Pretargeting of internalizing trastuzumab and cetuximab with a 18F-tetrazine tracer in xenograft models.

ABSTRACT: BACKGROUND:Pretargeting-based approaches are being investigated for radioimmunoimaging and therapy applications to reduce the effective radiation burden to the patient. To date, only a few studies have used short-lived radioisotopes for pretargeting of antibodies, and such examples with internalizing antibodies are even rarer. Herein, we have investigated pretargeting methodology using inverse electron-demand Diels-Alder (IEDDA) for tracing two clinically relevant, internalizing monoclonal antibodies, cetuximab and trastuzumab. RESULTS:Bioorthogonal reaction between tetrazine and trans-cyclooctene (TCO) was used for tracing cetuximab and trastuzumab in vivo with a fluorine-18 (t ½ = 109.8 min) labelled tracer. TCO-cetuximab or TCO-trastuzumab was administered 24, 48, or 72 h prior to the i

SUBMITTER: Keinanen O 

PROVIDER: S-EPMC5712296 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature