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Investigations on the Ga(III) Complex of EOB-DTPA and Its 68Ga Radiolabeled Analogue
Published on: August 17, 2016
Radiolabeling and physicochemical characterization of terbium-161 DOTATATE
Karan S Tanwar1,2, Viraj V Sawant1,2, Dinesh Rawat1,2
1Department of Nuclear Medicine, Advanced Centre for Treatment Research and Education in Cancer (ACTREC), Tata Memorial Centre (TMC).
Nuclear Medicine Communications
|July 7, 2026
Summary
This study standardized the in-house radiolabeling of Lutetium-177 (177Lu) labeled DOTATATE, achieving high radiochemical purity and stability for potential targeted radionuclide therapy applications.
Area of Science:
- Nuclear medicine
- Radiopharmaceutical chemistry
- Oncology
Background:
- Somatostatin receptor-targeted radionuclide therapy is a promising cancer treatment.
- [161Tb]Tb-DOTATATE offers therapeutic potential but requires standardized production.
- Efficient and reproducible radiolabeling is crucial for clinical translation.
Purpose of the Study:
- To develop and standardize an in-house radiolabeling protocol for [161Tb]Tb-DOTATATE.
- To characterize the physicochemical properties of the radiolabeled compound.
- To assess the feasibility of clinical application of [161Tb]Tb-DOTATATE.
Main Methods:
- Radiolabeling of DOTATATE with [161Tb]Tb was performed in sodium acetate buffer with ascorbic acid at 100°C for 1 hour.
- Radiochemical yield and purity (RCP) were assessed using radio-thin-layer chromatography (TLC) and radio-high-performance liquid chromatography (HPLC).
- Radionuclide identity, hydrophilicity (log Po/w), plasma protein binding (PPB), and in-vitro stability in saline and human serum were evaluated.
Main Results:
- A radiolabeling yield exceeding 99% was achieved with 1-hour incubation, compared to 40% at 30 minutes.
- Radiochemical purity (RCP) was consistently >99% as determined by radio-TLC (ITLC method).
- The [161Tb]Tb-DOTATATE product demonstrated good hydrophilicity, acceptable plasma protein binding, and stability in vitro for up to 7 days.
Conclusions:
- A robust and reproducible in-house radiolabeling protocol for [161Tb]Tb-DOTATATE was successfully established.
- The radiolabeled compound exhibits excellent physicochemical properties suitable for clinical use.
- This standardization facilitates further preclinical and clinical investigations of [161Tb]Tb-DOTATATE in targeted radionuclide therapy.
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