Resistance to antibody‐drug conjugates in breast cancer: mechanisms and solutions

Impacts of clinicopathological factors on efficacy of trastuzumab deruxtecan in patients with HER2-positive metastatic breast cancer

(2022) Hiromichi Nakajima et al.   BREAST

165MO Trastuzumab-deruxtecan (T-DXd) in HER2-positive breast cancer patients (pts) with active brain metastases: Primary outcome analysis from the TUXEDO-1 trial

(2022) R. Bartsch et al.   ANNALS OF ONCOLOGY

Trastuzumab Deruxtecan versus Trastuzumab Emtansine for Breast Cancer

(2022) Javier Cortés et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Phase 1/1b Trial of PD 0332991 (Palbociclib) and T-DM1 in HER2 Positive Advanced Breast Cancer after Trastuzumab and Taxane Therapy

(2021) Barbara Haley et al.   Clinical Breast Cancer

Antibody‐drug conjugate MORAb‐202 exhibits long‐lasting antitumor efficacy in TNBC PDx models

(2021) Keiji Furuuchi et al.   CANCER SCIENCE

First-in-human Phase 1 Study of MORAb-202, An Antibody-drug Conjugate Comprising Farletuzumab Linked to Eribulin Mesylate, in Patients with Folate Receptor-α-positive Advanced Solid Tumors

(2021) Toshio Shimizu et al.   CLINICAL CANCER RESEARCH

FDA Approval Summary: Fam-trastuzumab deruxtecan-nxki for the treatment of unresectable or metastatic HER2-positive breast cancer

(2021) Preeti Narayan et al.   CLINICAL CANCER RESEARCH

Phase I study of the recombinant humanized anti-HER2 monoclonal antibody–MMAE conjugate RC48-ADC in patients with HER2-positive advanced solid tumors

(2021) Yingying Xu et al.   Gastric Cancer

Sacituzumab Govitecan in Metastatic Triple-Negative Breast Cancer

(2021) Aditya Bardia et al.   NEW ENGLAND JOURNAL OF MEDICINE

Impact of HER2 heterogeneity on treatment response of early-stage HER2-positive breast cancer: phase II neoadjuvant clinical trial of T-DM1 combined with pertuzumab

(2021) Otto Metzger Filho et al.   Cancer Discovery

LBA13 Predictive impact of biomarkers on pCR and survival after de-escalated neoadjuvant T-DM1 with or without endocrine therapy (ET) vs. trastuzumab+ET in HER2+/HR+ early breast cancer: WSG ADAPT TP trial

(2021) N. Harbeck et al.   ANNALS OF ONCOLOGY

514O An open-label, global, first-in-human study of SKB264 in patients with locally advanced or metastatic solid tumors

(2021) J. Rodon et al.   ANNALS OF ONCOLOGY

Biomarker analyses in the phase III ASCENT study of sacituzumab govitecan versus chemotherapy in patients with metastatic triple-negative breast cancer

(2021) A. Bardia et al.   ANNALS OF ONCOLOGY

LBA1 Trastuzumab deruxtecan (T-DXd) vs trastuzumab emtansine (T-DM1) in patients (Pts) with HER2+ metastatic breast cancer (mBC): Results of the randomized phase III DESTINY-Breast03 study

(2021) J. Cortés et al.   ANNALS OF ONCOLOGY

259P Weekly ladiratuzumab vedotin monotherapy for metastatic triple-negative breast cancer

(2021) M. Tsai et al.   ANNALS OF ONCOLOGY

329TiP KATE3: A phase III study of trastuzumab emtansine (T-DM1) in combination with atezolizumab or placebo in patients with previously treated HER2-positive and PD-L1–positive locally advanced or metastatic breast cancer

(2021) S. Loi et al.   ANNALS OF ONCOLOGY

271P First-in-human, phase I dose escalation and expansion study of anti-HER2 ADC MRG002 in patients with HER2 positive solid tumors

(2021) Y. Guo et al.   ANNALS OF ONCOLOGY

O2-1 Datopotamab Deruxtecan (Dato-DXd; DS-1062), a TROP2 ADC, in patients with advanced NSCLC: Updated results of TROPION-PanTumor01 phase 1 study*

(2021) Toshio Shimizu et al.   ANNALS OF ONCOLOGY

LBA15 Primary outcome of the phase III SYD985.002/TULIP trial comparing [vic-]trastuzumab duocarmazine to physician’s choice treatment in patients with pre-treated HER2-positive locally advanced or metastatic breast cancer

(2021) C. Saura Manich et al.   ANNALS OF ONCOLOGY

First-in-Human Study of PF-06647020 (Cofetuzumab Pelidotin), an Antibody–Drug Conjugate Targeting Protein Tyrosine Kinase 7, in Advanced Solid Tumors

(2021) Michael L. Maitland et al.   CLINICAL CANCER RESEARCH

Phase I study of A166 in patients with HER2-expressing locally advanced or metastatic solid tumors.

