Theranostics · Literature Radar
Targeted alpha therapy — Ac-225 PSMA and DOTATATE clinical experience, supply and dosimetry. Curated daily from Europe PMC (PubMed + PMC + preprints) and OpenAlex — free-full-text link on each open-access paper.
Meng C, Cheng Z, Ma X.
Malignant melanoma (MM) remains a formidable clinical challenge due to its high metastatic potential and the eventual emergence of resistance to current BRAF/MEK and immune checkpoint inhibitors. To a…
Zulfiqar H, Waqas M, Ali I.
The theranostic paradigm, combining molecular diagnosis and targeted radionuclide therapy in a single platform, has revolutionized precision oncology. Radiopharmaceutical theranostics enables targeted…
Cato TL, Singer JM.
Oak Ridge National Laboratory (ORNL) operates under multiple quality frameworks using a graded approach for research operations, hazardous radioactive and nuclear material handling, and nuclear reacto…
Ebrahimifard A, Bagheri S, Wang Q, Hojjat Shamami A et al.
This retrospective analysis interrogates the value of a multimodal biomarker paradigm to characterize molecular and clinical responses to [²²⁵Ac]Ac-PSMA-617-targeted α-therapy (TAT) in cohorts of heav…
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…
Sun B, Werner D, Ni J, Weidle S et al.
Prostate-specific membrane antigen (PSMA)-targeted α-therapy holds promise for the treatment of prostate cancer but has increased side effects compared with therapy using β-emitting PSMA ligands. This…
Lin ET.
Among prostate-specific membrane antigen (PSMA)-directed radioligand therapies (RLT), ¹⁷⁷Lu-PSMA-617 is supported by two peer-reviewed phase III randomised controlled trials in metastatic castration-r…
Polyak A, Matuschek C.
Bone radiopharmaceuticals have evolved from early palliative agents into integral components of targeted precision oncology and theranostics. This review comprehensively traces the historical trajecto…
Long H, Qiao XH, Li X, Kong XJ et al.
ObjectiveTo characterize publication growth, modality trends, and thematic evolution in prostate-specific membrane antigen (PSMA) radioligand therapy (RLT) for prostate cancer from 2015 to 2025, empha…
Brejeon A, Seo Y, VanBrocklin HF, Flavell RR et al.
The development of 134Ce as both a positron-emitting surrogate for 225Ac and a therapeutic Auger and conversion-electron (ACE) emitter has accelerated rapidly in recent years, positioning it as one of…
Medina Guevara Y, Rojas HC, Idrissou MB, Lepesevich LL et al.
The absence of estrogen receptor, progesterone receptor, and HER2 expression limits the utility of targeted therapies in triple-negative breast cancer (TNBC). Chemotherapy is the standard of care for …
Otsu M, Saito K, Nakashima K, Fujimoto H et al.
Neurotensin receptor 1 (NTSR1) is overexpressed in various types of cancer and known as a promising target for cancer therapy. Targeted alpha therapy (TAT) using α-emitting radionuclides with high lin…
Caravaca J, Seo Y, Cabello J, Siegel SB et al.
Clinical imaging of the α-therapy radionuclide ²²⁵Ac and its progeny has proven challenging with SPECT because of low detection efficiency and a poor signal-to-noise ratio (SNR). We propose an alterna…
Sayman HB, Aras O, Hekim MV, Sağlam K et al.
PurposeTo evaluate the feasibility, safety, and preliminary efficacy of systemic targeted alpha therapy with [²²⁵Ac]-PSMA in patients with recurrent high-grade glioma (HGG). Glioblastoma multiforme (G…
Wenker STM, Franssen GM, Molkenboer-Kuenen JDM, Konijnenberg MW et al.
PurposeTumor hypoxia correlates with a poor prognosis in many solid tumors, including head and neck squamous cell carcinoma (HNSCC). Carbonic anhydrase IX (CAIX) is an endogenous hypoxia-related marke…
Lee W, Chung JY, Adler S, Basuli F et al.
