Compositions, methods, and uses of an alpha emitter are provided in which the alpha emitter is coupled to carrier protein via a cleavable coupling moiety. The coupling moiety is preferably cleavable in an acidic tumor microenvironment, and as such will enrich the alpha emitter upon cleavage within the tumor microenvironment.

The .sup.18F-labeling of unprotected peptides and sugars via thioarylation using a Au(III)-[.sup.F]fluoroaryl complex is reported. The chemoselective method generates .sup.18F-labeled S-aryl bioconjugates in an aqueous environment in 15 min with high radiochemical yields and displays excellent functional group tolerance. This approach utilizes an air and moisture stable, robust organometallic Au(III) complex and highlights the versatility of designer organometallic reagents as efficient agents for rapid radiolabeling.

The present invention relates to zwitterionic metal chelators and their use as imaging, diagnostic, chemical processing, and treatment agents. These zwitterionic metal chelators have desirable properties that maximize solubility in aqueous environments, minimize non-specific interactions, and retain the ability to target thus resulting in an improved performance in a variety of medical, agricultural, and chemical processes. In in vivo and medical applications, zwitterionic metal chelators improve the signal-to-background ratio and therapeutic window as compared to other metal chelators while retaining high stability.

The present invention relates to a stable pharmaceutical composition of tetrofosmin or pharmaceutically acceptable salts thereof. It also relates to a lyophilized non-radioactive kit which upon reconstitution with .sup.99mTc-pertechnetate solution gives a stable .sup.99mTc-tetrofosmin radiopharmaceutical composition. It also provides process for the preparation of said radiopharmaceutical compositions and their use in diagnostic imaging procedures. The compositions provide desirable technical attributes such as stability, high radiochemical purity (RCP) and desired bio-distribution.

A compound of general formula I

##STR00001## where A is a chelator selected from the group of

##STR00002## k is independently at each occurrence 0, 1, or 2; m is independently at each occurrence 1, 2, 3, 4 or 5; n is independently at each occurrence 0, 1, 2 or 3; p is independently at each occurrence 1, 2 or 3; q is independently at each occurrence 1, 2 or 3; u is independently at each occurrence 0 or 1; X and Y are substituted or unsubstituted amino acids; L is a bifunctional linker selected from group of

##STR00003## where v, x, and y are independently of each other 0, 1, 2, or 3 and z is 0, 1, 2, 3, 4 or 5; and R is H, methyl or ethyl.

The present invention relates to zwitterionic metal chelators and their use as imaging, diagnostic, chemical processing, and treatment agents. These zwitterionic metal chelators have desirable properties that maximize solubility in aqueous environments, minimize non-specific interactions, and retain the ability to target thus resulting in an improved performance in a variety of medical, agricultural, and chemical processes. In in vivo and medical applications, zwitterionic metal chelators improve the signal-to-background ratio and therapeutic window as compared to other metal chelators while retaining high stability.

The present invention relates to zwitterionic metal chelators and their use as imaging, diagnostic, chemical processing, and treatment agents. These zwitterionic metal chelators have desirable properties that maximize solubility in aqueous environments, minimize non-specific interactions, and retain the ability to target thus resulting in an improved performance in a variety of medical, agricultural, and chemical processes. In in vivo and medical applications, zwitterionic metal chelators improve the signal-to-background ratio and therapeutic window as compared to other metal chelators while retaining high stability.

The present invention relates to methods and kits for radiolabelling a chelate-functionalized targeting agent with a metal radionuclide being gallium-68, using a stabiliser that prevents radiolysis (product degradation) of the chelate-functionalized targeting agent, wherein said stabiliser is selected from the group consisting of: ascorbic acid, dehydroascorbic acid, gentisic acid, cysteine and methionine, sodium ascorbate, or a salt thereof, preferably as a solution. The invention further relates to the use of said stabilizer against radiolytic decomposition of a radiolabelled chelate-functionalized targeting agent composition and methods of detecting a prostate tumour or cancer using the method for radiolabelling.

Provided herein are a variety of metal chelators as well as methods of use thereof.

A method for preparing a complex comprising a radioisotope of gallium for use in radiotherapy or in a medical imaging procedure, said method comprising adding a gallium radioisotope solution obtained directly from a gallium radionuclide generator to a composition comprising a pharmaceutically acceptable buffer and optionally also a pharmaceutically acceptable basic reagent, in amounts sufficient to increase the pH to a level in the range of 3 to 8, wherein the composition further comprises a chelator that is able to chelate radioactive gallium within said pH range and at moderate temperature, said chelator being optionally linked to a biological targeting agent. Kits and compositions for use in the method are also described and claimed.