(2021) Xichun Hu et al.   JOURNAL OF CLINICAL ONCOLOGY

First-in-Human, Phase 1 Dose-Escalation Study of Biparatopic Anti-HER2 Antibody–Drug Conjugate MEDI4276 in Patients with HER2-positive Advanced Breast or Gastric Cancer

(2021) Mark D. Pegram et al.   MOLECULAR CANCER THERAPEUTICS

Datopotamab deruxtecan (Dato-DXd), a novel TROP2-directed antibody-drug conjugate, demonstrates potent antitumor activity by efficient drug delivery to tumor cells

(2021) Daisuke Okajima et al.   MOLECULAR CANCER THERAPEUTICS

Antibody-drug conjugates with dual payloads for combating breast tumor heterogeneity and drug resistance

(2021) Chisato M. Yamazaki et al.   Nature Communications

Parallel Genomic Alterations of Antigen and Payload Targets Mediate Polyclonal Acquired Clinical Resistance to Sacituzumab Govitecan in Triple-Negative Breast Cancer

(2021) James T. Coates et al.   Cancer Discovery

Neoadjuvant Trastuzumab, Pertuzumab, and Docetaxel vs Trastuzumab Emtansine in Patients With ERBB2-Positive Breast Cancer

(2021) Thomas Hatschek et al.   JAMA Oncology

Global patterns of breast cancer incidence and mortality: A population‐based cancer registry data analysis from 2000 to 2020

(2021) Shaoyuan Lei et al.   Cancer Communications

Phase 1b clinical trial of ado-trastuzumab emtansine and ribociclib for HER2-positive metastatic breast cancer

(2021) Laura M. Spring et al.   npj Breast Cancer

Site-Specific Antibody Conjugation to Engineered Double Cysteine Residues

(2021) Qun Zhou et al.   Pharmaceuticals

Targeting HER2 heterogeneity in breast cancer

(2021) Erika Hamilton et al.   CANCER TREATMENT REVIEWS

Neoadjuvant T-DM1/pertuzumab and paclitaxel/trastuzumab/pertuzumab for HER2+ breast cancer in the adaptively randomized I-SPY2 trial

(2021) Amy S. Clark et al.   Nature Communications

RAB5A expression is a predictive biomarker for trastuzumab emtansine in breast cancer

(2021) Olav Engebraaten et al.   Nature Communications

ARX788, a novel anti-HER2 antibody-drug conjugate, shows anti-tumor effects in preclinical models of trastuzumab emtansine-resistant HER2-positive breast cancer and gastric cancer

(2020) Mark Barok et al.   CANCER LETTERS

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

Hypoxia Attenuates Trastuzumab Uptake and Trastuzumab-Emtansine (T-DM1) Cytotoxicity Through Redistribution of Phosphorylated Caveolin-1

(2020) Vineesh Indira Chandran et al.   MOLECULAR CANCER RESEARCH

HER2-Low Breast Cancer: Pathological and Clinical Landscape

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

SKB264 ADC: A first-in-human study of SKB264 in patients with locally advanced unresectable/metastatic solid tumors who are refractory to available standard therapies.

(2020) Yongheng Liu et al.   JOURNAL OF CLINICAL ONCOLOGY

Primary analysis of KAITLIN: A phase III study of trastuzumab emtansine (T-DM1) + pertuzumab versus trastuzumab + pertuzumab + taxane, after anthracyclines as adjuvant therapy for high-risk HER2-positive early breast cancer (EBC).

(2020) Nadia Harbeck et al.   JOURNAL OF CLINICAL ONCOLOGY

First-in-human phase I study of ALT-P7, a HER2-targeting antibody-drug conjugate in patients with HER2-positive advanced breast cancer.

(2020) Yeon Hee Park et al.   JOURNAL OF CLINICAL ONCOLOGY

CX-2009, a CD166-directed probody drug conjugate (PDC): Results from the first-in-human study in patients (Pts) with advanced cancer including breast cancer (BC).

