Definition and research guide
This page combines a MeSH definition, publication statistics and selected research abstracts. It is a starting point for reading the literature, not a medical textbook or a systematic evidence review.
Content available: 4 complete abstracts (838 words), 10 references. Full article text is not stored or reproduced here; follow the PMID, DOI or PMC links to read the original sources and their access terms.
Definition
Compounds that are used in medicine as sources of radiation for radiotherapy and for diagnostic purposes. They have numerous uses in research and industry. (Martindale, The Extra Pharmacopoeia, 30th ed, p1161)
Definition: NLM Medical Subject Headings (MeSH) scope note (Public domain (U.S. National Library of Medicine); attribution requested). View the MeSH record.
Also known as: Radiopharmaceutical.
Where it fits in the MeSH classification
- Broader topics
- Diagnostic Uses of Chemicals; Molecular Mechanisms of Pharmacological Action; Indicators and Reagents
Research landscape
PubMed indexes 62,960 records tagged with the MeSH heading “Radiopharmaceuticals” (counts retrieved 2026-10-29). 12,874 of them (20.4%) were published from 2020 onward, and the busiest period so far is 2010-2019 with 23,798 records.
Reviews account for 8,271 records (13.1%) and meta-analyses for 638. Randomized controlled trials number 811 (1.3%) as a share of all records on the topic. Randomized trials make up only a small share of this literature, so much of what is known comes from laboratory, observational or descriptive work.
Show the data
| Period | Records |
|---|---|
| through 1999 | 4,327 |
| 2000-2009 | 21,961 |
| 2010-2019 | 23,798 |
| 2020 onward | 12,874 |
Publication-type chart data
| Type | Records | Share |
|---|---|---|
| Reviews | 8,271 | 13.1% |
| Meta-analyses | 638 | 1.0% |
| Randomized controlled trials | 811 | 1.3% |
Method: PubMed query "Radiopharmaceuticals"[MeSH Terms] with publication-type and date filters, retrieved 2026-10-29.
Reading the evidence in pharmacology
Drug evidence builds in layers: laboratory pharmacology describes how a compound acts, pharmacokinetic studies describe how the body handles it, and randomized trials test whether it helps and what harms it causes. Post-marketing surveillance and observational studies reveal rarer adverse effects but cannot prove causation. This page is educational and is not a recommendation to start, stop or change any medicine; decisions about treatment belong with a qualified clinician.
Evidence from open-access studies
These open-access studies come from PubMed’s best-match results for this heading (papers whose main topic it is), ranked here by citation count, with one recent addition. Each abstract is reproduced in full under its recorded open licence so that you can read the authors’ own words. They illustrate the literature; they are not a systematic summary of it. Citation counts measure attention, not reliability or clinical benefit.
Emerging PET Imaging Agents and Targeted Radioligand Therapy: A Review of Clinical Applications and Trials [1]
Abstract reading summary — source excerpts
- Opening excerpt
- Targeted radioligand therapy (RLT) is an emerging field in anticancer therapeutics with great potential across tumor types and stages of disease.
- Closing excerpt
- Here, we provide a primer for practicing radiologists, particularly nuclear medicine clinicians, to understand novel PET imaging agents and their clinical applications, as well as the availability of companion targeted radiotherapeutics, the status of their regulatory approval, the potential challenges associated with their use, and the future opportunities and perspectives.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (201 words)
Targeted radioligand therapy (RLT) is an emerging field in anticancer therapeutics with great potential across tumor types and stages of disease. While much progress has focused on agents targeting somatostatin receptors and prostate-specific membrane antigen (PSMA), the same advanced radioconjugation methods and molecular targeting have spurred the development of numerous theranostic combinations for other targets. A number of the most promising agents have progressed to clinical trials and are poised to change the landscape of positron emission tomography (PET) imaging. Here, we present recent data on some of the most important emerging molecular targeted agents with their exemplar clinical images, including agents targeting fibroblast activation protein (FAP), hypoxia markers, gastrin-releasing peptide receptors (GRPrs), and integrins. These radiopharmaceuticals share the promising characteristic of being able to image multiple types of cancer. Early clinical trials have already demonstrated superiority to 18F-fluorodeoxyglucose (18F-FDG) for some, suggesting the potential to supplant this longstanding PET radiotracer. Here, we provide a primer for practicing radiologists, particularly nuclear medicine clinicians, to understand novel PET imaging agents and their clinical applications, as well as the availability of companion targeted radiotherapeutics, the status of their regulatory approval, the potential challenges associated with their use, and the future opportunities and perspectives.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 40863874 · DOI · PMC12390037
Chemical Tools to Characterize the Coordination Chemistry of Radionuclides for Radiopharmaceutical Applications [2]
Abstract reading summary — source excerpts
- Opening excerpt
- During the past decade, the advancement and approval of novel radiopharmaceuticals for clinical application has led to a resurgence of the field of radiochemistry and specifically the coordination chemistry of radionuclides.
