The present invention relates to combinations of at least two components, component A and component B, component A being an inhibitor of PI3K kinase, and component B being a targeted thorium conjugate. Another aspect of the present invention relates to the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of breast and prostate cancer.

The present invention relates to combinations of at least two components, component A and component B, component A being an inhibitor of PI3K kinase, and component B being a targeted thorium conjugate. Another aspect of the present invention relates to the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of breast and prostate cancer.

The present invention relates to a labeling technique which can facilitate the metabolism in the liver after administration to patients without the reduction in the antibody function, thereby reducing accumulation of radionuclides in an organ such as the liver, and provides a modified antibody containing an IgG antibody and an IgG-binding peptide bound to the IgG antibody. The IgG-binding peptide has an amino acid sequence consisting of 13 to 17 amino acid residues, such as GPDCAYH(Xaa1)GELVWCTFH wherein Xaa1 represents a lysine residue, a cysteine residue, an aspartic acid residue, a glutamic acid residue, 2-aminosuberic acid, or diaminopropionic acid, and a compound represented by the following formula (II-1) is linked at a position of the lysine residue via a modification linker to the N terminus of the IgG-binding peptide.

##STR00001##

A system and method for automatic production of astatine-211 labeled molecules is described. The invention represents a significant advantage in the preparation of At-211 radiopharmaceuticals including better reproducibility, reduced production time and increased radiation safety. The invention also enables routine automatic synthesis of radiopharmaceuticals in a clinical setting, in conjunction or at short distance from a cyclotron unit capable of producing the radionuclide.

The invention provides a method for the purification of complexed .sup.227Th from a mixture comprising complexed .sup.227Th and .sup.223Ra (complexed or in solution), said method comprising: i) preparing a first solution comprising a mixture of complexed .sup.227Th ions and .sup.223Ra ions in a first aqueous buffer; ii) loading said first solution onto a separation material; iii) eluting complexed .sup.227Th from said separation material whereby to generate a second solution comprising complexed .sup.227Th; iv) Optionally rinsing said separation material using a first aqueous washing medium;

The invention additionally provides a purified .sup.227Th solution, a pharmaceutical product and its use in treatment of disease such as cancer and a kit for generation of such a product.

Antibody drug conjugates (ADC's) comprising a drug conjugated to antibody or antigen binding fragments thereof that bind to Globo series antigen disclosed herein, as well as methods of use thereof. Methods of use include, without limitation, cancer therapies and diagnostics. The antibodies of the disclosure can bind to certain cancer cell surfaces. Exemplary targets of the antibodies disclosed herein can include carcinomas, such as sarcoma, skin cancer, leukemia, lymphoma, brain cancer, glioblastoma, lung cancer, breast cancer, oral cancer, head-and-neck cancer, nasopharyngeal cancer, esophagus cancer, stomach cancer, liver cancer, bile duct cancer, gallbladder cancer, bladder cancer, pancreatic cancer, intestinal cancer, colorectal cancer, kidney cancer, cervix cancer, endometrial cancer, ovarian cancer, testical cancer, buccal cancer, oropharyngeal cancer, laryngeal cancer and prostate cancer.

Antibody drug conjugates (ADC's) comprising a drug conjugated to antibody or antigen binding fragments thereof that bind to Globo series antigen disclosed herein, as well as methods of use thereof. Methods of use include, without limitation, cancer therapies and diagnostics. The antibodies of the disclosure can bind to certain cancer cell surfaces. Exemplary targets of the antibodies disclosed herein can include carcinomas, such as sarcoma, skin cancer, leukemia, lymphoma, brain cancer, glioblastoma, lung cancer, breast cancer, oral cancer, head-and-neck cancer, nasopharyngeal cancer, esophagus cancer, stomach cancer, liver cancer, bile duct cancer, gallbladder cancer, bladder cancer, pancreatic cancer, intestinal cancer, colorectal cancer, kidney cancer, cervix cancer, endometrial cancer, ovarian cancer, testical cancer, buccal cancer, oropharyngeal cancer, laryngeal cancer and prostate cancer.

The present disclosure relates to the delivery of active agents, e.g., drug substances, using as carriers for their delivery biocompatible copolymers comprising side chain-linked amino acids having active agents bound to their alpha-amino and/or alpha-carboxyl groups, either directly or via linker molecules. The active agent-containing copolymers can be functionalized to contain cell type- or tissue type-specific targeting moieties.

The present technology provides compounds as well as compositions including such compounds useful for the treatment of cancers where the compounds are represented by the following formula (I) or a pharmaceutically acceptable salt thereof, wherein M is an alpha-emitting radionuclide.

##STR00001##

A system and method for automatic production of astatine-211 labeled molecules is described. The invention represents a significant advantage in the preparation of At-211 radiopharmaceuticals including better reproducibility, reduced production time and increased radiation safety. The invention also enables routine automatic synthesis of radiopharmaceuticals in a clinical setting, in conjunction or at short distance from a cyclotron unit capable of producing the radionuclide.