HER dimerization inhibitors: Developing pertuzumab as an anticancer agent in women's oncology

Don S. Dizon, Sharmila Makhija

Research output: Contribution to journalArticlepeer-review

1 Scopus citations


Background: Pertuzumab is a novel monoclonal antibody that blocks the dimerization domain of the human epidermal growth factor receptor (HER)-2/neu receptor, disabling its ability to form heterodimers with the other members of its family. Objective: We review the background and scientific rationale, but more specifically cover current clinical trial outcomes of pertuzumab in solid tumors, with an emphasis on the work completed in women's cancers. Methods: Clinical trial results published or presented at national meetings are included in this review. Results: Pertuzumab shows promising activity with trastuzumab in the treatment of metastatic breast cancer. The results in ovarian cancer have been limited thus far but a post hoc analysis of the results of a completed randomized Phase II trial of gemcitabine with or without pertuzumab suggests that low HER3 levels may mark a group of women who may benefit from the addition of pertuzumab to chemotherapy. Conclusions: The efficacy of pertuzumab independent of HER-2/neu overexpression remains under investigation. Still, the benefits seen in HER-2/neu positive breast cancer is encouraging. Work in ovarian cancer remains preliminary but the possibility of using pertuzumab in a targeted population with low HER3 levels warrants further evaluation.

Original languageEnglish (US)
Pages (from-to)1363-1369
Number of pages7
JournalExpert Opinion on Drug Discovery
Issue number11
StatePublished - Nov 2008
Externally publishedYes


  • Breast cancer
  • EGFR pathway
  • HER dimerization inhibitors
  • HER-2/neu
  • Ovarian cancer

ASJC Scopus subject areas

  • Drug Discovery


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