A61K47/6855

ANTI-TUMOR COMPOUND AND PREPARATION METHOD AND USE THEREOF

The present application relates to an anti-tumor compound and a preparation method and use thereof, and in particular to a compound or a tautomer, a mesomer, a racemate, an enantiomer or a diastereoisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof.

Endolysosomal targeting conjugates for improved delivery of cargo molecules to the endolysosomal compartment of target cells

Endolysosomal targeting conjugates that are engineered to deliver cargo molecules such as cytotoxic drugs or imaging labels with improved efficiency to late endosomes and/or lysosomes in target cells such as tumor cells are described. The endolysosomal targeting conjugate includes a targeting component and a cargo component. The targeting component is configured to bind to a cell surface molecule of a target cell and the cargo component includes a cargo molecule. The targeting component and the cargo component may be fused by a covalent bond or associated by a non-covalent bond. The targeting component may bind to the cell surface molecule or the cargo component with higher affinity in the extracellular space than in an endolysosomal compartment of the target cell.

Thailanstatin analogs

The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.

CAMPTOTHECIN DERIVATIVE AND CONJUGATE THEREOF
20220411436 · 2022-12-29 ·

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.

COMBINATION MCL-1 INHIBITORS WITH ANTI-BODY DRUG CONJUGATES

The present disclosure generally relates to methods of treating cancer by administering an MCL-1 inhibitor and an antibody-drug conjugate.

Polymer linkers and their uses
11529422 · 2022-12-20 · ·

Provided herein are poly-1-hydroxymethylethylene hydroxymethyl formal (PHF)-based drug delivery systems. Also disclosed are methods of making antibody-drug conjugates and methods of treatment using these conjugates.

METHODS OF TREATING CANCER

Methods of treating cancer with a combination of a WEE1 inhibitor and a DNA-damaging agent in patients having SLFN11-deficient cancer cells are disclosed herein.

METHODS OF TREATING HER2 POSITIVE BREAST CANCER WITH TUCATINIB IN COMBINATION WITH AN ANTI-HER2 ANTIBODY-DRUG CONJUGATE
20220387618 · 2022-12-08 ·

The present disclosure relates to a method for treating or ameliorating the effects of a HER2 positive breast cancer in a subject by administration of a combination of tucatinib and an anti-HER2 antibody-drug conjugate (e.g., ado-trastuzumab emtansine or trastuzumab deruxtecan). In some embodiments, the methods provided herein are useful for treating or ameliorating the effects of a brain metastasis in a subject having a HER2 positive breast cancer by administration of a combination of tucatinib and an anti-HER2 antibody-drug conjugate (e.g., ado-trastuzumab emtansine or trastuzumab deruxtecan).

SIALIDASE-HER2-ANTIBODY FUSION PROTEINS AND METHODS OF USE THEREOF

The invention relates generally to recombinant sialidase and anti-HER2 immunoglobulin antigen-binding domain fusion proteins. The invention also provides antibody conjugates including a sialidase and an anti-HER2 antibody or a portion thereof. The invention further relates to methods of using the sialidase fusion proteins or antibody conjugates for treating cancer.

Anti-Her2 single chain antibody and coding sequence and use thereof

Provided are an anti-Her2 nanobody and a coding sequence and the use thereof. In particular, provided is a nanobody combating human epidermal growth factor receptor-2 (Her2/ERBB2). Disclosed are the nanobody and the a gene sequence encoding the nanobody, a corresponding expression vector and a host cell capable of expressing the nanobody, and a method for producing the nanobody of the present invention and the related use thereof. The present invention may also provide an immunoconjugate of the nanobody and the use thereof, especially the use in the diagnosis and treatment of Her2 positive tumor.