IP Library › Granted Patent US 12,622,984
Granted Patent B2
US 12,622,984 · App. 18/477,509 · Granted May 12, 2026

High purity copper radiopharmaceutical compositions and diagnostic and therapeutic uses thereof

Inventors: Leila Jaafar-Thiel (Erlangen, DE); Melpomeni Fani (Basel, CH); Jacopo Millul (Basel, CH); Francesco De Rose (Munich, DE)
Assignees: Nuclidium AG; University of Basel
A61K51/0482A61B5/055A61K31/30A61K51/0455A61K51/0459A61K51/083A61K51/088C07B59/002A61K2121/00A61K2123/00C07B2200/05
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Quick Facts
Patent No.
US 12,622,984
App. No.
18/477,509
Granted
May 12, 2026
Kind
B2
Abstract

The present disclosure relates to the field of nuclear imaging and therapy, and more specifically to high purity copper radiotracer compositions useful in imaging, such as positron emission tomography (PET) and single-photon emission computerized tomography (SPECT), and therapy. More specifically, the present disclosure relates to novel compositions useful in imaging and treatment of conditions such as prostate cancer, somatostatin receptor-expressing tumors, like neuroendocrine tumor, epithelial tumors, as well as to methods wherein such compositions are prepared.

Claims (201)

1 . A pharmaceutical composition comprising a compound and a pharmaceutically acceptable excipient, wherein the compound is of Formula 30:

or is a pharmaceutically acceptable salt thereof;

wherein:

R 1 is R a ;

R 2 and R 3 are each R a or together form a C 2-9 heterocycle with the nitrogen atoms to which they are attached;

R a , independently for each occurrence, is selected from H, C 1-10 alkyl, C 2-10 alkenyl, C 3-10 alkynyl, C 3-10 cycloalkyl, C 6-10 aryl, C 2-9 heterocyclyl, or C 5-9 heteroaryl, wherein each C 1-10 alkyl, C 2-10 alkenyl, C 3-10 alkynyl, C 3-10 cycloalkyl, C 6-10 aryl, C 2-9 heterocyclyl, or C 5-9 heteroaryl is optionally substituted by one or more substituents selected from —OH, —OR′, ═O, ═S, —SH, —SR′, —NH 2 , —NHR′, —N(R′) 2 , —NHCOR′, —NR′COR′, halogen, —CN, —CO 2 H, —CO 2 R′, —CHO, —COR′, —CONH 2 , —CONHR′, —CON(R′) 2 , —NO 2 , —OP(O)(OH) 2 , —SO 3 H, —SO 3 R′, —SOR′, and —SO 2 R′, wherein R′, independently for each occurrence, is C 1-10 alkyl or C 3-10 cycloalkyl;

n is an integer from 1 to 20;

m is an integer from 1 to 20; and

*Cu is 61 Cu obtained by deuteron irradiation of nat Ni or 60 Ni on a niobium backing or by proton irradiation of 61 Ni on a niobium backing; and

wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%;

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%;

(c) the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤6000 Bq/g;

(d) the 61 Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%; or

(e) the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤800 Bq/g and 58 Co activity concentration of ≤800 Bq/g.

2 . The composition of claim 1 , wherein R 1 is methyl or H.

3 . The composition of claim 1 , wherein R 2 is H and R 3 is H.

4 . The composition of claim 1 , wherein R 2 and R 3 together form a C 2-9 heterocycle with the nitrogen atoms to which they are attached.

5 . The composition of claim 4 , wherein the C 2-9 heterocycle is a 6-membered heterocycle selected from a piperazine, hexahydropyrimidine, hexahydropyridazine, 1,2,3-triazinane, 1,2,4-triazinane, and 1,3,5-triazinane.

6 . The composition of claim 1 , wherein the compound of Formula 30 is of Formula 30a or Formula 30b:

7 . The composition of claim 6 , wherein R 1 is H or methyl.

