This disclosure provides anti-5T4 antibodies, variants thereof and humanized versions. The newly disclosed antibodies exhibited high affinity to the 5T4 protein and can be used to treat cancers.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
This disclosure provides anti-GPC3 antibodies, including murine antibodies, humanized antibodies, and those with further optimized CDR sequences. The newly disclosed antibodies exhibited higher cell-based binding efficiency than the leading anti-GPC3 antibody candidate under clinical development.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 5/027 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a gamma-amino acid is involved, e.g. statine
C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
Antibodies having highly selective specificity to the human CDH17 protein are identified that are useful for treating cancer. The antibodies can be used to prepare antibody-drug conjugates, which exhibit efficient in vitro and in vivo tumor cell killings.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
The present invention relates to a GPC3 antibody drug conjugate and a use thereof, and specifically provides an antibody drug conjugate, or a pharmaceutically acceptable salt, solvate, or solvate of the salt thereof. The antibody drug conjugate has a structure as shown in formula I, Ab being an anti-GPC3 antibody. The antibody drug conjugate has good tumor cell growth inhibition activity in vivo and in vitro, and has good application prospects.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
The present application relates to a 5T4 antibody-drug conjugate and a use thereof, and specifically provides an antibody-drug conjugate, or a pharmaceutically acceptable salt or solvate thereof or a solvate of the salt. The antibody-drug conjugate has a structure as shown in formula I, wherein Ab is an anti-5T4 antibody. The antibody-drug conjugate has good tumor cell growth inhibition activity both in vivo and in vitro, and has a good application prospect. Ab-(L-D)p Formula I
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
Provided are CD40 agonist antibodies which have greatly higher CD40 activation activity in the presence of concurrent tumor-associated antigen (TAA) binding than without such concurrent binding. Such TAA-dependent CD40 agonism results in greatly improved therapeutic index, reducing or totally eliminating adverse events commonly associated with CD40 activation, such as cytokine release syndrome or liver toxicity. Also provided are bi- and multi-specific antibodies and polypeptides, such as chimeric antigen receptors, that incorporate these antibodies, optionally with an anti-TAA unit. Methods of using the antibodies or polypeptides for treating and diagnosing diseases such as cancer are also provided.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
8.
LINKER DRUG, AND PREPARATION METHOD AND USE OF ANTIBODY-DRUG CONJUGATE THEREOF
A linker-drug conjugate, an antibody-drug conjugate, and a preparation method therefor and the use thereof. The linker-drug conjugate has a structure as shown in formula I, i.e., M-X-D (formula I), wherein M is a chemical structure comprising a maleimide (m) fragment or a cyclooctyne fragment, X is a linker fragment composed of 1-5 amino acids or derivatives thereof, and D is a cytotoxin. The linker-drug conjugate can release Payload by means of an enzymatic hydrolysis reaction in the case of removal of hydrophobic structure PAB, which can not only reduce the hydrophobicity of the Linker-Drug and reduce the content of a polymer produced in the preparation of ADC, but also can exhibit the corresponding cell killing activity.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07D 207/452 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
C07C 33/16 - Alcohols containing rings other than six-membered aromatic rings containing rings with more than six ring members
C07D 495/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
Provided are CD40 agonist antibodies which have greatly higher CD40 activation activity in the presence of concurrent tumor-associated antigen (TAA) binding than without such concurrent binding. Such TAA-dependent CD40 agonism results in greatly improved therapeutic index, reducing or totally eliminating adverse events commonly associated with CD40 activation, such as cytokine release syndrome or liver toxicity. Also provided are bi- and multi-specific antibodies and polypeptides, such as chimeric antigen receptors, that incorporate these antibodies, optionally with an anti-TAA unit. Methods of using the antibodies or polypeptides for treating and diagnosing diseases such as cancer are also provided.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
Provided are CD40 agonist antibodies which have greatly higher CD40 activation activity in the presence of concurrent tumor-associated antigen (TAA) binding than without such concurrent binding. Such TAA-dependent CD40 agonism results in greatly improved therapeutic index, reducing or totally eliminating adverse events commonly associated with CD40 activation, such as cytokine release syndrome or liver toxicity. Also provided are bi- and multi-specific antibodies and polypeptides, such as chimeric antigen receptors, that incorporate these antibodies, optionally with an anti-TAA unit. Methods of using the antibodies or polypeptides for treating and diagnosing diseases such as cancer are also provided.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Provided are antibody prodrugs that include an immunoglobulin superfamily constant region, such as CH3, or variant coupled to one or more chains of the antibody, optionally through a cleavable linker. It is discovered that the constant domain and variants serve as effective and safe masking moieties that inhibit the activity of the antibody. Once removed from the antibody, such as by a corresponding enzyme at a target treatment tissue, the antibody prodrug releases the active antibody. In tissues where no such enzyme is present, the antibody prodrug stays inactive, avoiding adverse effects in such tissues.
