A61K51/083

Transduced T cells expressing human SSTR2 and application thereof
11634471 · 2023-04-25 · ·

The present invention is directed to transduced T cells expressing at least 100,000 molecules of human somatostatin receptor 2 (SSTR2), which improves PET/CT imaging sensitivity. The present invention is also directed to transduced T cells expressing SSTR2 and chimeric antigen receptor (CAR). In one embodiment, the CAR is specific to human ICAM-1 and the CAR comprises a binding domain that is scFv of anti-human ICAM-1, or an I domain of the αL subunit of human lymphocyte function-associated antigen-1. In another embodiment, the CAR is specific to human CD19, and the CAR comprises a binding domain that is scFv of anti-human CD19. The present invention is further directed to using the above transduced T cells for monitoring T cell distribution in a patient by PET/CT imaging and/or treating cancer.

STRUCTURAL OPTIMIZATION METHOD TO IMPROVE THE THERANOSTIC PERFORMANCE OF PEPTIDE RECEPTOR-TARGETED RADIONUCLIDE THERAPY FOR CANCERS

The present invention provides in certain embodiments a carcinoma-targeting conjugate comprising Formula I wherein T is a SST2R targeting ligand, L is a linker, and X is a chelator, for the therapeutic treatment of cancer, and methods of use thereof.

MULTIFUNCTIONAL COMPOUNDS FOR USE IN MEDICAL IMAGING AND THERAPY
20230149569 · 2023-05-18 ·

The disclosure provides multifunctional compounds for use in medical imaging and therapy, the compounds comprising two or more of (i) a chelating ligand moiety (CL); (ii) an optical probe moiety (OP); and (iii) a biological targeting moiety (BT). The disclosure further provides related compositions and methods.

STABILIZED COMPOSITIONS OF RADIONUCLIDES AND USES THEREOF
20230144360 · 2023-05-11 ·

Provided herein are radiopharmaceutical compositions and uses thereof. The radiopharmaceutical compositions can comprise one or more stabilizing agents, an aqueous vehicle, and a conjugate that comprises a targeting ligand and a radionuclide bound to a metal chelator. The targeting ligand can be a small molecule compound or a peptide such as a monocyclic peptide. The targeting ligand can be configured to bind with a tumor target. The stabilizing agent can comprise a radiolysis stabilizer, a free metal chelator, and/or a pH stabilizer. Further provided herein are methods of preparing the radiopharmaceutical compositions and methods of treating cancer by administering the described radiopharmaceutical compositions.

Chelating AAZTA conjugates and complexes thereof

A chelating compound of formula (I) or a pharmaceutically acceptable salt thereof and its complexes with metals or radioisotopes thereof. The invention further relates to the preparation of such ligand and complexes as well as to their use as diagnostic or therapeutic agents. ##STR00001##

Composition Containing a Somatostatin Analogue for Radiopharmaceutical Use

The present invention relates to a somatostatin analogue composition for radiopharmaceutical use, in particular for diagnostic or therapeutic use. More specifically the somatostatin analogue is a receptor-selective somatostatin peptide antagonist.

PHARMACEUTICAL COMPOSITIONS AND RELATED METHODS OF DELIVERY

The pharmaceutical compositions described herein include a suspension which comprises an admixture in solid form of a therapeutically effective amount of a therapeutic agent and at least one salt of a medium chain fatty acid and a hydrophobic medium, e.g. castor oil or glyceryl tricaprylate or a mixture thereof. The pharmaceutical compositions described herein contain medium chain fatty acid salts and are substantially free of alcohols. The pharmaceutical compositions may be encapsulated in a capsule. Methods of treating or preventing diseases by administering such compositions to affected subjects are also disclosed.

[161Tb]-BASED RADIOPEPTIDES

A radiopeptide is provided which comprises (a) a radionuclide, wherein the radionuclide is terbium-161, (b) a chelator coordinating terbium-161, and (c) a peptide or peptide analogue, which is a somatostatin receptor (SSTR) antagonist. The radiopeptide is suitable for use in the treatment of tumor diseases.

SSTR-TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF

Conjugates of an active agent such as DM1 attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer.

PARA-AMINOHIPPURIC ACID (PAH) AS A RENAL PROTECTIVE SUBSTANCE
20220304964 · 2022-09-29 ·

The present application discloses para-aminohippuric acid (PAhI) or a pharmaceutically acceptable salt or carboxylic acid derivate thereof for use in a method for the reduction of nephrotoxic side effects of radiolabeled and non-radiolabeled therapeutic and diagnostic compounds in a subject. Also disclosed are pharmaceutical compositions comprising a radiolabeled and/or non-radiolabeled pharmaceutical compound and para-aminohippuric acid (PAH) or a pharmaceutically acceptable salt or carboxylic acid derivate thereof, and a pharmaceutically acceptable excipient, diluent, carrier or a combination thereof. Another subject of the present application is a method for the reduction of nephrotoxic side effects of radiolabeled and non-radiolabeled therapeutic and diagnostic compounds in a subject comprising administering to a subject para-aminohippuric acid (PAH) or a pharmaceutically acceptable salt or carboxylic acid derivate thereof in combination with a radiolabeled or non-radiolabeled therapeutic or diagnostic compound.