8 . The composition of claim 1 , wherein the compound is selected from:

Compound

Structure

*Cu-NODAGA-F1

*Cu-NODAGA-F2

*Cu-NODAGA-F3

*Cu-NODAGA-F4

or is a pharmaceutically acceptable salt thereof.

9 . The composition of claim 1 , wherein the composition is characterized at end of synthesis by radiochemical purity of ≥97%.

10 . The composition of claim 1 , wherein the composition is characterized at end of synthesis by radiochemical purity of ≥98%.

11 . The composition of claim 1 , wherein the composition is characterized at end of synthesis by radiochemical purity of ≥99%.

12 . The composition of claim 1 , wherein the composition has a pH from 4 to 7.

13 . A method of generating one or more images of a subject comprising:

administering to the subject an effective amount of the composition of claim 1 ; and

generating one or more images of at least a part of the subject's body.

14 . The method of claim 13 , wherein the one or more images are generated using positron emission tomography (PET), PET-computer tomography (PET-CT), or single-photon emission computerized tomography (SPECT).

15 . The method of claim 14 , wherein the one or more images are generated using PET-CT.

16 . A theranostic method comprising:

(a) administering to a subject an effective amount of a first pharmaceutical composition, wherein the composition is according to claim 1 ;

(b) generating one or more images of at least a part of the subject's body; and

(c) administering to the subject an effective amount of a second pharmaceutical composition comprising a compound, wherein the compound is of Formula 30:

or is a pharmaceutically acceptable salt thereof;

wherein:

R 1 is R a ;

R 2 and R 3 are each R a or together form a C 2-9 heterocycle with the nitrogen atoms to which they are attached;

R a , independently for each occurrence, is selected from H, C 1-10 alkyl, C 2-10 alkenyl, C 3-10 alkynyl, C 3-10 cycloalkyl, C 6-10 aryl, C 2-9 heterocyclyl, or C 5-9 heteroaryl, wherein each C 1-10 alkyl, C 2-10 alkenyl, C 3-10 alkynyl, C 3-10 cycloalkyl, C 6-10 aryl, C 2-9 heterocyclyl, or C 5-9 heteroaryl is optionally substituted by one or more substituents selected from —OH, —OR′, ═O, ═S, —SH, —SR′, —NH 2 , —NHR′, —N(R′) 2 , —NHCOR′, —NR′COR′, halogen, —CN, —CO 2 H, —CO 2 R′, —CHO, —COR′, —CONH 2 , —CONHR′, —CON(R′) 2 , —NO 2 , —OP(O)(OH) 2 , —SO 3 H, —SO 3 R′, —SOR′, and —SO 2 R′, wherein R′, independently for each occurrence, is C 1-10 alkyl or C 3-10 cycloalkyl;

n is an integer from 1 to 20;

m is an integer from 1 to 20; and

*Cu is 67 Cu.

17 . The method of claim 16 , wherein:

the compound of the first pharmaceutical composition is [ 61 Cu]Cu-NODAGA-F1 and the compound of the second pharmaceutical composition is [ 67 Cu]Cu-NODAGA-F1;

the compound of the first pharmaceutical composition is [ 61 Cu]Cu-NODAGA-F2 and the compound of the second pharmaceutical composition is [ 67 Cu]Cu-NODAGA-F2;

the compound of the first pharmaceutical composition is [ 61 Cu]Cu-NODAGA-F3 and the compound of the second pharmaceutical composition is [ 67 Cu]Cu-NODAGA-F3; or

the compound of the first pharmaceutical composition is [ 61 Cu]Cu-NODAGA-F4 and the compound of the second pharmaceutical composition is [ 67 Cu]Cu-NODAGA-F4.

18 . The method of claim 16 , further comprising determining, via the one or more images of the subject, the presence or absence of a disease in the subject based on the presence or absence of localization of the 61 Cu radionuclide of the first pharmaceutical composition in the subject's body.

19 . The method of claim 18 , wherein the disease is selected from cancers, inflammatory diseases, infectious diseases, and immune diseases.

