Abstract: The present invention relates to diethylenetriamine pentaacetic acid (DTPA) derivates and metal complexes thereof, and radiation sources and contrast agents including the metal complexes. More particularly, the present invention relates to DTPA derivatives, which contain iodine and are useful as contrast agents for diagnosing renal function, metal complexes of the DTPA derivatives with 99mTc, 166Ho, 111In, 90Y, 153Sm, 186Re, 188Re, 68Ga, or 177Lu, which are useful as liquid radiation sources for treating vascular stenosis and contrast agents for diagnosing renal function, and radiation sources and contrast agents including the metal complexes. The DTPA derivatives and metal complexes thereof are safe because the metal complexes are excreted via the kidneys and bladder within several minutes from the time of use as liquid radiation sources for treating vascular stenosis, and are cost-effective because they are potentially useful as contrast agents and as agents for diagnosing renal function.

Abstract: The present invention concerns cell-penetrating peptides which comprise an amino acid sequence consisting of GLX9WRAX9WRX1LX2RSLX9WX3X4X5X6X7X8 (SEQ ID No: 1), wherein X1 is A, L or G, X2 is W or none, X3 is R or K, X4 is K, L or S, X5 is L or K, X6 is R or W, X7 is K or S, and X8 is A, V or Q, and X9 is W, F or Y. These CPPs can be used as vectors for delivering nucleic acids and/or proteins and/or peptides to cells, in vitro or in vivo.

Abstract: Epidermal growth factor (EGF) produced by an excretory recombinant approach was tested for its efficacy in treating various skin wounds. In a randomized double blind controlled study, local cream samples prepared with human EGF at a final concentration of as low as 0.02% (g/g) in topically suitable carrier were found to have an enhancing effect on the recovery of diabetes foot ulcers. This promotional effect is statistically significant and has resulted in a reduced mean healing time of over 3 weeks when compared with that of control. Both the 0.02% (g/g) and 0.04% (g/g) human EGF supplemented samples in comparison with control showed a trend of stimulatory effect when a recovery of 50% of an ulcer was considered. The EGF samples were also shown to be highly effective in promoting treatments of wounds resulting from bedsores and surgeries.

Abstract: The present disclosure concerns methods of administering and detecting a distinguishable agent in a sample from and assessing the condition of an organ in a subject. In a particular embodiment, the present invention concerns methods of detecting and comparing the cholate shunt, in a subject, preferably in a subject with chronic hepatitis C. In certain embodiments, the methods may comprise obtaining a sample from a subject such as a blood or saliva sample after administering an oral and intravenous dose of a distinguishable agent such as cholate and analyzing the sample clearance of the distinguishable agent from the subject and comparing the clearance levels in order to assess hepatic health. In another embodiment, the methods may comprise analyzing a sample from a subject for the presence of a distinguishable agent such as cholate and applying information obtained from analyzing the presence of the distinguishable agent to determine a treatment for a medical condition of the subject.

Abstract: The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver short interfering nucleic acid (siNA). The compositions described herein are generally referred to as formulated molecular compositions (FMC) or lipid nanoparticles (LNP).

Abstract: Polymers comprising a polyethylenimine, a biodegradable group, and a relatively hydrophobic group are useful for the delivery of bioactive agents to cells.

Abstract: Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and in treating or preventing prostate cancer. The agents define a new-subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention.

Abstract: Positron emitting compounds and methods of their production are provided. The compounds have the formula: (F)m G (R)n wherein each R is a group comprising at least one carbon, nitrogen, phosphorus or sulfur atom and G is joined to R through said carbon, nitrogen, phosphorus or sulfur atom; G is silicon or boron; m is 2 to 5 and n is 1 to 3 with m+n=3 to 6 when G is silicon; m is 1 to 3 and n is 1 to 3 with m+n=3 to 4 when G is boron; and wherein the compound further comprises one or more counterions when the above formula is charged; and wherein at least one F is 18 F.

