Jay A. Spicer

Treatment of metastatic bone pain with strontium-89

We have utilized 89Sr as palliative treatment for bone pain secondary to metastatic cancer in the skeleton of over 200 patients. The best results have been in patients with carcinoma of the prostate (80% response rate) and breast (89%). Results in a small number of patients with a variety of other cell types were not nearly as encouraging. Strontium-89 provides excellent palliation in the management of bone pain secondary to prostate and breast carcinoma.

Radionuclide Therapy of Intractable Bone Pain: Emphasis on Strontium-89

Management of bone pain in patients with multiple osseous metastases is a significant clinical problem. Phosphorus-32 has been used as systemic radioisotope therapy for the management of bone pain for over 40 years. However, significant hematological depression usually results and its use is limited. More recently, the bone-seeking radiopharmaceuticals strontium-89, samarium-153-ethylenediaminetetramethylene phosphonic acid, and rhenium-186-hydroxyethylidene diphosphonate have all been used as palliative treatment for patients with clinically significant bone pain. Excellent clinical responses with acceptable hematological toxicity have been observed. The clinical results rival those of external beam radiation therapy, with fewer systemic and hematological side effects. Systemic radionuclide therapy is indicated in the management of patients with painful metastatic prostate cancer in bone as soon as they escape primary hormonal management. This therapy also should play a role in the management of many patients with advanced breast cancer metastatic to bone. The role of radionuclidic therapy in osseous metastases from other malignancies is still being investigated. These compounds also hold promise as primary therapy for tumors of osseous origin. Systemic radionuclide therapy of painful bony metastases will become common in nuclear medicine practice in the next decade.

A case for 77-bromine labelled radiopharmaceuticals.

Abstract The use of radiobromine as a label for radiopharmaceuticals was demonstrated by the synthesis of 82 Br-2,4-dibromoesterone, using the procedure of Slaunwhite and Neely . Structure determination of the brominated steroid was accomplished by the use of melting point data, paper chromatoraphy and mass spectra analysis. Tissue distribution studies in animals demonstrated rapid blood clearance and excretion in the bile. Calculated radiation exposure dose for 77 Br-2,4-dibromoestrone is less than 131 I-Rose Bengal. A significant difference in tissue distribution was found when the data for 82 Br-2,4-dibromoesterone was compared to literature values for 82 Br-7,8-dibromoesterone. Comparison with 131 I-Rose Bengal and 99 m Tc-pyrodoxylideneglutamate suggest 77 Br-2,4-dibromoestrone would be a tracer of potential value for liver and gallbladder function studies.

Prolonged clearance of intraperitoneal 16α-[125I]iodo-17β-estradiol in presence of ascites

Abstract Radioestrogens have potential as adjunct therapeutic agents against ovarian carcinomas, because selected radionuclides can deposit lethal doses of radiation to tumor cells and many ovarian carcinomas and their metastases express estrogen receptors. Because intraperitoneal administration is a possible approach, we investigated absorption from the peritoneal cavity of a radioiodoestradiol after intraperitoneal application in rats with and without ovarian tumors and ascites and compared the distribution of the radioactivity with that obtained after intravenous injection. In the absence of ascites, 70% of the intraperitoneal dose was cleared into the intestine within 2 hours after injection, indicating fast absorption from the peritoneal cavity. In the presence of ascites, clearance of intraperitoneal radioiodoestradiol was considerably slower; at 2 hours after injection, 50% of the injected dose remained in the ascites, mostly as radioiodoestradiol. Uptake of radioactivity in estrogen receptor-rich tissues, e.g., uterus, after intraperitoneal injection was high (about 20: 1 over blood), regardless of the presence of ascites, but moderately lower than that observed after intravenous injection of radioiodoestradiol. (AM J OBSTET GYNECOL 1991;165:1847-53.)

A Kit for the Preparation of Basic 99mTc Penicillamine for Renal Scanning

Abstract A kit for preparing basic (pH 8.4) 99mTc-penicillamine complex for renal studies is described. The radiopharmaceutical prepared from the kit localizes in the kidneys, primarily in the renal cortex. Data is presented which demonstrates that the kit method for 99mTc-penicillamine results in biological distribution of the 99mTc-penicillamine complex equivalent to that observed for the older extemporaneous method of preparation. The per cent of injected dose localized in the kidneys of rabbits at one hour is 18.3 ± 3.1%, which compares favorably with other 99mTc-complexes used for renal imaging.

A rapid one-step kit for the routine preparation of basic 99mTc penicillamine

Abstract Basic (pH 8.4) 99 m Tc penicillamine (TPEN) is an excellent agent forimaging renal functional morphology. The radiopharmaceutical development of this renal-scanning agent has progressed from daily, “on-demand”, preparation through a two-step kit with short shelf life to the presently reported rapid, one-step, freeze-dried kit, without loss of clinical effectiveness. Renal uptake is comparable to the earlier preparations, and the freeze-dried kit has a shelf life in excess of 2 months.

Iodinated estradiols, intermediate products and methods of production

A method of preparation of estradiol derivatives labeled by iodine, especially 123 I, substitution at C-16 are synthesized according to the present invention. A triflate intermediate is prepared from which either 16-alpha-123 I-17-beta-estradiol or 16-beta-123 I-17-beta-estradiol are prepared by described methods. Both 16-alpha-123 I- and 16-beta-123 I-17-beta-estradiol made according to the methods described herein have a high relative specific acitvity. The methods are sufficiently rapid so that the relatively short half-life of 123 I is readily accommodated without substantial radioactive decay of the label.