(2020) Valentina Boni et al.   JOURNAL OF CLINICAL ONCOLOGY

A phase I dose escalation study evaluating the safety and tolerability of a novel anti-HER2 antibody-drug conjugate (PF-06804103) in patients with HER2-positive solid tumors.

(2020) Funda Meric-Bernstam et al.   JOURNAL OF CLINICAL ONCOLOGY

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

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

Trastuzumab emtansine (T-DM1) in patients with HER2-positive metastatic breast cancer and brain metastases: exploratory final analysis of cohort 1 from KAMILLA, a single-arm phase IIIb clinical trial☆

(2020) F. Montemurro et al.   ANNALS OF ONCOLOGY

YES1 amplification confers trastuzumab–emtansine (T-DM1) resistance in HER2-positive cancer

(2020) Lei Wang et al.   BRITISH JOURNAL OF CANCER

Sacituzumab Govitecan: First Approval

(2020) Yahiya Y. Syed   DRUGS

Biomarkers of Gemtuzumab Ozogamicin Response for Acute Myeloid Leukemia Treatment

(2020) Laurène Fenwarth et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Hsp90 inhibition and co‐incubation with pertuzumab induce internalization and degradation of trastuzumab: Implications for use of T‐DM1

(2020) Marianne Skeie et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

ARX788, a Site-specific anti-HER2 Antibody Drug Conjugate, Demonstrates Potent and Selective Activity in HER2 Low and T-DM1 Resistant Breast and Gastric Cancers

(2020) Lillian Skidmore et al.   MOLECULAR CANCER THERAPEUTICS

PF-06804103, a site-specific anti-HER2 antibody-drug conjugate for the treatment of HER2-expressing breast, gastric, and lung cancers

(2020) Edmund I. Graziani et al.   MOLECULAR CANCER THERAPEUTICS

The Changing Paradigm for the Treatment of HER2-Positive Breast Cancer

(2020) Aena Patel et al.   Cancers

Characterization of T‐DM1‐resistant breast cancer cells

(2020) Juliette Sauveur et al.   Pharmacology Research & Perspectives

Sacituzumab govitecan in previously treated hormone receptor-positive/HER2-negative metastatic breast cancer: final results from a phase I/II, single-arm, basket trial

(2020) K. Kalinsky et al.   ANNALS OF ONCOLOGY

Design and Validation of Linkers for Site-Specific Preparation of Antibody–Drug Conjugates Carrying Multiple Drug Copies Per Cysteine Conjugation Site

(2020) Amit Kumar et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Trastuzumab emtansine plus atezolizumab versus trastuzumab emtansine plus placebo in previously treated, HER2-positive advanced breast cancer (KATE2): a phase 2, multicentre, randomised, double-blind trial

(2020) Leisha A Emens et al.   LANCET ONCOLOGY

Immune Checkpoint Inhibitors for the Treatment of Cancer: Clinical Impact and Mechanisms of Response and Resistance

(2020) Sreya Bagchi et al.   Annual Review of Pathology-Mechanisms of Disease

The role of caveolin-1 in the biofate and efficacy of anti-tumor drugs and their nano-drug delivery systems

(2020) Canyu Yang et al.   Acta Pharmaceutica Sinica B

Safety of trastuzumab emtansine (T-DM1) in patients with HER2-positive advanced breast cancer: Primary results from the KAMILLA study cohort 1

(2019) Filippo Montemurro et al.   EUROPEAN JOURNAL OF CANCER

[fam‐] trastuzumab deruxtecan, antitumor activity is dependent on HER2 expression level rather than on HER2 amplification

(2019) Naoki Takegawa et al.   INTERNATIONAL JOURNAL OF CANCER

Neutralization of BCL-2/XL Enhances the Cytotoxicity of T-DM1 In Vivo

(2019) Jason J. Zoeller et al.   MOLECULAR CANCER THERAPEUTICS

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

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

Antibody-drug conjugate T-DM1 treatment for HER2+ breast cancer induces ROR1 and confers resistance through activation of Hippo transcriptional coactivator YAP1

(2019) Syed S. Islam et al.   EBioMedicine

Relationship between tumor biomarkers and efficacy in MARIANNE, a phase III study of trastuzumab emtansine ± pertuzumab versus trastuzumab plus taxane in HER2-positive advanced breast cancer

