skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: Rhodium-105 Bombesin Analogs for Prostate Cancer Radiotherapy

Abstract

Over the period of this grant (11/01/2001 to 12/31/2005), the consistent and reproducible production of Rh-105, synthesis and evaluation of three new chelate systems based on hydroxymethyl phosphines, development of a new non-hydroxymethyl phosphine N{sub 2}P{sub 2} chelate system, conjugation of two of the chelates to the bombesin peptide analog BBN[7-14]NH{sub 2}, evaluation of the bombesin conjugates and their Rh-105 complexes for stability, cell binding affinity, and in vivo biodistribution in normal mice has been developed. The BBN analogs bind to GRP receptors that are overexpressed on PC-3 prostate tumor cells. A dedicated glove box is used for the separation and isolation of {sup 105}Rh from the target ({sup 104}Ru). All tubing/connections/valves from the point of the Cl{sub 2} tank are made of Teflon to minimize/eliminate the introduction of any metal into the process (e.g., iron from stainless steel corrosion). The separation of {sup 105}Rh produced from the enriched {sup 104}Ru target involves oxidation of the enriched {sup 104}Ru metal target to ruthenium tetroxide with chlorine gas and sodium hydroxide solution to generate hypochlorite in situ. The RuO4 is removed by distillation and the {sup 105}Rh remaining in the reaction vial is converted into {sup 105}Rh-chloride by acidification with hydrochloricmore » acid and heating. The {sup 105}Rh production process has become reproducible over the past year to consistently make 10-30 mCi of {sup 105}Rh from 1-3 mg of an enriched (99.21%) {sup 104}Ru target. The process itself involves irradiation of the enriched {sup 104}Ru target in the core of the reactor (University of Missouri Research Reactor (MURR)) for one week to yield 16-40 mCi of {sup 105}Rh. The irradiated target is processed to separate the Rh-105 in high specific activity from the {sup 104}Ru target. The irradiated target is dissolved in NaOH (2M, 3 mL) by bubbling Cl{sub 2} gas through the solution (generating NaOCl in situ) to generate RuO{sub 4} and Rh(III). The RuO{sub 4} is distilled from the solution into an HCl trap to allow for recovery of the enriched Ru as RuO{sub 2}. The {sup 105}Rh remains in the reaction vessel, and on acidification with 0.1 M HCl, {sup 105}Rh-chloride is available for use. A schematic of the purification and Ru-104 recovery process is shown.« less

Authors:
Publication Date:
Research Org.:
The University of Missouri
Sponsoring Org.:
USDOE
OSTI Identifier:
951630
Report Number(s):
DOE-ER63192- FINAL REPORT
MU Projects: CG004257/CG004258/CG004259/ CG004260; TRN: US201001%%573
DOE Contract Number:  
FG02-01ER63192
Resource Type:
Technical Report
Country of Publication:
United States
Language:
English
Subject:
36 MATERIALS SCIENCE; ACIDIFICATION; HYDROCHLORIC ACID; IN VIVO; NEOPLASMS; OXIDATION; PROSTATE; PEPTIDES; PHOSPHINES; PURIFICATION; RADIOTHERAPY; RESEARCH REACTORS; RHODIUM 105; RUTHENIUM; SODIUM HYDROXIDES; STAINLESS STEELS; TUMOR CELLS

Citation Formats

Silvia S. Jurisson, PhD. Rhodium-105 Bombesin Analogs for Prostate Cancer Radiotherapy. United States: N. p., 2005. Web. doi:10.2172/951630.
Silvia S. Jurisson, PhD. Rhodium-105 Bombesin Analogs for Prostate Cancer Radiotherapy. United States. doi:10.2172/951630.
Silvia S. Jurisson, PhD. Sat . "Rhodium-105 Bombesin Analogs for Prostate Cancer Radiotherapy". United States. doi:10.2172/951630. https://www.osti.gov/servlets/purl/951630.
@article{osti_951630,
title = {Rhodium-105 Bombesin Analogs for Prostate Cancer Radiotherapy},
author = {Silvia S. Jurisson, PhD},
abstractNote = {Over the period of this grant (11/01/2001 to 12/31/2005), the consistent and reproducible production of Rh-105, synthesis and evaluation of three new chelate systems based on hydroxymethyl phosphines, development of a new non-hydroxymethyl phosphine N{sub 2}P{sub 2} chelate system, conjugation of two of the chelates to the bombesin peptide analog BBN[7-14]NH{sub 2}, evaluation of the bombesin conjugates and their Rh-105 complexes for stability, cell binding affinity, and in vivo biodistribution in normal mice has been developed. The BBN analogs bind to GRP receptors that are overexpressed on PC-3 prostate tumor cells. A dedicated glove box is used for the separation and isolation of {sup 105}Rh from the target ({sup 104}Ru). All tubing/connections/valves from the point of the Cl{sub 2} tank are made of Teflon to minimize/eliminate the introduction of any metal into the process (e.g., iron from stainless steel corrosion). The separation of {sup 105}Rh produced from the enriched {sup 104}Ru target involves oxidation of the enriched {sup 104}Ru metal target to ruthenium tetroxide with chlorine gas and sodium hydroxide solution to generate hypochlorite in situ. The RuO4 is removed by distillation and the {sup 105}Rh remaining in the reaction vial is converted into {sup 105}Rh-chloride by acidification with hydrochloric acid and heating. The {sup 105}Rh production process has become reproducible over the past year to consistently make 10-30 mCi of {sup 105}Rh from 1-3 mg of an enriched (99.21%) {sup 104}Ru target. The process itself involves irradiation of the enriched {sup 104}Ru target in the core of the reactor (University of Missouri Research Reactor (MURR)) for one week to yield 16-40 mCi of {sup 105}Rh. The irradiated target is processed to separate the Rh-105 in high specific activity from the {sup 104}Ru target. The irradiated target is dissolved in NaOH (2M, 3 mL) by bubbling Cl{sub 2} gas through the solution (generating NaOCl in situ) to generate RuO{sub 4} and Rh(III). The RuO{sub 4} is distilled from the solution into an HCl trap to allow for recovery of the enriched Ru as RuO{sub 2}. The {sup 105}Rh remains in the reaction vessel, and on acidification with 0.1 M HCl, {sup 105}Rh-chloride is available for use. A schematic of the purification and Ru-104 recovery process is shown.},
doi = {10.2172/951630},
journal = {},
number = ,
volume = ,
place = {United States},
year = {Sat Dec 31 00:00:00 EST 2005},
month = {Sat Dec 31 00:00:00 EST 2005}
}

Technical Report:

Save / Share: