Radiolabeled compound for use in a method of treating carbonic anhydrase ix positive diseases
Patent Information
- Application Number
- HK62026128301
- Authority / Receiving Office
- HK · HK
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2023-06-20
- Filing Date
- 2026-09-02
- Publication Date
- 2026-10-09
- Estimated Expiration
- 2044-06-18
Smart Images
Figure 00000107_0000 
Figure 00000107_0001 
Figure 00000107_0002
Abstract
Description
This invention relates to a radiolabeled compound for targeted radionuclide therapy. Specifically, this invention relates to a radiolabeled compound for treating carbonic anhydrase IX (CAIX)-positive diseases, thereby improving drug delivery and enhancing therapeutic efficacy (antitumor activity). Abstract
Claims
CLAIMS1. A compound for use in a method of treating a carbonic anhydrase IX (CAIX) positive disease in a human patient, the method comprising the steps of:(i) optionally administering to the patient an imaging dose of the compound labeled with68Ga, to obtain an image of body parts or tissues to be examined, and(ii) administering to the patient a treatment dose of the compound labeled with 177Lu, to treat the CAIX positive disease;wherein the DOTA moiety comprised in the compound of Formula (1 ) chelates the68Ga or177Lu to form the compound labeled with68Ga or 177Lu; wherein, preferably the compound labeled with177Lu administered in step (ii) is administered once per cycle of one to six weeks, preferably once per cycle of four to six weeks, and most preferably once per cycle of four weeks; and wherein, if the patient is not administered an imaging dose of the compound labeled with68Ga in step (i), the compound labeled with177Lu administered instep (ii) is administered once per cycle of one to six weeks, preferably once per cycle of four to six weeks, and most preferably once per cycle of four weeks.
2. The compound for use according to claim 1 , wherein said method comprises the steps of:(i) administering to the patient an imaging dose of the compound labeled with 68Ga, to obtain an image of body parts or tissues to be examined, and(ii) administering to the patient a treatment dose of the compound labeled with 177Lu, to treat the CAIX positive disease.
3. The compound for use according to claim 1 or 2, wherein(a) the imaging dose of the compound labeled with68Ga is from 50 to 250 MBq, preferably from 100 to 200 MBq, more preferably from 145 to 225 MBq, such as about 185 MBq, and / or(b) the treatment dose of the compound labeled with177Lu is from 1 .0 to 25.0 GBq, preferably from 2.0 to 20.0 GBq, more preferably from 3.0 to 19 GBq.
4. The compound for use according to any of claims 1 to 3, wherein the compound labeled with177Lu is administered once per cycle of one to six weeks, preferably once per cycle of four to six weeks, and most preferably once per cycle of four weeks.
5. The compound for use according to any of claims 1 to 4, wherein the compound labeled with177Lu-labeled is administered over one to ten cycles, preferably over four to eight cycles, and more preferably over four to six cycles.
6. The compound for use according to any of claims 1 to 5, wherein the treatment dose of the compound labeled with177Lu that is administered in at least one cycle, and preferably in each cycle, is selected from the following:(1 ) a treatment dose of from 2.0 to 6.0 GBq, such as about 3.7 GBq,(2) a treatment dose of from 6.0 to 10.0 GBq, such as about 7.4 GBq,(3) a treatment dose of from 10.0 to 14.0 GBq, such as about 11.1 GBq,(4) a treatment dose of from 14.0 to 18.0 GBq, such as about 14.8 GBq, and(5) a treatment dose of from 18.0 to 20.0 GBq, such as about 18.5 GBq.
7. The compound for use according to any of claims 1 to 6, wherein the compound labeled with68Ga and / or the compound labeled with177Lu is administered intravenously, and preferably intravenously by infusion.
8. The compound for use according to any of claims 1 to 7, wherein the compound labeled with68Ga and / or the compound labeled with177Lu is provided as a solution in a pharmaceutically acceptable injectable carrier.
9. The compound for use according to claim 8, wherein the solution of the compound labeled with68Ga has a concentration of from 250 to 950 MBq / 8.1 mL, and the solution of the compound labeled with177Lu has a concentration of from 150 to 900 MBq / mL.
10. The compound for use according to any of claims 1 to 9, wherein the CAIX positive disease is cancer, and preferably the human patient has unresectable, locally advanced, or metastatic solid tumors.
11. The compound for use according to any of claims 1 to 10, wherein the CAIX positive disease is a cancer selected from the group consisting of renal cell carcinoma (RCC), in particular clear cell renal cell carcinoma (ccRCC), colorectal carcinoma (CRC), pancreatic ductal adenocarcinoma (PDAC), glioblastoma (GBM), mesothelioma, cholangiocarcinoma (CCA), ovarian carcinoma, non-small cell lung cancer (NSCLC), in particular squamous nonsmall cell lung cancer (SNSCLC), brain cancer, pancreatic cancer, thyroid cancer, lung cancer, renal cancer, breast cancer, in particular triple-negative breast cancer (TNBC), head and neck cancer, in particular squamous carcinoma of head and neck (SCCHN), urothelial carcinoma and bladder cancer.
12. The compound for use according to any of claims 1 to 11 , wherein the CAIX positive disease is a cancer selected from the group consisting of ccRCC, CRC, PDAC, SNSCLC, TNBC and SCCHN, and preferably from ccRCC, CRC and PDAC.
13. The compound for use according to any of claims 1 to 12, wherein the compound labeled with68Ga and / or the compound labeled with177Lu is administered after one or more other therapeutic agents or therapies, such as DNA damage response (DDR) inhibitors, chemotherapeutic agents, immunomodulatory agents, proton pump inhibitors (PPIs), histamine H2-receptor antagonists, tyrosine kinase inhibitors, cell therapy, external beam radiation, or any other targeted therapies.