(2019) Edith A. Perez et al.   BMC CANCER

Trastuzumab emtansine with or without pertuzumab versus trastuzumab with taxane for human epidermal growth factor receptor 2–positive advanced breast cancer: Final results from MARIANNE

(2019) Edith A. Perez et al.   CANCER

Neoadjuvant Trastuzumab Emtansine and Pertuzumab in Human Epidermal Growth Factor Receptor 2–Positive Breast Cancer: Three-Year Outcomes From the Phase III KRISTINE Study

(2019) Sara A. Hurvitz et al.   JOURNAL OF CLINICAL ONCOLOGY

Trastuzumab deruxtecan (DS-8201a) in patients with advanced HER2-positive breast cancer previously treated with trastuzumab emtansine: a dose-expansion, phase 1 study

(2019) Kenji Tamura et al.   LANCET ONCOLOGY

A Novel Anti-HER2 Antibody-Drug Conjugate XMT-1522 for HER2-Positive Breast And Gastric Cancers Resistant to Trastuzumab Emtansine

(2019) Vadim Le Joncour et al.   MOLECULAR CANCER THERAPEUTICS

Bispecific antibodies: a mechanistic review of the pipeline

(2019) Aran F. Labrijn et al.   NATURE REVIEWS DRUG DISCOVERY

Lysosomal P-gp-MDR1 Confers Drug Resistance of Brentuximab Vedotin and Its Cytotoxic Payload Monomethyl Auristatin E in Tumor Cells

(2019) Peggy Liu-Kreyche et al.   Frontiers in Pharmacology

A Novel HER3-Targeting Antibody-Drug Conjugate, U3-1402, Exhibits Potent Therapeutic Efficacy through the Delivery of Cytotoxic Payload by Efficient Internalization

(2019) Yuuri Hashimoto et al.   CLINICAL CANCER RESEARCH

Antibody–drug conjugates for cancer

(2019) Cindy H Chau et al.   LANCET

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

Breast cancer

(2019) Nadia Harbeck et al.   Nature Reviews Disease Primers

Safety and Efficacy of T-DM1 Plus Neratinib in Patients With Metastatic HER2-Positive Breast Cancer: NSABP Foundation Trial FB-10

(2019) Jame Abraham et al.   JOURNAL OF CLINICAL ONCOLOGY

HER2, chromosome 17 polysomy and DNA ploidy status in breast cancer; a translational study

(2019) Altuna Halilovic et al.   Scientific Reports

NSABP B-47/NRG Oncology Phase III Randomized Trial Comparing Adjuvant Chemotherapy With or Without Trastuzumab in High-Risk Invasive Breast Cancer Negative for HER2 by FISH and With IHC 1+ or 2+

(2019) Louis Fehrenbacher et al.   JOURNAL OF CLINICAL ONCOLOGY

Trastuzumab Deruxtecan in Previously Treated HER2-Positive Breast Cancer

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

Phase I study of alpelisib (BYL-719) and trastuzumab emtansine (T-DM1) in HER2-positive metastatic breast cancer (MBC) after trastuzumab and taxane therapy

(2018) Sarika Jain et al.   BREAST CANCER RESEARCH AND TREATMENT

Anti-Trop2 antibody-conjugated bioreducible nanoparticles for targeted triple negative breast cancer therapy

(2018) Soyoung Son et al.   INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Neoadjuvant trastuzumab, pertuzumab, and chemotherapy versus trastuzumab emtansine plus pertuzumab in patients with HER2-positive breast cancer (KRISTINE): a randomised, open-label, multicentre, phase 3 trial

(2018) Sara A Hurvitz et al.   LANCET ONCOLOGY

A HER2-Targeting Antibody–Drug Conjugate, Trastuzumab Deruxtecan (DS-8201a), Enhances Antitumor Immunity in a Mouse Model

(2018) Tomomi Nakayama Iwata et al.   MOLECULAR CANCER THERAPEUTICS

Mechanisms of Acquired Resistance to Trastuzumab Emtansine in Breast Cancer Cells

(2018) Guangmin Li et al.   MOLECULAR CANCER THERAPEUTICS

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

HER2 genomic amplification in circulating tumor DNA and estrogen receptor positivity predict primary resistance to trastuzumab emtansine (T-DM1) in patients with HER2-positive metastatic breast cancer

(2018) Hitomi Sakai et al.   Breast Cancer

Metformin-induced caveolin-1 expression promotes T-DM1 drug efficacy in breast cancer cells

(2018) Yuan-Chiang Chung et al.   Scientific Reports

Phase ib study of trastuzumab emtansine (TDM1) in combination with lapatinib and nab-paclitaxel in metastatic HER2-neu overexpressed breast cancer patients: Stela results.

