1033 results about "Drug conjugation" patented technology

Provided is an antibody-drug conjugate for use in the treatment of cancer in which one or more KRAS mutants, particularly a KRAS G12V mutant, a KRAS G12D mutant, and a KRAS G12C mutant, are expressed. Also provided are a drug and a drug-linker conjugate for use in the antibody-drug conjugate.　The present inventors have produced an antibody-drug conjugate with which a heterocyclic compound represented by formula (II) and having an activity of inducing the decomposition of KRAS mutant proteins can be delivered to cancer in which EGFRs are expressed, the production being achieved by linking the compound to an anti-EGFR antibody. The present inventors have also discovered a drug-linker conjugate for use in the antibody-drug conjugate or a salt thereof. In cancer in which EGFRs are expressed, the antibody-drug conjugate induces the decomposition of one or more KRAS mutants, particularly a KRAS G12V mutant protein, a KRAS G12D mutant protein, and a KRAS G12C mutant protein, thereby inhibiting the KRAS mutants and exhibiting an anti-tumor effect.

Provided are an antibody-drug conjugate, a preparation method therefor, and use thereof. The antibody-drug conjugate has a structure represented by the formula Ab-[M-L-E-D]x, has a superior drug-to-antibody ratio, and has an excellent targeted killing effect on various cancers or tumors.

Provided are an antibody-drug conjugate and the use thereof, in particular an antibody-drug conjugate targeting B7H3. Also provided are an antibody targeting B7H3 and the use thereof.

Provided are a camptothecin compound, an antibody drug conjugate, and a preparation method therefor and the use thereof. Specifically provided is a camptothecin compound as represented by formula (K) or a pharmaceutically acceptable salt thereof. The provided camptothecin compound and the antibody drug conjugate thereof have a good cytotoxic activity and can inhibit the proliferation of tumor cells.

Provided are a ligand-drug conjugate represented by general formula Pc-(L-D)n or a pharmaceutically acceptable salt thereof, and further provided is a linker for conjugation represented by formula (L). The linker can efficiently and highly selectively perform chemical conjugation with a thiol group on cysteine, and the antibody-drug conjugate formed has good stability.

Provided are a bispecific antibody, a drug conjugate thereof, and a use thereof. The bispecific antibody comprises an EGFR binding domain and an HER3 binding domain. The provided bispecific antibody and the drug conjugate thereof have excellent endocytosis effects, proliferation inhibition activity and tumor growth inhibition activity, as well as good in vivo safety.

Linkers for linking a therapeutic agent to other moieties, such as an Fc region of an antibody. A linker having two or more maleimide functional groups, which may be subjected to a nucleophilic conjugate addition reaction. A method for increasing the duration of action of a therapeutic agent by linking a novel linker to the Fc region of an antibody. Antibody drug conjugates having a longer duration of action than the drug alone.

The invention relates to application of a combination of an anti-B7H3 antibody-drug conjugate and selulimab in preparation of a drug for treating cancer. The invention also relates to application of a pharmaceutical composition and a pharmaceutical kit comprising the combination in treatment of cancer.

The invention discloses a multi-active targeting tumor nano-drug with a multimode imaging function and an immune activation effect and a preparation method thereof, and belongs to the technical field of nano-drugs. The preparation method comprises the following steps: coupling inorganic metal-based nano particles / nano drugs with a multimode imaging function or / and targeting active organic biomolecules with specific functions and specific therapeutic drugs through a silane cross-linking agent or a combination of the silane cross-linking agent and a carbodiimide condensing agent; the active targeting type organic-inorganic composite nano-drug aggregate with a multi-mode imaging function and an immune activation effect is prepared. Wherein the inorganic component is a metal-based heterostructure nanoparticle with a multimode imaging function, and the organic component is a bioactive molecule or / and a specific therapeutic drug. The obtained nano-drug aggregate is stable in system, uniform and controllable in size and good in biocompatibility, and has specific targeting, such as specific targeting liver cancer cells.

The current disclosure provides binding polypeptides (e.g., antibodies), and effector moiety conjugates thereof (e.g., antibody-drug conjugates or ADCs), comprising a site-specifically engineered drug-glycan linkage within native or engineered glycans of the binding polypetpide. The current disclosure also provides nucleic acids encoding the antigen-binding polypeptides, recombinant expression vectors and host cells for making such antigen-binding polypeptides. Methods of using the antigen-binding polypeptides disclosed herein to treat disease are also provided.

The present disclosure provides antibodies specifically targeting CD142, antibody drug conjugates, preparation and uses thereof. An antibody, or antigen-binding fragment thereof, that binds to CD142 is covalently linked to a cytotoxic payload via a linker. Antibodies, or antigen-binding fragments thereof, and antibody drug conjugates that bind to CD142 exhibit a cytotoxic effect on tumor cells.

