title: Kit for the preparation of111In-labeled pertuzumab injection for imaging response of HER2-positive breast cancer to trastuzumab (Herceptin).
abstract: We previously reported that111In-labeled pertuzumab imaged trastuzumab (Herceptin)-mediated changes in HER2 expression preclinically in breast cancer tumors. To advance111In-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%) with111In 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.
authors.affiliation: Department of Pharmaceutical Sciences, University of Toronto, Ontario, Canada M5S 2M2.
authors.forename: Karen
authors.initials: K
authors.lastname: Lam
authors.affiliation: Department of Pharmaceutical Sciences, University of Toronto, Ontario, Canada M5S 2M2; STTARR Innovation Centre, University Health Network, Toronto, Ontario, Canada M5G 1L7.
authors.forename: Deborah A
authors.initials: DA
authors.lastname: Scollard
authors.affiliation: Department of Pharmaceutical Sciences, University of Toronto, Ontario, Canada M5S 2M2.
authors.forename: Conrad
authors.initials: C
authors.lastname: Chan
authors.affiliation: Department of Oncology, Juravinski Cancer Centre, McMaster University, Hamilton, Ontario, Canada L8V 5C2.
authors.forename: Mark N
authors.initials: MN
authors.lastname: Levine
authors.affiliation: 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.
authors.forename: Raymond M
authors.initials: RM
authors.lastname: Reilly
keywords: Good manufacturing practices (GMP); HER2; Indium-111; Pertuzumab; Radiopharmaceutical kit