20 . The method of claim 16 , wherein the one or more images are generated by using positron emission tomography (PET), PET-computer tomography (PET-CT), or single-photon emission computerized tomography (SPECT).

21 . The composition of claim 1 , wherein the composition at end of synthesis is characterized by one or more of:

a 100m Ag specific activity ≤0.1 Bq/g;

a 108m Ag specific activity ≤0.1 Bq/g; or

a 109 Cd specific activity ≤0.1 Bq/g.

22 . The composition of claim 1 , wherein the composition at end of synthesis is characterized by having:

a 56 Co specific activity ≤1500 Bq/g;

a 57 Co specific activity ≤100 Bq/g;

a 58 Co specific activity ≤15000 Bq/g; and

a 6° co specific activity ≤15 Bq/g.

23 . The composition of claim 1 , wherein the chemical purity of the composition at end of synthesis is characterized by having

Al≤1.1 ng/MBq;

Co≤0.2 ng/MBq;

Fe≤1.6 ng/MBq;

Pb≤0.7 ng/MBq; or

Zn≤0.7 ng/MBq.

24 . The composition of claim 1 , wherein the composition at end of synthesis is characterized by activity concentration of ≥8 MBq/mL.

25 . The composition of claim 1 , wherein the composition at end of synthesis is characterized by activity concentration of 8-15 MBq/mL.

26 . The composition of claim 1 , wherein the 61 Cu is characterized at end of synthesis by radionuclidic purity of ≥99.9999%.

27 . The composition of claim 1 , wherein the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤80 Bq/g.

28 . The composition of claim 1 , wherein the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤8 Bq/g.

29 . The composition of claim 1 , wherein the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤4000 Bq/g.

30 . The composition of claim 7 , wherein the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤2000 Bq/g.

31 . The composition of claim 1 , wherein the compound is

or is a pharmaceutically acceptable salt thereof.

32 . The compound of claim 7 , wherein the compound is

or is a pharmaceutically acceptable salt thereof.

33 . The compound of claim 1 , wherein the compound is

or is a pharmaceutically acceptable salt thereof.

34 . The compound of claim 1 , wherein the compound is

or is a pharmaceutically acceptable salt thereof.

35 . A method of detecting a FAP-overexpressing cancer in a human subject, the method comprising:

administering to the subject an effective amount of the composition of claim 1 ; and

generating one or more images of a part of a subject's body.

36 . The method of claim 35 , wherein the cancer is selected from non-small cell lung cancer, triple-negative breast cancer, colorectal carcinoma, gastric cancer, ovarian cancer, and pancreatic cancer.

37 . The composition of claim 1 , wherein the composition is characterized at end of synthesis by radiochemical purity of ≥95%.

38 . The composition of claim 1 , wherein the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%.

39 . The composition of claim 1 , wherein the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤6000 Bq/g.

40 . The composition of claim 1 , wherein the 61 Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%.

41 . The composition of claim 1 , wherein the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤800 Bq/g and 58 Co activity concentration of ≤800 Bq/g.

42 . The composition of claim 1 , wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%;

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%;

(c) the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤6000 Bq/g;

(d) the 61 Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%; and

(e) the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤800 Bq/g and 58 Co activity concentration of ≤800 Bq/g.

43 . The composition of claim 1 , wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%;

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%;

(d) the 61 Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%; and

(e) the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤800 Bq/g and 58 Co activity concentration of ≤800 Bq/g.

44 . The composition of claim 1 , wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%;

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%;

(c) the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤6000 Bq/g; and

(d) the 61 Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%.

45 . The composition of claim 1 , wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%;

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%; and

(d) the 61 Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%.

46 . The composition of claim 1 , wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%; and

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%.

47 . The composition of claim 8 , wherein the composition is characterized at end of synthesis by radiochemical purity of ≥97%.

48 . The composition of claim 8 , wherein the composition is characterized at end of synthesis by radiochemical purity of ≥98%.

