This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof pharmaceutical compositions containing them, and to their use in therapy for the prevention treatment of cancer.

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.

Methods of administering immunoconjugates that bind to FOLR1 are provided. The methods comprise administering an anti-FOLR1 immunoconjugate to a person in need thereof, for example, a cancer patient, at a therapeutically effective dosing regimen that results in minimal adverse effects.

The present disclosure relates to a benzoselenophene-based compound, a method of preparing the benzoselenophene-based compound, and a pharmaceutical composition and antibody-drug conjugate including the benzoselenophene-based compound.

Disclose herein are dosing regimens for a combination of carboplatin and a targeted NaPi2b antibody-drug conjugates for treating cancer.

Described herein are methods, formulations and kits for treating a patient with triple-negative breast cancer with nanoparticle complexes comprising a carrier protein (e.g., albumin), paclitaxel and a binding agent specific for a target antigen expressed by the cells (e.g., an anti-VEGF antibody).

The present invention concerns novel and improved antibody-conjugates for targeting CD30. The inventors found that when antibody-conjugates were prepared using a specific mode of conjugation, they exhibit an improved therapeutic index. The mode of conjugation comprises a first step (i) of contacting a glycoprotein comprising 1-4 core N-acetylglucosamine moieties with a compound of the formula S(F.sup.1).sub.x-P in the presence of a catalyst, wherein S(F.sup.1).sub.x is a sugar derivative comprising x functional groups F.sup.1 capable of reacting with a functional group Q.sup.1, x is 1 or 2 and P is a nucleoside mono- or diphosphate, and wherein the catalyst is capable of transferring the S(F.sup.1).sub.x moiety to the core-GlcNAc moiety, to obtain a modified antibody; and a second step (ii) of reacting the modified antibody with a linker-conjugate comprising a functional group Q.sup.1 capable of reacting with functional group F.sup.1 and a target molecule D connected to Q.sup.1 via a linker L.sup.2 to obtain the antibody-conjugate wherein linker L comprises S—Z.sup.3-L.sup.2 and wherein Z.sup.3 is a connecting group resulting from the reaction between Q.sup.1 and F.sup.1. The invention also relates to a use for improving the therapeutic index of an antibody-conjugate and to a method for targeting CD30-expressing cells.

The invention relates generally to antibodies that bind PSMA, and methods of making and using these anti-PSMA antibodies in a variety of therapeutic, diagnostic and prophylactic indications.

As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the following formula: -L.sup.1-L.sup.2-L.sup.P-NH—(CH.sub.2)n.sup.1-L.sup.a-(CH.sub.2)n.sup.2-C(═O)— wherein the anti-HER2 antibody is connected to the terminal L.sup.1, and the antitumor compound is connected to the carbonyl group of the —(CH.sub.2)n.sup.2-C(═O)— moiety with the nitrogen atom of the amino group at position 1 as the connecting position. ##STR00001##

The present invention relates to an anti-tumor/anti-tumor-associated fibroblast (TAF)/anti-hapten trispecific antibody (TsAb). The anti-hapten domain enables TsAb to arm various hapten-conjugated anti-cancer drugs (nanocarrier drugs, small molecule drugs, protein drugs, and radioactive drugs). The anti-tumor domain enables TsAb-armed drugs to target tumor cells, while the anti-TAF domain enables the TsAb-armed drugs to target TAFs. The present invention allows the simultaneous killing of tumor cells and TAFs by various drugs through arming with TsAb.