Dual mode 18F-labelled theranostic compounds and uses thereof

Patent metadata

Field	Value
Publication number	US-12427209-B2
Application number	US-201917415649-A
Country	US
Kind code	B2
Filing date	Dec 18, 2019
Priority date	Dec 18, 2018
Publication date	Sep 30, 2025
Grant date	Sep 30, 2025

Abstract

A compound or molecular complex. The compound or molecular complex comprises: a metal chelator configured for chelation with a radioactive isotope or a non-radioactive isotope; and a trifluoroborate (BF 3 )-containing moiety configured for 19 F/ 18 F exchange or a precursor thereof; and optionally a cell-targeting domain.

First claim

The invention claimed is:

1. A compound or molecular complex comprising:
a metal chelator configured for chelation with a radioactive metal isotope or a non-radioactive metal isotope;
a cell-targeting domain; and
a trifluoroborate (BF 3 )-containing moiety configured for 19 F/ 18 F exchange or a boronate precursor that is capable of conversion to an 18 F-labeled trifluoroborate;
wherein the compound or molecular complex is selected from the group consisting of:

2. A method of imaging and treating a disease or condition in a subject, the method comprising:
(i) administering a compound or molecular complex according to claim 1 to the subject, wherein the BF 3 -containing moiety of the compound or molecular complex is labelled with 18 F, the metal chelator of the compound or molecular complex is chelated with a radioactive metal isotope or a non-radioactive metal isotope, and the cell targeting domain targets a cellular marker of the disease or condition, and imaging the subject to confirm the presence of the cellular marker; and
(ii) administering the compound or molecular complex to the subject, wherein the BF 3 -containing moiety is labeled with 19 F and/or 18 F, and the metal chelator is chelated with a therapeutic radioactive isotope.

3. A method of imaging and/or treating a disease or condition in a subject using a compound or molecular complex according to claim 1 in combination with a bispecific antibody, wherein the bispecific antibody is specific for both a cellular marker of the disease or condition and the metal chelator of the compound or molecular complex, the method comprising administering the bispecific antibody to the subject and one or both of the following steps:
(i) administering the compound or molecular complex to the subject wherein the BF 3 containing moiety of the compound or molecular complex is labelled with 18 F, wherein the metal chelator of the compound or molecular complex is chelated with a radioactive metal isotope or a non-radioactive metal isotope, and imaging the subject to confirm the presence of the cellular marker
(ii) administering the compound or molecular complex to the subject, wherein the BF 3 -containing moiety is labeled with 19 F and/or 18 F, and the metal chelator is chelated with a therapeutic radioactive isotope.

4. The method of claim 3 , wherein the compound or molecular complex is administered to the subject as a complex with the bispecific antibody.

5. The method of claim 3 , wherein the bispecific antibody is administered to the subject prior to administering the compound or molecular complex to the subject in a pre-targeting step during which the bispecific antibody binds to the cellular marker.

Assignees

• Provincial Health Services Authority
• Univ British Columbia

Inventors

• Perrin David
• Roxin Aron
• Lepage Mathieu
• Huh Sungjoon
• Liu Zhibo
• Kandasamy Rajaguru
• Benard Francois
• Lin Kuo-Shyan
• Kuo Hsiou-Ting
• Zhang Chengcheng

Classifications

• C07F5/027

  Organoboranes and organoborohydrides · CPC title

• A61K51/083

  the peptide being octreotide or a somatostatin-receptor-binding peptide · CPC title

• C07B59/002

  Heterocyclic compounds · CPC title

• A61K51/088 Primary

  conjugates with carriers being peptides, polyamino acids or proteins (antibodies A61K51/10) · CPC title

• A61K51/048

  DTPA (diethylenetriamine tetraacetic acid) · CPC title