- Closing excerpt
- This Review provides an in-depth survey of common, contemporary characterization strategies for the coordination chemistry of radionuclides, including case studies to demonstrate context and relevance for the prospective development of clinically translatable radiopharmaceuticals.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (142 words)
During the past decade, the advancement and approval of novel radiopharmaceuticals for clinical application has led to a resurgence of the field of radiochemistry and specifically the coordination chemistry of radionuclides. In addition to well established radionuclides, short-lived radioisotopes of other elements are becoming accessible using new isotope production methods, necessitating the development of coordination chemistry compatible with the aqueous chemistry of such elements under tracer level conditions. As radiochemistry with radioactive metal ions relevant for radiopharmaceuticals is conducted at the nano- to picomole scale, conventional chemical characterization techniques can generally not be applied. Therefore, careful consideration and interfacing of tracer-level compatible techniques and macroscopic characterization methods is required. This Review provides an in-depth survey of common, contemporary characterization strategies for the coordination chemistry of radionuclides, including case studies to demonstrate context and relevance for the prospective development of clinically translatable radiopharmaceuticals.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 41147499 · DOI · PMC12746417
Characteristics of 18F-FAPI-04 PET/CT in patients with peritoneal metastasis and to predict treatment efficacy, a head-to-head comparison with 18F-FDG PET/CT [3]
Abstract reading summary — source excerpts
- Opening excerpt
- Background18F-FAPI-04 PET/CT shows promise in detecting peritoneal metastases (PM), but its superiority over 18F-FDG PET/CT for lesion detection and predicting chemotherapy benefit remains unclear.
- Closing excerpt
- Conclusion18F-FAPI-04 PET/CT outperforms 18F-FDG in PM detection, with semi-quantitative parameters predicting chemotherapy response.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (235 words)
Background18F-FAPI-04 PET/CT shows promise in detecting peritoneal metastases (PM), but its superiority over 18F-FDG PET/CT for lesion detection and predicting chemotherapy benefit remains unclear.PurposeTo compare 18F-FAPI-04 and 18F-FDG PET/CT imaging features in PM and assess predictive value of 18F-FAPI-04 for chemotherapy efficacy.Methods39 pathologically confirmed PM patients with digestive malignancies underwent concurrent 18F-FAPI-04 and 18F-FDG PET/CT. Semi-quantitative parameters, including SUVmax, tumor/liver ratio (T/L), tumor/mediastinal blood pool ratio (T/B), were analyzed. The tracer uptake was compared via Wilcoxon tests. The relationships between 18F-FAPI-04 uptake with FAP and α-SMA expression were analyzed using Pearson correlation. Patients were divided into different short-term outcome groups (responders vs. non-responders) according to RECIST criteria (v.1.1) after chemotherapy. Post-chemotherapy outcomes were evaluated using logistic regression.ResultsPatients (median age 62; 16 females, 23 males) included pancreatic (n = 17), cholangiocarcinoma (n = 8), gastric (n = 6), and colorectal cancers (n = 8). 18F-FAPI-04 demonstrated significantly higher SUVmax, T/L, and T/B than 18F-FDG (P 18F-FAPI-04 parameters positively correlated with FAP and α-SMA expression. In univariate analysis, 18F-FAPI-04 uptake differed significantly between responders and non-responders. Multivariate analysis identified SUVmax as an independent predictor (OR = 1.354, 95%CI:1.025-1.788, P = 0.033). Optimal 18F-FAPI-04 cut-offs for distinguishing outcomes were SUVmax=11.05 (AUC = 0.783; sensitivity = 70.60%, specificity = 80.40%), T/L = 7.53 (AUC = 0.717; 58.82%, 81.82%), and T/B = 8.76 (AUC = 0.751; 64.71%, 86.37%).Conclusion18F-FAPI-04 PET/CT outperforms 18F-FDG in PM detection, with semi-quantitative parameters predicting chemotherapy response.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 40457405 · DOI · PMC12128257
Targeting Fibroblast Activation Protein with [177Lu]Lu-FAP-2286 in Patients with Advanced Solid Tumors in the Phase I LuMIERE Trial [4]
Abstract reading summary — source excerpts
- Opening excerpt
- PurposeFibroblast activation protein (FAP) is an attractive target for radiopharmaceutical therapy.
