Abstract: Provided is a composition for cytotoxic T cell depletion, comprising an anti-LAG-3 antibody or a binding fragment thereof having the properties described in (i) to (iii) below: (1) having in vitro ADCC activity; (ii) reducing, in a low fucose form, the number of LAG-3 positive cells in vivo; and (iii) binding to activated human T cells. Also provided are methods for depleting cytotoxic T cells using the disclosed anti-LAG-3 antibody or binding fragment thereof.

Abstract: Provided are novel antibody-pyrrolodiazepine derivatives and novel antibody-pyrrolodiazepine derivative conjugates, as well as methods of using the same, and a novel CLDN6 and/or CLDN9 antibody. The disclosed compounds are of the class of alkyl benzene sulfonyl ureas, useful as oral anti-diabetics, and include substituted benzo[e]pyrrolo[1,2-?][1,4]diazepine.

Abstract: The present invention aims to provide a medicament capable of treating and/or preventing diseases associated with oxidative stress by inhibiting the protein-protein interaction between Keap1 and Nrf2 and activating Nrf2. The present invention relates to a compound represented by the following formula (1): wherein each symbol is as described in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. In addition, the present invention also relates to a medicament containing the aforementioned compound, for the prophylaxis and/or treatment of diseases involving oxidative stress selected from the group consisting of chronic kidney disease, non-alcoholic steatohepatitis, chronic obstructive pulmonary disease, radiation skin disorder, radiation mucosal disorder, cardiac failure, pulmonary arterial hypertension, Parkinson's disease, Friedreich's ataxia, multiple sclerosis, age-related macular degeneration, retinitis pigmentosa and glaucoma.

Abstract: To provide a method for obtaining a dealkoxyphenylation product with a high yield from a substrate such as a sugar bound to an alkoxyphenyl group through an oxygen atom. A dealkoxyphenylation product can be obtained with a high yield under mild conditions by reacting a substrate that is bound to a phenyl group substituted by C1 to C5 alkoxy at the para- or ortho-position through an oxygen atom with ?3-iodane in a fluorous alcohol and water.

Abstract: The present disclosure relates to the field of pharmaceutical preparations, dosage regimens, and administration of an antibody-drug conjugate (ADC). More specifically, the ADC is composed of an anti-cadherin-6 (CDH6) antibody connected via a linker to an anticancer agent, such as topoisomerase I inhibitor.

Abstract: Provided are novel antibody-pyrrolodiazepine derivative and novel antibody-pyrrolodiazepine derivative conjugates, as well as methods of using the same, and a novel CLDN6 and/or CLDN9 antibody. The disclosed compounds are of the class of alkyl benzene sulfonyl ureas, useful as oral anti-diabetics, and include substituted benzo[e]pyrrolo[1,2-?][1,4]diazepine.

Abstract: The present invention provides a low molecular compound that inhibits phosphatidylserine synthase 1 or a pharmaceutically acceptable salt thereof, a pharmaceutical containing thereof, and a therapeutic agent for cancer having a suppressed function of phosphatidylserine synthase 2. The compound represented by formula (1) or a pharmaceutically acceptable salt thereof, wherein R1, ring Q1, ring Q2, and W are as defined in the specification.

Abstract: A pharmaceutical product for administration of an anti TROP2 antibody-drug conjugate in combination with an ATR inhibitor is provided. The anti-TROP2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an anti-TROP2 antibody) is conjugated to an anti-TROP2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the anti-TROP2 antibody-drug conjugate and the ATR inhibitor are administered in combination to a subject: Formula (I).

Abstract: It is an object of the present invention to provide an antibody binding to CDH6 and having internalization activity, an antibody-drug conjugate of the antibody and a drug having antitumor activity, a pharmaceutical product comprising the antibody-drug conjugate and having therapeutic effects on a tumor, a method for treating a tumor using the antibody, the antibody-drug conjugate or the pharmaceutical product, and the like. The present invention provides an anti-CDH6 antibody having internalization activity, an antibody-drug conjugate of the antibody and a drug having antitumor activity, a pharmaceutical product comprising the antibody or the antibody-drug conjugate, and a method for treating a tumor.

