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Precision medicine theranostics and diagnostics a combination thereof

a technology of theranostics and precision medicine, applied in the field of theranostics, can solve the problem of challenging selection problem of ligands toward different integrin subtypes, and achieve the effect of safety and efficacy

Inactive Publication Date: 2020-03-19
SATZ STANLEY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes compounds that can be used to diagnose and treat various disorders related to metastasis and angiogenesis, such as breast cancer, lung cancer, and gastric cancer. These compounds contain a unique peptidomimetic that targets specific proteins associated with these diseases. The compounds have been tested in animals and found to be safe and effective. This patent provides a valuable tool for the diagnosis and treatment of these disorders using PET, SPECT, and MRI imaging techniques.

Problems solved by technology

Despite numerous studies reported in the literature, ligand selectivity toward different integrin subtypes is still a challenging problem mainly because most of the 3D-structures of integrin subtypes remain unknown (Marinelli, L.; et al.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Proposed Example 1

[0039]Example 1: a preferred compound of the invention, comprising Lu-177 DOTAGA IAC, is administered to a human patient at a fixed dose of 7.4 GBq (every 12 weeks) up to a cumulative dose which is tolerated by the patient (maximum 29.6 GBq). The preferred compound preferably is administered intravenously. Nivolumab is administered twice for each treatment of the preferred Lu-177 DOTAGA IAC compound, at a dose of 3 mg / Kg: one administration seven days before (d−7) and the other administration seven days after (d−positive7) administration of the compound of the invention, with the aim of achieving an effective PD-1 / PD-L1 blockade, but also in the need not to overlap the anticipated lymphocyte nadir related to the lymphocytopenia-induced effect of the compound of the invention.

[0040]Studies have shown that intravenous administration of amino acids has a renal protective effect. An infusion of amino acids (containing lysine and arginine) could be done 30 to 45 minutes...

example 2

Proposed Example 2

[0041]Example 2: In a proposed example, the compound of the present invention was administered to a patient suffering from HER2+ breast cancer. The patient was given the compound of the invention (e.g., in an amount of from about 3.7-7.4 GBq) administered intravenously, and representing a dosage. One or more, and preferably a plurality of subsequent treatments of a similar amount are dosed to the patient intravenously, a couple to a few weeks from the first dosage. In this example, an additional therapeutic may be administered on either side of a window based on when the patient receives the inventive compound doses, e.g., such as seven days prior to a dose and seven days after a dose.

example 3

Proposed Example 3

[0042]Example 3: The patient was treated as in proposed example 1, above, however, prior to treatment with the Lu-177 DOTAGA IAC, the patient was diagnosed using the preferred diagnostic composition, comprising Ga-68-NODAGA IAC.

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Abstract

The component ‘drug’ new molecule for combining metals into complexes through a ring structure (DOTA) or linear structure, and a radionuclidic component, and chelating agent wherein embodiments may include a companion diagnostic, and in which embodiments further include anti-integrin precision medicines for cancers expressing αvβ3 and αvβ5 integrins, second component for combining metals into complexes through a ring or linear structure, and one or more radionuclidic components, a chelating agent for diagnosis and / or therapy (theranostic) in which the embodiments further include a anti-integrin peptidomimetic for precision medicine for cancers expressing αvβ3 and αvβ5 integrins.

Description

CROSS-REFERENCE TO RELATED APPLICATION[0001]This application claims the benefit of priority to U.S. Provisional Application Ser. No. 62 / 729,959, filed on Sep. 11, 2018, the complete contents of which are herein incorporated by reference.BACKGROUND OF THE INVENTION1. Field of the Invention[0002]The present invention relates to the field of cancer diagnosis and therapy, theranostics, and the creation of novel molecules; more particularly an integrin peptidomimetic, an isotope and a chelating agent for treating, diagnosing and staging cancers, and, in particular, cancers overexpressing the human epidermal growth factor positive receptor 2 protein (HER2+) and triple negative breast cancer and relates to the synthesis and reaction of potent and selective small molecule integrin antagonists containing appropriate linkers and functional groups for chemical reaction with other molecules which contain reactive nucleophiles such as thiols such that a covalent linkage is formed between a moiet...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K51/08
CPCA61K51/088A61K2123/00C07K16/2818A61K51/083A61K51/0497A61K51/0459A61P35/00A61K45/06A61K51/1021C07K16/22C07K2317/77A61K51/1096G01N33/574A61K51/1027
Inventor SATZ, STANLEY
Owner SATZ STANLEY
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