Next Article in Journal
Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate
Previous Article in Journal
Extracellular Vesicles from Thyroid Carcinoma: The New Frontier of Liquid Biopsy
Previous Article in Special Issue
Targeting Multiple Receptors to Increase Checkpoint Blockade Efficacy
Article Menu
Issue 5 (March-1) cover image

Export Article

Open AccessReview

HER2 Directed Antibody-Drug-Conjugates beyond T-DM1 in Breast Cancer

1
Department of Internal Medicine III with Haematology, Medical Oncology, Haemostaseology, Infectiology and Rheumatology, Oncologic Center, Salzburg Cancer Research Institute—Laboratory for Immunological and Molecular Cancer Research (SCRI-LIMCR), Paracelsus Medical University Salzburg, 5020 Salzburg, Austria
2
Cancer Cluster Salzburg, 5020 Salzburg, Austria
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(5), 1115; https://doi.org/10.3390/ijms20051115
Received: 3 February 2019 / Revised: 24 February 2019 / Accepted: 26 February 2019 / Published: 5 March 2019
(This article belongs to the Special Issue Receptor-Targeted Cancer Therapy)
  |  
PDF [371 KB, uploaded 12 March 2019]
  |     |  

Abstract

Since the discovery of the human epidermal growth factor receptor 2 (HER2) as an oncogenic driver in a subset of breast cancers and the development of HER2 directed therapies, the prognosis of HER2 amplified breast cancers has improved meaningfully. Next to monoclonal anti-HER2 antibodies and tyrosine kinase inhibitors, the antibody-drug conjugate T-DM1 is a pillar of targeted treatment of advanced HER2-positive breast cancers. Currently, several HER2 directed antibody-drug conjugates are under clinical investigation for HER2 amplified but also HER2 expressing but not amplified breast tumors. In this article, we review the current preclinical and clinical evidence of the investigational drugs A166, ALT-P7, ARX788, DHES0815A, DS-8201a, RC48, SYD985, MEDI4276 and XMT-1522. View Full-Text
Keywords: ADC; HM2-MMAE; (vic-)trastuzumab duocarmazine; Trastuzumab deruxtecan; TAK-522; Trastuzumab emtansine; anti-HER2/PBD-MA; HER2 low; mode of action ADC; HM2-MMAE; (vic-)trastuzumab duocarmazine; Trastuzumab deruxtecan; TAK-522; Trastuzumab emtansine; anti-HER2/PBD-MA; HER2 low; mode of action
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
SciFeed

Share & Cite This Article

MDPI and ACS Style

Rinnerthaler, G.; Gampenrieder, S.P.; Greil, R. HER2 Directed Antibody-Drug-Conjugates beyond T-DM1 in Breast Cancer. Int. J. Mol. Sci. 2019, 20, 1115.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top