IP Library › Granted Patent US 12,721,912
Granted Patent B2
US 12,721,912 · App. 19/395,958 · Granted Sep 1, 2026

Radiopharmaceutical compositions for actinium in targeted radionuclide therapy

Inventors: Jarno Jalomäki (Helsinki, FI); Salla Seppänen (Helsinki, FI); Riku Parviainen (Helsinki, FI)
Assignee: Curium US LLC
A61K51/088A61K9/08A61K47/02A61K47/10A61K47/22
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 12,721,912
App. No.
19/395,958
Granted
Sep 1, 2026
Kind
B2
Abstract

The present disclosure provides a high-energy, low toxicity radiopharmaceutical composition comprising actinium that performs as an anti-tumor agent for targeted radionuclide therapy and has improved shelf-life stability. Specifically, the radiopharmaceutical composition may include 225 Ac-PSMA I&T, sodium ascorbate, and optionally hydrochloric acid. The radiopharmaceutical composition may be suitable for administration to a patient in need thereof, such as for the purpose of treating prostate cancer.

Claims (32)

1 . A method comprising:

administering a radiopharmaceutical composition to a patient in need thereof, wherein the composition comprises:

225 Ac-PSMA I&T in an amount that provides a radioactivity concentration of 250 kBq/mL to 1100 kBq/mL; and

sodium ascorbate in an amount of 0.1 mg/mL to 100 mg/mL;

wherein the composition has a radiochemical purity of 90% to 100% when administered; and

wherein the composition has a radiochemical purity of ≥90% at least 72 hours from production when stored at about 5° C. to about 40° C.

2 . The method of claim 1 , wherein the composition comprises 225 Ac-PSMA I&T in an amount that provides a radioactivity concentration of 500 kBq/mL to 1000 kBq/mL.

3 . The method of claim 1 , wherein the composition comprises 225 Ac-PSMA I&T in an amount that provides a radioactivity concentration of 250 kBq/mL to 500 kBq/mL.

4 . The method of claim 1 , wherein the composition comprises 225 Ac-PSMA I&T in an amount that provides a radioactivity concentration of 500 kBq/mL to 800 kBq/mL.

5 . The method of claim 1 , wherein the composition has a radiochemical purity of about 90% to about 100% at 96 hours after storage at a temperature of 5° C. to 40° C.

6 . The method of claim 1 , wherein the composition has a radiochemical purity of about 90% to about 100% at 120 hours after storage at a temperature of 5° C. to 40° C.

7 . The method of claim 1 , wherein the composition further comprises hydrochloric acid and wherein the molar ratio of hydrochloric acid to sodium ascorbate is from 1:0 to 1:500.

8 . The method of claim 1 , wherein the composition has a pH from about 5.5 to about 7.5.

9 . The method of claim 1 , wherein the composition further comprises ethanol in an amount of about 1% to about 20% (v/v).

10 . The method of claim 1 , wherein the composition further comprises EDTA or disodium EDTA.

11 . The method of claim 1 , wherein the composition further comprises DTPA.

12 . The method of claim 1 , wherein the composition is administered to the patient for 1 or more cycles of treatment.

13 . The method of claim 1 , wherein the composition is administered to the patient for 3 or more cycles of treatment.

14 . The method of claim 1 , wherein the composition is administered to the patient for 9 or more cycles of treatment.

15 . The method of claim 1 , wherein the composition is administered to the patient for 12 or more cycles of treatment.

16 . The method of claim 1 , wherein the composition has a total administered volume between 10 mL to 50 mL.

17 . The method of claim 1 , wherein the composition has a total administered volume between 20 mL to 100 mL.

18 . The method of claim 1 , wherein the composition comprises about 2 μg/mL to about 12 μg/mL PSMA I&T.