A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
12.
TREATMENT OF NASOPHARYNGEAL CARCINOMA BY USING ANTIBODY CONJUGATE TARGETING EGFR
The present invention relates to a treatment of nasopharyngeal carcinoma by using an antibody conjugate targeting EGFR. Specifically, it is found that antibody-drug conjugate MYK-3 administered at 2.3 mg/kg once every three weeks can effectively treat advanced EGFR-positive and HER2-negative gastric cancer, recurrent metastatic nasopharyngeal carcinoma, recurrent or metastatic head and neck squamous cell carcinoma, advanced EGFR-positive biliary tract adenocarcinoma, advanced EGFR-positive non-small cell lung cancer, and other cancers. Compared with a lower dose of 2.0 mg/kg, 2.3 mg/kg of MYK-3 in clinical use demonstrated a good tumor inhibitory or delaying effect in patients and controllable adverse effects, suggesting good safety.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
The present invention provides an antibody-drug conjugate and use thereof. The antibody-drug conjugate has a structure represented by formula I, namely Ab-(L-D)p, wherein Ab is an anti-GPC3 antibody, L is a linker, and D is a cytotoxin. The antibody-drug conjugate of the present invention has good activity in inhibiting tumor cell growth in vivo and in vitro, and has relatively low cytotoxicity.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
Provided are anti-CD47 antibodies and fragments thereof. The antibodies and fragments thereof specifically bind to the CD47 protein. Methods of using the antibodies or fragments thereof for treating and diagnosing diseases such as cancer and atherosclerosis are also provided.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
15.
BIFUNCTIONAL MOLECULES TARGETING PD-L1 AND TGF-BETA
Provided are anti-PD-L1 antibodies with superior activities in blocking the PD-1 and PD-L1 interactions. Also provided are multifunctional molecules that include the anti-PD-L1 antibodies or fragments thereof fused to an extracellular domain of human TGF-beta receptor type-2.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
Provided are anti-TIGIT antibodies and fragments thereof. The antibodies and fragments thereof specifically bind to the TIGIT protein. Methods of using the antibodies or fragments thereof for treating and diagnosing diseases such as cancer and viral infections are also provided.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
Provided are anti-CD47 antibodies and fragments thereof. The antibodies and fragments thereof specifically bind to the CD47 protein. Methods of using the antibodies or fragments thereof for treating and diagnosing diseases such as cancer and atherosclerosis are also provided.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
Provided are anti-PD-L1 antibodies with superior activities in blocking the PD-1 and PD-L1 interactions. Also provided are multifunctional molecules that include the anti-PD-L1 antibodies or fragments thereof fused to an extracellular domain of human TGF-beta receptor type-2.
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 14/71 - ReceptorsCell surface antigensCell surface determinants for growth factorsReceptorsCell surface antigensCell surface determinants for growth regulators
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 39/00 - Medicinal preparations containing antigens or antibodies
Provided are anti-TIGIT antibodies and fragments thereof. The antibodies and fragments thereof specifically bind to the TIGIT protein. Methods of using the antibodies or fragments thereof for treating and diagnosing diseases such as cancer and viral infections are also provided.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
Provided are anti-PD-L1 antibodies with superior activities in blocking the PD-1 and PD-L1 interactions. Also provided are multifunctional molecules that include the anti-PD-L1 antibodies or fragments thereof fused to an extracellular domain of human TGF-beta receptor type-2.
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 14/71 - ReceptorsCell surface antigensCell surface determinants for growth factorsReceptorsCell surface antigensCell surface determinants for growth regulators
Provided are anti-CD47 antibodies and fragments thereof. The antibodies and fragments thereof specifically bind to the CD47 protein. Methods of using the antibodies or fragments thereof for treating and diagnosing diseases such as cancer and atherosclerosis are also provided.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
Provided are anti-CD47 antibodies and fragments thereof. The antibodies and fragments thereof specifically bind to the CD47 protein. Methods of using the antibodies or fragments thereof for treating and diagnosing diseases such as cancer and atherosclerosis are also provided.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants