Therapeutic radiopharmaceuticals have moved from niche applications to an increasingly important component of modern oncology. Agents such as [¹⁷⁷Lu]Lu-PSMA-617, [¹⁷⁷Lu]Lu-DOTATATE, and [²²⁵Ac]Ac-labeled compounds are reshaping treatment for prostate cancer, neuroendocrine tumors, and beyond. As clinical indications expand, so does the need to optimize how these agents are dosed. Standard fixed-activity regimens fail to account for interpatient, intrapatient, and inter-lesional variability in pharmacokinetics, target expression, and absorbed dose — leaving efficacy on the table for some and narrowing the therapeutic index for others.
Dose optimization in this context is a fundamentally pharmacological challenge. It spans the design of targeting vectors, the characterization of radiopharmaceutical biodistribution, the development of dosimetry-guided individualization strategies, and the identification of predictive biomarkers that inform patient selection and treatment response. Theranostic pairing — using a diagnostic radioligand to predict therapeutic dosing — represents one of the field’s most promising approaches to precision dosing, and its pharmacological basis remains an active area of investigation.
This Research Topic invites contributions that address the pharmacological determinants of dose optimization for therapeutic radiopharmaceuticals across the pipeline, from preclinical development to clinical translation. We welcome studies exploring radiolabeled compound design, pharmacokinetic and pharmacodynamic modeling, dosimetry methodologies, combination strategies
with chemotherapy or immunotherapy, and biomarker development for patient stratification. Research linking absorbed dose to tumor response at the cellular, tissue, and whole-body level is particularly encouraged.
Relevant themes include, but are not limited to:
•Radiopharmaceutical design, radiolabeling, and targeting moiety optimization
•Pharmacokinetics and biodistribution modeling
•Dosimetry-guided treatment individualization
•Theranostic approaches and companion diagnostics
•Combination of radiopharmaceuticals with chemotherapy, immunotherapy, targeted therapy, or radiosensitizers
•Biomarkers predictive of response, resistance, and therapeutic index
•Alpha- versus beta-emitter pharmacology, radiobiology, and dosing considerations
•Preclinical models for dose–response characterization and clinical translation
•Artificial Intelligence in dosimetry
•Toxicologic profile and adverse effects of therapeutic radiopharmaceuticals
We welcome Original Research Articles, Reviews, Mini-Reviews, Systematic Reviews, and Perspectives. Submissions should provide mechanistic or translational insight into the pharmacological aspects of radiopharmaceutical dosing and connect findings to the broader goal of improving cancer treatment outcomes.
Article types and fees
This Research Topic accepts the following article types, unless otherwise specified in the Research Topic description:
Brief Research Report
Case Report
Clinical Trial
Data Report
Editorial
FAIR² Data
General Commentary
Hypothesis and Theory
Methods
Articles that are accepted for publication by our external editors following rigorous peer review incur a publishing fee charged to Authors, institutions, or funders.
Article types
This Research Topic accepts the following article types, unless otherwise specified in the Research Topic description:
Important note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.