19 . The method of claim 1 , wherein the composition comprises a specific activity of 0.112 MBq/nmol±0.025 MBq/nmol, 0.112 MBq/nmol±0.020 MBq/nmol, 0.112 MBq/nmol±0.015 MBq/nmol, 0.112 MBq/nmol±0.010 MBq/nmol, or 0.112 MBq/nmol±0.005 MBq/nmol.

20 . The method of claim 1 , wherein the composition comprises no more than (NMT) 0.1 mg of PSMA I&T per administered dose.

21 . A method comprising:

administering a radiopharmaceutical composition to a patient in need thereof, wherein the composition comprises 225 Ac-PSMA I&T in an amount that provides a radioactivity concentration of 250 kBq/mL to 1100 kBq/mL,

wherein the composition has a radiochemical purity of 95% to 100% when administered, and

wherein the composition has a radiochemical purity of ≥95% at least 72 hours from production when stored at about 5° C. to about 40° C.

22 . The method of claim 21 , wherein the composition has a radiochemical purity of ≥95% at least 96 hours from production when stored at about 5° C. to about 40° C.

23 . The method of claim 21 , wherein the composition has a radiochemical purity of ≥95% at least 120 hours from production when stored at about 5° C. to about 40° C.

24 . A method of administering a radiopharmaceutical composition, the method comprising injecting the composition into a patient in need thereof, the composition comprising 225 Ac-PSMA I&T and sodium ascorbate in a solution having a pH of 5.5 to 7.5, wherein the solution has a radiochemical purity of more than 90% when administered.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 5, 2026
From: JALOMÄKI, JARNO; SEPPÄNEN, SALLA; PARVIAINEN, RIKU
To: CURIUM US LLC
Reel/Frame 073702/0317 →
Continuity (6)
Division 19204235 · May 9, 2025
Provisional Application 63753208 · Feb 3, 2025
Provisional Application 63691082 · Sep 5, 2024
Provisional Application 63645572 · May 10, 2024
Provisional Application 63644943 · May 9, 2024
Related Publication 20260077075A1 · Mar 19, 2026
References Cited (98)
US 10398791B2 · Eder et al. · 2019 [cited by applicant]
US 10471160B2 · Eder et al. · 2019 [cited by applicant]
US 10980901B2 · Morgenstern et al. · 2021 [cited by applicant]
US 20230302163A1 · McCann · 2023 [cited by applicant]
WO 2018108287A1 · 2018 [cited by applicant]
WO 2023015212A1 · 2023 [cited by applicant]
WO 2025129334A1 · 2025 [cited by applicant]
Hooijman, et al., “Development of [225 Ac] Ac-PSMA-I&T for Targeted Alpha Therapy According to GMP Guidelines for Treatment of mCRPC,” Pharmaceutics, 2021, vol. 13, No. 715, 15 pages. [cited by applicant]
International Search Report and Written Opinion for PCT Application No. PCT/US2025/028745, dated Sep. 10, 2025, 13 pages. [cited by applicant]
Ling, et al., “Evaluation of the tolerability and safety of [225Ac]Ac-PSMA-I&T in patients with metastatic prostate cancer: a phase I dose escalation study,” BCM Cancer, Jan. 29, 2024, vol. 24, No. 146, 8 pages. [cited by applicant]
Notice of Allowance for U.S. Appl. No. 19/204,235, dated Aug. 20, 2025, 8 pages. [cited by applicant]
Banerjee S., et al., “Lutetium-177 Therapeutic Radiopharmaceuticals: Linking Chemistry, Radiochemistry, and Practical Applications,” Chemical Reviews, Apr. 13, 2015, vol. 115, pp. 2934-2974. [cited by applicant]
Bjurlin M.A. “Imaging and Evaluation of Patients with High-risk Prostate Cancer,” Nature Reviews, Urology, 2015, pp. 1-12. [cited by applicant]
Chatalic K., et al., “213Bi-labeled PSMA-Targeting Agents for Alpha Radionuclide Therapy of Prostate Cancer,” Journal of Nuclear Medicine, May 1, 2016, vol. 57, No. 2, pp. 1-4. [cited by applicant]
Cheryl D., et al., “Anthropometric Reference Data for Children and Adults: United States, 2015-2018,” National Center for Health Statistics, 2015-2018, vol. 3, No. 46, 44 pages. [cited by applicant]
De Kruijff R.M., et al., “A Critical Review of Alpha Radionuclide Therapy How to Deal with Recoiling Daughters?” Pharmaceuticals, Jun. 10, 2015, vol. 8, pp. 321-336. [cited by applicant]
Demirci E., et al., “ [cited by applicant]
Foss C.A., et al., “Radiolabeled Small-molecule Ligands for Prostate-specific Membrane Antigen: in Vivo Imaging in Experimental Models of Prostate Cancer,” Clinical Cancer Research, Jun. 1, 2005, vol. 11, No. 11, pp. 40… [cited by applicant]
Ghosh A., et al., “Tumor Target Prostate Specific Membrane Antigen (PSMA) and Its Regulation in Prostate Cancer,” Journal of Cellular Biochemistry, 2004, vol. 91, pp. 528-539. [cited by applicant]
Hillier S., et al., “[13II]MIP-135, A Small Molecule Prostate-specific Membrane Antigen (PSMA) Inhibitor for Targeted Therapy of Prostate Cancer (PCa),” Journal of Nuclear Medicine, May 2011, vol. 52, No. 361, 2 pages. [cited by applicant]
Hillier S., et al., “[13II]MIP-1466, A Small Molecule Prostate-specific Membrane Antigen (PSMA) Inhibitor for Targeted Radiotherapy of Prostate Cancer (PCa),” Journal of Nuclear Medicine, May 2012, vol. 53, No. 170, 2 p… [cited by applicant]
Hubenak J.R., et al., “Mechanisms of Injury to Normal Tissue After Radiotherapy: a Review,” Plastic and Reconstructive Surgery, Jan. 2014, vol. 133, No. 1, pp. 49e-56e. [cited by applicant]
Jurcic J.G., et al., “Phase I Trial of Targeted Alpha-particle Therapy with Actinium-225 (225-Ac)-Lintuzumab and Low-dose Cytarabine (LDAC) in Patients Age 60 or Older with Untreated Acute Myeloid Leukemia (AML),” Blood… [cited by applicant]
Kairemo K., et al., “Design of 225Ac-PSMA for Targeted Alpha Therapy in Prostate Cancer,” Annals of Translational Medicine, 2024, pp. 1-13, doi: 10.21037/atm-23-1842. [cited by applicant]
Knight R.D., “Physics for Scientists and Engineers,” A Strategic Approach, vol. 5, pp. 1352-1381. [cited by applicant]
Kratochwil C., et al., “Ac-225-DOTATOC—an Empiric Dose Finding for Alpha Particle Emitter Based Radionuclide Therapy of Neuroendocrine Tumors,” Journal of Nuclear Medicine, May 2015, vol. 56, No. 3, 4 pages. [cited by applicant]
Llhan H., et al., “Response to (225) Ac-PSMA-I&T after failure of long-term (177) Lu-PSMA RLT in mCRPC,” European Journal of Nuclear Medicine and Molecular Imaging, Imaging, 2021, vol. 48, 1262-1263. [cited by applicant]
