Preclinical comparison of four [¹⁸F, ^natGa]rhPSMA-7 isomers: influence of the stereoconfiguration on pharmacokinetics.

ABSTRACT:

Introduction

Radiohybrid (rh) ligands, a novel class of prostate-specific membrane antigen (PSMA)-targeted radiopharmaceuticals, can be labeled either with [¹⁸F]fluorine via isotopic exchange or with radiometals (such as [⁶⁸Ga]Gallium, [¹⁷⁷Lu]Lutetium, [²²⁵Ac]Actinium). Among these, [¹⁸F, ^natGa]rhPSMA-7 has recently entered clinical assessment.

Aim

Since [¹⁸F, ^natGa]rhPSMA-7 is composed of four stereoisomers ([¹⁸F, ^natGa]rhPSMA-7.1, -7.2, -7.3 and -7.4), we initiated a preclinical selection process to identify the isomer with the most favorable pharmacokinetics for further clinical investigation.

Methods

A synthetic protocol for enantiopure [¹⁹F,

SUBMITTER: Wurzer A 

PROVIDER: S-EPMC7721954 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature