Abstract: An antibody targeting human Trop2 simultaneously is coupled to a camptothecin drug to form an antibody-drug conjugate with stable treatment and excellent uniformity, and the drug-to-antibody ratio (DAR) is 6.0-8.0. The antibody-drug conjugate has a structure shown in general formula I, wherein Ab refers to an antibody targeting Trop simultaneously, which is coupled to a linker-camptothecin drug. In addition, also disclosed are a preparation and purification method for the antibody-drug conjugate, and an application in tumor treatment. Further, also disclosed is a linker-drug compound that can be coupled to Ab to form an antibody-drug conjugate.

Abstract: A bispecific antibody simultaneously targeting two different epitopes or targets is coupled with a camptothecin drug to form a bispecific antibody-toxin conjugate that is stable in treatment and excellent in uniformity, and a drug-to-antibody ratio (DAR) thereof is 6.0-8.0. The antibody-toxin conjugate has a structure as represented by general formula (I), wherein Ab represents the bispecific antibody simultaneously targeting two different epitopes or targets, which is coupled with a linker-camptothecin drug. In addition, the present invention further relates to a preparation and purification method for the antibody-toxin conjugate, and an application thereof in tumor treatment. Furthermore, the present invention further relates to a linker-drug compound capable of being coupled with Ab to form the antibody-toxin conjugate.

Abstract: A bispecific antibody simultaneously targeting two different epitopes or targets is coupled with a camptothecin drug to form a bispecific antibody-toxin conjugate that is stable in treatment and excellent in uniformity, and a drug-to-antibody ratio (DAR) thereof is 6.0-8.0. The antibody-toxin conjugate has a structure as represented by general formula (I), wherein Ab represents the bispecific antibody simultaneously targeting two different epitopes or targets, which is coupled with a linker-camptothecin drug. In addition, the present invention further relates to a preparation and purification method for the antibody-toxin conjugate, and an application thereof in tumor treatment. Furthermore, the present invention further relates to a linker-drug compound capable of being coupled with Ab to form the antibody-toxin conjugate.

Abstract: The invention discloses a deuterated camptothecin derivative and its antibody-drug conjugate (ADC), and combines the deuteration technology with camptothecin ADC to discover improved deuterated camptothecin ADC drug, so that it has higher safety and efficacy and can better meet the clinical challenge.

Abstract: A camptothecin drug having a highly stable hydrophilic connecting unit and its conjugate, or its pharmaceutically acceptable salt thereof, including methods for preparation thereof, and its applications in preventing and/or treating cancer. The conjugate can specifically bind to receptors highly expressed in tumor cells. The conjugates have excellent water solubility, stability, and homogeneity, and can be used for preventing and/or treating tumors and/or other diseases.

Abstract: An antitumor pharmaceutical camptothecin derivative and an antibody-drug conjugate thereof. By means of a series of molecular structure modifications, an optimal camptothecin antitumor drug is obtained, so as to be more suitable as a drug for antibody conjugation.

Abstract: The present application discloses a camptothecin drug and its antibody conjugate. Based on a comprehensive understanding of ADC drugs, the inventor designed a series of active anti-tumor exatecan-derivatives. The designed anti-tumor molecular compound showed good anti-tumor activity in the experiment.

Abstract: By inserting cysteine (C) into a heavy chain and/or a light chain of a target antibody at specific insertion site, and performing a site-specific conjugation through a free thiol group (—SH) from the site-specific inserted cysteine and a linker conjugated with a highly potent small molecule cytotoxin, a cysteine modified antibody-drug conjugate with good homogeneity is provided. The specific insertion sites of cysteine are position 205 and/or position 206 (Kabat numbering scheme) of the light chain of the antibody, and/or position 439 (Kabat numbering scheme) of the heavy chain.

Abstract: Disclosed in the present invention is a cysteine-modified antibody-toxin conjugate. The cysteine-modified antibody-toxin conjugate is characterized in that: the antibody is an antibody in which cysteine is inserted on a fixed point, and insertion sites of the cysteine comprising one or more of the following sites: a 110th site, a IIIth site and a 142th site of a light chain in a Kappa/?L light chain constant region, and a 254th site, a 255th site, a 258th, a 259th site, a 354th site, a 355th site, a 357th site, a 378th site, a 379th site, a 386th site, a 387th site or a 410th site of a heavy chain of a heavy chain constant region of an IgG antibody.

Abstract: A bicyclic octapeptide derivative is conjugated to a corresponding target-binding group by a special chemical structure. The structure of the derivative is stable in blood plasma and decomposes into a drug as an active ingredient in a specific biological environment, thereby maximizing killing effect on target cells and minimizing toxic side effects on non-target cells. The derivative can be used in the treatment of various malignant tumors.

Abstract: The present invention provides a special drug conjugate having a hydrophilic acidic stabilization junction. Compared with a conjugate having a lower drug loading, due to the introduction of the acidic stabilization junction, the conjugate in the present invention can also have a higher drug loading (that is, each targeted reagent has more hydrophilic drug junctions), keeps a desired PK property and has a same or better activity in a body.

Abstract: By inserting cysteine (C) into a heavy chain and/or a light chain of a target antibody at specific insertion site, and performing a site-specific conjugation through a free thiol group (—SH) from the site-specific inserted cysteine and a linker conjugated with a highly potent small molecule cytotoxin, a cysteine modified antibody-drug conjugate with good homogeneity is provided.