IP Library › Granted Patent US 12,558,440
Granted Patent B2
US 12,558,440 · App. 18/135,595 · Granted Feb 24, 2026

Radiopharmaceutical and methods

Inventor: Joe McCann (Toronto, CA)
Assignee: Point Biopharma, Inc.
A61K51/0497A61K47/12A61K47/22A61K47/65A61K51/0482A61P35/00A61K9/0019A61K51/0402A61K51/121
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 12,558,440
App. No.
18/135,595
Granted
Feb 24, 2026
Kind
B2
Abstract

The radiopharmaceutical 177 Lu-PSMA I&T is provided, including in high purities with extended shelf life. Further provided are methods of synthesis of 177 Lu-PSMA I&T and pharmaceutical compositions and methods of treatment that comprise 177 Lu-PSMA I&T.

Claims (11)

1 . An aqueous pharmaceutical composition comprising:

(a) a complex of lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA which is enriched in isomer (2A),

which complex is produced by an incorporation reaction comprising

(i) combining lutetium-177 and EuK-Sub-kf-iodo-y-DOTAGA, wherein the EuK-Sub-kf-iodo-y-DOTAGA is enriched in isomer (1A),

in a reaction buffer having a final concentration of one or more ascorbate compounds of 55 mg/mL to 75 mg/mL and in the absence of a gentisate compound;

(ii) heating the reaction composition to a temperature no greater than 90° C. to form the complex, which complex has 99% or greater lutetium-177 incorporation;

(b) one or more ascorbate compounds present in a total concentration from 55 mg/mL to 75 mg/mL of the pharmaceutical composition; and

(c) one or more gentisate compounds present in a total concentration of 16 mg/mL to 36 mg/mL of the pharmaceutical composition;

wherein the complex formed in step (a), after being formed and cooled, is admixed with the ascorbate and gentisate compounds and brought to a volume such that the resulting pharmaceutical composition has a volumetric radioactivity of 250 to 1000 MBq/mL and the radiochemical purity of the pharmaceutical composition is at least 95% following storage at a temperature of 30° C. for 3 days following preparation of the composition.

2 . The pharmaceutical composition of claim 1 wherein the radiochemical purity of the pharmaceutical composition is at least 95% following storage at a temperature of 30° C. for 5 days following preparation of the composition.

3 . The pharmaceutical composition of claim 1 wherein the EuK-Sub-kf-iodo-y-DOTAGA of step (a) (i) is enantiomerically pure isomer (1A).

