	US 12,390,540 B2
	Dual mode radiotracer and -therapeutics
Alexander Josef Wurzer, Munich (DE); Hans-Jürgen Wester, Ilmmünster (DE); and Matthias Johannes Eiber, Vaterstetten (DE)
Assigned to Technische Universität München, Munich (DE); and Technische Universität München—Klinikum Rechts der Isar, Munich (DE)
Filed by Technische Universität München, Munich (DE); and Technische Universität München—Klinikum Rechts der Isar, Munich (DE)
Filed on Jun. 24, 2022, as Appl. No. 17/849,297.
Application 17/849,297 is a continuation of application No. 16/634,759, granted, now 11,413,360, previously published as PCT/EP2018/070533, filed on Jul. 30, 2018.
Claims priority of application No. 17183795 (EP), filed on Jul. 28, 2017.
Prior Publication US 2022/0370649 A1, Nov. 24, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 51/04 (2006.01)

CPC A61K 51/0497 (2013.01) [A61K 51/0402 (2013.01); A61K 51/0482 (2013.01)]

16 Claims

1. A ligand-SIFA-chelator conjugate, comprising, within in a single molecule three separate moieties:

(a) one or more ligands which are capable of binding to prostate-specific membrane antigen (PSMA),

(b) a silicon-fluoride acceptor (SIFA) moiety which comprises a covalent bond between a silicon and a fluorine atom and which can be labelled with ¹⁸F by isotopic exchange of ¹⁹F by ¹⁸F or which is labelled with ¹⁸F, and

(c) one or more chelating groups, optionally containing a chelated nonradioactive or radioactive cation, wherein the one or more chelating groups comprises a hydrophilic chelator;

wherein the conjugate is formulated for in vivo administration for nuclear diagnostic imaging or targeted radiotherapy of a disease associated with an overexpression of prostate-specific membrane antigen.