Human Dose Assessment of Ga-NODAGA-RGD-BBN Heterodimer Peptide Based on Animal Data

Overview

Journal J Med Phys

Date 2023 Jan 23

PMID 36684706

Authors

Naeimeh Amraee

Behrouz Alirezapour

Mohammad Hosntalab

Hassan Yousefnia

Affiliations

Soon will be listed here.

Abstract

Aims: Calculation of the absorbed dose in human organs is one of the first steps for developing new radiopharmaceuticals. The aim of this study is to estimate the human absorbed dose of a newly developed Ga-NODAGA-RGD-BBN radiolabeled compound.

Materials And Methods: Ga-NODAGA-RGD-BBN was prepared by varying different parameters at optimized conditions. The stability of the radiolabeled peptide in phosphate-buffered saline (PBS) and in human serum was evaluated for 120 min. Afterward, the biodistribution of the complex was assessed in normal and tumor-bearing mice, at least for 120 min postinjection. Finally, the human absorbed dose of Ga-NODAGA-RGD-BBN was estimated based on mice data using Radiation Dose Assessment Resource and Spark method.

Results: Ga-NODAGA-RGD-BBN was produced with radiochemical purity of more than 98% (high-performance liquid chromatography/ radio thin layer chromatography (RTLC)) with high stability in PBS buffer and in human serum at least for 2 h. The complex demonstrated high uptake in gastrin-releasing peptide receptor-expressing tumors compared to other nontarget organs. Furthermore, the dose assessment for the complex showed that the kidneys receive the highest absorbed dose in comparison with other organs.

Conclusion: The result of this study showed that 68Ga-NODAGA-RGD-BBN is an effective and radiolabeled ligand for tumor detection, however more studies are still needed.

References

Shanehsazzadeh S, Yousefnia H, Jalilian A, Zolghadri S, Lahooti A . Estimated human absorbed dose for (68)Ga-ECC based on mice data: comparison with (67)Ga-ECC. Ann Nucl Med. 2015; 29(6):475-81. DOI: 10.1007/s12149-015-0967-5. View

. Radiological Protection in Biomedical Research. A report of Committee 3 adopted by the International Commission on Radiological Protection. Ann ICRP. 1991; 22(3):1-28, v-xxiv. View

Li Q, Zhang C, Tan W, Gu G, Guo Z . Novel Amino-Pyridine Functionalized Chitosan Quaternary Ammonium Derivatives: Design, Synthesis, and Antioxidant Activity. Molecules. 2017; 22(1). PMC: 6155944. DOI: 10.3390/molecules22010156. View

Yousefnia H, Zolghadri S, Jalilian A, Tajik M, Ghannadi-Maragheh M . Preliminary dosimetric evaluation of (166)Ho-TTHMP for human based on biodistribution data in rats. Appl Radiat Isot. 2014; 94:260-265. DOI: 10.1016/j.apradiso.2014.08.017. View

Ferlay J, Shin H, Bray F, Forman D, Mathers C, Parkin D . Estimates of worldwide burden of cancer in 2008: GLOBOCAN 2008. Int J Cancer. 2011; 127(12):2893-917. DOI: 10.1002/ijc.25516. View

Stabin M, Sparks R, Crowe E . OLINDA/EXM: the second-generation personal computer software for internal dose assessment in nuclear medicine. J Nucl Med. 2005; 46(6):1023-7. View

Stabin M, Siegel J . Physical models and dose factors for use in internal dose assessment. Health Phys. 2003; 85(3):294-310. DOI: 10.1097/00004032-200309000-00006. View

Moody T, Lee L, Ramos-Alvarez I, Iordanskaia T, Mantey S, Jensen R . Bombesin Receptor Family Activation and CNS/Neural Tumors: Review of Evidence Supporting Possible Role for Novel Targeted Therapy. Front Endocrinol (Lausanne). 2021; 12:728088. PMC: 8441013. DOI: 10.3389/fendo.2021.728088. View

Nagalla S, Barry B, Falick A, Gibson B, Taylor J, Dong J . There are three distinct forms of bombesin. Identification of [Leu13]bombesin, [Phe13]bombesin, and [Ser3,Arg10,Phe13]bombesin in the frog Bombina orientalis. J Biol Chem. 1996; 271(13):7731-7. DOI: 10.1074/jbc.271.13.7731. View

10.

Mirzaei A, Jalilian A, Aghanejad A, Mazidi M, Yousefnia H, Shabani G . Preparation and Evaluation of (68)Ga-ECC as a PET Renal Imaging Agent. Nucl Med Mol Imaging. 2015; 49(3):208-16. PMC: 4532689. DOI: 10.1007/s13139-015-0323-7. View

11.

Brenner D . Effective dose: a flawed concept that could and should be replaced. Br J Radiol. 2008; 81(967):521-3. DOI: 10.1259/bjr/22942198. View

12.

Yousefnia H, Zolghadri S, Shanehsazzadeh S . Estimated human absorbed dose of ¹⁷⁷Lu-BPAMD based on mice data: Comparison with ¹⁷⁷Lu-EDTMP. Appl Radiat Isot. 2015; 104:128-35. DOI: 10.1016/j.apradiso.2015.06.033. View

13.

Aghanejad A, Jalilian A, Ardaneh K, Bolourinovin F, Yousefnia H, Samani A . Preparation and Quality Control of (68)Ga-Citrate for PET Applications. Asia Ocean J Nucl Med Biol. 2016; 3(2):99-106. PMC: 4937647. View

14.

Hanahan D, Weinberg R . Hallmarks of cancer: the next generation. Cell. 2011; 144(5):646-74. DOI: 10.1016/j.cell.2011.02.013. View

15.

Shanehsazzadeh S, Lahooti A, Yousefnia H, Geramifar P, Jalilian A . Comparison of estimated human dose of (68)Ga-MAA with (99m)Tc-MAA based on rat data. Ann Nucl Med. 2015; 29(8):745-53. DOI: 10.1007/s12149-015-0997-z. View

16.

Fournier P, Dumulon-Perreault V, Ait-Mohand S, Langlois R, Benard F, Lecomte R . Comparative study of 64Cu/NOTA-[D-Tyr6,βAla11,Thi13,Nle14]BBN(6-14) monomer and dimers for prostate cancer PET imaging. EJNMMI Res. 2012; 2:8. PMC: 3323469. DOI: 10.1186/2191-219X-2-8. View

17.

Fischer R, Hill R, Warshay D . Effects of psychodysleptic drug psilocybin on visual perception. Changes in brightness preference. Experientia. 1969; 25(2):166-9. DOI: 10.1007/BF01899102. View

18.

Smith C, Volkert W, Hoffman T . Gastrin releasing peptide (GRP) receptor targeted radiopharmaceuticals: a concise update. Nucl Med Biol. 2003; 30(8):861-8. DOI: 10.1016/s0969-8051(03)00116-1. View

19.

Naderi M, Zolghadri S, Yousefnia H, Ramazani A, Jalilian A . Preclinical Study of Ga-DOTATOC: Biodistribution Assessment in Syrian Rats and Evaluation of Absorbed Dose in Human Organs. Asia Ocean J Nucl Med Biol. 2016; 4(1):19-29. PMC: 4937676. DOI: 10.7508/aojnmb.2016.04.004. View

20.

Tonini T, Rossi F, Claudio P . Molecular basis of angiogenesis and cancer. Oncogene. 2003; 22(42):6549-56. DOI: 10.1038/sj.onc.1206816. View