung Cancer

(2013) Justin F. Gainor et al.   JOURNAL OF CLINICAL ONCOLOGY

Implications of receptor-mediated endocytosis and intracellular trafficking dynamics in the development of antibody drug conjugates

(2013) Michael Ritchie et al.   mAbs

Antibody-Drug Conjugates in Cancer Therapy

(2012) Eric L. Sievers et al.   Annual Review of Medicine

A population pharmacokinetic/pharmacodynamic model of thrombocytopenia characterizing the effect of trastuzumab emtansine (T-DM1) on platelet counts in patients with HER2-positive metastatic breast cancer

(2012) Brendan C. Bender et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Clinical pharmacology of trastuzumab emtansine (T-DM1): an antibody–drug conjugate in development for the treatment of HER2-positive cancer

(2012) Sandhya Girish et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Frequent Mutational Activation of the PI3K-AKT Pathway in Trastuzumab-Resistant Breast Cancer

(2012) S. Chandarlapaty et al.   CLINICAL CANCER RESEARCH

Chemokine-based immunotherapy: delivery systems and combination therapies

(2012) Elham Mohit et al.   Immunotherapy

Results of a Pivotal Phase II Study of Brentuximab Vedotin for Patients With Relapsed or Refractory Hodgkin's Lymphoma

(2012) Anas Younes et al.   JOURNAL OF CLINICAL ONCOLOGY

A mechanistic compartmental model for total antibody uptake in tumors

(2012) Greg M. Thurber et al.   JOURNAL OF THEORETICAL BIOLOGY

Impact of linker and conjugation chemistry on antigen binding, Fc receptor binding and thermal stability of model antibody-drug conjugates

(2012) Mauro Acchione et al.   mAbs

Intratumoral heterogeneity of HER2 gene amplification in breast cancer: its clinicopathological significance

(2012) Hyesil Seol et al.   MODERN PATHOLOGY

The Effect of Different Linkers on Target Cell Catabolism and Pharmacokinetics/Pharmacodynamics of Trastuzumab Maytansinoid Conjugates

(2012) H. K. Erickson et al.   MOLECULAR CANCER THERAPEUTICS

Brentuximab vedotin

(2012) Anas Younes et al.   NATURE REVIEWS DRUG DISCOVERY

ERBB2 Inhibition and Heart Failure

(2012) Gregory M. Cote et al.   NEW ENGLAND JOURNAL OF MEDICINE

Trastuzumab Emtansine for HER2-Positive Advanced Breast Cancer

(2012) Sunil Verma et al.   NEW ENGLAND JOURNAL OF MEDICINE

Humanized Anti-Trop-2 IgG-SN-38 Conjugate for Effective Treatment of Diverse Epithelial Cancers: Preclinical Studies in Human Cancer Xenograft Models and Monkeys

(2011) T. M. Cardillo et al.   CLINICAL CANCER RESEARCH

Antibody-Drug Conjugates of Calicheamicin Derivative: Gemtuzumab Ozogamicin and Inotuzumab Ozogamicin

(2011) A. D. Ricart   CLINICAL CANCER RESEARCH

Antibody Conjugate Therapeutics: Challenges and Potential

(2011) B. A. Teicher et al.   CLINICAL CANCER RESEARCH

Expression of Trop2 Cell Surface Glycoprotein in Normal and Tumor Tissues

(2011) Lara P. Stepan et al.   JOURNAL OF HISTOCHEMISTRY & CYTOCHEMISTRY

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

(2010) Teemu T. Junttila et al.   BREAST CANCER RESEARCH AND TREATMENT

Antibody–drug conjugates: targeted drug delivery for cancer

(2010) Stephen C Alley et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Assessment of EGFR Mutation Status in Lung Adenocarcinoma by Immunohistochemistry Using Antibodies Specific to the Two Major Forms of Mutant EGFR

(2010) Marie Brevet et al.   JOURNAL OF MOLECULAR DIAGNOSTICS

Maytansinoid-Antibody Conjugates Induce Mitotic Arrest by Suppressing Microtubule Dynamic Instability

(2010) E. Oroudjev et al.   MOLECULAR CANCER THERAPEUTICS

Antibody-Drug Conjugates for the Treatment of Non-Hodgkin's Lymphoma: Target and Linker-Drug Selection

(2009) A. G. Polson et al.   CANCER RESEARCH

Strongly Enhanced Antitumor Activity of Trastuzumab and Pertuzumab Combination Treatment on HER2-Positive Human Xenograft Tumor Models

(2009) W. Scheuer et al.   CANCER RESEARCH

Potent antibody drug conjugates for cancer therapy

(2009) Peter D Senter   CURRENT OPINION IN CHEMICAL BIOLOGY

The Pharmacologic Basis for Antibody-Auristatin Conjugate Activity

(2009) S. C. Alley et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Antibody-Drug Conjugates for Cancer Therapy

(2008) Paul J. Carter et al.   CANCER JOURNAL

Mechanisms and strategies to overcome chemotherapy resistance in metastatic breast cancer

(2008) Helen M. Coley   CANCER TREATMENT REVIEWS

Phase I trial with the CD44v6-targeting immunoconjugate bivatuzumab mertansine in head and neck squamous cell carcinoma

(2008) Herbert Riechelmann et al.   ORAL ONCOLOGY

Targeted Cancer Therapy: Conferring Specificity to Cytotoxic Drugs

(2007) Ravi V. J. Chari   ACCOUNTS OF CHEMICAL RESEARCH