Mandel S.J., et al., “Superiority of Iodine-123 Compared with Iodine-131 Scanning for Thyroid Remnants in Patients with Differentiated Thyroid Cancer,” Clinical Nuclear Medicine, Jan. 2001, vol. 26, No. 1, pp. 6-9. [cited by applicant]
McDevitt M.R., et al., “Design and Synthesis of [cited by applicant]
Miederer M., et al., “Preclinical Evaluation of the alpha-Particle Generator Nuclide 225AC for Somatostatin Receptor Radiotherapy of Neuroendocrine Tumors,” Cancer Therapy: Preclinical, Jun. 1, 2008, vol. 14, No. 11, pp… [cited by applicant]
Milenic D.E., et al., “Targeting of Radio-isotopes for Cancer Therapy,” Cancer Biology & Therapy, Apr. 2004, vol. 3, No. 4, pp. 361-370. [cited by applicant]
Nomura N., et al., “Prostate Specific Membrane Antigen (PSMA) Expression in Primary Gliomas and Breast Cancer Brain Metastases,” Cancer Cell International, 2014, vol. 14, No. 26, pp. 1-8. [cited by applicant]
Petitioner, [cited by applicant]
Petitioner [cited by applicant]
Pomper M.G., et al., “ [cited by applicant]
Price E.W., et al., “Matching Chelators to Radiometals for Radiopharmaceuticals,” Chemical Society Reviews, Oct. 30, 2013, 31 pages. [cited by applicant]
Prostate Cancer., “Surveillance, Epidemiology, and End Results Program,” National Cancer Institute, 15 pages. [cited by applicant]
Ross J.S., et al., “Correlation of Primary Tumor Prostate-specific Membrane Antigen Expression with Disease Recurrence in Prostate Cancer,” Clinical Cancer Research, Dec. 15, 2003, vol. 9, pp. 6357-6362. [cited by applicant]
Scheinberg D.A., et al., “Actinium-225 in Targeted Alpha-particle Therapeutic Applications,” Current Radiopharmaceuticals, Oct. 2011, vol. 4, No. 4, pp. 306-320. [cited by applicant]
Sgouros G., et al., “MIRD Pamphlet No. 22 (Abridged): Radiobiology and Dosimetry of alpha-Particle Emitters for Targeted Radionuclide Therapy,” Journal of Nuclear Medicine, Feb. 2010, vol. 51, pp. 311-328. [cited by applicant]
Sharifi N., et al., “Androgen Deprivation Therapy for Prostate Cancer,” JAMA, Jul. 13, 2005, vol. 294, No. 2, pp. 238-244. [cited by applicant]
Silver D.A., et al., “Prostate-specific Membrane Antigen Expression in Normal and Malignant Human Tissues,” Clinical Cancer Research, Jan. 1997, vol. 3, pp. 81-85. [cited by applicant]
Turkbey B., et al., “Multiparametric Prostate Magnetic Resonance Imaging in the Evaluation of Prostate Cancer,” Cancer Journal for Clinicians, 2016, vol. 66, pp. 326-336. [cited by applicant]
Viola-Villegas N., et al., “The Coordination Chemistry of 1,4,7, 10-tetraazacyclododecane-N,N′, N″, N″m-Tetraacetic Acid (H4DOTA): Structural Overview and Analyses on Structure-stability Relationships,” Coordination Che… [cited by applicant]
Weineisen M., et al., “Synthesis and Preclinical Evaluation of DOTAGA-conjugated PSMA Ligands for Functional Imaging and Endoradiotherapy of Prostate Cancer,” European Journal of Nuclear Medicine and Molecular Imaging, … [cited by applicant]
Wernicke A.G., et al., “Prostate-specific Membrane Antigen Expression in Tumor-associated Vasculature of Breast Cancers,” Acta Pathologica, Microbiologica et Immunologica Scandinavica, 2014, vol. 122, pp. 482-489. [cited by applicant]
Zhao L., et al., “Clinical Pharmacology Considerations in Biologics Development,” Acta Pharmacologica Sinica, 2012, vol. 33, pp. 1339-1347. [cited by applicant]
Baum, R.P.; Langbein, T.; Singh, A.; Shahinfar, M.; Schuchardt, C.; Volk, G.F.; Kulkarni, H. “Injection of Botulinum Toxin for Preventing Salivary Gland Toxicity after PSMA Radioligand Therapy: An Empirical Proof of a P… [cited by applicant]
Chatalic, K.L.; Heskamp, S.; Konijnenberg, M.; Molkenboer-Kuenen, J.D.; Franssen, G.M.; Clahsen-van Groningen, M.C.; et al. “Towards Personalized Treatment of Prostate Cancer:PSMA I&T, a Promising Prostate-Specific Memb… [cited by applicant]
Cornford, P.; Bellmunt, J.; Bolla, M.; Briers, E.; De Santis M,.; Gross, T.; et al. “EAU-ESTRO-SIOG Guidelines on Prostate Cancer. Part II: Treatment of Relapsing, Metastatic, and Castration-Resistant Prostate Cancer.” … [cited by applicant]
De Medeiros, R.B.; Grigolon, M.V.; Araújo, T.P.; Srougi, M. “Metastatic castration-resistant prostate cancer (mCRPC) treated with 225Ac-PSMA-617. Case report.” Braz. J. Oncol. 2019, 15, 1-9. [cited by applicant]
Delpassand, E.S.; Hashmi, M.J.; Kazakin, J.; Nawaz, O., Garufi G.; Schindler, J.; Nordquist, L. “Preliminary efficacy and safety results from the TATCIST trial: A PSMA-directed targeted alpha therapy with FPI-2265 (225A… [cited by applicant]
Fendler, W.P.; Rahbar, K.; Herrmann, K.; Kratochwil, C.; Eiber, M. “177Lu-PSMA Radioligand Therapy for Prostate Cancer.” J Nucl Med. 2017, 58(8), 1196-1200. [cited by applicant]
Feuerecker, B.; Tauber, R.; Knorr, K.; Heck, M.; Beheshti, A.; Seidl, C.; et al. “Activity and Adverse Events of Actinium-225-PSMA-617 in Advanced Metastatic Castration-resistant Prostate Cancer After Failure of Lutetiu… [cited by applicant]
Gallyamov, M.; Meyrick, D.; Barley, J.; Lenzo, N. “Renal outcomes of radioligand therapy: Experience of 177lutetium—prostate specific membrane antigen ligand therapy in metastatic castrate-resistant prostate cancer.” Cl… [cited by applicant]
Gosewisch, A.; Schleske, M.; Gildehaus, F. J.; Berg, I.; Kaiser, L.; Brosch, J.; et al. “Image-based dosimetry for 225Ac-PSMA-I&T therapy using quantitative SPECT.” Eur. J. Nucl. Med. Mol. Imaging 2021, 48, 1260-1261. [cited by applicant]
Graf, F.; Fahrer, J.; Maus, S.; Morgenstern, A.; Bruchertseifer, F.; Venkatachalam, S.; et al. “DNA Double Strand Breaks as Predictor of Efficacy of the Alpha-Particle Emitter Ac-225 and the Electron Emitter Lu-177 for … [cited by applicant]
Haberkorn, U.; Eder, M.; Kopka, K.; Babich, J.W.; Eisenhut M. “New Strategies in Prostate Cancer: Prostate-Specific Membrane Antigen (PSMA) Ligands for Diagnosis and Therapy.” Clin Cancer Res. 2016, 22(1), 9-15. [cited by applicant]