Abstract: The invention relates to compounds having a binding affinity for both the ?v?3 receptor and a (neuro)peptide receptor, in particular the somatostatin receptor, which compound comprises a first peptide part comprising at least once the amino acid sequence Arg-Gly-Asp, and a second peptide part coupled thereto, optionally via a linker, which second peptide part is a (neuro)peptide.

Abstract: The use of contrast agents of molecular weight lower than 5000 Dalton and including at least one residue of a biliary acid for the preparation of diagnostic contrast compositions for the microvascular permeability assessment is disclosed.

Abstract: A liposome containing a hydrophobic iodine compound such as a 1,3,5-triiodobenzene derivative having at least one substituent containing 18 or more carbon atoms as a membrane component, and an X-ray contrast medium containing the liposome for use in radiography of a vascular disease and the like.

Abstract: Disclosed is the surprising discovery that aminophospholipids, such as phosphatidylserine and phosphatidylethanolamine, are specific, accessible and stable markers of the luminal surface of tumor blood vessels. The present invention thus provides aminophospholipid-targeted diagnostic and therapeutic constructs for use in tumor intervention. Antibody-therapeutic agent conjugates and constructs that bind to aminophospholipids are particularly provided, as are methods of specifically delivering therapeutic agents, including toxins and coagulants, to the stably-expressed aminophospholipids of tumor blood vessels, thereby inducing thrombosis, necrosis and tumor regression.

Abstract: Screening methods for identifying compounds that bind to or activate (D1 or D5 dopamine receptors individually or in combination) or potentially regulate skeletal muscle mass or function in vivo. Also disclosed are screening methods for identifying compounds that prolong or augment the activation of D1 or D5 dopamine receptors or of D1 or D5 dopamine receptor signal transduction pathways and increase D1 or D5 dopamine receptor expression. Pharmaceutical compositions comprising D1 or D5 dopamine receptor agonists, antibodies to D1 or D5 dopamine receptors and methods for increasing skeletal muscle mass or function or for the treatment of skeletal muscle atrophy using D1 or D5 dopamine receptors as the target for intervention and methods for treatment of muscular dystrophies are described.

Abstract: Radiopharmaceutical compositions which are stabilized by addition of a mixture of a hydrophilic thioether and a hydrophilic 6-hydroxy-chroman derivative.

Abstract: Radiopharmaceutical compositions which are stabilized by addition of a hydrophilic thioether.

Abstract: A method for improving intracellular administration of a therapeutic agent is provided comprising: contacting cells with a compound comprising a charged derivative of a therapeutic agent having a therapeutic activity, the charged derivative being conjugated to a protein having a biological activity of being transported across a cell membrane into a cell; and having the cell transport the compound into the cell where the cell metabolizes at least a portion of the compound to form a charged metabolite product that possesses the therapeutic activity of the therapeutic agent, the charged metabolite product being less prone to being transported across the cell membrane out of the cell relative to the compound and less prone to being transported across the cell membrane out of the cell relative to the therapeutic agent.

Abstract: Radiopharmaceutical compositions which are stabilized by addition of a hydrophilic 6-hydroxy-chroman derivative.

Abstract: Metal nanoparticles are described that are useful for enhancing the contrast of x-rays or other radiation sources. A method is disclosed whereby the agents are administered intravenously or intra-arterially to detect coronary senses and other vascular features. It is also disclosed how directing moieties attached to the metal particles are used to detect specific targets.

Abstract: Improved methods for detecting lesions in dense breast tissue are disclosed. The methods of the invention generally feature administration to a subject of an LHRH antagonist in an amount and for a period of time sufficient to reduce the density of breast tissue prior to generating an image of the breast tissue, for example by mammography, to detect a lesion in the breast tissue. Packaged formulations for reducing breast density in a subject prior to generating an image of the subject's breast tissue, comprising an LHRH antagonist packaged with instructions for using the LHRH antagonist to reduce breast density in a subject prior to imaging the breast tissue, are also disclosed.

