Kit for the preparation of 111In-labeled pertuzumab injection for imaging response of HER2-positive breast cancer to trastuzumab (Herceptin)

Karen Lam; Deborah A Scollard; Conrad Chan; Mark N Levine; Raymond M Reilly

doi:10.1016/j.apradiso.2014.10.011

Kit for the preparation of ¹¹¹In-labeled pertuzumab injection for imaging response of HER2-positive breast cancer to trastuzumab (Herceptin)

Appl Radiat Isot. 2015 Jan:95:135-142. doi: 10.1016/j.apradiso.2014.10.011. Epub 2014 Oct 23.

Authors

Karen Lam¹, Deborah A Scollard², Conrad Chan¹, Mark N Levine³, Raymond M Reilly⁴

Affiliations

¹ Department of Pharmaceutical Sciences, University of Toronto, Ontario, Canada M5S 2M2.
² Department of Pharmaceutical Sciences, University of Toronto, Ontario, Canada M5S 2M2; STTARR Innovation Centre, University Health Network, Toronto, Ontario, Canada M5G 1L7.
³ Department of Oncology, Juravinski Cancer Centre, McMaster University, Hamilton, Ontario, Canada L8V 5C2.
⁴ Department of Pharmaceutical Sciences, University of Toronto, Ontario, Canada M5S 2M2; Department of Medical Imaging, University of Toronto, Ontario, Canada M5T 1W7; Toronto General Research Institute, University Health Network, Toronto, Ontario, Canada M5G 2M9. Electronic address: raymond.reilly@utoronto.ca.

PMID: 25464190
DOI: 10.1016/j.apradiso.2014.10.011

Abstract

We previously reported that ¹¹¹In-labeled pertuzumab imaged trastuzumab (Herceptin)-mediated changes in HER2 expression preclinically in breast cancer tumors. To advance ¹¹¹In-labeled pertuzumab to a Phase I/II clinical trial, a kit was designed for preparing this agent in a form suitable for human administration. Unit-dose kits containing pertuzumab modified with 2-(4-isothiocyanatobenzyl)-diethylenetriaminepentaacetic acid (BzDTPA) were prepared that labeled to high efficiency (>90%) with ¹¹¹In and met specifications for pharmaceutical quality. The kits were stable for 4 months and the final radiopharmaceutical was stable for 24h. Imaging studies demonstrated high and specific uptake in HER2-positive tumors in mice using this clinical kit formulation.

Keywords: Good manufacturing practices (GMP); HER2; Indium-111; Pertuzumab; Radiopharmaceutical kit.