Borylated Amino Acid compositions comprising tyrosine derivatives BTS and BTS(OMe) and novel methods of making BTS and BTS(OMe) are disclosed herein. Consequently, the BTS and/or BTS(OMe) can be scaled up to commercial scale and administered to patients as a Neutron Capture Agent and provide a method of treating cancer, immunological disorders, and other disease by utilizing a Neutron Capture Therapy modality.

The present invention relates to compositions and methods for imaging and treating various diseases and disorders, including cancers. The composition of the invention can include a plurality of biodegradable micro-beads, each embedding a plurality of nano-beads, further including a polymer, a radionuclide, a radionuclide chelator, a radioligand, a chemotherapeutic agent, and a cell-penetrating peptide. Upon injection into a blood vessel supplying a cancer tumor, the micro-beads lodge into the tumor and degrade, releasing the nano-beads with a therapeutic or diagnostic agent. The compositions and methods of the invention provide a more homogeneous and deeper distribution of radiation or chemotherapeutic agents throughout the target tumor. The micro-beads provide a local, sustained, and controlled delivery nano-beads including therapeutic or diagnostic agents.

An environmentally sensitive membrane binding polypeptide, pH (low)-sensitive membrane peptide (pHLIP) has improved insertion kinetics balanced with solubility to selectively target acidic tissues.

A neutron capture therapy system and a target for a particle beam generating device, which may improve the heat dissipation performance of the target, reduce blistering and extend the service life of the target. The neutron capture therapy system includes a neutron generating device and a beam shaping assembly. The neutron generating device includes an accelerator and a target, and a charged particle beam generated by acceleration of the accelerator interacts with the target to generate a neutron beam. The target includes an acting layer, a backing layer and a heat dissipating layer, the acting layer interacts with the charged particle beam to generate the neutron beam, the base layer supports the action layer, and the heat dissipating layer includes a tubular member composed of tubes arranged side by side.

Boron Enriched Linker (“BEL”) compositions and methods of making BELs are disclosed herein. Consequently, the BELs can be conjugated to antibodies or antibody fragments to create Antibody Boron Conjugates (“ABCs”) to provide a method of treating cancer, immunological disorders and other disease by utilizing a Neutron Capture Therapy modality.

A method for preparing a lyophilized preparation of BPA includes a solution preparation process and a freeze-drying process, where the solution preparation process includes: (1) dissolving BPA and polyol in an aqueous solution by using a base to obtain a clear solution; (2) regulating the clear solution back to 7.5<pH≤8.5 by using an acid, to obtain a BPA solution; and the freeze-drying process includes: (3) subpackaging the BPA solution and freeze-drying under a condition with a vacuum of 10-20 Pa, to obtain the lyophilized preparation. The lyophilized preparation of BPA prepared through the method has good stability and a small content of impurities.

The present invention relates to a boron carrying agent for integrated tumor diagnosis and treatment, and a preparation method therefor and use thereof. Provided is a compound represented by formula I: wherein an R group is hydrogen or alkyl. A boron atom connected to the benzene ring may be 10B or natural boron, and at least one fluorine atom in —BF 3- is radiolabeled. The present invention generally relates to the fields of radiopharmaceuticals and nuclear medicine. The compound in the present invention can be used for a drug for integrated diagnosis and treatment in tumor diagnosis and BNCT treatment, and by means of the same chemical structure, a reliable distribution result of a drug in vivo is provided.

Borylated Amino Acid (“BAA”) compositions and methods of making BAAs are disclosed herein. Consequently, the BAAs can be administered to patients as a Neutron Capture Agent and provide a method of treating cancer, immunological disorders and other disease by utilizing a Neutron Capture Therapy modality.

Borylated Di-Peptide Amino Acid (“Bdi-AA”) compositions and Di-Peptide Amino Acid (di-AA) compositions and methods of making Bdi-AAs and di-AAs are disclosed herein. Consequently, the Bdi-AAs and di-AAs can be administered to patients as a Neutron Capture Agent and provide a method of treating cancer, immunological disorders, and other disease by utilizing a Neutron Capture Therapy modality.

An object of the present invention is to provide an injection solution for boron neutron capture therapy. Provided is an injection solution for boron neutron capture therapy, containing p-boronophenylalanine or a pharmaceutically acceptable salt thereof, with a ratio of boron 10 of boron atoms in a compound of 75% or more; a sugar alcohol; an antioxidant; and water, the injection solution having a pH of 6.5 to 7.8 and an osmotic pressure ratio of 1.0 to 1.8, the injection solution being to be administered by intravenous drip injection.