Radiotherapeutic and companion imaging agents to target MC1R

Patent metadata

Field	Value
Publication number	US-12508329-B2
Application number	US-202217810956-A
Country	US
Kind code	B2
Filing date	Jul 6, 2022
Priority date	May 6, 2015
Publication date	Dec 30, 2025
Grant date	Dec 30, 2025

Abstract

The subject matter disclosed herein relates generally to cancer therapy and to anticancer compounds and imaging agents. More specifically, the subject matter disclosed herein relates to agents that target MC1R and their use in the treatment of cancer. Methods of screening for MC1R targeted agents are also disclosed.

First claim

What is claimed is:

1 . A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound having the following structure:

wherein:
M is selected from the group consisting of 90 Y, 177 Lu, 18 F, 64 Cu, 67 Cu, 89 Zr, 124 I, 123 I, 152 Eu, 212 Pb, 99m Tc, 225 Ac, 68 Ga, and 111 In.

2 . The pharmaceutical composition of claim 1 , wherein M is selected from the group consisting of 225 Ac, 68 Ga, and 111 In.

3 . The pharmaceutical composition of claim 1 , wherein the pharmaceutically acceptable carrier comprises water.

4 . The pharmaceutical composition of claim 1 , wherein the pharmaceutically acceptable carrier comprises water and one or more pharmaceutically acceptable salts.

5 . A method for treating cancer in a subject, the method comprising administering to the subject an effective amount of a compound having the following structure:

wherein:
M is selected from the group consisting of 90 Y, 177 Lu, 18 F, 64 Cu, 67 Cu, 89 Zr, 124 I, 123 I, 152 Eu, 212 Pb, 99m Tc, 225 Ac, 68 Ga, and 111 In.

6 . The method of claim 5 , wherein M is selected from the group consisting of 225 Ac, 68 Ga, and 111 In.

7 . The method of claim 5 , wherein M is 225 Ac.

8 . The method of claim 5 , wherein the cancer is melanoma.

9 . The method of claim 5 , wherein the cancer is metastatic melanoma.

10 . The method of claim 5 , wherein the cancer is cutaneous melanoma.

11 . The method of claim 5 , wherein the cancer is pancreatic cancer.

12 . The method of claim 5 , wherein the administering is an intravenous injection.

13 . A compound having the following structure:

or a pharmaceutically acceptable salt thereof, wherein:
L is a direct bond or has one of the following structures:

14 . The compound of claim 13 , further comprising a radionuclide.

15 . The compound of claim 14 , wherein the radionuclide is an alpha-particle or beta-particle emitter.

16 . The compound of claim 14 , wherein the radionuclide is selected from the group consisting of 90 Y, 177 Lu, 18 F, 64 Cu, 67 Cu, 89 Zr, 124 I, 123 I, 152 Eu, 212 Pb, 99m Tc, 225 Ac, 68 Ga, and 111 In.

17 . The compound of claim 14 , wherein the radionuclide is selected from the group consisting of 225 Ac, 68 Ga, and 111 In.

18 . The compound of claim 14 , wherein the radionuclide is selected from the group consisting of 225 Ac, 68 Ga, and 111 In.

19 . The compound of claim 14 , wherein the radionuclide is 225 Ac.

Assignees

• H Lee Moffitt Cancer Ct & Res
• Modulation Therapeutics Inc
• Univ Wake Forest Health Sciences

Inventors

• Morse David
• Gillies Robert
• Mclaughlin Mark
• Wadas Thaddeus
• Kil Hyun Joo
• Tafreshi Narges

Classifications

• G01N33/5751

  of the skin, e.g. melanoma · CPC title

• A61K38/08

  Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)} · CPC title

• A61P35/04

  specific for metastasis · CPC title

• C07K14/705

  Receptors; Cell surface antigens; Cell surface determinants {(tumour specific antigens C07K14/4748)} · CPC title

• A61K38/00

  Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) · CPC title