49 . The composition of claim 8 , wherein the composition is characterized at end of synthesis by radiochemical purity of ≥99%.

50 . The composition of claim 8 , wherein the composition has a pH from 4 to 7.

51 . The composition of claim 8 , wherein the composition at end of synthesis is characterized by one or more of:

a 110m Ag specific activity ≤0.1 Bq/g;

a 108m Ag specific activity ≤0.1 Bq/g; or

a 109 Cd specific activity ≤0.1 Bq/g.

52 . The composition of claim 8 , wherein the composition at end of synthesis is characterized by having:

a 56 Co specific activity ≤1500 Bq/g;

a 57 Co specific activity ≤100 Bq/g;

a 58 Co specific activity ≤15000 Bq/g; and

a 6O Co specific activity ≤15 Bq/g.

53 . The composition of claim 8 , wherein the chemical purity of the composition at end of synthesis is characterized by having

Al≤1.2 ng/MBq;

Co≤0.2 ng/MBq;

Fe≤1.7 ng/MBq;

Pb≤0.8 ng/MBq; or

Zn≤0.8 ng/MBq.

54 . The composition of claim 8 , wherein the composition at end of synthesis is characterized by activity concentration of ≥8 MBq/mL.

55 . The composition of claim 8 , wherein the composition at end of synthesis is characterized by activity concentration of 8-15 MBq/mL.

56 . The composition of claim 8 , wherein the 61 Cu is characterized at end of synthesis by radionuclidic purity of ≥99.9999%.

57 . The composition of claim 8 , wherein the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤80 Bq/g.

58 . The composition of claim 8 , wherein the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤8 Bq/g.

59 . The composition of claim 8 , wherein the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤4000 Bq/g.

60 . The composition of claim 8 , wherein the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤2000 Bq/g.

61 . The composition of claim 8 , wherein the composition is characterized at end of synthesis by radiochemical purity of ≥95%.

62 . The composition of claim 8 , wherein the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%.

63 . The composition of claim 8 , wherein the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤6000 Bq/g.

64 . The composition of claim 8 , wherein the 61 Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%.

65 . The composition of claim 8 , wherein the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤800 Bq/g and 58 Co activity concentration of ≤800 Bq/g.

66 . The composition of claim 8 , wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%;

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%;

(c) the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤6000 Bq/g;

(d) the 61 Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%; and

(e) the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤800 Bq/g and 58 Co activity concentration of ≤800 Bq/g.

67 . The composition of claim 8 , wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%;

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%;

(d) the 61 Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%; and

(e) the 61 Cu is characterized at end of synthesis by 56 Co activity concentration of ≤800 Bq/g and 58 Co activity concentration of ≤800 Bq/g.

68 . The composition of claim 8 , wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%;

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%;

(c) the 61 Cu is characterized at end of synthesis by sum of radionuclidic impurities of ≤6000 Bq/g; and

(d) the 61 Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%.

69 . The composition of claim 8 , wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%;

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61Cu on 99.999%;and

(d) the 61Cu is characterized at end of synthesis +12 hours by radionuclidic purity of ≥99.985%.

70 . The composition of claim 8 , wherein

(a) the composition is characterized at end of synthesis by radiochemical purity of ≥95%; and

(b) the composition is characterized at end of synthesis by radionuclidic purity for 61 Cu of ≥99.999%.

71 . A method of generating one or more images of a subject comprising: administering to the subject an effective amount of the composition of claim 8 ; and generating one or more images of at least a part of the subject's body.

72 . The method of claim 71 , wherein the one or more images are generated using positron emission tomography (PET), PET-computer tomography (PET-CT), or single-photon emission computerized tomography (SPECT).

73 . The method of claim 72 , wherein the one or more images are generated using PET-CT.

