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Int J Mol Sci. 2019 Mar 5;20(5). pii: E1115. doi: 10.3390/ijms20051115.

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

Author information

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. g.rinnerthaler@salk.at.
2
Cancer Cluster Salzburg, 5020 Salzburg, Austria. g.rinnerthaler@salk.at.
3
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. s.gampenrieder@salk.at.
4
Cancer Cluster Salzburg, 5020 Salzburg, Austria. s.gampenrieder@salk.at.
5
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. r.greil@salk.at.
6
Cancer Cluster Salzburg, 5020 Salzburg, Austria. r.greil@salk.at.

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.

KEYWORDS:

(vic-)trastuzumab duocarmazine; ADC; HER2 low; HM2-MMAE; TAK-522; Trastuzumab deruxtecan; Trastuzumab emtansine; anti-HER2/PBD-MA; mode of action

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