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.

The present invention is related to a compound comprising a cyclic peptide

of formula (I)

##STR00001##

and an N-terminal modification group A attached to Xaa1,
wherein
each and any one of Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6 and Xaa7 is a residue of an amino acid, and
Yc is a structure of formula (X)

##STR00002##

Shielding enzymes are made by modifying the enzyme surface with silica precursors and then depositing silica to a desired thickness while retaining biological activity of the enzyme.

The present disclosure relates to imaging and endoradiotherapy of diseases involving chemokine receptor 4 (CXCR4). Provided are compounds which bind or inhibit CXCR4 and furthermore carry at least one moiety which is amenable to labeling. Provided are also medical uses of such compounds.

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.

Disclosed is the use of a radiolabeled anti-nanobody in the prognosis and diagnosis of cancers. In particular, disclosed is an immunoconjugate for detecting a PD-L1 molecule. The immunoconjugate comprises the VHH chain of a specific anti-PD-L1 nanobody and a radionuclide, and can be used for non-invasive detecting of expression of the object PD-L1 to be detected. The immunoconjugate of the invention has small size and high specificity, and is suitable for systemic detection which simultaneously targets primary and metastatic tumors, and has high accuracy and low radiation dose.

An isolated cancer-targeting peptide that includes at least two copies of the amino acid sequence PFLP (SEQ ID NO: 1) or PFLF (SEQ ID NO: 2). Also disclosed is a pharmaceutical composition for treating cancer. The composition contains the isolated cancer-targeting peptide and an anti-cancer agent. Further disclosed is a bispecific anti-cancer antibody that includes the isolated cancer-targeting peptide and an antigen-binding peptide that stimulates T cell activity. Methods are provided for treating cancer by administering the pharmaceutical composition or the bispecific anti-cancer antibody. Further provided is a method for diagnosing cancer by administering a radionuclide-labeled cancer-targeting peptide to an individual and imaging a location of the radionuclide.

An isolated cancer-targeting peptide that includes at least two copies of the amino acid sequence PFLP (SEQ ID NO: 1) or PFLF (SEQ ID NO: 2). Also disclosed is a pharmaceutical composition for treating cancer. The composition contains the isolated cancer-targeting peptide and an anti-cancer agent. Further disclosed is a bispecific anti-cancer antibody that includes the isolated cancer-targeting peptide and an antigen-binding peptide that stimulates T cell activity. Methods are provided for treating cancer by administering the pharmaceutical composition or the bispecific anti-cancer antibody. Further provided is a method for diagnosing cancer by administering a radionuclide-labeled cancer-targeting peptide to an individual and imaging a location of the radionuclide.

The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A.sup.1 represents a chelate group; R.sup.1 represents a hydrogen atom or the like; R.sup.2 represents a hydrogen atom or the like; and Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4, and Z.sup.5 are the same or different and each represent a nitrogen atom or CR.sup.3 or the like wherein R.sup.3 represents a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group or the like; L.sup.1 represents a group represented by the formula (3) wherein R.sup.13, R.sup.14, R.sup.15, and R.sup.16 are the same or different and each represent a hydrogen atom or the like; L.sup.2 represents an optionally substituted C.sub.1-6 alkylene group; and L.sup.3 represents as optionally substituted C.sub.1-6 alkylene group.

##STR00001##

A conjugate for treating an individual suffering from a disease, wherein the conjugate is comprised of: a targeting peptide comprising a sequence substantially identical to CAR, or a variant thereof; and at least one therapeutic molecule and methods for making and administering same. Also disclosed is a combination product for use in the treatment of a disease, wherein the combination product comprises: (a) a targeting peptide comprising a sequence substantially identical to CAR, or a variant thereof; (b) a liposome, wherein the targeting peptide is encapsulated within the liposome; and (c) an effective amount of an anti-inflammatory agent and methods for making and administering same.