A proposed production method for astatinated (At-211) Trastuzumab for use in a Phase I clinical trial

Abstract

Astatine-211 is a nuclide with a short half-life of 7.2 h, that show promise for targeted alpha therapy of disseminated cancer. Despite nuclide production being straight-forward using a medium energy cyclotron and an uncomplicated target, not many cyclotrons are currently producing the nuclide. In this work we propose a stream-lined method to produce astatine labelled antibodies that enable production of clinical doses at other sites, remote from the nuclide producing cyclotron. Preconjugating the antibody prior to labelling, quick and efficient astatine recovery from the irradiated target in combination with optimized nuclide production logistics and an efficient synthesis for labelling are all key components to produce a clinical amount, > 300 MBq, of astatinated Trastuzumab.