Preliminary studies on 177Lu-labeled sodium pyrophosphate (177Lu-PYP) as a potential boneseeking radiopharmaceutical for bone pain palliation

3^rd World Congress on Cancer Science & Therapy

October 21-23, 2013 DoubleTree by Hilton Hotel San Francisco Airport, CA, USA

I. A. Abbasi

Accepted Abstracts: J Cancer Sci Ther

Abstract :

Objective:99mTc-Sn-PYP (technetium- 99m labeled tin pyrophosphate) has been widely used as a radiopharmaceutical for bone scanning as well as in nuclear cardiology .It is also found in the body in trace amounts. 177 Lu is presently considered as an excellent radionuclide for developing bone pain palliation agents. PYP is an analogue of MDP and MDP has been labeled with 177 Lu. No study on preparing a complex of 177 Lu with PYP has been reported yet. Based on these facts, it was hypothesized that a bone-seeking 177 Lu -PYP (lutetium-177 labeled pyrophosphate) radiopharmaceutical could be developed as an agent for palliative radiotherapy of bone pain due to skeletal metastases. Methods: 177 Lu was produced by irradiating lutetium foil (11 mg) natural target at a flux ~1.0×10 14 n/cm 2 /s for 12 h in the swimming pool type reactor. 177 Luin the form of 177 LuCl 3 was labeled with PYP. The radiochemical purity and labeling efficiencies were determined by paper chromatography. Labeling of 177 Lu with PYP was optimized and a labeled sample was subjected to HPLC analysis. To determine the charge on the 177 Lu-PYP complex, radio-electrophoresis was conducted for 1 hour under a voltage of 300 V and 45 mA current using 0.025 M phosphate buffer (pH 6.9). Bio evaluation studies with rabbit under γ-camera were also performed to verify the skeletal uptake. Results: The quality control using paper radio-chromatography has shown >99% radiochemical purity of 177 Lu-PYP complex. Radio-chromatography also showed maximum labeling at ligand/metal ratio=60:1. HPLC analysis showed 1.42±0.01 min retention time of 177 Lu-PYP complex. No decrease in labeling was observed at higher temperatures. Gamma-camera images of 177 Lu-PYP in normal rabbit at 24 h post injection also showed high skeletal uptake. Conclusion: The study demonstrated that sodium pyrophosphate could be labeled with 177 Lu with high radiochemical yields (>99%). Negatively charged 177 Lu-PYP complex retain stability for a day and at high temperatures too. Gamma-camera images of 177 Lu-PYP in normal rabbit at 24h post injection showed high skeletal uptake, suggesting that it may be useful as a bone- pain palliation agent for the treatment of bone metastases. Keywords: 177 Lu-labeled PYP, skeletal metastases, bone pain palliation, gamma-camera imaging.