Abstract: An object of the present invention is to provide an antibody specifically binding to CDH6 and having a high internalization activity, an antibody-drug conjugate comprising the antibody and a high antitumor activity, a pharmaceutical product having the antibody-drug conjugate and having a therapeutic effect on a tumor, a method for treating a tumor using the antibody, the antibody-drug conjugate or the pharmaceutical product, and the like. According to the present invention, it is possible to provide an anti-CDH6 antibody prepared having internalization activity, an anti-CDH6 antibody-drug conjugate prepared by connecting the anti-CDH6 antibody and a novel PBD derivative and exhibiting high anti-tumor activity, a pharmaceutical product and a therapeutic method for treating tumors using these.

Abstract: Desired is development of novel CDN derivatives having STING agonist activity; and a therapeutic agents and/or therapeutic methods using the novel CDN derivatives for diseases associated with STING agonist activity. Further desired is development of a therapeutic agents and/or therapeutic methods capable of delivering the novel CDN derivatives specifically to targeted cells and organs for diseases associated with STING agonist activity. The present invention provides novel CDN derivatives having potent STING agonist activity, and antibody-CDN derivative conjugates including the novel CDN derivatives.

Abstract: The present invention relates to an antibody that binds to GARP and is useful as a therapeutic agent for a tumor, and a method for treating a tumor using the aforementioned antibody. It is an object of the present invention to provide an antibody, which inhibits the function of Treg in a tumor and is thereby used as a pharmaceutical product having therapeutic effects, a method for treating a tumor using the aforementioned antibody, and the like. An anti-GARP antibody that binds to GARP and exhibits inhibitory activity to Treg function and exhibits ADCC activity is obtained, and moreover a pharmaceutical composition for use in tumor therapy, comprising the aforementioned antibody, etc. is obtained.

Abstract: A method for improving blood kinetics of a peptide is provided. The method for improving blood kinetics of a peptide includes a step of preparing a peptide having a modified amino acid sequence.

Abstract: The present disclosure provides novel compounds or salts thereof, or crystals of the compounds or the salts, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl.

Abstract: A novel peptide which comprises an amino acid sequence represented by SEQ ID NO: 23, and specifically inhibits the protease activity of a target molecule.

Abstract: The present invention provides a novel endo-?-N-acetylglucosaminidase that is isolated from a fungus belonging to the genus Rhizomucor and is active under high-temperature conditions; various mutant enzymes thereof; genes encoding the enzymes; a recombinant plasmid; a transformant transformed with the plasmid; and the like.

Abstract: An object of the present invention is to provide a combination drug having an EZH1/2 dual inhibitor in combination with another medical agent and exerting an excellent anticancer effect. Provided is a combination drug having an EZH1/2 dual inhibitor in combination with another medical agent and exerting an excellent anticancer effect.

Abstract: A method for producing an antibody-drug conjugate composition, comprising: (i) a step of reacting an antibody with a reducing agent in a buffer to reduce interchain disulfides, and (ii) a step of reacting drug linker intermediates with the antibody having thiol groups obtained in the step (i), wherein the reaction temperature in the step (i) is ?10° C. to 10° C., and the average number of bound drugs in the produced antibody-drug conjugate composition is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, in the produced antibody-drug conjugate composition is 50% or more; and an antibody-drug conjugate composition, wherein the content of antibody-drug conjugates wherein the average number of bound drugs is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, is 50% or more.

Abstract: As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the formula: L1-L2-LP-NH—(CH2)n1-La-Lb-Lc or -L1-L2-LP- wherein the anti-HER2 antibody is connected to the terminal L1, and the antitumor compound is connected to the terminal Lc or LP with the nitrogen atom of the amino group at position 1 as the connecting position.

Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the following formula (I): wherein X1 represents a nitrogen atom or CR9, R1 represents a hydrogen atom, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a halogen atom, R3 represents a hydrogen atom or a halogen atom, R4 represents a hydrogen atom or a halogen atom, and R5 represents a C1-C3 alkylsulfonyl group, a substituted C1-C6 alkyl group, a substituted C1-C6 haloalkyl group, a substituted C1-C6 alkoxy group, or a substituted C1-C6 alkylamino group, or a pharmacologically acceptable salt thereof.

Abstract: A method for producing an antibody-drug conjugate composition, comprising: (i) a step of reacting an antibody with a reducing agent in a buffer to reduce interchain disulfides, and (ii) a step of reacting drug linker intermediates with the antibody having thiol groups obtained in the step (i), wherein the reaction temperature in the step (i) is ?10° C. to 10° C., and the average number of bound drugs in the produced antibody-drug conjugate composition is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, in the produced antibody-drug conjugate composition is 50% or more; and an antibody-drug conjugate composition, wherein the content of antibody-drug conjugates wherein the average number of bound drugs is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, is 50% or more.

Abstract: To provide a novel pharmaceutical use of a peptide. A pharmaceutical composition for the treatment or prevention of retinitis pigmentosa, comprising a peptide which comprises the amino acid sequence shown in SEQ ID NO: 30 and inhibits the protease activity.

Abstract: SPINK2 mutant peptide conjugates are provided that inhibit KLK5. The KLK5 inhibitory peptide conjugates are Fc fusion peptides in which, in certain embodiments, the Fc region of the fusion peptides are the Fc region of human IgG1 or a fragment thereof. The KLK5 inhibitory peptide conjugates include an amino acid sequence of one of SEQ ID NOs: 34, 36, 38, 40, 42, 44, 46, 48, 96, 50, 52, 54, 56, 58, or 60. Pharmaceutical compositions that include the KLK5 inhibitory peptide conjugates useful for treating KLK5-related diseases are also provided.

Abstract: A method for identifying a subject suffering from a cancer, comprising: obtaining a biological sample from the human patient diagnosed as suffering from a cancer; evaluating an amount of expression of the hTROP2 gene at mRNA level in the biological sample; evaluating an amount of expression of the SLFN11 gene at mRNA level in the biological sample, wherein the biological sample is one that is determined to have a high amount of expression of the hTROP2 gene; and identifying the human patient who provided the biological sample, wherein the biological sample is one that is determined to have a high amount of expression of the SLFN11 gene, as a subject to whom a medicament containing an anti-hTROP2 antibody is to be given.

Abstract: The present invention provides a pharmaceutical composition comprising an antibody which binds specifically to human TLR7 or monkey TLR7 and does not bind to mouse TLR7 or rat TLR7, and has an activity of inhibiting a function of human TLR7 or monkey TLR7, and the like.

Abstract: Provided is a compound that can promote angiogenesis by inhibiting the function of TSP1, and is useful for the treatment or prophylaxis of diseases such as critical limb ischemia.

Abstract: The present invention provides an approach to enhancing the production of a foreign protein serving as a protein-based pharmaceutical product in host cells such as cultured cells derived from a mammal. The present invention provides transfected cells having a novel Hspa8 gene promoter, and a method for secreting and producing a foreign protein at high levels using the transfected cells.

Abstract: A pharmaceutical composition, wherein an antibody-drug conjugate in which a drug-linker represented by the following formula (wherein A represents a connecting position to an antibody) is conjugated to the antibody via a thioether bond, and a tubulin inhibitor are administered in combination, and a method of treatment, wherein the antibody-drug conjugate and the tubulin inhibitor are administered in combination to a subject.

Abstract: A therapeutic agent for a metastatic brain tumor comprising, as an active component, an antibody-drug conjugate in which a drug-linker represented by the following formula (wherein A represents a connecting position to an antibody) is conjugated to the antibody via a thioether bond and/or a method of treatment for a metastatic brain tumor, comprising administering the antibody-drug conjugate to a subject in need of the treatment for a metastatic brain tumor.