The present disclosure relates to nanoparticles for delivering a drug targeting brain cancer, whose surface is modified with a peptide for targeting brain cancer, a preparation method thereof, and a use thereof, and more particularly, to nanoparticles for delivering a drug targeting brain cancer, including porous silicon nanoparticles encapsulating an anticancer drug and a peptide with an ability to target brain cancer cells bound to the surface of the nanoparticles, a preparation method thereof, and a use thereof. The nanoparticles according to the present disclosure can be used as an effective drug delivery system for treating glioblastoma by allowing a conventional anticancer agent exhibiting low tissue specificity and solubility to be specifically delivered to glioblastoma in which a caveolin receptor is overexpressed through the blood-brain barrier to induce a more efficient glioblastoma therapeutic effect.

Dendrimer-based compositions and methods are provided, that are useful for administering pharmaceutical compositions to target cells and tissues for treatment of ocular diseases including macular degeneration, diabetic retinopathy, and retinitis pigmentosa.

Described herein are methods of lowering the endotoxin content from a polyanionic polymer conjugate. In particular, methods of reducing the endotoxin content from a polyanionic polymer conjugate that can be useful for a variety of drug delivery applications are described herein.

Aspects of the invention include a polymer comprising: a plurality of repeating units, each repeating unit comprising a polymer backbone group directly or indirectly covalently linked to one or two side chain moieties; wherein: each polymer backbone group is independently a ROMP-polymerized monomer; each one of the one or two side chain moieties independently comprises a peptide moiety or a non-peptide therapeutic moiety; wherein the polymer comprises a plurality of peptide moieties; each polymer backbone group is covalently attached to at least one other polymer backbone group; 100% of the ROMP-polymerized monomers are each individually attached to the one or two side chain moieties; and at least one side chain moiety of the polymer comprises a non-peptide therapeutic moiety, one polymer-terminating group comprises a non-peptide therapeutic moiety, and/or each of both polymer-terminating groups comprises a non-peptide therapeutic moiety.

An antibody includes a polyamidoamine (PAMAM) dendrimer and a first functional group. The polyamidoamine (PAMAM) dendrimer includes a plurality of branches and each of the branches has a phenylboronic acid (PBA) terminal group. The first functional group is bonded to at least one of the PBA terminal groups.

Provided herein are peptides comprising an amino acid sequence having at least about 85% sequence identity to RYRPRAPIIAVT (SEQ ID NO: 1). These cationic peptides inhibit PKM2 methylation and may be used in the treatment of breast cancer and other diseases or conditions in which PKM2 is overexpressed. Such PKM2 peptides may be delivered to cancer cells using pH sensitive unimolecular nanoparticles comprising anionic polymers.

The invention relates to a therapeutic combination for use as a medicament, wherein the therapeutic combination comprises: (a) a first pharmaceutical composition comprising a first proteinaceous molecule and at least one saponin covalently bound to said first proteinaceous molecule; and (b) a second pharmaceutical composition comprising a second proteinaceous molecule, comprising an effector moiety, wherein the binding site of the first proteinaceous molecule and the binding site of the second proteinaceous molecule are the same. The invention also relates to the first pharmaceutical composition for use as a medicament. The invention also relates to the first pharmaceutical composition, further comprising the second proteinaceous molecule. The invention also relates to the first pharmaceutical composition, further comprising the second proteinaceous molecule, for use as a medicament. Furthermore, the invention relates to the first pharmaceutical composition, further comprising the second proteinaceous molecule, for use in the treatment or prophylaxis of cancer in a patient in need thereof.

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.

The present invention relates to antibody-drug conjugates comprising (i) an antibody or antigen-binding fragment thereof, (ii) a polymer comprising a particular repeat unit, which is covalently bound to one or more biologically active moieties, such as small molecule drugs, optionally via a linker, and (iii) a polymer-antibody linker moiety which is covalently bound to both the polymer and the antibody or antigen-binding fragment thereof. Additionally, the present invention relates to pharmaceutical compositions comprising the antibody-drug conjugates and to use of the antibody-drug conjugates in medicine.

The invention relates to a therapeutic combination, comprising a first proteinaceous molecule comprising a first binding site for binding to a first epitope of a first cell-surface molecule, the first proteinaceous molecule provided with at least one saponin covalently bound to an amino-acid residue of said first proteinaceous molecule, and comprising a second pharmaceutical composition comprising a second proteinaceous molecule different from the first proteinaceous molecule, the second proteinaceous molecule comprising a second binding site for binding to a second epitope of a second cell-surface molecule different from the first cell-surface molecule, and comprising an effector moiety, wherein the second epitope is different from the first epitope. An aspect of the invention is a composition comprising the first proteinaceous molecule and the second proteinaceous molecule of the invention. The invention also relates to an antibody-drug conjugate comprising the first proteinaceous molecule of the invention and an effector moiety. An aspect of the invention relates to a pharmaceutical composition comprising the composition or the antibody-drug conjugate of the invention, and optionally further comprising a pharmaceutically acceptable excipient. The invention also relates to the therapeutic combination or the composition or the antibody-drug conjugate or the pharmaceutical composition of the invention, for use as a medicament. The invention also relates to the therapeutic combination of the invention for use in the treatment or prophylaxis of a cancer.