Continuity (5)
Continuation 17486875 · Sep 27, 2021
Continuation 17374984 · Jul 13, 2021
Provisional Application 63143664 · Jan 29, 2021
Provisional Application 63051335 · Jul 13, 2020
Related Publication 20240108765A1 · Apr 4, 2024
References Cited (53)
US 10398791B2 · Eder et al. · 2019 [cited by applicant]
US 10596276B2 · De Palo et al. · 2020 [cited by applicant]
US 11129912B1 · Mccann · 2021 [cited by applicant]
US 11439714B2 · Mccann et al. · 2022 [cited by applicant]
US 11491246B2 · Mccann · 2022 [cited by applicant]
US 11904027B2 · De Palo et al. · 2024 [cited by applicant]
US 20070244316A1 · Amedio et al. · 2007 [cited by applicant]
US 20070269375A1 · Chen et al. · 2007 [cited by applicant]
US 20200030467A1 · De Palo et al. · 2020 [cited by applicant]
US 20220016274A1 · Mccann · 2022 [cited by applicant]
US 20220062447A1 · Mccann et al. · 2022 [cited by applicant]
US 20230302163A1 · Mccann · 2023 [cited by applicant]
US 20240285811A1 · Barbato et al. · 2024 [cited by applicant]
US 20250025584A1 · Fleshner et al. · 2025 [cited by applicant]
WO 2015171792A1 · 2015 [cited by applicant]
WO 2016149188A1 · 2016 [cited by applicant]
WO 2018108287A1 · 2018 [cited by applicant]
WO 2018222778A1 · 2018 [cited by applicant]
WO 2020061458A1 · 2020 [cited by applicant]
WO 2020064693A1 · 2020 [cited by applicant]
WO WO2020157177A1 · 2020 [cited by examiner]
WO 2022013610A2 · 2022 [cited by applicant]
WO 2022111800A1 · 2022 [cited by applicant]
WO 2022112323A1 · 2022 [cited by applicant]
WO 2023097329A1 · 2023 [cited by applicant]
Advisory Action for U.S. Appl. No. 17/486,875, dated Mar. 14, 2022. [cited by applicant]
Final Office Action dated Oct. 17, 2022 in U.S. Appl. No. 17/486,875 (US 20220016274). [cited by applicant]
Non-final Office action for U.S. Appl. No. 17/486,875, dated Oct. 29, 2021. [cited by applicant]
Pending U.S. Appl. No. 17/934,450, filed Sep. 22, 2022. [cited by applicant]
Reexamination Request; Reexam control No. 90/015,012. [cited by applicant]
Written Opinion for related (common priority) International Application PCT/IB2021/000467, mailed Feb. 8, 2022. [cited by applicant]
International Search Report for related (common priority) International Application PCT/IB2021/000467, mailed Feb. 8, 2022. [cited by applicant]
Order and Reexamination Request for U.S. Appl. No. 90/015,012, dated Jun. 6, 2022. [cited by applicant]
Asti, M. , et al., “Semiautomated labelling and fractionation of yttrium-90 and lutetium-177 somatostatin analogues using disposable syringes and vials”, Nucl. Med. Comm., 33(11), 1144-1152. [cited by applicant]
Baum, R. P, et al., “77Lu-Labeled Prostate-Specific Membrane Antigen Radioligand Therapy of Metastatic Castration-Resistant Prostate Cancer: Safety and Efficacy”, J. Nucl. Med., 57DOI: 1 0.2967Inumed.1 1 5.1 68443, 2016… [cited by applicant]
Chakrabarti , et al., “Prevention of radiolysis of monoclonal antibody during labeling”, Nucl. Med., 37(8), Aug. 1996, 1384-1388. [cited by applicant]
Chatalic, K. L.S, et al., “Towards personalized treatment of prostate cancer: PSMA I&T, a promising prostate-specific membrane antigen-targeted theranostic agent”, Theranostics, 6(6), 2016, 849-861. [cited by applicant]
Iori, M. , et al., “Labelling of 90Y- and 177Lu-DOTA-Bioconjugates for Targeted Radionuclide Therapy: A Comparison among Manual, Semiautomated, and Fully Automated Synthesisonuclide Therapy: A Comparison among Manual, S… [cited by applicant]
Maus , et al., “Aspects on Radiolabeling of 177Lu-DOTA-TATE: After C18 Purification Re-addition of Ascorbic Acid is Required to Maintain Radiochemical Purity”, International Journal of Diagnostic Imaging 1(1)DOI:10.5430… [cited by applicant]
Scott , et al., “Studies into radiolytic decomposition of fluorine-18 labeled radiopharmaceuticals for positron emission tomography”, Appl. Radiat. Isot., 67(1), Jan. 2009, 88-94. [cited by applicant]
Sorensen, M. A, et al., “Automated synthesis of 68Ga/177Lu-PSMA on the Trasis miniAllinOne”, J. Label. Compd. Radiopharm., 63(8)https://doi.org/10.1002/jlcr.3846, Jun. 30, 2020, 393-403 and supplemeantal Information. [cited by applicant]
Vyas, M. , “Nuclear Reactor to the hot lab: An overview of the Radiochemistry of Lu 177 (Lutetium)”, ANZSNM-2019, 1-43. [cited by applicant]
Weineisen, M. , et al., “68Ga and I 77Lu-labeled PSMA I&T: Optimization of a PSMA-targeted theranostic concept and first proof-of-concept human studies”, J. Nucl. Med., 56(8)DOI: https://doi.org/10.2967/jnumed.115.15855… [cited by applicant]
Weineisen, M. , et al., “Materials and Methods”, J. Nuclear Med., 56(8), 1-8. [cited by applicant]
Weineisen, M. , et al., “Synthesis and preclinical evaluation of DOTAGA-conjugated PSMA ligands for functional imaging and endoradiotherapy of prostate cancer”, EJNMMI Research, 4(63)https://doi.org/10.1186/s13550-014-0… [cited by applicant]
Emmett, L., “Results of a Prospective Phase 2 Pilot Trial of [cited by applicant]
Hooijman, E. L, “Development of [ [cited by applicant]
Liu, S., “Ascorbic Acid: Useful as a Buffer Agent and Radiolytic Stabilizer for Metalloradiopharmaceuticals”, Bioconjugate Chem., 14(5), https://doi.org/10.1021/bc034109i, Aug. 19, 2003, 1052-1056. [cited by applicant]
Rosar, F., “Efficacy and Safety of [ [cited by applicant]
Schmidt, A., “Effect of Carbohydration on the Theranostic Tracer PSMA I&T”, ACS Omega, 3(7), doi:10.1021/acsomega.8b00790, Jul. 25, 2018, 8278-8287. [cited by applicant]
Schuchardt, C., “Prostate-Specific Membrane Antigen Radioligand Therapy Using [cited by applicant]
Thisgaard, H., “Evaluation of Cobalt-Labeled Octreotide Analogs for Molecular Imaging and Auger Electron-Based Radionuclide Therapy”, J Nucl Med., 55(8), DOI: https://doi.org/10.2967/jnumed.114.137182, Aug. 2014, 1311-1… [cited by applicant]
Uijen, M., “Kidney absorbed radiation doses for [ [cited by applicant]