- Closing excerpt
- The safety and preliminary efficacy findings support its continued development in phase II.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (260 words)
PurposeFibroblast activation protein (FAP) is an attractive target for radiopharmaceutical therapy. Phase I of the LuMIERE study (ClinicalTrials.gov, NCT04939610) investigated the safety of [177Lu]Lu-FAP-2286 (177Lu-FAP-2286) in heavily pretreated patients with advanced solid tumors and identified the recommended phase II dosage (RP2D).Patients and methodsLuMIERE is a prospective, open-label, nonrandomized, phase I/II, multicenter study. Phase I followed a Bayesian optimal interval design evaluating four escalating activity levels of 177Lu-FAP-2286 (3.70, 5.55, 7.40, and 9.25 GBq). Patients were selected by positive [68Ga]Ga-FAP-2286 (68Ga-FAP-2286, also known as [68Ga]Ga-HKG301) PET/CT imaging on all target lesions [maximum standardized uptake value (SUVmax) ≥1.5× SUVmean of mediastinal blood pool]. 177Lu-FAP-2286 was administered intravenously every 6 weeks for ≤6 cycles. The primary endpoint was dosage-limiting toxicities (DLT) and treatment-emergent adverse events (TEAE).ResultsOf 35 patients imaged with 68Ga-FAP-2286, 27 received 177Lu-FAP-2286 (3.70 GBq, n = 3; 5.55 GBq, n = 6; 7.40 GBq, n = 7; 9.25 GBq, n = 11). Two DLTs were observed: one patient who received 5.55 GBq of 177Lu-FAP-2286 experienced grade 4 lymphopenia, and one patient who received 9.25 GBq experienced grade 3 hemoptysis; these were the only treatment-related grade ≥3 TEAEs. All-cause grade ≥3 TEAEs were reported for 11 patients (40.7%). The RP2D for 177Lu-FAP-2286 monotherapy was determined to be 9.25 GBq. Preliminary Response Evaluation Criteria in Solid Tumors efficacy findings demonstrated a partial response in 1 patient and stable disease in 10 patients (maintained for at least two assessments in 6 patients).Conclusions177Lu-FAP-2286 was well tolerated in patients with advanced solid tumors. The safety and preliminary efficacy findings support its continued development in phase II.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 42223513 · DOI · PMC13335097
Key reviews and meta-analyses
The most cited review-type papers among PubMed’s best-match results for this heading, listed with bibliographic details only. Follow the links for the full text and access terms.
