IP Library › Granted Patent US 12,734,259
Granted Patent B2
US 12,734,259 · App. 19/392,245 · Granted Sep 15, 2026

Compounds comprising a fibroblast activation protein ligand and use thereof

Inventors: Frank Osterkamp (Berlin, DE); Dirk Zboralski (Berlin, DE); Eberhard Schneider (Brandenburg, DE); Christian Haase (Berlin, DE); Matthias Paschke (Berlin, DE); Aileen Höhne (Berlin, DE); Jan Ungewiss (Berlin, DE); Christiane Smerling (Berlin, DE); Ulrich Reineke (Berlin, DE); Anne Bredenbeck (Berlin, DE)
Assignee: 3B PHARMACEUTICALS GMBH
A61K51/088C07K7/08A61K38/00
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Quick Facts
Patent No.
US 12,734,259
App. No.
19/392,245
Filed
Nov 18, 2025
Granted
Sep 15, 2026
Kind
B2
Art Unit
1618
USPC
424/1.69
Abstract

The present invention is related to a compound comprising a cyclic peptide and a chelator, and its use.

Claims (39)

1 . A compound, which is:

or a pharmaceutically acceptable salt thereof, or a solvate thereof,

wherein 68 Ga is complexed to 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator of the compound.

2 . The compound of claim 1 , wherein the solvate is a hydrate.

3 . A compound:

wherein 68 Ga is complexed to 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator of the compound.

4 . A composition comprising the compound of claim 1 and a pharmaceutically acceptable excipient.

5 . A composition comprising the compound of claim 3 and a pharmaceutically acceptable excipient.

6 . A method of preparing the compound of claim 1 , comprising radiolabeling

or the pharmaceutically acceptable salt thereof, or the solvate thereof, with 68 Ga.

7 . A method of preparing the compound of claim 3 , comprising radiolabeling

with 68 Ga.

8 . A method of diagnosing a cancer in a patient in need thereof, comprising administering to the patient in need thereof a diagnostically effective amount of the compound of claim 1 .

9 . The method of claim 8 , further comprising imaging the patient.

10 . The method of claim 9 , wherein the imaging is performed using Positron Emission Tomography (PET) or a combination of PET with CT (PET/CT).

11 . A method of diagnosing a tumor in a patient in need thereof, comprising administering to the patient in need thereof a diagnostically effective amount of the compound of claim 1 .

12 . The method of claim 11 , further comprising imaging the patient.

13 . The method of claim 12 , wherein the imaging is performed using Positron Emission Tomography (PET) or a combination of PET with CT (PET/CT).

14 . A method of diagnosing a disease in a patient in need thereof, comprising administering to the patient in need thereof a diagnostically effective amount of the compound of claim 1 , wherein the disease is selected from the group consisting of bladder cancer, breast cancer, cervical cancer, colorectal cancer, cholangiocarcinoma, endometrial cancer, esophageal cancer, gastric cancer, gastrointestinal stromal tumors, head and neck cancer, liver cancer, lung cancer, melanoma, mesothelioma, neuroendocrine tumors and carcinomas, ovarian cancer, pancreatic cancer, prostate cancer, renal cell carcinoma, salivary carcinoma, sarcoma, squamous cell carcinoma, and thyroid cancer.

15 . A method of diagnosing a cancer in a patient in need thereof, comprising administering to the patient in need thereof a diagnostically effective amount of the compound of claim 3 .

16 . The method of claim 15 , further comprising imaging the patient.

17 . The method of claim 16 , wherein the imaging is performed using Positron Emission Tomography (PET) or a combination of PET with CT (PET/CT).

18 . A method of diagnosing a tumor in a patient in need thereof, comprising administering to the patient in need thereof a diagnostically effective amount of the compound of claim 3 .

19 . The method of claim 18 , further comprising imaging the patient.

20 . The method of claim 19 , wherein the imaging is performed using Positron Emission Tomography (PET) or a combination of PET with CT (PET/CT).

21 . The method of claim 18 , wherein the tumor is a solid tumor.

22 . The method of claim 18 , wherein the tumor is an epithelial tumor.

23 . A method of diagnosing a disease in a patient in need thereof, comprising administering to the patient in need thereof a diagnostically effective amount of a compound:

wherein 68 Ga is complexed to 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator of the compound, and

wherein the disease is breast cancer, non-small cell lung cancer, pancreatic cancer, or bladder cancer.

24 . The method of claim 23 , wherein the disease is breast cancer.

25 . The method of claim 23 , wherein the disease is non-small cell lung cancer.

26 . The method of claim 23 , wherein the disease is pancreatic cancer.

27 . The method of claim 23 , wherein the disease is bladder cancer.

28 . The method of claim 23 , further comprising imaging the patient.

29 . The method of claim 28 , wherein the imaging is performed using Positron Emission Tomography (PET) or a combination of PET with CT (PET/CT).

30 . A kit comprising:

 or a pharmaceutically acceptable salt thereof; and

instructions to label with 68 Ga for preparation of the compound of claim 1 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 10, 2026
From: OSTERKAMP, FRANK; ZBORALSKI, DIRK; SCHNEIDER, EBERHARD; HAASE, CHRISTIAN; PASCHKE, MATTHIAS; HÖHNE, AILEEN; UNGEWISS, JAN; SMERLING, CHRISTIANE; REINEKE, ULRICH; BREDENBECK, ANNE
To: 3B PHARMACEUTICALS GMBH
Reel/Frame 074336/0064 →
Priority Claims (2)
EP 19000325 · Jul 8, 2019 · regional
EP 19198813 · Sep 20, 2019 · regional
Continuity (3)
Continuation 19328329 · Sep 15, 2025
Continuation 17625139 · Jul 8, 2020
Related Publication 20260061086A1 · Mar 5, 2026
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