(2018) Tejal Amar Patel et al.   JOURNAL OF CLINICAL ONCOLOGY

Trastuzumab Emtansine for Residual Invasive HER2-Positive Breast Cancer

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

Trastuzumab Emtansine With or Without Pertuzumab Versus Trastuzumab Plus Taxane for Human Epidermal Growth Factor Receptor 2–Positive, Advanced Breast Cancer: Primary Results From the Phase III MARIANNE Study

(2017) Edith A. Perez et al.   JOURNAL OF CLINICAL ONCOLOGY

Trastuzumab emtansine versus capecitabine plus lapatinib in patients with previously treated HER2-positive advanced breast cancer (EMILIA): a descriptive analysis of final overall survival results from a randomised, open-label, phase 3 trial

(2017) Véronique Diéras et al.   LANCET ONCOLOGY

Trastuzumab emtansine versus treatment of physician's choice in patients with previously treated HER2-positive metastatic breast cancer (TH3RESA): final overall survival results from a randomised open-label phase 3 trial

(2017) Ian E Krop et al.   LANCET ONCOLOGY

Caveolae-Mediated Endocytosis as a Novel Mechanism of Resistance to Trastuzumab Emtansine (T-DM1)

(2017) Matthew Sung et al.   MOLECULAR CANCER THERAPEUTICS

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

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

Safety and efficacy of the addition of pertuzumab to T-DM1 ± taxane in patients with HER2-positive, locally advanced or metastatic breast cancer: a pooled analysis

(2017) Jing Zhang et al.   Drug Design Development and Therapy

HER2 in Breast Cancer Stemness: A Negative Feedback Loop towards Trastuzumab Resistance

(2017) et al.   Cancers

Trastuzumab emtansine (T-DM1) plus docetaxel with or without pertuzumab in patients with HER2-positive locally advanced or metastatic breast cancer: results from a phase Ib/IIa study

(2016) M. Martin et al.   ANNALS OF ONCOLOGY

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

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

Overcoming Therapeutic Resistance in HER2-Positive Breast Cancers with CDK4/6 Inhibitors

(2016) Shom Goel et al.   CANCER CELL

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

(2016) John Y. Li et al.   CANCER CELL

Neratinib induces ErbB2 ubiquitylation and endocytic degradation via HSP90 dissociation in breast cancer cells

(2016) Yingqiu Zhang et al.   CANCER LETTERS

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

TNFα-Induced Mucin 4 Expression Elicits Trastuzumab Resistance in HER2-Positive Breast Cancer

(2016) María F. Mercogliano et al.   CLINICAL CANCER RESEARCH

Relationship between Tumor Biomarkers and Efficacy in EMILIA, a Phase III Study of Trastuzumab Emtansine in HER2-Positive Metastatic Breast Cancer

(2016) J. Baselga et al.   CLINICAL CANCER RESEARCH

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

Relationship between tumor biomarkers and efficacy in TH3RESA, a phase III study of trastuzumab emtansine (T-DM1)vs. treatment of physician's choice in previously treated HER2-positive advanced breast cancer

(2016) Sung-Bae Kim et al.   INTERNATIONAL JOURNAL OF CANCER

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

Linkers Having a Crucial Role in Antibody–Drug Conjugates

(2016) Jun Lu et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Cell cycle checkpoint in cancer: a therapeutically targetable double-edged sword

(2016) Roberta Visconti et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Combining ABCG2 Inhibitors with IMMU-132, an Anti-Trop-2 Antibody Conjugate of SN-38, Overcomes Resistance to SN-38 in Breast and Gastric Cancers

(2016) C.-H. Chang et al.   MOLECULAR CANCER THERAPEUTICS

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

(2016) Kyoji Tsuchikama et al.   Protein & Cell

Lysosomal Physiology

(2015) Haoxing Xu et al.   Annual Review of Physiology

Sacituzumab Govitecan (IMMU-132), an Anti-Trop-2/SN-38 Antibody–Drug Conjugate: Characterization and Efficacy in Pancreatic, Gastric, and Other Cancers