74 . A theranostic method comprising:

(a) administering to a subject an effective amount of a first pharmaceutical composition, wherein the composition is according to claim 8 ;

(b) generating one or more images of at least a part of the subject's body; and

(c) administering to the subject an effective amount of a second pharmaceutical composition comprising a compound, wherein the compound is of Formula 30:

or is a pharmaceutically acceptable salt thereof;

wherein:

R 1 is R a ;

R 2 and R 3 are each R a or together form a C 2-9 heterocycle with the nitrogen atoms to which they are attached;

R a , independently for each occurrence, is selected from H, C 1-10 alkyl, C 2-10 alkenyl, C 3-10 alkynyl, C 3-10 cycloalkyl, C 6-10 aryl, C 2-9 heterocyclyl, or C 5-9 heteroaryl, wherein each C 1-10 alkyl, C 2-10 alkenyl, C 3-10 alkynyl, C 3-10 cycloalkyl, C 6-10 aryl, C 2-9 heterocyclyl, or C 5-9 heteroaryl is optionally substituted by one or more substituents selected from —OH, —OR', ═O, ═S, —SH, —SR', —NH 2 , —NHR', —N(R') 2 , —NHCOR', —NR'COR', halogen, —CN, —CO 2 H, —CO 2 R', —CHO, —COR', —CONH 2 , —CONHR', —CON(R') 2 , —NO 2 , —OP(O)(OH) 2 , —SO 3 H, —SO 3 R', —SOR', and —SO 2 R', wherein R', independently for each occurrence, is C 1-10 alkyl or C 3-10 cycloalkyl;

n is an integer from 1 to 20;

m is an integer from 1 to 20; and

*Cu is 67 Cu.

75 . The method of claim 74 , wherein:

the compound of the first pharmaceutical composition is [ 61 Cu]Cu-NODAGA-F1 and the compound of the second pharmaceutical composition is [ 67 Cu]Cu-NODAGA-F1;

the compound of the first pharmaceutical composition is [ 61 Cu]Cu-NODAGA-F2 and the compound of the second pharmaceutical composition is [ 67 Cu]Cu-NODAGA-F2;

the compound of the first pharmaceutical composition is [ 61 Cu]Cu-NODAGA-F3 and the compound of the second pharmaceutical composition is [ 67 Cu]Cu-NODAGA-F3; or

the compound of the first pharmaceutical composition is [ 61 Cu]Cu-NODAGA-F4 and the compound of the second pharmaceutical composition is [ 67 Cu]Cu-NODAGA-F4.

76 . The method of claim 74 , further comprising determining, Via the one or more images of the subject, the presence or absence of a disease in the subject based on the presence or absence of localization of the 61 Cu radionuclide of the first pharmaceutical composition in the subject's body.

77 . The method of claim 76 , wherein the disease is selected from cancers, inflammatory diseases, infectious diseases, and immune diseases.

78 . The method of claim 74 , wherein the one or more images are generated by using positron emission tomography (PET), PET-computer tomography (PET-CT), or single-photon emission computerized tomography (SPECT).

79 . A method of detecting a FAP-overexpressing cancer in a human subject, the method comprising:

administering to the subject an effective amount of the composition of claim 8 ; and

generating one or more images of a part of a subject's body.

80 . The method of claim 79 , wherein the cancer is selected from non-small cell lung cancer, triple-negative breast cancer, colorectal carcinoma, gastric cancer, ovarian cancer, and pancreatic cancer.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2023
From: FANI, MELPOMENI; MILLUL, JACOPO
To: UNIVERSITÄT BASEL
Reel/Frame 065734/0127 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2023
From: JAAFAR-THIEL, LEILA; DE ROSE, FRANCESCO; PORCELLI, CATERINA
To: NUCLIDIUM AG
Reel/Frame 065745/0508 →
Continuity (5)
Continuation 18474218 · Sep 25, 2023
Provisional Application 63520329 · Aug 17, 2023
Provisional Application 63416479 · Oct 14, 2022
Provisional Application 63409687 · Sep 23, 2022
Related Publication 20240172953A1 · May 30, 2024
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