USA flag logo/image

An Official Website of the United States Government

SYNTHESIS OF IMAGABLE IODINATED ESTRADIOL - PHASE I

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
509
Program Year/Program:
1984 / SBIR
Agency Tracking Number:
509
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
Biomedical Research Laboratori
7899 Mastin Overland Park, KS 66204
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 2
Fiscal Year: 1984
Title: SYNTHESIS OF IMAGABLE IODINATED ESTRADIOL - PHASE I
Agency: HHS
Contract: N/A
Award Amount: $269,150.00
 

Abstract:

THE HIGH INCIDENCE OF BREAST CANCER IN WOMEN MAKES THIS DISEASE THE LEADING CANCER TYPE IN THIS POPULATION. THE PROPER STAGING OF THIS CANCER AND THE DETERMINATION OF THE PRESENCE OR ABSENCE OF ESTROGEN RECEPTORS PLAY MAJOR ROLES IN DETERMINING THE COURSE OF TREATMENT. PRESENTLY AVAILABLEMETHODS FOR SUCH STAGING AND ESTROGEN RECEPTOR IDENTIFICATION REQUIRE INVASIVE TECHNIQUES (SUCH AS SURGICALBIOPSY) AND "IN VITRO" ASSAYS. EXTERNAL IMAGING OF THESE TUMORS AND THEIR METASTASES BY USE OF A HIGHLY SPECIFIC ESTROGEN RECEPTOR - BINDING AGENT CONTAINING A SUITABLE RADIOISOTOPE WOULD BE VERY ADVANTAGEOUS BECAUSE OF ITS POTENTIAL SIMPLICITY, NON-INVASIVENESS AND SPEED. PREVIOUS RESEARCH WITH 17 B-ESTRADIOL POSSESSING (127)I (NATURAL NON-RADIOACTIVE IODINE) OR (125)I AT THE 16A POSITION ESTABLISHED THE HIGH ESTROGEN RECEPTOR SPECIFICITY, LOW NONSPECIFIC BINDING AND RELATIVELY SLOW METABOLIC DEGRADATION OF THIS COMPOUND. THE ISOTOPE (123)I (COMMERCIALLY AVAILABLE) HAS A Y-EMISSION ENERGY EXCELLENT FOR IMAGING WITH STANDARD NUCLEAR MEDICAL EQUIPMENT, BUT TO DATE, CANNOT BE EFFICIENTLY INTRODUCED INTO THE 16A POSITIONOF 17 B-ESTRADIOL BY THE METHODS CURRENTLY USED FOR (127)I OR (125)I, BECAUSE THE REACTION TIME REQUIRED FOR IODINATIONIS 1.5 - 2 TIMES THE HALF-LIFE OF (123)I (13H). THE OBJECTIVES OF THIS PROPOSED PHASE I WORK ARE TO DEVELOP A NEW SYNTHESIS OF 16A-I-17 B-ESTRADIOL AND ITS RAPID PURIFICATION, TO APPLY THIS SYNTHETIC METHOD TO THE PRODUCTION OF 16A-(123)I-17 B-ESTRADIOL, AND TO INVESTIGATE THE "IN VITRO" AND "IN VIVO" (RATS) PROPERTIES OF 16A-(123) I-17 B-ESTRADIOL IN ORDER TO ASSESS ITS SUITABILITY FOR THE IMAGING OF ESTROGEN RECEPTOR-POSITIVE VERSUS ESTROGEN RECEPTOR-NEGATIVE BREAST TUMORS AND METASTASES. THE WORK PERFORMED IN THIS PHASE WILL ALLOW THE DEVELOPMENT OF SYNTHETIC, BIOCHEMICAL AND IMAGING EXPERTISE WHICH WILL AID IN THE DEVELOPMENT OF RELATED (123)I-LABELED COMPOUNDS, SUCH AS PROGESTERONE AND TESTESTERONE ANALOGS OR DERIVATIVESWHICH MAY BE USEFUL IN THE CHARACTERIZATION OF OTHER TUMOR TYPES.

Principal Investigator:

Richard J. Baranczuk
8169420646

Business Contact:

Small Business Information at Submission:

Biomedical Research Laboratory
9017 East 35th Street Kansas City, MO 64129

EIN/Tax ID:
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No