Alpha-therapy in bone-metastatic mCRPC — ALSYMPCA legacy, sequencing with Lu-177 PSMA, and updated guidance. Curated daily from Europe PMC (PubMed + PMC + preprints) and OpenAlex — free-full-text link on each open-access paper.
The theranostic paradigm, combining molecular diagnosis and targeted radionuclide therapy in a single platform, has revolutionized precision oncology. Radiopharmaceutical theranostics enables targeted…
BackgroundRadium-223 dichloride (radium-223) is an α-emitting radionuclide approved for treating metastatic castration-resistant prostate cancer (mCRPC) with symptomatic bone metastases and no viscera…
Jokar N, Pashazadeh A, Juweid ME, Najdian A et al.
Targeted alpha therapy (TAT) has moved from a largely experimental approach into clinically relevant radiopharmaceutical therapy, although evidence varies across radionuclides and products. Alpha part…
Bone radiopharmaceuticals have evolved from early palliative agents into integral components of targeted precision oncology and theranostics. This review comprehensively traces the historical trajecto…
Akhmetova D, Rusakova V, Matveev D, Toloknyannikova D et al.
Combined chemo-radionuclide therapy offers a promising strategy to improve cancer treatment by integrating various therapeutic mechanisms within a single drug delivery system (DDS). Metal-organic fram…
IntroductionTwo radiopharmaceuticals are approved for metastatic castration-resistant prostate cancer (mCRPC): Radium-223 and ¹⁷⁷Lu-PSMA-617. While short-term hematologic toxicity is well-studied, the…
The approval of Radium 223 (Ra-223) has played an important role in the management of patients with metastatic castrate-resistant prostate cancer (mCRPC) by demonstrating improved symptom control and …
ObjectiveReal-world outcomes of Ra-223 in Asian populations vary and are influenced by reimbursement policies that restrict use to symptomatic patients. We aimed to identify baseline predictors of tre…
Most patients with metastatic castration-resistant prostate cancer (mCRPC) do not benefit from treatment with immune checkpoint inhibitors targeting programmed cell death (ligand) 1 (PD-(L)1). Radiati…
Lazić I, Stanković A, Todorović N, Forkapić S et al.
Targeted Alpha Therapy (TAT) is often defined by the favorable physical properties of alpha particles, particularly their high linear energy transfer and short tissue range. However, these properties …
Objective evaluation of quantitative-imaging (QI) methods based on how reliably they measure true values is important for clinical translation. Performing such evaluation with patient data is highly d…
Design, setting, and participantsExploratory post hoc analysis of the international, randomised, open-label phase 3 PEACE-3 trial including 446 patients with asymptomatic or mildly symptomatic mCRPC a…
Radium-223 (Ra-223) is used for patients with bone-metastatic castration-resistant prostate cancer (CRPC). However, the prognostic value of regional lymph node metastasis at CRPC diagnosis for surviva…
Schwengber WK, Sanders J, Pinteric A, Armitage L et al.
Radiopharmaceutical therapy (RPT) uses radionuclides linked to targeting ligands to bind tumor-associated receptors or antigens and deliver ionizing radiation to malignant cells. Approved agents inclu…
BackgroundRadium-223 dichloride (Ra-223) is an effective treatment for metastatic castration-resistant prostate cancer (mCRPC) with bone metastases. However, predictive factors associated with treatme…
ObjectiveTo identify independent prognostic factors in castration-resistant prostate cancer (CRPC) patients with visceral metastases, construct and internally validate a prognostic nomogram for indivi…
McKay RR, Ballman KV, Atherton PJ, Ajmera A et al.
PurposeBone metastases (BM) occur in approximately 30% of patients with metastatic renal cell carcinoma (mRCC) and are associated with poor survival and symptomatic skeletal events (SSEs). Radium-223,…
Yazdani E, Manafi-Farid R, Karamzade-Ziarati N, Salimi Y et al.
Objective. Currently, [223Ra]RaCl2alpha-radiation radiopharmaceutical therapy (αRPT) has been clinically approved for treating patients with metastatic castration-resistant prostate cancer (mCRPC) by …
PurposeMetastatic castration-resistant prostate cancer (mCRPC) is bone-predominant, requiring objective imaging biomarkers to guide Ra-223 therapy. We evaluated overall metabolic bone volume (OMBV) an…
IntroductionThe combination of enzalutamide and radium-223 has demonstrated clinical efficacy in metastatic castration-resistant prostate cancer; however, real-world evidence remains limited, particul…
Merdžo I, Brossard C, Lepareur N, Platas-Iglesias C et al.
Two new decadentate macrocyclic chelators, bpycropa and phencropa, were synthesized by incorporating 2,2'-bipyridine and 1,10-phenanthroline units, respectively, into the picolinate-functionalized aza…
Shiota M, Fujiwara M, Sumiyoshi T, Enokida H et al.
Circulating tumor DNA (ctDNA) testing has emerged as a cancer precision medicine approach. We investigated the genomic landscape and clinical utility of ctDNA in patients receiving 223Ra dichloride fo…
BackgroundThe combination of olaparib plus radium-223 improved progression-free survival in patients with metastatic castration-resistant prostate cancer with bone metastases (BM) in the multicenter, …
ObjectiveTo compare the clinical efficacy of the curved vertebroplasty system combined with targeted radionuclide therapy (radium-223/strontium-89) versus conventional percutaneous vertebroplasty (PVP…
BackgroundThe REASURE study investigated imaging biomarkers in men receiving ²²³Ra treatment for prostate cancer bone metastases. We used REASURE data to compare and contrast the roles of [¹⁸F]NaF PET…
ObjectiveTo define the time course of fracture risk with radium-223 in combination with androgen receptor pathway inhibitor (ARPi) therapy and assess the clinical impact of concomitant bone-protective…
Marulanda-Corzo V, Coraci S, Kakkar P, Okobi TJ et al.
Radiopharmaceutical therapy, a form of targeted radionuclide therapy, has emerged as a rapidly advancing area in prostate cancer management, with significant developments in 2025. The field, which beg…
The integration of [¹⁷⁷Lu]Lu-prostate-specific membrane antigen (PSMA) therapy into the treatment paradigm for advanced prostate cancer has improved survival and quality of life; however, resistance a…
IntroductionPersonalised medicine approaches are redefining the therapeutic landscape for men with metastatic castration-resistant prostate cancer (mCRPC). While poly(ADP-ribose) polymerase (PARP) inh…
PurposeRadium-223 (Ra-223) is a bone-targeting radiopharmaceutical used to treat symptomatic bone metastases in men with castration-resistant prostate cancer (CRPC), but there are no reliable biomarke…
Katzdobler L, Delker A, Giussani A, Hürkamp K et al.
The radiopharmaceutical 223Ra-dichloride (Xofigo®) has been approved for palliative treatment of metastatic castration-resistant prostate cancer. During the treatment and caregiving, patients who rece…
PurposeRadium-223 is an α-emitting radiopharmaceutical that improves survival in metastatic castration-resistant prostate cancer (mCRPC). Preclinical data suggest synergy between poly(ADP-ribose) poly…
BackgroundThis study examined oncologic outcomes associated with Radium-223 (Ra-223) administered at different treatment lines in patients with metastatic castration-resistant prostate cancer (mCRPC) …
Introduction/backgroundApproval of [177Lu]Lu-PSMA-617 has changed the usual sequencing of treatments for metastatic castration-resistant prostate cancer (mCRPC). There is limited data on outcomes and …
BACKGROUND: Radium-223 (Ra-223) has been approved for the treatment of metastatic castration-resistant prostate cancer (mCRPC) with predominant osseous metastases. PSA flare phenomenon with Ra-223 lim…
Southwell JW, Gumiela M, Cowell J, Brandt MR et al.
The stable coordination of radium-223 (²²³Ra) for targeted alpha therapy remains elusive. Herein, 17 chelators were investigated for the complexation of ²²³Ra, of which 13 have previously not been rep…
The effectiveness and safety of radium-223 (Ra-223) in patients with metastatic castration-resistant prostate cancer (mCRPC) and bone metastasis in real-world clinical practice in China remain to be f…
RationaleRadium-223 dichloride (²²³RaCl₂) is an FDA-approved alpha-emitting radiopharmaceutical that targets bone metastases in metastatic castration-resistant prostate cancer (mCRPC). This study inve…
Karimi H, Shaffer TH, Stauff E, Kandula VVR et al.
Radiopharmaceutical therapy (RPT) has emerged as a transformative modality in oncology, particularly for patients with metastatic or inoperable tumors. By leveraging molecularly targeted carriers conj…
Gillessen S, Gallardo E, Choudhury A, Saad F et al.
