Vol. 4, 2019

Original research papers

Radiation in Medicine

TWO LABELED EDTMP RADIOPHARMACEUTICALS WITH Sm-153 AND Lu-177 FOR HUMAN BONE RADIOTHERAPY

Hesham MH Zakaly, Mostafa Y. A. Mostafa, M Zhukovsky

Pages: 36–40

DOI: 10.37392/RapProc.2019.08

177Lu and 153Sm are perspective radionuclides used in nuclear medicine. High-energy beta particles and the relative half-life of the radionuclides are used to achieve an effective palliative treatment of bone metastases. In this paper, the effect of the drug carrier EDTMP (i.e. ethylene diamine tetramethylene phosphonate) on the ionic form of 177Lu and 153Sm is presented. The absorbed doses of 177Lu and 153Sm in ionic form labeled with EDTMP in different organs and tissues are determined by IDAC-Dose 2.1 (Internal Dose Assessment by Computer) software and WinAct software which is used to calculate cumulative activity. 177Lu and 153Sm are lanthanide radionuclides which actively accumulate in the liver and bones when used in ionic form. In the case of labeling with EDTMP, the distribution and elimination of the drug occur according to the kinetics of the carrier, EDTMP. The use of an osteotropic complex (drugs attracted to and targeting bones) allows creating a large dose in the pathological areas and minimizes the damage of healthy organs and tissues. 177Lu and 153Sm labeled with EDTMP decrease the liver dose absorption and increase the bone surface absorption for a more effective treatment and minimizing side effects. The effective dose per administered activity is 0.189 mGy/MBq for 177Lu-ionic form, 0.232 mGy/MBq for 153Sm-ionic form and 0.242 mGy/MBq for 177Lu-EDTMP and 0.139 mGy/MBq for 153sm-EDTMP.

  1. S. Chakraborty et al., "177Lu-EDTMP: a viable bone pain palliative in skeletal metastasis," Cancer Biother. Radiopharm., vol. 23, no. 2, pp. 202 – 213, Apr. 2008.
    DOI: 10.1089/cbr.2007.374
    PMid: 18454689
  2. P. Anderson, R. Nuñez, "Samarium lexidronam (153Sm-EDTMP): skeletal radiation for osteoblastic bone metastases and osteosarcoma," Expert Rev. Anticancer Ther., vol. 7, no. 11, pp. 1517 – 1527, Nov. 2007.
    DOI: 10.1586/14737140.7.11.1517
    PMid: 18020921
  3. A. Ahonen et al., "Samarium-153-EDTMP in bone metastases," J. Nucl. Biol. Med., vol. 38, suppl. 1, pp. 123 – 127, Dec. 1994.
    PMid: 7543288
  4. I. G. Finlay, M. D. Mason, M. Shelley, "Radioisotopes for the palliation of metastatic bone cancer: a systematic review," Lancet Oncol., vol. 6, no. 6, pp. 392 – 400, Jun. 2005.
    DOI: 10.1016/S1470-2045(05)70206-0
    PMid: 15925817
  5. S. E. Abram, "Radiopharmaceutical Therapy for Palliation of Bone Pain From Osseous Metastases," in The Year book of anesthesiology and pain management, D. H. Chestnut, Eds., 1st ed., Maryland Heights (MO), USA: Mosby, 2006, pp. 256 – 257.
    DOI: 10.1016/s1073-5437(08)70502-3
  6. T. Das, H. D. Sarma, A. Shinto, K. K. Kamaleshwaran, S. Banerjee, "Formulation, preclinical evaluation, and preliminary clinical investigation of an in-house freeze-dried EDTMP kit suitable for the preparation of 177Lu-EDTMP," Cancer Biother. Radiopharm., vol. 29, no. 10, pp. 412 – 421, Dec. 2004.
    DOI: 10.1089/cbr.2014.1664
    PMid: 25409337
  7. K. F. Eckerman, R. W. Leggett, WinAct version 1.0, ORNL, Oak Ridge (TN), USA, 2002.
    Retrieved from: https://www.ornl.gov/crpk/software
    Retrieved on: Mar. 22, 2019
  8. H. M. H. Zakaly, M. Y. A. Mostafa, M. Zhukovsky, "Dosimetry Assessment of Injected 89Zr-Labeled Monoclonal Antibodies in Humans," Radiat. Res., vol. 191, no. 5, pp. 466 - 474, May 2019.
    DOI: 10.1667/RR15321.1
    PMid: 30896281
  9. M. Y. A. Mostafa, H. M. H. Zakaly, M. Zhukovsky, "Assessment of exposure after injection of 99mTc-labeled intact monoclonal antibodies and their fragments into humans," Radiol. Phys. Technol., vol. 12, no. 1, pp. 96 – 104, Mar. 2019.
    DOI: 10.1007/s12194-018-00496-1
    PMid: 30604358
  10. S. Chakraborty, T. Das, H. D. Sarma, M. Venkatesh, S. Banerjee, "Comparative studies of 177Lu-EDTMP and 177Lu-DOTMP as potential agents for palliative radiotherapy of bone metastasis," Appl. Radiat. Isot., vol. 66, no. 9, pp. 1196 – 1205, Sep. 2008.
    DOI: 10.1016/j.apradiso.2008.02.061
    PMid: 18372188
  11. L. Vigna et al., "Characterization of the [(153)Sm]Sm-EDTMP pharmacokinetics and estimation of radiation absorbed dose on an individual basis," Phys. Med., vol. 27, no. 3, pp. 144 – 152, Jul. 2011.
    DOI: 10.1016/j.ejmp.2010.08.001
    PMid: 20864370
  12. D. M. Taylor, R. W. Leggett, "A generic biokinetic model for predicting the behaviour of the lanthanide elements in the human body," Radiat. Prot. Dosim., vol. 105, no. 1 - 4, pp. 193 – 198, 2003.
    DOI: 10.1093/oxfordjournals.rpd.a006222
    PMid: 14526955
  13. M. Andersson, L. Johansson, K. Eckerman, S. Mattsson, "IDAC-Dose 2.1, an internal dosimetry program for diagnostic nuclear medicine based on the ICRP adult reference voxel phantoms," EJNMMI Res., vol. 7, no. 88, Nov. 2017.
    DOI: 10.1186/s13550-017-0339-3
    PMid: 29098485
    PMCid: PMC5668221
  14. H. M. H. Zakaly, M. Y. A. Mostafa, M. Zhukovsky, "Radiopharmaceutical dose distribution in different organs and tissues for Lu-177 with different carrier," AIP Conf. Proc., vol. 2174, no. 1, 2019.
    DOI: 10.1063/1.5134421
  15. Education and Training in Radiological Protection for Diagnostic and Interventional Procedures, vol. 39, ICRP Publication no. 113, ICRP, Ottawa, Canada, 2009.
    Retrieved from: https://journals.sagepub.com/doi/pdf/10.1177/ANIB_39_5
    Retrieved on: May 8, 2019