Glypican-3 (GPC3), highly expressed in the most common liver cancer hepatocellular carcinoma (HCC) but absent from normal liver, represents an attractive tumor-selective target. We evaluated GPC3-targ…
Kvassheim M, Karlberg A, Blakkisrud J, Stokke C.
Biokinetics for potential alpha-emitter peptide receptor radionuclide therapies (PRRTs) were simulated to estimate tumour-to-kidney absorbed dose ratios for 225Ac, 227Th, 212Pb, 230U, 226Ac, 211At, an…
Saad F, Hotte S, Jayaram A, Artigas C et al.
Abstract Prolonged survival demonstrated with the alpha-emitting radionuclide radium-223 dichloride and the prostate-specific membrane antigen (PSMA)-targeting radioligand [ 177 Lu]Lu-PSMA-617 in pati…
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 …
Jeanjean P, Swaidan A, Tse C, Kwock S et al.
Glioblastoma represents the most lethal form of brain cancer, characterized by a 5-y survival rate of approximately 4%. Fibroblast activation protein (FAP), expressed within both the tumor microenviro…
Du S, Bobba KN, Peter R, Gullberg GT et al.
BackgroundTargeted alpha therapy (TAT) using actinium-225 (²²⁵Ac) holds great promise for cancer treatment, and to advance ²²⁵Ac therapy it is required to develop accurate dosimetry method. ²²⁵Ac daug…
García-Arce D, Luna-Gutiérrez M, Cruz-Nova P, Vidal-Limon A et al.
Prostate-specific membrane antigen (PSMA) is a validated theranostic target with clinical relevance extending beyond prostate cancer to PSMA-expressing neovasculature in solid tumors. Despite the succ…
Amghar M, Hielscher T, Rausch T, Özgür H et al.
BackgroundProstate-specific membrane antigen-targeted radioligand therapy (PSMA-RLT) demonstrates clinical efficacy in metastatic castration-resistant prostate cancer (mCRPC), yet robust biomarkers fo…
Winter RC, Bauder-Wüst U, Schäfer M, Remde Y et al.
Metastatic cancer remains a major challenge, demanding more effective and biologically informed therapeutic strategies. Targeted Radionuclide Therapy (TRT) holds significant promise, but its optimizat…
Chi WY.
Background: Trophoblast cell surface antigen 2 (TROP2, encoded by TACSTD2) is a transmembrane glycoprotein overexpressed in multiple aggressive epithelial carcinomas. While antibody drug conjugates ta…
Rishi Chakraborty
Peptide Receptor Radionuclide Therapy (PRRT) Lu-177 DOTATATE resistance in well-differentiated Grade 3 Neuroendocrine Tumors (NETs) is a type of acquired therapeutic resistance in well differentiated …
Babeker H, Nwangele E, Monzer A, Pougoue Ketchemen J et al.
PurposeMUC-16-targeted antibodies can deliver contrast agents (diagnostic) and/or cytotoxic payloads (therapy) to the tumor site. MUC-16 is overexpressed in 80% of epithelial ovarian cancer (EOC) and …
Hao Zhang, Yekuan Shi, Yanqin Yu, Zongxi He et al.
Abstract Objective Metastatic castration-resistant prostate cancer (mCRPC) remains associated with poor long-term outcomes, and survival under current treatment is modest. Prostate-specific membrane a…
Liu Y, Xu T, Yang H, Huang Z et al.
PurposeTo investigate the association between baseline NETPET score and prognosis in patients with neuroendocrine tumors (NETs) receiving [225Ac]Ac-DOTATATE therapy.MethodsThis retrospective study inc…
Adrien Holzgreve, Sophie C. Siegmund, Liam Widjaja, Rudolf A. Werner
management of patients with advanced prostate cancer, firmly anchored in clinical guidelines [8].This article provides an update on established PSMA theranostics using beta-emitting ligands, based on …
Jiang T, Xiao Z.
