Theranostics in Oncology: Integrating Molecular Imaging and Targeted Radionuclide Therapy for Precision Cancer Care
Review Summary
A state-of-the-art review examining the biological basis, clinical applications, technological advances and future direction of theranostics in precision oncology.
Theranostics combines molecular imaging with targeted radionuclide therapy to support individualized cancer diagnosis, patient selection, treatment and response assessment. Established applications include neuroendocrine tumours, prostate cancer and differentiated thyroid carcinoma.
To provide a state-of-the-art overview of the biological foundations, clinical applications and emerging evidence for theranostics in modern oncology.
The review critically evaluates developments in radiopharmaceutical research, quantitative molecular imaging, personalized dosimetry and artificial intelligence, alongside emerging molecular targets and next-generation radiopharmaceutical technologies.
Theranostics has transformed treatment pathways for selected malignancies. Wider clinical implementation, however, requires stronger comparative evidence, improved global radionuclide access and integration of new technologies into routine clinical practice.
Promising areas include alpha-particle therapy, AI-guided personalized dosimetry, FAP-targeted theranostics, radiogenomics, radionuclide–immunotherapy combinations and expanded radionuclide production.
Evidence Identification & Synthesis
The manuscript uses a narrative-review methodology and prioritises clinically relevant and influential evidence.
PubMed/MEDLINE, Embase, Scopus, Web of Science and Google Scholar.
Earlier landmark publications were additionally included where required for historical context.
Priority was given to randomized trials, multicentre studies, pivotal phase II/III trials, international guidelines, consensus statements and high-quality reviews.
Formal systematic-review methods, quantitative meta-analysis and formal risk-of-bias scoring were not performed.
One Molecular Target — Diagnosis & Therapy
Theranostics links molecular imaging and targeted radionuclide treatment through a common tumour-associated biological target.
Identify the Target → Image Its Expression → Select the Patient → Deliver Targeted Therapy
Radiolabelled ligands can demonstrate target expression non-invasively before therapy and subsequently deliver therapeutic radionuclides to the same biological target. This creates a molecular framework connecting diagnosis, treatment selection and response assessment.
Molecular Target
Identify a tumour-associated receptor, transporter or other molecular characteristic suitable for selective targeting.
Molecular Imaging
Radiolabelled diagnostic ligands demonstrate target expression and whole-body tumour distribution.
Patient Selection
Imaging identifies patients whose disease expresses the target and who may therefore benefit from targeted radionuclide therapy.
Targeted Therapy
A therapeutic radionuclide is delivered selectively to target-positive malignant tissue.
Where Theranostics Is Being Applied
The review distinguishes mature, evidence-based applications from newer and still-emerging indications.
SSTR-Targeted Theranostics
Somatostatin receptor imaging enables selection for peptide receptor radionuclide therapy. The review highlights 177Lu-DOTATATE PRRT and the NETTER-1 evidence supporting treatment of SSTR-positive neuroendocrine tumours.
PSMA-Targeted Theranostics
PSMA PET provides both disease imaging and target confirmation. 177Lu-PSMA-617 radioligand therapy has demonstrated important clinical benefit in metastatic castration-resistant prostate cancer.
Radioiodine Theranostics
Differentiated thyroid cancer represents the historical prototype of oncologic theranostics, using the sodium- iodide symporter for both disease localisation and radioiodine treatment.
Bone-Targeted Radionuclides
Bone-seeking radiopharmaceuticals exploit osteoblastic activity. The review discusses 223Ra as an alpha-emitting therapy with demonstrated benefit in selected metastatic prostate cancer.
Emerging Application
HER2, FAP, GRPR, estrogen receptor, CXCR4, PD-L1 and integrins are among investigated targets, although therapeutic breast-cancer theranostics remain largely experimental.
Beyond Established Indications
The theranostic model is increasingly being investigated across additional solid and haematological malignancies, with evidence maturity varying considerably between targets and tumour types.
Established & Emerging Targets
Expansion of oncologic theranostics depends heavily on identifying molecular targets with favourable tumour expression, accessibility and therapeutic characteristics.
Prostate-Specific Membrane Antigen
A clinically established theranostic target in advanced prostate cancer and one of the leading examples of imaging-guided radioligand therapy.
Somatostatin Receptor
A validated target in well-differentiated neuroendocrine tumours and the biological basis of PRRT.
Fibroblast Activation Protein
FAP-targeted agents exploit the tumour microenvironment and represent an important emerging platform for imaging and radioligand therapy.
Human Epidermal Growth Factor Receptor 2
Molecular imaging may permit whole-body assessment of HER2 expression and receptor heterogeneity, particularly in breast cancer.
