¹⁷⁷Lu-Labeled Agents for Neuroendocrine Tumor Therapy and Bone Pain Palliation in Uruguay

Title:¹⁷⁷Lu-Labeled Agents for Neuroendocrine Tumor Therapy and Bone Pain Palliation in Uruguay

Volume: 9 Issue: 1

Author(s): Henia Balter, Trindade Victoria, Terán Mariella, Gaudiano Javier, Ferrando Rodolfo, Paolino Andrea, Rodriguez Graciela, Hermida Juan, De Marco Eugenia and Oliver Patricia

Affiliation:

Keywords: ¹⁷⁷Lu-EDTMP, bone pain palliation, dosimetry, maximum tolerated dose, phase 0/I study, toxicity.

Abstract: Lutetium-177 is an emerging radionuclide due its convenient chemical and nuclear properties. In this paper we describe the development and evaluation in Uruguay of the targeted ¹⁷⁷Lu labelled radiopharmaceuticals EDTMP (for bone pain palliation) and DOTA-TATE (neuroendocrine tumors). We optimized the preparation of these ¹⁷⁷Lu radiopharmaceuticals including radiolabelling, quality control methods, in vitro and in vivo stability and their therapeutic application in patients. Radiation dosimetry aspects of ¹⁷⁷Lu are also included.

Nine male patients with prostate cancer and four female patients with breast carcinoma with multiple bone metastatic lesions were treated with ¹⁷⁷Lu-EDTMP.

Four patients with gastroentheropancreatic neuroendocrine tumors (GEP-NET) and one patient with bronchial NET were treated with 1- 3 cycles with a cumulative dose of 4.44-22.2 GBq of ¹⁷⁷Lu-DOTA-TATE.

Scintigraphic images of the patients treated with ¹⁷⁷Lu-EDTMP evidenced high and rapid uptake in bone metastasis, remaining after 7 days post administration. Images allow skeletal visualization with high definition and demonstrate increased uptake in bone metastases.

For ¹⁷⁷Lu-DOTA-TATE, partial remissions were obtained in 4 patients and the remaining patient did not show significant progression 3 months after the second cycle. No serious adverse effects were registered, even in two patients with confirmed renal disease and high risk for renal disease

Dosimetry assessments confirm the predictive value of the personalized therapy with radiolabelled peptides. We found it is possible to accumulate high therapeutic doses in tumours in sequential administrations of ¹⁷⁷Lu-DOTA-TATE, increasing the probability of biological response without significant impairment ofthe renal function in patients with risk factors.

These results demonstrate the attractive therapeutic properties of these two ¹⁷⁷Lu labelled agents and the feasibility of this metabolic therapy in regions far away from ¹⁷⁷Lu producing countries

Cite this article as:

Balter Henia, Victoria Trindade, Mariella Terán, Javier Gaudiano, Rodolfo Ferrando, Andrea Paolino, Graciela Rodriguez, Juan Hermida, Eugenia Marco De and Patricia Oliver, ¹⁷⁷Lu-Labeled Agents for Neuroendocrine Tumor Therapy and Bone Pain Palliation in Uruguay, Current Radiopharmaceuticals 2016; 9 (1) . https://dx.doi.org/10.2174/1874471008666150313112620