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HER3 as a Therapeutic Target in Cancer

BioDrugs volume 31, pages 63–73 (2017)Cite this article

Abstract

Targeting members of the human epidermal growth factor receptor family, especially EGFR and HER2, has been an established strategy for the treatment of tumors with abnormally activated receptors due to overexpression, mutation, ligand-dependent receptor dimerization and ligand-independent activation. Less attention has been paid to the oncogenic activity of HER3, although there is growing evidence that it mediates resistance to EGFR and HER2 pathway directed therapies. The main caveat for the development of effective HER3 targeted therapies is the absence of a strong enzymatic activity to target, as well as the limited potential for single-agent activity. In this review, we highlight the role of HER3 in cancer and, more specifically, in lung cancer. The basis for HER3 involvement in HER2 resistance and EGFR inhibition is discussed, as well as current pharmacologic strategies to combat HER3 inhibition.

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Authors and Affiliations

  1. Medical Oncology Department, Institute of Oncology Rosell (IOR), University Hospital Sagrat Cor, C/Viladomat 288, 08029, Barcelona, Spain

    Niki Karachaliou & Aaron E. Sosa

  2. Departmemt of Oncology, Division of Experimental Medicine, IRCCS San Raffaele Hospital, Milan, Italy

    Chiara Lazzari

  3. Ospedale Santa Maria delle Croci, Ravenna, Italy

    Alberto Verlicchi

  4. Germans Trias i Pujol Research Institute, Badalona, Spain

    Rafael Rosell

  5. Catalan Institute of Oncology, Germans Trias i Pujol University Hospital, Badalona, Spain

    Rafael Rosell

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  1. Niki Karachaliou
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  2. Chiara Lazzari
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  3. Alberto Verlicchi
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  4. Aaron E. Sosa
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  5. Rafael Rosell
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Corresponding author

Correspondence to Niki Karachaliou.

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NK, CL, AV, AS and RR declare no conflicts of interest.

Funding

This work was funded by La Caixa Foundation and Red Tematica de Investigacion Cooperativa en Cancer (RTICC; Grant RD12/0036/0072).

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Karachaliou, N., Lazzari, C., Verlicchi, A. et al. HER3 as a Therapeutic Target in Cancer. BioDrugs 31, 63–73 (2017). https://doi.org/10.1007/s40259-016-0205-2

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Keywords

  • Epidermal Growth Factor Receptor
  • Trastuzumab
  • Human Epidermal Growth Factor Receptor
  • Gefitinib
  • Erlotinib