C-X-C Chemokine Receptor Type 4
An emerging molecular target under investigation across selected solid and haematological malignancies.
Next-Generation Targets
GRPR, DLL3 and other molecular targets may further extend receptor-specific imaging and radionuclide therapy into new cancer populations.
Beyond the Radiopharmaceutical
The review highlights technologies capable of refining patient selection, activity prescription, image interpretation and response prediction.
Patient-Specific Treatment
Individualized dosimetry may allow administered activity to be adjusted to maximise tumour irradiation while limiting radiation exposure to healthy organs.
AI & Machine Learning
AI applications include image reconstruction, lesion detection, tumour segmentation, response prediction and treatment planning.
Radiomics & Biomarkers
SUV, metabolic tumour volume and radiomic features may help characterise tumour heterogeneity and refine patient stratification.
High-LET Radionuclides
Alpha emitters including 225Ac and 212Pb provide high-linear-energy-transfer radiation over a short tissue range and are being investigated in resistant disease.
Next-Generation Agents
Optimisation of binding affinity, internalisation, intracellular retention and pharmacokinetics may improve therapeutic efficacy and safety.
Molecular Integration
Integration of imaging phenotypes with genomic and molecular information represents a potential route toward increasingly precise treatment selection.
Where the Field Is Heading
The manuscript identifies several areas likely to shape the next generation of precision radionuclide therapy.
Alpha-Particle Therapy
High-LET targeted alpha therapy may expand options for tumours resistant to conventional beta-emitting radionuclide treatment.
AI-Guided Dosimetry
Artificial intelligence may improve image analysis, dose estimation, response prediction and individualized treatment planning.
FAP Theranostics
FAP-directed approaches may enable treatment across a broader range of tumours by targeting the tumour microenvironment.
Radiogenomics
Combining imaging phenotypes and genomic information may improve biological characterization and patient selection.
Combination Therapy
Radionuclide therapy combined with immunotherapy and other systemic treatments represents a promising area requiring further clinical evaluation.
Expanded Production
Greater radionuclide manufacturing capacity and more resilient supply chains will be necessary for equitable global expansion.
Barriers to Wider Clinical Adoption
Scientific progress alone will not guarantee equitable implementation of oncologic theranostics.
Clinical Validation
Many emerging indications still require high-quality comparative, randomized and long-term outcome data.
Radionuclide Availability
Limited manufacturing capacity and complex supply chains can restrict reliable access to diagnostic and therapeutic radionuclides.
Specialist Facilities
Theranostic services require nuclear medicine infrastructure, radiation protection systems and specialist multidisciplinary expertise.
Regulatory Variation
Differences in regulatory pathways and requirements can complicate implementation across health systems.
Cost & Reimbursement
Cost-effectiveness and reimbursement remain important considerations, particularly where advanced nuclear medicine resources are limited.
Dosimetry & Workflows
Standardized acquisition, analysis, dosimetry and multidisciplinary clinical pathways are required for broader reproducible implementation.
Precision Oncology Through Molecular Targeting
Its strongest evidence currently lies in selected malignancies such as neuroendocrine tumours, prostate cancer and differentiated thyroid carcinoma. Continued progress will depend on stronger comparative evidence, personalized dosimetry, next-generation radiopharmaceuticals, artificial intelligence, standardized clinical pathways and improved global access to radionuclides and specialist infrastructure.
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Review Article / Narrative Review
A state-of-the-art narrative review of the biological basis, clinical applications, emerging molecular targets, technological advances and future direction of oncologic theranostics.
PubMed/MEDLINE · Embase · Scopus · Web of Science · Google Scholar
The main search covered January 2015 to December 2026, with selected earlier landmark publications included for historical context.
Narrative Approach
Formal systematic-review techniques and meta-analysis were not conducted. Evidence was selected according to methodological quality, clinical relevance, scientific impact and contribution to the field.
No Formal Risk-of-Bias Assessment
The manuscript states that studies were not formally scored for quality and data were not quantitatively synthesized. Findings should therefore be interpreted in the context of an evolving evidence base.
Equal Contributions
The published declaration reports equal contributions from the authors.
Conflict of Interest & Funding
Conflict of Interest:
No conflict of interest.
Funding:
No funding received.
Editorial Timeline
CC BY 4.0
Published under the Creative Commons Attribution 4.0
International licence.
DOI: 10.64573/torgj2607004
Volume 2 · Issue 3 · September 2026
The Operating Room Global Journal (TORGJ).
ISSN 3105-3262.
Review Article.
DOI: 10.64573/torgj2607004.
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