Pancreatic ductal adenocarcinoma (PDAC) remains one of the most lethal malignancies, characterized by the limited efficacy of current therapies and an urgent need for novel treatment strategies. Targe…
Sakashita T, Onuma K, Sugasawa A, Sasaki I et al.
IntroductionTargeted alpha therapy using ²¹¹At offers high therapeutic efficacy with relatively low occupational radiation exposure. However, in veterinary medicine, staff exposure-particularly during…
Shabnam M, Shah SQ, Santos-Oliveira R.
Targeted alpha therapy (TAT) has the advantage of localized cytotoxicity using the high linear energy transfer capabilities of alpha particles. Actinium-225 ([225Ac]Ac) has been shown to be suitable f…
Adam DP, Yusufaly T, Marsh IR, Bastiaannet R et al.
Standard of care RPT may result in dose-limiting side effects of the salivary glands include sialadenitis and xerostomia that are inconsistent with outcomes from external beam for equivalent ADs. This…
Echigo H, Munekane M, Fuchigami T, Mishiro K et al.
Macropa has formed more stable complexes with 225Ac, although DOTA has been extensively used as a chelator for 225Ac. This study aimed to design and synthesize two novel 225Ac-labeled RGD peptides, [2…
Sgouros G, Ulaner GA, He B, Ghaly M et al.
Gastroenteropancreatic neuroendocrine tumors (GEP-NETs) are biologically and clinically heterogeneous tumors, most of which overexpress somatostatin receptors (SSTRs). The presence of SSTRs enables st…
Zhu J, Cao S, Li X, Qi Y et al.
BackgroundDosimetric studies of targeted alpha therapy (TAT) show that microscopic heterogeneity in geometry and source distribution strongly affects dose-effect relationships, underscoring the potent…
Zhao L, Clark PA, Shireman JM, Schepp CL et al.
BackgroundLeptomeningeal metastasis from a solid tumor carries a dismal prognosis with median survival of 3-5 months after diagnosis and treatment with external beam radiation therapy. It targets the …
Sabri ME, Moghaddasi L, Wilson P, Saran F et al.
BackgroundGlioblastoma (GB) is an aggressive primary brain tumor with local recurrence rates exceeding 90% and a five-year survival rate of approximately 5%. Standard treatments such as surgical resec…
Espino López R, Quiroga Castro CC, Boudjemeline M, Martinez LMA.
The development and validation of analytical methods are critical to ensure the quality, safety, and efficacy of radiopharmaceutical products. This study describes the development and comprehensive va…
Ghaemi B, Olkowski CP, Basuli F, Shi J et al.
Small cell lung cancer (SCLC) remains one of the most lethal malignancies, with a five-year survival of <10% despite advances in treatment. Seizure-related gene 6 (SEZ6), a type I transmembrane protei…
Dragonetti V, Mattana F, Ceci F.
BackgroundRadioligand therapy targeting the prostate-specific membrane antigen (PSMA) has been established as a key treatment for PSMA-positive metastatic castration-resistant prostate cancer followin…
Muzzioli R, Pisaneschi F, Gammon ST, Sutton MN et al.
Talazoparib (TZ) is a potent poly(ADP-ribose) polymerase 1/2 (PARP1/2) inhibitor that uniquely traps PARP complexes at sites of single-strand DNA damage thereby offering opportunities for targeted rad…
Agrawal R, Parghane RV, Joshi A, Prabhash K et al.
IntroductionA subset of prostate cancer progresses to aggressive state of metastatic castration-resistant prostate cancer (mCRPC), wherein multiple therapeutic options demonstrate limited success rate…
Zhang Z, Wang H, Zhuang H, Li F et al.
An 11-year-old boy with relapsed, poorly differentiated left adrenal neuroblastoma presented with multiple bone metastases, demonstrated by an 18 F-MFBG PET/CT with a Curie score of 4, despite prior m…
Gaddis K, Roach B, Copping R, Griswold J et al.
