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AN INSTANT KIT FOR 2-18FFLUORO-2-DEOXYGLUCOSE (FDG)

Award Number: R43EB005858
ORGANIZATION: NATIONAL INSTITUTE Of BIOMEDICAL IMAGING & BIOENGINEERING
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 09/14/2005
PERIOD OF PERFORMANCE END DATE: 03/31/2006

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AN INSTANT KIT FOR 2-18FFLUORO-2-DEOXYGLUCOSE (FDG) - DESCRIPTION (provided by applicant): Since the development of the high yield nucleophilic fluorination reaction by Hamacher et al. and the development of commercially available precursors for one or two step synthesis of F-18 labeled targeted molecules, a large number of molecular imaging probes have been developed. The radiotracer having the greatest impact on clinical care is F-18 2-fluoro-2-deoxyglucose (FDG). However, the present synthesis of FDG and other F-18 labeled probes requires a hot cell (or a mini-cell) and a sophisticated multi-valve synthesis system. The final step in making F-18 radiopharmaceuticals readily available is the development of a "kit" that can produce the F-18 radiopharmaceuticals by the simple addition of F-18 fluoride to a vial with, at most, a single small column purification. By analogy with the development of the Tc-99m Instant Kits, which made a series of Tc-99m radiotracers available with the simple addition of Tc-99m pertechnetate to a pre-made, commercially available non-radioactive kit, a F-18 Instant Kit would have the same effect on making not only FDG, but a series of important molecular imaging probes available without the expense and complications of the present day requirements. This will be accomplished using proprietary fluorous technology. Fluorous chemistry has evolved rapidly over the last decade to become a new general separation method used across a wide spectrum of applications. The separation is based on the solvophobicity of highly fluorinated compounds in either organic or aqueous phases. The fluorous phase therefore represents an orthogonal third phase whose properties can be exploited to simplify separation and purification. These fluorous tags are essentially chemically inert, therefore providing a handle by which to isolate and purify compounds without substantially changing the reactivity of the tagged molecule. Two synthetic approaches using fluorous derivatives of mannose triflate will be investigated as a one/two step process for producing FDG. Biocomparability with the present FDG formulation using Am Chem Soc and DSP criteria for purity and identity will be carried out and a prototype instant kit will be constructed. The successful completion of the work will lead to reduced cost for facilities (hot cells, complicated synthesis boxes) and increased flexibility to produce many F-18 compounds with a simple, one-time use "instant kit". Most importantly, it will lead to the wide-spread use of a series of F-18 molecular imaging probes.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2005 ( Subtotal = $130,387 )
2005	2005	MOLECULAR INSIGHT PHARMACEUTICALS INC	160 SECOND STREET	CAMBRIDGE	MA	02142	MIDDLESEX	USA	Discovery and Applied Research for Technological Innovations to Improve Human Health	000	1	9/14/2005	NEW	$130,387
														Subtotal = $130,387

Grand Total All Awards = $130,387

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AN INSTANT KIT FOR 2-18FFLUORO-2-DEOXYGLUCOSE (FDG)

Award Number: R43EB005858

ORGANIZATION: NATIONAL INSTITUTE Of BIOMEDICAL IMAGING & BIOENGINEERING

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 09/14/2005

PERIOD OF PERFORMANCE END DATE: 03/31/2006

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