Abstract: An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof. The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof. wherein the symbols in the formula are defined below: R1: e.g., a C1-C6 alkyl group; R2: a C1-C6 alkyl group; A: e.g., an oxygen atom; and R3: e.g., a C1-C6 alkyl group.

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

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.

Abstract: Disclosed are compositions and method related to variants of SPINK2 that bind to targets other than an endogenous target of SPINK2. In one embodiment, a peptide is provided that comprises the amino acid sequence SEQ ID NO: 1. In further embodiments, an amino acid sequences encoded by nucleotide positions 4 to 42 and/or nucleotide positions 94 to 189 in the nucleotide sequence of SEQ ID NO: 14 flank the amino terminus and the carboxyl terminus, respectively, of the amino acid sequence. In another embodiment, a peptide is provided that comprises an amino acid sequence derived from the amino acid sequence of SEQ ID NO: 1 in which a conservative substitution, deletion, 10 addition and/or insertion of 1 to 5 (inclusive) amino acids has occurred at amino acids other than the 1st X to the 12th X counting from the amino terminus.

Abstract: This invention provides a novel masked antibody. The masked antibody is a molecule that binds to a target antigen, which comprises a moiety binding to a target antigen, a first peptide recognizing a target antigen-binding site comprised in such moiety, and a second peptide comprising an amino acid sequence cleaved by a protease, wherein, after the second peptide is cleaved by a protease, the molecule has higher binding intensity to the target antigen, compared with that before it is cleaved.

Abstract: A pharmaceutical product for administration of an anti-TROP2 antibody-drug conjugate in combination with a PARP1 selective inhibitor is provided. The anti-TROP2 antibody-drug conjugate is an antibody-drug conjugate in which a drug-linker represented by the following formula (wherein A represents the connecting position to an anti-TROP2 antibody) is conjugated to an anti-TROP2 antibody via a thioether bond.

Abstract: The present invention provides a pharmaceutical composition in which valemetostat or a pharmaceutically acceptable salt thereof, particularly valemetostat tosylate, has excellent dissolution properties. It was found that excellent dissolution properties can be achieved by combining valemetostat or a pharmaceutically acceptable salt thereof with one or more of croscarmellose sodium and sodium starch glycolate.

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

Abstract: Provided are methods for producing a monoclonal antibody or a binding fragment thereof that binds to domain 3 of human LAG-3 and has one or more of the properties described in (ii) to (v), and the properties described in (i) and (vi) below: (i) having in vitro ADCC activity; (ii) reducing the number of LAG-3 positive cells in vivo in low fucose form; (iii) suppressing experimental autoimmune encephalomyelitis in vivo in low fucose form; (iv) binding to human activated T cells; (v) human LAG-3 binds to human major histocompatibility complex class II molecules in the presence of the antibody or the binding fragment thereof; and (vi) the presence of the antibody or the binding fragment thereof allowing human LAG-3 to exert human T cell suppression function.

Abstract: The present disclosure relates to the field of therapeutic methods for treating a cancer using an ADC. The present disclosure also relates to the field of pharmaceutical products comprising the ADC for treating a cancer. More specifically, the ADC is composed of an anti-cadherin-6 (CDH6) antibody connected via a linker to an anticancer agent, such as topoisomerase I inhibitor, and the cancer may be resistant to chemotherapy.

Abstract: Provided is a composition for cytotoxic T cell depletion, comprising an anti-LAG-3 antibody or a binding fragment thereof having the properties described in (i) to (iii) below: (i) having in vitro ADCC activity; (ii) reducing, in a low fucose form, the number of LAG-3 positive cells in vivo; and (iii) binding to activated human T cells. Also provided are methods for depleting cytotoxic T cells using the disclosed anti-LAG-3 antibody or binding fragment thereof.