Abstract: This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to peptides, methods and kits for making such peptides, and methods for using such peptides to image sites in a mammalian body labeled with technetium-99m (Tc-99m) via Tc-99m binding moieties. In particular, the peptide reagents of the invention are covalently linked to a polyvalent linker moiety, so that the polyvalent linker moiety is covalently linked to a multiplicity of the specific-binding peptides, and the Tc-99m binding moieties are covalently linked to a plurality of the specific-binding peptides, the polyvalent linker moiety, or to both the specific-binding peptides and the polyvalent linker moiety.

Abstract: Radioactive arsenic (.sup.72 As) labelled tissue specific ligands are prepared and used in the medical imaging of malignant breast or prostate tumors.

Abstract: Disclosed is a composition of matter useful in imaging tissue, the composition comprising a complex formed between technetium (Tc-99m) and 5-thio-D-glucose. Also disclosed is a method of in vivo imaging of acute ischemic tissue and tumors in a mammalian subject comprising delivering into the subject an effective amount of (Tc-99m)-5-thio-D-glucose, and scanning the subject to determine the distribution of the Tc-99m-TG complex in the subject. A method of preparing the composition of matter is also disclosed.

Abstract: A novel method for the mucosal administration of a substance to a mammal is provided. The method comprises contacting a mucosal surface of the mammal with the substance in combination with a Biovector. The Biovector has a core that comprises a natural polymer, or a derivative or a hydrolysate of a natural polymer, or a mixture thereof. A preferred natural polymer is a polysaccharide or an oligosaccharide. The core is optionally coated with an amphiphilic compound, such as a lipid.

Abstract: A compound useful for in vivo imaging of organs and tumors is provided of formula: ##STR1## wherein ##STR2## is a cobalamin, ##STR3## is derived from a corrin carboxylic acid group of said cobaltmin, Y is a linking group and X is a chelating group, optionally comprising a detectable radionuclide or a paramagnetic metal ion, and n is 1-3.

Abstract: This invention relates to bisamine bisthiol radiolabel binding moieties and synthetic methods therefor. Specifically, the invention provides radiolabel binding moieties that form an electrically neutral complex with technetium-99m.

Abstract: Diagnostic and therapeutic compositions in the form of complexes for enhancing transmembrane transport of a diagnostic or therapeutic agent and methods for their use. The complexes contain the .alpha., .gamma., or bis isomers of folate receptor-binding analogs of folate, a metal chelated by a ligand, and in one embodiment, a chemotherapeutic agent.

Abstract: This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to peptides, methods and kits for making such peptides, and methods for using such peptides to image sites in a mammalian body labeled with technetium-99m (Tc-99m) via a radiolabel-binding moiety which forms a neutral complex with Tc-99m.

Abstract: N-demethylated and N,N-demethylated derivatives of toluidine blue O and compositions which include these derivatives and the conformational isomers of toluidine blue O. Improved methods for the detection of dysplastic oral tissue using such compositions.Processes for synthesis of toluidine blue O products, in which a complexing agent is introduced prior to the last stage of oxidation of a three-step synthesis from N,N-dimethyl-.rho.-phenylenediamine.An HPLC method for characterizing toluidine blue O products in which the mobile phase is an aqueous solution of an organic acid.

Abstract: This invention relates to calcitonin receptor binding reagents comprising compounds which are covalently linked to a radiometal chelator. The invention is embodied as calcitonin receptor binding peptide derivatives and analogues of calcitonin which may be radiolabeled with a suitable isotope and used as radiodiagnostic or radiotherapeutic agents. Methods and kits for making, radiolabeling and using such reagents diagnostically and therapeutically in a mammalian body are also provided.

Abstract: This invention relates to radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic and radiotherapeutic agents. Specifically, the invention relates to calcitonin receptor binding compounds, preferably peptides, derivatives and analogues of calcitonin, and embodiments of such compounds radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such compounds, particularly peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to calcitonin receptor binding peptide derivatives and analogues of calcitonin radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to calcitonin receptor binding peptide derivatives and analogues of calcitonin radiolabeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re) for use as radiotherapeutic agents.

Abstract: This invention relates to an in-vivo diagnostic method based on near infrared radiation (NIR radiation) that uses water-soluble dyes and their biomolecule adducts, each having specific photophysical and pharmaco-chemical properties, as a contrast medium for fluorescence and transillumination diagnostics in the NIR range, to new dyes and pharmaceuticals containing such dyes.

Abstract: An intramolecularly-quenched, near infrared fluorescence probe that emits substantial fluorescence only after interaction with a target tissue (i.e., activation) is disclosed. The probe includes a polymeric backbone and a plurality of near infrared fluorochromes covalently linked to the backbone at fluorescence-quenching interaction-permissive positions separable by enzymatic cleavage at fluorescence activation sites. The probe optionally includes protective chains or fluorochrome spacers, or both. Also disclosed are methods of using the intramolecularly-quenched, near infrared fluorescence probes for in vivo optical imaging.

Abstract: A method for the treatment of cancer is disclosed which is capable of directing supra-lethal doses of radiation, called Hot-Spots, virtually exclusively to the cancer. The present invention involves a multi-step therapy process and includes a class of novel chemical agents. In accordance with the present invention, it was discovered that soluble precipitable materials can be made to accumulate as non-digestible precipitates in targeted cells as a result of enzyme action within the targeted cells. Accumulation is achieved by administering to the living host a soluble binary reagent made by attaching a targeting agent to a novel chemical agent which is a soluble precipitable material. The binary reagent binds to antigenic receptors on targeted cells which endocytose the binary reagent and transport it into the lysosomes where enzymes detach the soluble precipitable material from the targeting agent, causing it to precipitate, accumulate, and be retained in the cells.

Abstract: Novel methods for radiolabeling sulfhydryl group-bearing biomolecules, novel compositions useful for radiolabeling sulfhydryl group-bearing biomolecules, kits comprising such novel compositions and methods for imaging mammalian, preferably human, tissue employing radiolabelled biomolecules are described. The methods, compositions and kits of the present invention are useful for labeling sulfhydryl group-bearing biomolecules such as whole molecule proteins, protein fragments or peptides, in particular, monoclonal or polyclonal antibodies, and especially, antifibrin MH1 monoclonal antibody.

Abstract: The invention provides compositions, methods and kits for effecting therapy of a tumor in a patient. The compositions comprise (A) a first conjugate comprising a targeting moiety, a first member of a binding pair, and a first therapeutic agent, wherein the targeting moiety selectively binds to a marker substance produced by or associated with the tumor; (B) optionally, a clearing composition; and (C) a second conjugate comprising a complementary member of the binding pair and a second therapeutic agent, wherein the second therapeutic agent is the same as or different from the first therapeutic agent. The methods comprise sequentially administering (A), (B), and (C) to a patient. The kits comprise (A), (B), and (C) in separate containers.

Abstract: This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to peptides, methods and kits for making such peptides, and methods for using such peptides to image sites in a mammalian body labeled with technetium-99m (Tc-99m) via a radiolabel-binding moiety covalently attached to a specific binding peptide via an amino acid side-chain of the peptide.

Abstract: The invention pertains to compounds for binding lanthanide ions and actinide ions. The invention further pertains to compounds for binding radionuclides, and to methods of making radionuclide complexes. Also, the invention pertains to methods of extracting radionuclides. Additionally, the invention pertains to methods of delivering radionuclides to target locations. In one aspect, the invention includes a compound comprising: a) a calix[n]arene group, wherein n is an integer greater than 3, the calix[n]arene group comprising an upper rim and a lower rim; b) at least one ionizable group attached to the lower rim; and c) an ion selected from the group consisting of lanthanide and actinide elements bound to the ionizable group.

Abstract: Background: Between 1991 and 1997 sixty-seven patients with non-resectable hepatoma were treated with hepatic artery infusions (HAI) of cisplatinum. Patients were divided into groups for analysis based on alpha-fetoprotein elevation (AFP+) or no elevation (AFP-), hepatitis B/C status, the presence or absence of extra-hepatic metastases and primary treatment at our facility or initial therapy elsewhere.Methods: Forty-four patients received an initial course of 21-24 Gy whole liver external radiation with cisplatinum 50 mg/m.sup.2 IV on days 1 and 8 of radiation. Twenty-three patients did not receive external radiation and received HAI cisplatinum only. All patients were then treated with HAI cisplatinum at 50 mg/m.sup.2 on a monthly basis. The rationale for the advantage to HAI cisplatinum was evaluated by giving a tracer dose of radioactive .sup.195m cisplatinum for quantitative determinations by the intra-arterial route in six patients.

Abstract: Boron containing compounds are targeted to hormonally responsive cells by contacting the cells with a conjugate of a boron containing moiety conjugated to a ligand having binding specificity for an intracellular receptor of the cell. The conjugates are useful for imaging or killing hormonally responsive cells, such as hormonally responsive tumor cells. For target cell killing, the cells are contacted with a .sup.10 B containing moiety conjugated to a ligand having binding specificity for an intracellular hormone receptor of the cells. The .sup.10 B containing moiety becomes associated with the hormone receptor of the cells, which may then be irradiated with neutrons to kill the cells by boron neutron capture. For target cell imaging, the cells are contacted with a .sup.