Production, quality control, biodistribution assessment and preliminary dose evaluation of [177Lu]-tetra phenyl porphyrin complex as a possible therapeutic agent

Abstract

<p>Due to interesting therapeutic properties of <sup>177</sup>Lu and tumor avidity of tetraphenyl porphyrins (TPPs), <sup>177</sup>Lu-tetraphenyl porphyrin was developed as a possible therapeutic compound. <sup>177</sup>Lu of 2.6-3 GBq/mg specific activity was obtained by irradiation of natural Lu<sub>2</sub>O<sub>3</sub>sample with thermal neutron flux of 4 × 10<sup>13</sup> n.cm<sup>-2</sup>.s<sup>-1</sup>. Tetraphenyl porphyrin was synthetized and labeled with <sup>177</sup>Lu. Radiochemical purity of the complex was studied using Instant thin layer chromatography (ITLC) method. Stability of the complex was checked in final formulation and human serum for 48 h. The biodistribution of the labeled compound in vital organs of wild-type rats was studied up to 7 d. The absorbed dose of each human organ was calculated by medical internal radiation dose (MIRD) method. A detailed comparative pharmacokinetic study was performed for <sup>177</sup>Lu cation and [<sup>177</sup>Lu]-TPP. The complex was prepared with a radiochemical purity: >97±1% and specific activity: 970-1000 MBq/mmol. Biodistribution data and dosimetric results showed that all tissues receive approximately an insignificant absorbed dose due to rapid excretion of the complex through the urinary tract. [<sup>177</sup>Lu]-TPP can be an interesting tumor targeting agent due to low liver uptake and very low absorbed dose of approximately 0.036 to the total body of human.</p>

Radioimmunotheranostic Pair Based on the Anti-HER2 Monoclonal Antibody: Influence of Chelating Agents and Radionuclides on Biological Properties

“…In the case of [ 177 Lu]Lu-DOTA-trastuzumab, the longer circulation time may represent higher irradiation of non-target organs, especially those that are more vascularized. However, the data presented in this work for both RICs are in accordance with previously published data [ 54 , 55 ].…”

Montmorillonite Surface as a Catalyst for the Formation of Sat Metal Tetra (P-Sulphophenyl) Porphyrins

“…They have been used as photo-catalysts as in the photooxygenation of alkenes [4], thermal catalysts [5,6], electro-catalysts [7]. 177 Lu tetraphenyl porphyrin has been considered as a therapeutic agent [8]. An in vitro photodynamic therapy has been carried out on G361 cell lines by utilizing zinc-tetra(psulfophenyl)porphyrin (ZnTPPS) bound to cyclodextrin that induced single strand breaks of cellular DNA in the G361 melanoma cells [9].…”