Actinium-225 (t1/₂ = 9.92 days) is an important radioisotope for targeted alpha therapy applications. The limited supply obtained through the decay of thorium-229 has motivated accelerator-based produ…
Tagawa ST, Thomas C, Arham AB, Holmes A et al.
To test safety of two regimens at differing levels of radioactivity of PSMA-targeted alpha radionuclide 225Ac-J591. Patients with progressive, metastatic androgen pathway modulator resistant prostate …
Claude G, Balzer M, Brenner W, Bruchertseifer F et al.
BackgroundAnalytical data for 225Ac-labeled radiopharmaceuticals are currently obtained using thin-layer chromatography and high-performance liquid chromatography, the latter followed by offline fract…
Zhang J, Song Z, Chen Z, Luan X et al.
PurposeThis study aimed to elucidate the biological mechanisms underlying the therapeutic effects of targeted alpha therapy (TAT) using a novel ²¹¹At-labeled single-domain antibody drug ([²¹¹At]At-AuN…
Wang Z, Xiao D, Wang B, Tang W et al.
ObjectiveThis studyaims to systematically elucidate the mechanisms underlying hematologic toxicity in 225Ac-PSMA-617 treatment for metastatic castration-resistant prostate cancer (mCRPC), establish a …
Perrone E, Ghai K, Eismant A, Greifenstein L et al.
A 45-year-old woman with heavily pretreated, recurrent metastatic esthesioneuroblastoma and progressive symptomatic disease underwent first-in-human peptide receptor radionuclide therapy (PRRT) using …
Aluicio-Sarduy E, Wehner LE, Jeffery JJ, Levitt NP et al.
Targeted α-therapy (TAT) is a promising therapeutic strategy for advanced cancers, but redistribution of short-lived daughter radionuclides remains a key challenge. This is particularly true for ²²⁵Ac…
Merkx RIJ, Kleinendorst SC, Rijpkema M, Franssen GM et al.
The aim of this study was to assess whether zirconium-89 (89Zr)-labelled antibodies can act as a surrogate for actinium-225 (225Ac)-labelled antibodies to predict tumour- and organ dose. To this end, …
Shirin S, Shah SQ, Santos-Oliveira R.
Overexpression of FcRn in multiple hematologic and solid cancers makes it a promising target for monoclonal antibodies, though its presence in healthy tissue calls for proper assessment of toxicity. H…
Dixit T, Sawardekar M, Verma T, Sreeja P et al.
Prostate-specific membrane antigen (PSMA)-based theragnostics has transformed precision oncology by integrating molecular imaging and targeted radionuclide therapy in prostate cancer (PCa). This revie…
Amatullah A, Takaki N.
Abstract Techetium-99m, the decay product of Molybdenum-99, is the most utilized radioisotope for diagnostic purposes. The demand for 99m Tc is more than 80% of all nuclear medicine radioisotopes. In …
Chakraborty M, Lee KK, Hasson A, Kanagasundaram T et al.
Radiotheranostic agents combine targeted therapeutics and diagnostic imaging, offering more efficient and personalized treatment strategies. Positron emission tomography provides high sensitivity and …
Morgan KA, Grieve ML, Akhter DT, Lange JL et al.
Prostate-Specific Membrane Antigen (PSMA) is overexpressed in some prostate cancers and is a viable candidate for targeted radionuclide therapy. PSMA targeted delivery of α2+ particle-emitting actiniu…
Liu J, Fajnorova I, Ren Y, Poku K et al.
177 Lu-PSMA-617 (Pluvicto TM , Lu-177 RLT) is an FDA-approved targeted radioligand therapy (RLT) for metastatic castration-resistant prostate cancer (mCRPC), but its durability of response to this sin…
Ling SW, Konijnenberg M, Segbers M, Hooijman E et al.
Radiopharmaceutical therapy with 225Ac-labeled prostate-specific membrane antigen (225Ac-PSMA) has shown promising results in patients with metastatic castration-resistant prostate cancer (mCRPC). To …
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