Target intelligence / Profile preview

Rhenium-188 radiometal chelation complex (188Re complex)

Target
188Re complex
Molecular classification
Radiopharmaceutical, Beta-emitting radionuclide, Coordination complex, Theranostic agent
01

Overview

Rhenium-188 (188Re) is a high-energy beta-emitting radioisotope with a physical half-life of 16.9 hours, widely utilized in targeted radionuclide therapy. It is typically administered as a radiometal chelation complex, where the rhenium ion is stabilized by a ligand or conjugated to a targeting vector such as a monoclonal antibody, peptide, or small molecule. The complex functions by delivering localized ionizing radiation to specific biological sites, such as bone metastases or solid tumors, where the beta particles (maximum energy 2.12 MeV) induce lethal double-strand DNA breaks and oxidative stress. Beyond its therapeutic properties, 188Re also emits a 155 keV gamma photon, which enables real-time scintigraphic imaging and precise dosimetry, supporting a theranostic clinical workflow. Common applications include the treatment of hepatocellular carcinoma, palliative care for bone pain, and the management of non-melanoma skin cancers.

Other names
188Re-labeled complexRhenium-188 chelate188Re-radiopharmaceuticalRhenium-188 coordination complex188Re-labeled compound
02

Mechanism of action

The complex delivers high-energy beta particles (maximum energy 2.12 MeV) to targeted tissues, where the radiation induces double-strand DNA breaks and oxidative stress, leading to cell death and tumor reduction.

03

Biological functions

Ionizing radiation deliveryInduction of DNA damageBeta particle emissionGamma photon emissionCellular apoptosis induction
04

Disease associations

Bone metastasisHepatocellular carcinomaNon-melanoma skin cancerRheumatoid arthritisNeuroendocrine tumorB-cell lymphoma
05

Safety considerations

Myelosuppression (bone marrow toxicity)Radiation exposure to non-target organsNephrotoxicity (renal clearance issues)Handling and disposal of radioactive wastePotential for off-target radiation damage
06

Interacting drugs

Etidronic acid (HEDP)

5 more in the full profile.

07

Biomarkers

Bone turnover markers (e.g., alkaline phosphatase)Target receptor expression (e.g., CD20, PSMA, SSTR)Gamma scintigraphy for dosimetryTumor volume reduction via RECIST criteria

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