Ilhan, H.; Gosewisch, A.; Böning, G.; Völter, F.; Zacherl, M.; Unterrainer, M.; et al. “Response to (225) Ac-PSMA-I&T after failure of long-term (177) Lu-PSMA RLT in mCRPC.” Eur. J. Nucl. Med. Mol. Imaging 2021, 48, 126… [cited by applicant]
Kairemo, K. “Targeted alpha therapy: a new tool for advanced prostate cancer.” thelancet.com/oncology, Feb. 2024, 25(2):148-149. [cited by applicant]
Kairemo, K.; Kgatle, M.; Bruchertseifer, F.; Morgenstern, A.; Sathekge, M.M. “Design of 225Ac-PSMA for targeted alpha therapy in prostate cancer.” Ann Transl Med 2024. doi: 10.21037/atm-23-1842. [cited by applicant]
Khreish, F.; Eber,t N.; Ries, M.; Maus, S.; Rosar , F.; Bohnenberge,r H.; et al. “(225) Ac-PSMA-617/ (177) Lu-PSMA-617 tandem therapy of metastatic castration-resistant prostate cancer: Pilot experience.” Eur. J. Nucl. … [cited by applicant]
Kinoshita, Y.; Kuratsukuri, K.; Landas, S.; Imaida K.; Rovito, P.M.; Wang, C.Y.; Haas G.P. “Expression of prostate-specific membrane antigen in normal and malignant human tissues.” World J Surg. 2006, 30(4), 628-636. [cited by applicant]
Kratochwil, C.; Bruchertseifer, F.; Giesel, F.L.; Weis, M.; Verburg, F.A.; Mottaghy, F.; et al. “225Ac-PSMA-617 for PSMA-Targeted alpha-Radiation Therapy of Metastatic Castration-Resistant Prostate Cancer.” J. Nucl. Med… [cited by applicant]
Kratochwil, C.; Bruchertseifer, F.; Rathke, H.; Bronzel, M.; Apostolidis, C.; Weichert, W.; et al. “Targeted alpha-Therapy of Metastatic Castration-Resistant Prostate Cancer with (225) Ac-PSMA-617: Dosimetry Estimate an… [cited by applicant]
Kratochwil, C.; Bruchertseifer, F.; Rathke, H.; Hohenfellner, M.; Giesel, F.L.; Haberkorn, U.; Morgenstern, A. “Targeted alpha-Therapy of Metastatic Castration-Resistant Prostate Cancer with (225) Ac-PSMA-617: Swimmer-P… [cited by applicant]
Kratochwil, C.; Giesel, F.L.; Heussel, C.-P.; Kazdal D.; Endris, E.; Nientiedt, C.; et al. “Patients Resistant Against PSMA-Targeting a-Radiation Therapy Often Harbor Mutations in DNA Damage-Repair-Associated Genes.” J … [cited by applicant]
Kratochwil, C.; Giesel, FL.; Eder, M.; Afshar-Oromieh, A.; Benešová, M.; Mier, W.; et al. “[ [cited by applicant]
Kratochwil, C.; Schmidt, K.; Afshar-Oromieh, A.; Bruchertseifer, F.; Rathke, H.; Morgenstern, A.; et al. “Targeted alpha therapy of mCRPC: Dosimetry estimate of (213) Bismuth-PSMA-617.” Eur. J. Nucl. Med. Mol. Imaging 2… [cited by applicant]
Langbein, T.; Chausse, G.; Baum, R.P. “Salivary Gland Toxicity of PSMA Radioligand Therapy: Relevance and Preventive Strategies.” J. Nucl. Med. 2018, 59, 1172-1173. [cited by applicant]
Lawal, I.O.; Morgenstern, A.; Vorster, M.; Knoesen, O.; Mahapane, J.; Hlongwa, K.N.; et al. “Hematologic toxicity profile and efficacy of [225Ac]Ac-PSMA-617 α-radioligand therapy of patients with extensive skeletal meta… [cited by applicant]
Lee, D.Y.; Kim, Y.I. “Effects of 225Ac-Labeled Prostate-Specific Membrane Antigen Radioligand Therapy in Metastatic Castration-Resistant Prostate Cancer: A Meta-Analysis.” J Nucl Med. 2022, 63(6), 840-846. [cited by applicant]
Ma, J.; Li, L.; Liao, T.; Gong, W.; Zhang, C. “Efficacy and Safety of 225Ac-PSMA-617-Targeted Alpha Therapy in Metastatic Castration-Resistant Prostate Cancer: A Systematic Review and Meta-Analysis.” Front Oncol. 2022, … [cited by applicant]
Morgenstern, A.; Apostolidis, C.; Kratochwil, C.; Sathekge, M.; Krolicki, L.; Bruchertseifer, F. “An Overview of Targeted Alpha Therapy with (225)Actinium and (213)Bismuth.” Curr Radiopharm. 2018, 11(3), 200-208. [cited by applicant]
Nonnekens, J.; Chatalic, K.L.; Molkenboer-Kuenen, J.D.; Beerens, C.E.; Bruchertseifer, F.; Morgenstern, A.; et al. “(213) Bi-Labeled Prostate-Specific Membrane Antigen-Targeting Agents Induce DNA Double-Strand Breaks in… [cited by applicant]
Parida, G.K.; Panda, R.A.; Bishnoi, K.; Agrawal, K. “Efficacy and Safety of Actinium-225 Prostate-Specific Membrane Antigen Radioligand Therapy in Metastatic Prostate Cancer: A Systematic Review and Metanalysis.” Med Pr… [cited by applicant]
Pelletier, K.; Côté, G.; Fallah-Rad, N.; John, R.; Kitchlu, A. “Chronic kidney disease after 225Ac-PSMA617 therapy in patients with metastatic prostate cancer.” Kidney Int. Rep. 2021, 6, 853-856. [cited by applicant]
Puttemans, J.; Lahoutte, T.; D'Huyvetter, M.; Devoogdt, N. “Beyond the Barrier: Targeted Radionuclide Therapy in Brain Tumors and Metastases.” Pharmaceutics 2019, 11, 376. [cited by applicant]
Rathke, H.; Bruchertseifer, F.; Kratochwil, C.; Keller, H.; Giesel, F.L.; Apostolidis, C.; et al. “First patient exceeding 5-year complete remission after 225Ac-PSMA-TAT.” European Journal of Nuclear Medicine and Molecu… [cited by applicant]
Rathke, H.; Kratochwil, C.; Hohenberger, R.; Giesel, F.L.; Bruchertseifer, F.; Flechsig, P.; et al. “Initial clinical experience performing sialendoscopy for salivary gland protection in patients undergoing (225) Ac-PSM… [cited by applicant]
Rosar, F.; Krause, J.; Bartholomä, M.; Maus, S.; Stemler T.; Hierlmeier, I.; et al. “Efficacy and Safety of [225Ac]Ac-PSMA-617 Augmented [177Lu]Lu-PSMA-617 Radioligand Therapy in Patients with Highly Advanced mCRPC with… [cited by applicant]
Ruigrok, E.A.M, Tamborino, G.; de Blois E.; Roobol, S.J.; Verkaik, N.; De Saint-Hubert, M.; et al. “In vitro dose effect relationships of actinium-225- and lutetium-177-labeled PSMA-I&T.” Eur J Nucl Med Mol Imaging. 202… [cited by applicant]
Rosar, F.; Krause, J.; Bartholomä, M.; Maus,, S.; Stemler T.; Hierlmeier I.; et al. “Efficacy and Safety of [225Ac]Ac-PSMA-617 Augmented [177Lu]Lu-PSMA-617 Radioligand Therapy in Patients with Highly Advanced mCRPC with… [cited by applicant]
Satapathy, S.; Mittal, B.R.; Sood, A.; Das, C.K.; Singh, S.K.; Mavuduru, R.S.; Bora, G.S. “Health-Related Quality-of-Life Outcomes with Actinium-225-Prostate-Specific Membrane Antigen-617 Therapy in Patients with Heavil… [cited by applicant]
Satapathy, S.; Sood, A.; Das, C.K.; Mittal, B.R. “Evolving role of 225Ac-PSMA radioligand therapy in metastatic castration-resistant prostate cancer-a systematic review and meta-analysis.” Prostate Cancer Prostatic Dis.… [cited by applicant]
Sathekge, M.; Bruchertseifer, F.; Knoesen, O.; Reyneke, F.; Lawal, I.; Lengana, T.; et al. “(225) Ac-PSMA-617 in chemotherapy-naive patients with advanced prostate cancer: A pilot study.” Eur. J. Nucl. Med. Mol. Imaging… [cited by applicant]
Sathekge, M.; Bruchertseifer, F.; Vorster, M.; Lawal, I.O.; Knoesen, O.; Mahapane, J.; et al. “Predictors of Overall and Disease-Free Survival in Metastatic Castration-Resistant Prostate Cancer Patients Receiving (225) … [cited by applicant]
Sathekge, M.; Bruchertseifer, F.; Vorster, M.; Lawal, I.O.; Mokoala, K.; Reed, J.; et al. “225Ac-PSMA-617 radioligand therapy of de novo metastatic hormone-sensitive prostate carcinoma (mHSPC): preliminary clinical find… [cited by applicant]
Sathekge, M.; Knoesen, O.; Meckel, M.; Modiselle, M.; Vorster, M.; Marx, S. “(213) Bi-PSMA-617 targeted alpha-radionuclide therapy in metastatic castration-resistant prostate cancer.” Eur. J. Nucl. Med. Mol. Imaging 201… [cited by applicant]
Sathekge, M.M.; Bruchertseifer, F.; Lawal, I.O.; Vorster, M.; Knoesen, O.; Lengana, T.; et al. “Treatment of brain metastases of castration-resistant prostate cancer with (225)Ac-PSMA-617.” Eur. J. Nucl. Med. Mol. Imagi… [cited by applicant]
Sen, I.; Thakral, P.; Tiwari, P.; Pant, V.; Das, S.S.; Manda, D.; Raina, V. “Therapeutic efficacy of 225Ac-PSMA-617 targeted alpha therapy in patients of metastatic castrate resistant prostate cancer after taxane-based … [cited by applicant]
Sgouros ,G. “Dosimetry, Radiobiology and Synthetic Lethality: Radiopharmaceutical Therapy (RPT) With Alpha-Particle-Emitters.” Semin Nucl Med. 2020, 50(2), 124-132. [cited by applicant]
Van der Doelen, M.J.; Mehra, N.; van Oort, I.M.; Looijen-Salamon, M.G.; Janssen, M.J.R.; Custers, J.A.; et al. “Clinical outcomes and molecular profiling of advanced metastatic castration-resistant prostate cancer patie… [cited by applicant]
Vorster, M.; Sathekge, M. “Advances in PSMA Alpha Theragnostics.” Semin Nucl Med. 2024, S0001-2998(24), 00029-1. doi: 10.1053/j.semnuclmed.2024.03.004. [cited by applicant]
Weineisen, M.; Schottelius, M.; Simeček, J.; Baum, R.P.; Yildiz, A.; Beykan, S.; et al. “68Ga- and 177Lu-Labeled PSMA I&T: Optimization of a PSMA-Targeted Theranostic Concept and First Proof-of-Concept Human Studies.” J… [cited by applicant]
Yadav, M.P.; Ballal, S.; Sahoo, R.K.; Tripathi, M.; Seth, A.; Bal, C. “Efficacy and safety of (225) Ac-PSMA-617 targeted alpha therapy in metastatic castration-resistant Prostate Cancer patients.” Theranostics, 2020, 10… [cited by applicant]
Zacherl, M.J.; Gildehaus, F.J.; Mittlmeier, L.; Boening, G.; Gosewisch, A.; Wenter, V.; et al. “First clinical results for PSMA targeted alpha therapy using (225) Ac-PSMA-I&T in advanced mCRPC patients.” J. Nucl. Med. 2… [cited by applicant]
Notice of Allowance for U.S. Appl. No. 19/395,907, dated Apr. 14, 2026, 7 pages. [cited by applicant]