(2015) Thomas M. Cardillo et al.   BIOCONJUGATE CHEMISTRY

Antibody-drug conjugates as novel anti-cancer chemotherapeutics

(2015) C. Peters et al.   BIOSCIENCE REPORTS

A novel humanized anti-HER2 antibody conjugated with MMAE exerts potent anti-tumor activity

(2015) Xuejing Yao et al.   BREAST CANCER RESEARCH AND TREATMENT

SLC46A3 Is Required to Transport Catabolites of Noncleavable Antibody Maytansine Conjugates from the Lysosome to the Cytoplasm

(2015) K. J. Hamblett et al.   CANCER RESEARCH

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

(2015) S.-F. Yu et al.   CLINICAL CANCER RESEARCH

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

Human IgG4: a structural perspective

(2015) Anna M. Davies et al.   IMMUNOLOGICAL REVIEWS

Preclinical Efficacy of Ado-trastuzumab Emtansine in the Brain Microenvironment

(2015) Vasileios Askoxylakis et al.   JNCI-Journal of the National Cancer Institute

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

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

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

An FDA oncology analysis of antibody-drug conjugates

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

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

(2015) Philipp Müller et al.   Science Translational Medicine

Preclinical Efficacy of Ado-trastuzumab Emtansine in the Brain Microenvironment

(2015) Vasileios Askoxylakis et al.   JNCI-Journal of the National Cancer Institute

Associations between UGT1A1*6 or UGT1A1*6/*28 polymorphisms and irinotecan-induced neutropenia in Asian cancer patients

(2014) Fei-fei Han et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

FDA Approval: Ado-Trastuzumab Emtansine for the Treatment of Patients with HER2-Positive Metastatic Breast Cancer

(2014) L. Amiri-Kordestani et al.   CLINICAL CANCER RESEARCH

A RAB5/RAB4 recycling circuitry induces a proteolytic invasive program and promotes tumor dissemination

(2014) Emanuela Frittoli et al.   JOURNAL OF CELL BIOLOGY

Trastuzumab emtansine versus treatment of physician's choice for pretreated HER2-positive advanced breast cancer (TH3RESA): a randomised, open-label, phase 3 trial

(2014) Ian E Krop et al.   LANCET ONCOLOGY

SGN-LIV1A: A Novel Antibody-Drug Conjugate Targeting LIV-1 for the Treatment of Metastatic Breast Cancer

(2014) D. Sussman et al.   MOLECULAR CANCER THERAPEUTICS

Dual Targeting of HER2-Positive Cancer with Trastuzumab Emtansine and Pertuzumab: Critical Role for Neuregulin Blockade in Antitumor Response to Combination Therapy

(2013) G. D. L. Phillips et al.   CLINICAL CANCER RESEARCH

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

(2013) Michael Ritchie et al.   mAbs

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

(2012) Hyesil Seol et al.   MODERN PATHOLOGY

Trastuzumab Emtansine for HER2-Positive Advanced Breast Cancer

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

A Traceless Vascular-Targeting Antibody-Drug Conjugate for Cancer Therapy

(2011) Gonçalo J. L. Bernardes et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Influence of Affinity and Antigen Internalization on the Uptake and Penetration of Anti-HER2 Antibodies in Solid Tumors

(2011) S. I. Rudnick et al.   CANCER RESEARCH

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

HER2 as a target for breast cancer therapy

(2010) Elda Tagliabue et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

Phase II Study of the Antibody Drug Conjugate Trastuzumab-DM1 for the Treatment of Human Epidermal Growth Factor Receptor 2 (HER2) –Positive Breast Cancer After Prior HER2-Directed Therapy

(2010) Howard A. Burris et al.   JOURNAL OF CLINICAL ONCOLOGY

B-Cell Depletion In Vitro and In Vivo with an Afucosylated Anti-CD19 Antibody

(2010) R. Herbst et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

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

(2009) Hans K. Erickson et al.   BIOCONJUGATE CHEMISTRY

Therapeutic potential of an anti-CD79b antibody-drug conjugate, anti-CD79b-vc-MMAE, for the treatment of non-Hodgkin lymphoma

(2009) D. Dornan et al.   BLOOD

Targeting HER2-Positive Breast Cancer with Trastuzumab-DM1, an Antibody-Cytotoxic Drug Conjugate

(2008) G. D. Lewis Phillips et al.   CANCER RESEARCH

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

(2008) Jagath R Junutula et al.   NATURE BIOTECHNOLOGY