Disclosed herein are compositions, kits and methods for treating and detecting cancer, and more particularly radiolabeled conjugates used for targeted radiotherapy of cancer patients.

A process for the preparation of a carrier-free Ga-68 solution from an irradiated Zn target, systems comprising components used in the process, and compositions comprising Ga-68 prepared by the process. Purification of Ga-68 is carried out by feeding an irradiation target solution comprising Zn-68, Ga-68 and solid target assembly metals into a system comprising three chromatography columns in succession.

A compound of the Formula I or a pharmaceutically acceptable salt thereof, wherein R.sub.1, Ca, Cb, Cd, and n are the same as described in the specification. Disclosed is a method of diagnosing or monitoring a patient suffering from cancer, the method comprising: administering a pharmaceutical composition comprising an effective amount of an active agent, wherein the active agent is the compound of Formula I, a pharmaceutically acceptable salt of any of the foregoing thereof, or a combination thereof, together with a pharmaceutically acceptable carrier to the patient and diagnosing or monitoring the patient by hyperpolarized .sup.13C-MRI. Also disclosed is a method of synthesizing 1-.sup.13C-5-.sup.12C-diacid.

##STR00001##

Prostate-specific membrane antigen targeted high-affinity agents for endoradiotherapy of prostate cancer are disclosed.

The invention relates to a marking precursor incorporating a chelator or fluorination group for radiolabelling with .sup.44Sc, .sup.47Sc, .sup.55Co, .sup.62Cu, .sup.64Cu, .sup.67Cu, .sup.66Ga, .sup.67Ga, .sup.68Ga, .sup.89Zr, .sup.86Y, .sup.90Y, .sup.90Nb, .sup.99mTc, .sup.111In, .sup.135Sm, .sup.140Pr, .sup.159Gd, .sup.149Tb, .sup.160Tb, .sup.161Tb, .sup.165Er, .sup.166Dy, .sup.166Ho, .sup.175Yb, .sup.177Lu, .sup.186Re, .sup.188Re, .sup.213Bi and .sup.225Ac or with .sup.18F, .sup.131I or .sup.211At, and one or two biological targeting vectors which are coupled to the chelator or fluorinating group via one or more squaric acid groups.

The present disclosure relates to methods of administering [.sup.18F]-FACBC. The present disclosure also relates to use of [.sup.18F]-FACBC in methods for imaging, diagnosing, and monitoring of brain lesions.

In particular, the present invention relates to a PSMA binding ligand comprising an oligosaccharide building block which comprises a bond being cleavable by alpha-amylase.

Typically, this PSMA binding ligand further comprises a PSMA binding motif Q and a chelator residue A, wherein the PSMA binding motif Q and the chelator residue A are preferably linked via at least one linker L.sup.AQ comprising the oligosaccharide building block, the PSMA binding ligand thus preferably having the structure (I)

A-L.sup.AQ-Q

or a pharmaceutically acceptable salt or solvate thereof.

The invention relates to methods of treating cancer with CTT1403 having specificity for prostate-specific membrane antigen (PSMA).

[Problem] To provide a labeled fatty acid derivative for diagnostic imaging that enables the quantification of myocardial fatty acid metabolic activity. [Solution] The inventors, engaging in diligent research into methods that enable the quantification of fatty acid metabolic activity, discovered that a labeled fatty acid derivative represented by formula (1), in which [.sup.18F] has been substituted at a specific position of a long-chain carboxylic acid compound containing a sulfur atom, or a salt thereof, has good accumulation in the myocardium, and enables imaging of fatty acid metabolic activity via positron emission tomography (PET). Therefore, the labeled fatty acid derivative according to the present invention can be used as a radiotracer for swift and noninvasive quantification of myocardial fatty acid metabolic activity, diagnostic imaging of heart diseases such as ischemic heart disease, diagnostic imaging of the therapeutic effects yielded by a heart disease therapeutic agent, and so forth.

This disclosure relates to 1-amino-3,4-difluorocyclopentane-1-carboxylic acid, esters, derivatives, or salts having positron emitting radionuclides for use as radionuclide tracers. In certain embodiments, 1-amino-3,4-difluorocyclopentane-1-carboxylic acid is isotopically enriched with fluorine 18. In certain embodiments, the radionuclide tracer is amino-3-fluoro-4-[.sup.18F]fluorocyclopentane-1-carboxylic acid. In certain embodiments, the radionuclide tracers are useful to indicate the existence of and/or position of a tumor or cancerous cells in a subject.