Summary
Expert Opinion on Drug Discovery
November 2008, Vol. 3, No. 11, Pages 1363-1369 , DOI 10.1517/17460441.3.11.1363
HER dimerization inhibitors: developing pertuzumab as an anticancer agent in women's oncology
Don S Dizon
*
†1 MD FACP & Sharmila Makhija
*
2 MD
1Warren Alpert Medical School of Brown University, Women & Infants Hospital of Rhode Island, Program in Women's Oncology, 101 Dudley Street, RI 02905, Providence, USA +1 401 453 7520; +1 401 453 7529;
ddizon@wihri.org
2Emory University, Division of Gynecologic Oncology, Department of Obstetrics-Gynecology, Atlanta, GA, USA
†
Author for correspondence
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.
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