Abstract: A biodegradable, novel cationic lipopolymer comprising a branched polyethylenimine(PEI), a cholesterol derived lipid anchor, and a biodegradable linker which covalently links the branched PEI and cholesterol derived lipid anchor. One example of such a novel lipolymer is poly{(ethylene imine)-co-[N-2-aminoehtyl)ethylene imine]-co-[N-(N-cholesteryloxycabonyl-(2-aminoethyl))ethylene imine]} (“PEACE”). The cationic lipopolymers in the present invention can be used in drug delivery and are especially useful for delivery of a nucleic acid or any anionic bioactive agent to various organs and tissues after local or systemic administration. Methods of preparing and using the cationic lipopolymer gene carriers of the present invention to efficiently transfect cells, both in vitro and in vivo, are disclosed.

Abstract: Processes for the preparation, prepared solutions, and the use of radium-223 for the treatment of calcified tumors, bone tumors, treatment of bones, bone surfaces and soft tissues is described.

Abstract: The present invention is a system and method capable of increasing retinal and neural glucose oxidation by enhancing pyruvate dehydrogenase activity and therefore treats retinopathy and central nervous system disorders in both diabetic and non-diabetic patients. The current invention is a system and method of the treating of eye and nerve diseases using insulin pulses to a patient utilizing Chronic Intermittent Intravenous Insulin Therapy to achieve an increase in retinal and neural glucose oxidation by enhancing pryuvate dehydrogenase activity, therefore treating retinopathy and central nervous system disorders in both diabetic and non-diabetic patients.

Abstract: Improved methods for detecting lesions in dense breast tissue are disclosed. The methods of the invention generally feature administration to a subject of an LHRH antagonist in an amount and for a period of time sufficient to reduce the density of breast tissue prior to generating an image of the breast tissue, for example by mammography, to detect a lesion in the breast tissue. Packaged formulations for reducing breast density in a subject prior to generating an image of the subject's breast tissue, comprising an LHRH antagonist packaged with instructions for using the LHRH antagonist to reduce breast density in a subject prior to imaging the breast tissue, are also disclosed.

Abstract: A pharmaceutical composition and method, for treating human or non-human neoplastic disorders, e.g. colorectal disorders, comprising the administration of pharmaceutically effective amounts of galanin, octreotide and serotonin in a pharmaceutically acceptable carrier. The effective amount is 10 &mgr;g/kg body weight to about 60 &mgr;g/kg body weight of each of the three, preferably about 10 &mgr;g/kg to about 20 &mgr;g/kg of each of the three.

Abstract: A method of imaging apoptosis in vivo, using radiolabeled annexin, is described. Methods for tumor radiotherapy are also provided.

Abstract: Polysaccharide-somatostatin analogs of the formula: wherein the somatostatin analog is directly or indirectly coupled from a terminal N-amino group of the somatostatin analog to a polysaccharide, and the polysaccharide-somatostatin analog is provided with an effective negative charge. The compounds are useful in diagnosing and treating cancers.

Abstract: An immunoassay method including reacting a sample from a patient with a bispecific antibody, wherein the bispecific antibody includes one antibody specific for a compound to be detected and a second antibody specific for a compound foreign to said patient sample, and subsequently reacting the patient sample with a polymer probe, wherein the polymer probe includes a compound recognized by the second antibody in the bispecific antibody complex and further includes at least two detectable signals; the bispecific antibody; and the polymer probe of the immunoassay method are disclosed.

Abstract: The present invention relates to a radiolabeled non-steroidal compound having the formula: 1

Abstract: A compound comprising a ligand portion which has binding affinity for an opioid receptor, and a therapeutically or diagnostically effective group selected from radionuclide chelating agents, fluorochromes, toxins, drugs, polyboron moieties, proteins, biological response modifiers, chemical moieties capable of binding to other molecules of interest, and radioisotopes selected from therapeutically effective alpha and beta emitters, and diagnostically effective gamma emitters. The compound may be used in a method of treating cancer, and in a method of imaging opioid receptors either inside or outside of the central nervous system.

Abstract: Diamine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided.