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Theranostics

Molecular classification
Medical paradigm, Not a molecular target
01

Overview

Theranostics is a precision medicine field that integrates diagnostic imaging and targeted therapy into a single clinical workflow. It is not a specific biological molecule or receptor, but rather a pharmacological approach where a diagnostic agent is used to identify patients who express a specific molecular target, followed by the administration of a therapeutic agent that binds to that same target [1, 2]. This 'see what you treat and treat what you see' methodology allows for highly personalized treatment plans, as the imaging step serves as a real-time biomarker for drug delivery and potential efficacy [3]. In oncology, this paradigm is most famously applied using radiopharmaceuticals, such as the use of Lutetium-177 for treating neuroendocrine tumors (targeting somatostatin receptors) and metastatic castration-resistant prostate cancer (targeting PSMA) [4]. By utilizing the specific binding affinity of a ligand for its receptor, theranostics enables the delivery of high doses of radiation or chemotherapy directly to malignant cells while minimizing exposure to healthy surrounding tissues [5]. This approach represents a shift from conventional 'one-size-fits-all' medicine toward more effective, individualized patient care [6].

Other names
TheragnosticsDiagnostic-therapeutic combinationPrecision medicine approachTargeted radionuclide therapy
02

Mechanism of action

Theranostics is not a single drug mechanism but a clinical strategy that pairs a diagnostic biomarker-targeting agent with a therapeutic agent that hits the same target. Typically, a diagnostic radioisotope is used to visualize the density and location of specific receptors (e.g., PSMA or SSTR) via PET/CT imaging; if the target is present, a therapeutic radioisotope (often a beta-emitter like Lutetium-177) is conjugated to the same or a similar targeting ligand to deliver localized cytotoxic radiation directly to the tumor cells [1, 2].

03

Biological functions

Not a biological function
04

Disease associations

CancerNeuroendocrine tumorProstate cancerThyroid cancer
05

Safety considerations

Radiation-induced nephrotoxicityHematological toxicity (anemia, leukopenia, thrombocytopenia)Off-target uptake (e.g., salivary gland damage in PSMA therapy)XerostomiaRadiation safety and waste management challenges
06

Interacting drugs

Lutetium (177Lu) vipivotide tetraxetan (Pluvicto)

4 more in the full profile.

07

Biomarkers

Prostate-specific membrane antigen (PSMA) expressionSomatostatin receptor (SSTR) expressionFibroblast activation protein (FAP) expressionSodium-iodide symporter (NIS) expression

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