The present invention discloses a method for preparing a linker-drug conjugate and its intermediates. Specifically, a method for preparing compound LE14 is provided, which comprises subjecting an intermediate compound of formula II to an amide condensation reaction with a compound of formula III or its mesylate in the presence of a condensing agent, a base, and a solvent to obtain a compound of formula I. This method can produce a high-purity intermediate II, which is directly condensed with isotecan mesylate to obtain compound I, and then subjected to subsequent reactions to obtain the final product LE14. The preparation method of the present invention has one or more of the following advantages: using intermediate II as the starting material for the production process reduces process steps, facilitates product quality control, significantly reduces impurities in the final product, and improves purity. Furthermore, using the more economical isotecan for the condensation reaction significantly reduces production costs, making it more suitable for industrial production.

The present disclosure relates to treatment of tumors with an anti-HER2 antibody drug conjugate in combination with an anti-HER2 antibody. Specifically, the invention relates to an application of an antibody drug conjugate combined with an antigen binding protein combined with HER2 in preparation of drugs for treating tumors, and the structure of the antibody drug conjugate is as shown in formula (I). # imgabs0 #

Provided are a ligand-drug conjugate having a novel structure and a linker for conjugation. Specifically, provided are a ligand-drug conjugate having a structural general formula of Pc-(La-D)n or Pc-(Lb-D)n, a corresponding linker for conjugation, a pharmaceutical composition containing the conjugate, and a use of the conjugate as an anti-tumor drug.

Disclosed in the present invention are a monoclonal antibody against an interleukin-6 protein and the use thereof. The present invention provides a nucleic acid molecule, a vector, a cell, a composition, a product, a bispecific antibody, a CAR, an antibody-drug conjugate and a pharmaceutical composition comprising an anti-IL-6 monoclonal antibody or an antigen-binding fragment thereof; and further provides the use of the monoclonal antibody or the antigen-binding fragment thereof, the nucleic acid molecule, the vector, the cell, the composition and the product in the detection of IL-6 or a nucleic acid fragment encoding same, in the preparation of a product for detecting IL-6, in a pharmaceutical composition for preventing or treating diseases related to abnormal IL-6 expression, and in the preparation of a pharmaceutical composition for regulating the expression level or activity of IL-6.

Methods and apparatus for protein and drug design using multicapitate (“two or more headed”) neural networks, wherein one head, a sequence head, is trained to generate the sequence of a protein, and another head, a structure head, is trained to generate the structure of the protein; and wherein the neural network is configured to accept a representation of a specified condition as input, and output a representation of a protein's sequence and structure. The structure head and sequence head each have their own loss functions, and the weights of the neural network body are shared, and jointly updated during training. Non-limiting examples of specified input conditions include representations of associated proteins and / or sets of properties of the desired output protein. Some embodiments of the invention include for the design and synthesis of effective peptide drug ligands, synthetic biologic antibody drugs, antibody drug conjugates, and monoclonal antibody (mAb) drugs.

The invention discloses a triggering probiotic-drug conjugate and a preparation method and application thereof, and belongs to the technical field of oral drug delivery systems, the triggering probiotic-drug conjugate comprises probiotics, an adhesive inner layer formed by coordination of tannic acid and Fe < 3 + >, and an outer layer formed by pterostilbene-phospholipid bridged by ROS-responsive thioether bonds and cholesterol; the inner layer coats the surfaces of the probiotics through coordination, and the outer layer coats the outer part of the inner layer through self-assembly. An outer lipid layer is decomposed under high-concentration ROS in an inflammation colon area, and probiotics coated with pterostilbene and a tannic acid layer are released. Pterostilbene relieves inflammation and rebuilds a pathological microenvironment, and catechol groups in a tannic acid layer and the surface of the intestinal tract generate multiple interactions to promote planting of probiotics. In UC mouse models, the conjugates exhibit enhanced therapeutic effects by inhibiting inflammation, restoring intestinal barrier function, and improving intestinal microbiota homeostasis. The invention has important transformation potential in clinical application of gastrointestinal diseases.

The invention relates to an anti-LIV-1 antibody and a drug conjugate (ADC) thereof. The anti-LIV-1-antibody or the antigen binding fragment thereof comprises three light chain complementarity determining regions and / or three heavy chain complementarity determining regions of a specific amino acid sequence. Specifically, the invention also provides nucleic acid for coding the antibody or the antigen binding fragment thereof, a cell containing the nucleic acid, a pharmaceutical composition containing the antibody or the antigen binding fragment thereof, the nucleic acid and the cell, and application of the LIV-1 antibody or the antigen binding fragment thereof in prevention, treatment, detection or diagnosis of LIV-1 related diseases. The anti-LIV-1 antibody or the antigen binding fragment thereof provided by the invention has good affinity to LIV-1 and cells expressing LIV-1. The anti-LIV-1 antibody drug conjugate has a good tumor inhibition effect on an animal tumor transplantation model, and is small in side effect and toxicity and high in safety.

The present invention relates to antibodies and antibody-drug conjugates, and more particularly to antibodies and antibody-drug conjugates (ADCs) targeting TROP2 and / or NECTIN4 as well as compositions containing said antibodies or ADCs and therapeutic applications thereof.

The present disclosure relates to a ligand-drug conjugate of a novel structure or a pharmaceutically acceptable salt thereof. Specifically, the present disclosure provides a ligand-drug conjugate having a structural general formula represented by Pc-(L-D)n or a pharmaceutically acceptable salt thereof, a method for preparing same, a pharmaceutical composition comprising the conjugate, and use thereof in treating a tumor.

The invention relates to an antibody or an antibody fragment targeting TROP2, an antibody drug conjugate containing the antibody or the antibody fragment, and a preparation method and application of the antibody or the antibody fragment.

The invention relates to an antibody drug conjugate which is shown in a formula (I) and contains two or more bioactive molecules with different action mechanisms, a preparation method of the antibody drug conjugate, and application of the antibody drug conjugate in prevention and / or treatment of diseases related to abnormal cell activity, including but not limited to prevention and / or treatment of tumor diseases. # imgabs0 #

Provided are an antibody specifically binding to hEGFR or an antigen-binding fragment thereof, and a bispecific antibody, antibody-drug conjugate and pharmaceutical composition comprising the antibody. Further provided is the use of the antibody or the antigen-binding fragment thereof or the bispecific antibody.

The invention discloses an anti-receptor tyrosine kinase-like orphan receptor 1 antibody and a conjugate of the anti-receptor tyrosine kinase-like orphan receptor 1 antibody and a small molecule drug. Also disclosed is the use of the ligand-cytotoxic drug conjugate and a pharmaceutical composition comprising the same in the preparation of a medicament for the treatment of cancer.

The present disclosure relates to antibody-drug conjugates, and more particularly to antibody-drug conjugates (ADCs) loaded with inhibitors of Ras mutations as well as compositions containing the ADC molecules and therapeutic applications thereof.

Disclosed are drug conjugates comprising a targeting moiety conjugated to a drug molecule, wherein the targeting moiety binds to a cell adhesion moiety and / or receptor expressed on a Schwann cell to mediate targeted delivery of the drug conjugate to the Schwann cell, and wherein the drug molecule modifies expression or activity of a disease-associated molecule, and / or confers a cytotoxic effect, in the Schwann cell. Further disclosed herein are methods of targeted delivery of a drug to the Schwann cells.

Provided are an antibody-drug conjugate, a method for preparing same, and use thereof. The antibody-drug conjugate has a structure represented by formula Ab-[M-L-E-D] x, a superior drug-to-antibody ratio, and an excellent targeted killing effect on various cancers or tumors.

The present invention relates to an antibody or an antigen-binding fragment thereof binding to CLDN18.2, an antibody-drug conjugate comprising same, and a use of the antibody and the antibody-drug conjugate. An anti-CLDN18.2 monoclonal antibody according to the present invention comprises a fully human antibody sequence, thereby having low in vivo immunogenicity, and exhibits excellent antigen affinity and binding ability specific to a low expression to a high expression level of the CLDN18.2 protein. Thus, the antibody is expected to exhibit high specificity and safety as an antibody-based therapeutic agent such as in the form of a monoclonal antibody and / or an antigen-binding fragment (scFv), an antibody-drug conjugate (ADC), an immune cell engager, a chimeric antigen receptor (CAR), a multispecific antibody, and the like. In addition, the antibody according to the present invention may undergo cellular internalization, enables an anti-CLDN18.2 antibody-drug conjugate comprising said antibodies to be conveniently prepared, and has excellent yield and quality and thus is expected to be highly likely to be developed as a drug. A drug conjugate comprising the anti-CLDN18.2 antibody according to the present invention has excellent in vivo anticancer efficacy and has an expanded therapeutic index (TI) and thus is expected to be usefully employable for the treatment and / or prevention of cancer diseases expressing CLDN18.2 and related diseases.

Relates to a compound or a ligand-drug conjugate thereof, or an isomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof. The invention also relates to a preparation method and application of the compound or the ligand-drug conjugate thereof.

The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of membrane type 1 metalloprotease (MT1-MMP). The invention also describes drug conjugates comprising said peptides, conjugated to one or more effector and / or functional groups which have utility in imaging and targeted cancer therapy.