BackgroundThe primary analysis of the European Organisation for Research and Treatment of Cancer (EORTC) 1333/PEACE-3 study demonstrated that enzalutamide plus radium-223 (Ra223) improved radiological…
²²³Ra, a potent α-emitting radionuclide, is currently limited to treating bone metastases in clinical practice. This constraint stems from the lack of stable chelating agents capable of withstanding i…
Miller SR, Dewaraja Y, Rowe SP, Reichert ZR et al.
Radiopharmaceuticals therapy (RPT) has been a major breakthrough in the treatment of prostate cancer. This therapy utilizes radioactive isotopes targeted specifically to prostate cancer, combining the…
We present an advanced mCRPC case treated with combined [ 177 Lu]Lu-PSMA-617 and [ 223 Ra]Radiumdichloride. The regimen was well tolerated, with mild xerostomia, fatigue (CTCAE 1), and moderate anemia…
BACKGROUND: Radium-223 dichloride (Ra-223) improves survival in men with metastatic castration-resistant prostate cancer (mCRPC) and bone metastases, but its interaction with bone-modifying agents rem…
BackgroundProstate cancer (PCa) bone lesions are bone-forming, which contribute to an immunosuppressive bone-tumor microenvironment (bone-TME). Targeting PCa-induced bone with the radiopharmaceutical …
Block M, Cleton A, Zieschang C, Johanssen S et al.
Introductionα-emitting radiopharmaceuticals are increasingly being evaluated as potential cancer therapeutics. In this study, the authors evaluated the distribution of thorium-227 (²²⁷Th) and its firs…
ObjectivesThis practice parameter was revised collaboratively by the American College of Radiology (ACR), the American College of Nuclear Medicine (ACNM), the American Radium Society (ARS), and the So…
ObjectiveTo investigate clinical factors associated with prognosis in patients with metastatic castration-resistant prostate cancer (mCRPC) and bone metastases treated with radium-223 dichloride (²²³R…
BackgroundRadium-223 (Ra-223) received U.S. Food and Drug Administration (FDA) approval for treating castration-resistant prostate cancer with symptomatic bone metastases, excluding visceral metastase…
Targeted alpha therapy (TAT) using alpha particle-emitting radionuclides is in the spotlight after the approval of ²²³RaCl₂ for patients with metastatic castration-resistant prostate cancer and the de…
Among all existing radionuclides, only a few are of interest for therapeutic applications and more specifically for targeted alpha therapy (TAT). From this selection, actinium-225, astatine-211, bismu…
The targeted alpha therapy radium-223 (²²³Ra) can prolong survival in men with castration-resistant prostate cancer (CRPC) who have symptomatic bone metastases and no known visceral metastases. Precli…
BackgroundAbiraterone acetate plus prednisone or prednisolone improves progression-free survival and overall survival in patients with metastatic castration-resistant prostate cancer. Radium-223 impro…
Targeted Alpha Therapy Working Group, Parker C, Lewington V, Shore N et al.
ImportanceTargeted alpha therapy attempts to deliver systemic radiation selectively to cancer cells while minimizing systemic toxic effects and may lead to additional treatment options for many cancer…
Alpha-emitters are radionuclides that decay through the emission of high linear energy transfer α-particles and possess favorable pharmacologic profiles for cancer treatment. When coupled with monoclo…
Poeppel TD, Handkiewicz-Junak D, Andreeff M, Becherer A et al.
Radium Ra-223 dichloride (radium-223, Xofigo®) is a targeted alpha therapy approved for the treatment of castration-resistant prostate cancer (CRPC) with symptomatic bone metastases and no known visce…
Targeted radionuclide therapy (TRT) is a branch of cancer medicine concerned with the use of radioisotopes, radiolabelled molecules, nanoparticles, or microparticles that either naturally accumulate i…
Sartor O, Coleman RE, Nilsson S, Heinrich D et al.
BackgroundBaseline clinical variables are prognostic for overall survival (OS) in patients with castration-resistant prostate cancer (CRPC). Their prognostic and predictive value with agents targeting…
Suominen MI, Fagerlund KM, Rissanen JP, Konkol YM et al.
Purpose: Radium-223 dichloride (radium-223, Xofigo), a targeted alpha therapy, is currently used for the treatment of patients with castration-resistant prostate cancer (CRPC) with bone metastases. Th…
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