Abstract: The present invention provides an antigen-binding molecule (e.g. antibody) with improved cytosol-penetrating ability, the molecule comprising an amino acid substitutions on at least one selected from the group consisting of CDRL1, CDRL2 and CDRL3 in a light-chain variable region, or an antigen-binding fragment (antibody fragment) thereof; and pharmaceutical compositions comprising the antigen-binding molecule; methods for delivering the antigen-binding molecule specifically into the cytosol of a target cell; methods of removing, suppressing, or activating a cytosolic antigen in a target cell-specific manner by using the antigen-binding molecule; and pharmaceutical compositions for diagnosing, preventing, or treating a disease in a subject comprising the antigen-binding molecule.

Abstract: An objective of the present disclosure is to provide anti-CD137 antigen-binding molecules which have immunocyte-activating effect, cytotoxic activity, or anti-tumor activity, and meanwhile have reduced effect on non-tumor tissues such as normal tissues and produce less side effects, and methods of using the same. Anti-CD137 antigen-binding molecules which have immunocyte-activating effect, cytotoxic activity, or anti-tumor activity, and meanwhile have reduced effect on non-tumor tissues such as normal tissues and produce less side effects, are provided by discovering and producing CD137 antigen-binding molecules whose binding activity to CD137 depends on various substances (for example, small molecule compounds) in target tissues. Methods of using the same, pharmaceutical formulations, and such are also provided. The present disclosure also provides an antigen-binding molecule whose binding activity to an antigen varies depending on a small molecule compound, a preparation method thereof, and uses thereof.

Abstract: The invention relates to cytosol penetrating antigen binding molecules containing cell surface antigen binding domains, cytosolic antigen binding domains and cytosol penetrating domains; pharmaceutical compositions comprising said antigen binding molecules; methods of delivering said antigen binding molecules specifically into cytosols of target cells; methods of depleting, suppressing or activating cytosolic antigens specifically in target cells by using said antigen binding molecules; and pharmaceutical compositions for preventing or treating diseases in patients comprising said antigen binding molecules. The invention also relates to cytosol penetrating antigen binding molecules containing cytosol penetrating domains and Fc regions, wherein the Fc regions comprising one or more amino acid modifications that enhance multimerization of said cytosol penetrating antigen binding molecules.

Abstract: In one embodiment, a multispecific antigen-binding molecule that recognizes an antigen on an antigen-presenting cell and an antigen on a target cell, which is capable of crosslinking the antigen-presenting cell and the target cell, is provided.

Abstract: In a non-limiting embodiment, the present invention relates to antigen-binding molecules containing an altered TRIM21-binding domain and having an altered cytosolic half-life; pharmaceutical compositions containing such an antigen-binding molecule; methods for using such an antigen-binding molecule; methods for increasing or decreasing the cytosolic half-life of an antigen-binding molecule containing a TRIM21-binding domain; and methods for producing an antigen-binding molecule containing an altered TRIM21-binding domain and having an increased or decreased cytosolic half-life. The present invention also relates to substitutions at specific positions in a TRIM21-binding domain that increase or decrease the cytosolic half-life of an antigen-binding molecule containing a TRIM21-binding domain.

Abstract: The present invention relates to a first antigen-binding molecule, a second antigen-binding molecule, and a combination thereof. The second antigen-binding molecule binds to an antigen/antigen-binding molecule complex containing a first antigen and the first antigen-binding molecule, and enhances the binding activity of the first antigen-binding molecule to the first antigen.