- Research article Diagnosis of bone metastases: a meta-analysis comparing ¹⁸FDG PET, CT, MRI and bone scintigraphy [5]
- Research article Evidence-Based Management of Hepatocellular Carcinoma: Systematic Review and Meta-analysis of Randomized Controlled Trials (2002-2020) [6]
- Research article Meta-analysis of 18F-FDG PET/CT in the diagnosis of infective endocarditis [7]
- Research article Systematic review and meta-analysis on the diagnostic performance of FDG-PET/CT in detecting bone marrow involvement in newly diagnosed Hodgkin lymphoma: is bone marrow biopsy still necessary? [8]
- Research article Comparison of 18F-based PSMA radiotracers with [68Ga]Ga-PSMA-11 in PET/CT imaging of prostate cancer-a systematic review and meta-analysis [9]
- Research article Meta-analysis: comparison of F-18 Fluorodeoxyglucose-positron emission tomography and bone scintigraphy in the detection of bone metastases in patients with breast cancer [10]
References
- Palihati M, Das JP, Yeh R, Capaccione K. Emerging PET Imaging Agents and Targeted Radioligand Therapy: A Review of Clinical Applications and Trials. . 2025. PMID 40863874 · DOI · PMC12390037
- Boros E, Comba P, Engle JW, Harriswangler C, Lapi SE, Lewis JS, et al.. Chemical Tools to Characterize the Coordination Chemistry of Radionuclides for Radiopharmaceutical Applications. . 2025. PMID 41147499 · DOI · PMC12746417
- Zhang Y, Xu M, Wang Y, Yu F, Chen X, Wang G, et al.. Characteristics of 18F-FAPI-04 PET/CT in patients with peritoneal metastasis and to predict treatment efficacy, a head-to-head comparison with 18F-FDG PET/CT. . 2025. PMID 40457405 · DOI · PMC12128257
- McConathy J, Koshkin VS, Menda Y, Rodon J, Goenka AH, Moy RH, et al.. Targeting Fibroblast Activation Protein with [177Lu]Lu-FAP-2286 in Patients with Advanced Solid Tumors in the Phase I LuMIERE Trial. . 2026. PMID 42223513 · DOI · PMC13335097
- Yang HL, Liu T, Wang XM, Xu Y, Deng SM. Diagnosis of bone metastases: a meta-analysis comparing ¹⁸FDG PET, CT, MRI and bone scintigraphy. Eur Radiol. 2011. PMID 21887484 · DOI
- Haber PK, Puigvehí M, Castet F, Lourdusamy V, Montal R, Tabrizian P, et al.. Evidence-Based Management of Hepatocellular Carcinoma: Systematic Review and Meta-analysis of Randomized Controlled Trials (2002-2020). Gastroenterology. 2021. PMID 34126063 · DOI · PMC12276942
- Mahmood M, Kendi AT, Ajmal S, Farid S, O'Horo JC, Chareonthaitawee P, et al.. Meta-analysis of 18F-FDG PET/CT in the diagnosis of infective endocarditis. J Nucl Cardiol. 2019. PMID 29086386 · DOI
- Adams HJ, Kwee TC, de Keizer B, Fijnheer R, de Klerk JM, Littooij AS, et al.. Systematic review and meta-analysis on the diagnostic performance of FDG-PET/CT in detecting bone marrow involvement in newly diagnosed Hodgkin lymphoma: is bone marrow biopsy still necessary?. Ann Oncol. 2014. PMID 24351400 · DOI
- Huang S, Ong S, McKenzie D, Mirabelli A, Chen DC, Chengodu T, et al.. Comparison of 18F-based PSMA radiotracers with [68Ga]Ga-PSMA-11 in PET/CT imaging of prostate cancer-a systematic review and meta-analysis. Prostate Cancer Prostatic Dis. 2024. PMID 38017295 · DOI · PMC11543591
- Shie P, Cardarelli R, Brandon D, Erdman W, Abdulrahim N. Meta-analysis: comparison of F-18 Fluorodeoxyglucose-positron emission tomography and bone scintigraphy in the detection of bone metastases in patients with breast cancer. Clin Nucl Med. 2008. PMID 18209527 · DOI
About this article
- Sources
- NLM Medical Subject Headings (definition, synonyms); NCBI PubMed (counts, identifiers); Europe PMC (open-access abstracts and citation counts).
- Verification
- Every reference was resolved against PubMed on 2026-10-31; title, year and DOI matched.
- Review state
- automated source verified; no human expert review has been recorded yet.
- Version
- 1, last updated 2026-10-29.
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Evidence strength
EvidenceHelix's computed view of the study designs behind this topic: how common meta-analyses, randomized trials and reviews are, how recent the literature is, and a plain-language reading. It describes the design mix of the literature. It is not a quality appraisal of any study, and it is not medical advice.