Evaluation of a freeze-dried kit for EDTMP-based bone-seeking radiopharmaceuticals.
A freeze-dried kit developed for formulation of ethylenediamine-tetramethylenephosphonic acid (EDTMP) chelates with "pain-palliation" radiolanthanides (e.g., 153Sm and 177Lu) or "diagnostic" 99mTc has been evaluated, meeting quality and safety criteria required for medicinal use. The EDTMP kit enables an instant one-step preparation of a radiopharmaceutical of high radiochemical purity (>99%) and has a sufficiently long shelf life. Comparative biodistribution studies of 177Lu-EDTMP and 99mTc-EDTMP prepared from the kit revealed similar tissue uptake and clearance to those obtained for pre-formulated 153Sm-EDTMP. The most significant difference was observed for 99mTc-EDTMP, which shows a high retention in kidney, reaching ca. 2% ID after 90min p.i.v.Although preliminary clinical evaluations suggest that 99mTc-EDTMP possesses limited value for bone scintigraphy, application of the radiopharmaceutical for specific diagnostic purposes may still be considered, e.g., investigation of bone metastases or ossification processes in inflammatory spondyloarthropathy.
Garnuszek
Piotr
P
Department of Radiopharmaceuticals, National Institute of Public Health, 30/34 Chelmska St., 00-725, Warsaw, Poland. pg.il.waw.pl
Pawlak
Dariusz
D
Licińska
Iwona
I
Kamińska
Anna
A
D000818:Animals; D004355:Drug Stability; D005063:Europium / Q000737:chemistry; D005069:Evaluation Studies as Topic; D005612:Freeze Drying; D006801:Humans; D007202:Indicators and Reagents; D007553:Isotope Labeling; D008297:Male; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use; D009943:Organophosphorus Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D011868:Radioisotopes / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D051381:Rats; D012493:Samarium / Q000737:chemistry; D013167:Spondylitis, Ankylosing / Q000532:radiotherapy; D013667:Technetium / Q000737:chemistry; D014018:Tissue Distribution
D007202:Indicators and Reagents; D009942:Organometallic Compounds; D009943:Organophosphorus Compounds; D015609:Organotechnetium Compounds; D011868:Radioisotopes; D019275:Radiopharmaceuticals; C119503:lutetium ethylenediaminetetramethylene phosphonic acid; C475628:technetium Tc 99m ethylenediamine-tetramethylenephosphonic acid; D012493:Samarium; D005063:Europium; D013667:Technetium; C061972:samarium Sm-153 lexidronam