Assessment of the radiation absorbed dose produced by 177Lu-iPSMA, 225Ac-iPSMA and 223RaCl2 to prostate cancer cell nuclei in a bone microenvironment model

Erika Azorín-Vega; Eva Rojas-Calderón; Guillermina Ferro-Flores; Liliana Aranda-Lara; Nallely Jiménez-Mancilla; Miguel A Nava-Cabrera

doi:10.1016/j.apradiso.2019.01.020

Assessment of the radiation absorbed dose produced by ¹⁷⁷Lu-iPSMA, ²²⁵Ac-iPSMA and ²²³RaCl₂ to prostate cancer cell nuclei in a bone microenvironment model

Appl Radiat Isot. 2019 Apr:146:66-71. doi: 10.1016/j.apradiso.2019.01.020. Epub 2019 Jan 29.

Authors

Erika Azorín-Vega¹, Eva Rojas-Calderón², Guillermina Ferro-Flores³, Liliana Aranda-Lara⁴, Nallely Jiménez-Mancilla⁵, Miguel A Nava-Cabrera⁶

Affiliations

¹ Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac, 52750, Estado de México, Mexico. Electronic address: erica.azorin@inin.gob.mx.
² Departamento de Ciencias Ambientales, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac, 52750, Estado de México, Mexico. Electronic address: leticia.rojas@inin.gob.mx.
³ Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac, 52750, Estado de México, Mexico.
⁴ Facultad de Medicina, Universidad Autónoma del Estado de México, Toluca, 50180, Mexico.
⁵ CONACyT, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac, 52750, Estado de México, Mexico.
⁶ Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac, 52750, Estado de México, Mexico; Facultad de Medicina, Universidad Autónoma del Estado de México, Toluca, 50180, Mexico.

PMID: 30753987
DOI: 10.1016/j.apradiso.2019.01.020

Abstract

This research aimed to assess the radiation absorbed dose produced by ¹⁷⁷Lu-iPSMA (¹⁷⁷Lu-prostate specific membrane antigen inhibitor), ²²⁵Ac-iPSMA and ²²³RaCl₂ to prostate cancer cell nuclei in a simplified model of bone by using an experimental in-vitro prostate cancer LNCaP cell biokinetic study and Monte Carlo simulation with the MCNPX code. Results showed that ²²⁵Ac-iPSMA releases a nine hundred-fold radiation dose greater than ¹⁷⁷Lu-iPSMA and 14 times more than ²²³RaCl₂ per unit of activity retained in bone. ²²⁵Ac-iPSMA could be the best option for treatment of bone metastases in prostate cancer.

Keywords: Actinium-225; Lutetium-177; PSMA inhibitors; Prostate cancer; Theranostic radiopharmaceuticals.

MeSH terms

Actinium / pharmacokinetics
Actinium / therapeutic use*
Antigens, Surface
Bone Neoplasms / metabolism
Bone Neoplasms / radiotherapy*
Bone Neoplasms / secondary*
Cell Line, Tumor
Cell Nucleus / metabolism
Cell Nucleus / radiation effects
Computer Simulation
Glutamate Carboxypeptidase II / antagonists & inhibitors
Humans
Lutetium / pharmacokinetics
Lutetium / therapeutic use*
Male
Models, Biological
Monte Carlo Method
Prostatic Neoplasms / metabolism
Prostatic Neoplasms / radiotherapy*
Prostatic Neoplasms / secondary*
Radioisotopes / pharmacokinetics
Radioisotopes / therapeutic use*
Radiopharmaceuticals / pharmacokinetics
Radiopharmaceuticals / therapeutic use
Radiotherapy Dosage
Radium / pharmacokinetics
Radium / therapeutic use*
Tumor Microenvironment / radiation effects

Substances

Actinium-225
Antigens, Surface
Radioisotopes
Radiopharmaceuticals
Lutetium
Radium-223
Lutetium-177
FOLH1 protein, human
Glutamate Carboxypeptidase II
Actinium
Radium