Learn more about Targeted Radionuclide Therapy (TRT) and Theranostics
Targeted radiopharmaceuticals are transforming oncology, but TRT development is fundamentally different. Many programs are developed as theranostic pairs, where imaging agents guide patient selection, biodistribution, and treatment decisions.
Sponsors must make high-stakes decisions early, defining injected activity, mass dose, fractionation, and therapeutic index, while managing dual PK, imaging-based biodistribution, and increasing regulatory expectations.
Model-informed approaches enable confident early decisions, supporting target selection, defining a clear Target Product Profile (TPP), and optimizing dose strategy to reduce late-stage risk and strengthen regulatory confidence for targeted radiopharmaceuticals, radioligands, and radioconjugates.
Sponsors must manage:
At the same time, regulatory expectations are increasing. Dose optimization is no longer optional; it is a core requirement shaping FDA and EMA interactions today.
Without clear demonstration early, programs risk delays, rework, and limited label flexibility, making early decisions critical to achieving speed, differentiation, and regulatory confidence.
One partner delivering a unified MIDD strategy, integrating mechanistic and empirical modeling across the radiopharmaceutical development lifecycle from early translation through regulatory strategy and submission support.
Integrates target expression, binding, and internalization with dosimetry and radiation modeling to quantify organ and tumor absorbed dose, and to predict biodistribution, tumor uptake, and therapeutic index
Applies biodistribution population PK and exposure–response modeling to optimize dosing, inform key development decisions, and deliver regulatory-ready evidence
In targeted radionuclide therapy and targeted radiopharmaceutical development, MIDD integrates biodistribution, dosimetry, and clinical data into a unified strategy.
This approach supports:
This integrated approach enables teams to move from data collection to decision-making with confidence, reducing uncertainty across radiopharmaceutical development.
Idea
Nonclinical
Phase 1: Safety
Phase 2: Activity
Phase 3: Efficacy
Post-Marketing
Integrated Clinical Pharmacology Support
Quantitative Systems Pharmacology (QSP)
Population PK and Exposure/Dose-Response (PMx)
MBMA, Real-World Evidence
Without an integrated strategy, these challenges can lead to late-stage rework, regulatory delays, or constrained labels.
How do we optimize injected activity, mass dose, and fractionation strategy beyond tolerability alone?
Are imaging and dosimetry data being fully integrated to drive development decisions?
How do we balance tumor radiation exposure with organ safety?
Can we competitively justify dosing strategy while enabling future label flexibility and expansion?
Are we aligned with evolving FDA, EMA, and Project Optimus expectations?
Are imaging agents effectively informing patient selection, biodistribution, and dose optimization strategies?
Certara brings integrated expertise across clinical pharmacology, QSP, PBPK, pharmacometrics, and regulatory strategy to deliver end-to-end model-informed drug development (MIDD) solutions for targeted radiopharmaceuticals and targeted radionuclide therapies.
We help teams:
Senior Director, Clinical Pharmacology and Translational Medicine
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Associate Director, Clinical Pharmacology
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Director
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Whether defining your first-in-human dose, evaluating biodistribution and dosimetry, optimizing treatment strategy, or preparing for regulatory interactions, Certara helps targeted radionuclide therapy (TRT) and theranostics teams reduce uncertainty and make confident, model-informed development decisions.
We help teams
Radiopharmaceutical development and targeted radionuclide therapy (TRT) use radioactive isotopes linked to targeting molecules to selectively deliver radiation to tumors while minimizing exposure to healthy tissue. Many targeted radiopharmaceuticals are developed as theranostic pairs, combining imaging and therapeutic agents.
Radiopharmaceutical development and TRT development involve complex decisions around biodistribution, dosimetry, therapeutic index, fractionation, and organ toxicity. Model-informed approaches help sponsors optimize dose strategies, predict tumor uptake, and generate regulatory-ready evidence earlier in targeted radiopharmaceutical development.
Certara integrates Quantitative Systems Pharmacology (QSP), Pharmacometrics, PBPK, dosimetry, and regulatory strategy to support radiopharmaceutical development and targeted radiopharmaceutical development from target selection through submission readiness.
Model-informed approaches can help address key challenges in radiopharmaceutical development and targeted radiopharmaceutical development, including:
Imaging agents support targeted radiopharmaceutical development and theranostic development by helping characterize biodistribution, assess target engagement, support patient selection, estimate absorbed dose, and guide therapeutic decisions throughout development.
Sponsors benefit most from engaging early in radiopharmaceutical development and targeted radiopharmaceutical development programs, particularly during:
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