Disclosed are pharmaceutical compositions comprising a lyophilized compound of formula (I): (I) or a pharmaceutically acceptable salt thereof, and methods of using the same for treating cancer.

The invention relates to a ligand-effector moiety provided with at least one saponin and antibody-effector moiety provided with at least one saponin. An aspect of the invention is a composition comprising the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention. The invention also relates to an antibody-drug conjugate comprising covalently linked saponin and to an antibody-oligonucleotide conjugate comprising covalently linked saponin. An aspect of the invention relates to a pharmaceutical composition comprising the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention, and optionally further comprising a pharmaceutically acceptable excipient. The invention also relates to the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin, for use as a medicament. The invention also relates to the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention for use in the treatment or prophylaxis of a cancer.

Provided is a compound as a compound obtained by conjugating a tertiary amine compound or an imine compound, which is useful as a drug, with a polymer, in which a structure D.sup.+ forming a quaternary ammonium salt or an iminium salt from D, a tertiary amine compound or an imine compound and a polymer residue Poly having a carboxy group are bonded to each other via a structure —C(R.sup.1)(R.sup.2)OC(═O)YANHC(═O)—.

The present disclosure relates to unimolecular core-shell nanoparticle, nanoclusters thereof, and platelet biomimetic nanoclusters thereof. The disclosed compositions are useful for treating a subject with a disease or condition, such as a cardiovascular disease. In a further aspect, the cardiovascular disease can be a vascular stenosis or restenosis. Also described herein are methods of making and using the unimolecular core-shell nanoparticle, nanoclusters thereof, and platelet biomimetic nanoclusters thereof. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

The invention relates to antibody-drug conjugates (ADC) that are potentiated by co-administration of the ADC with a moiety comprising covalently linked saponin. The invention also relates to antibody-oligonucleotide conjugates (AOC) that are potentiated by co-administration of the AOC with a moiety comprising covalently linked saponin. The invention also relates to ADCs and AOCs which are conjugated with a saponin via a covalent linker. The invention further relates to an effector moiety such as a toxin or an antisense oligonucleotide such as for example a BNA, conjugated with a saponin via a covalent linkage. The invention also relates to a BNA covalently conjugated with a targeting moiety such as an antibody. The invention also relates to therapeutic combinations comprising a first pharmaceutical composition comprising a conjugate of a cell-targeting moiety such as an antibody and an antisense oligonucleotide such as a BNA covalently bound thereto, and comprising a second pharmaceutical composition comprising either a free saponin, or a conjugate of a cell-targeting moiety such as an antibody with a saponin covalently linked thereto. Furthermore, the invention relates to any of these conjugates or therapeutic compositions or therapeutic combinations, for use as a medicament. The invention also relates to any of these conjugates or therapeutic compositions or therapeutic combinations, for use in a method for the treatment or the prophylaxis of a cancer. Finally, the invention relates to methods for producing any of these conjugates of the invention.

The invention relates to an endosomal and/or lysosomal escape enhancing conjugate comprising a saponin optionally linked to a targeting molecule such as an antibody and optionally linked to an effector molecule such as a toxin or an oligonucleotide. The invention also relates to a therapeutic combination of such an endosomal and/or lysosomal escape enhancing conjugate of the invention and a functionalized binding molecule comprising an effector molecule, wherein the endosomal and/or lysosomal escape enhancing conjugate comprises an enhancer of said effector molecule, i.e. a saponin. In particular the invention relates to such a therapeutic combination for use as a medicament, in particular for use in the treatment of a tumour. The invention further relates to a method of treating cancer or an autoimmune disease by administering an effective dose of the therapeutic combination to a patient in need thereof or by administering an effective dose of the endosomal and/or lysosomal escape enhancing conjugate comprising a saponin complexed with a targeting molecule such as an immunoglobulin specific for a tumor-cell surface molecule and complexed with an effector molecule, to a patient in need thereof. The invention also relates to a functionalized saponin with endosomal/lysosomal escape enhancing activity.

The present disclosure provides compositions and methods for the treatment of cancer. Specifically, the compositions of the present technology include novel clearing agents that may be used in pretargeted radioimmunotherapy.

A polymer-prostaglandin conjugate comprising: a polymer backbone comprising a plurality of moieties of formula (I): where: T represents a triazole moiety; Q is independently selected at each occurrence and may be present or absent and when present represents a linking group; R is selected from the group consisting of linear or branched hydrocarbon; D is selected from prostaglandins; and L is a group of formula (II) wherein R.sup.5 is selected from hydrogen and C.sub.1 to C.sub.6 alkyl; (R) indicates the end of the group bonded to the R group; and (D) indicates the end of the group attached to the group D.

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Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.

The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.