Patent classifications
A61K47/59
Antibody-conjugates with improved therapeutic index for targeting CD30 tumours and method for improving therapeutic index of antibody-conjugates
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.
COMPOSITIONS COMPRISING DESOXIMETASONE AND TAZAROTENE
The present disclosure provides formulations comprising desoximetasone, tazarotene, a polymer comprising polyurethane, and a solvent. Also provided herein are methods of co-administering desoximetasone and tazarotene.
COMPOSITIONS COMPRISING DESOXIMETASONE AND TAZAROTENE
The present disclosure provides formulations comprising desoximetasone, tazarotene, a polymer comprising polyurethane, and a solvent. Also provided herein are methods of co-administering desoximetasone and tazarotene.
CATIONIC ANTIMICROBIAL OLIGO-GUANIDINIUM DENDRIMERS AND COMPOSITIONS
A new synthesized non-peptide cationic oligo-guanidinium dendrimers containing a number of positive charges, 6, 9, 12, and 18 for use as antimicrobial agents and a method for synthesizing non-peptide cationic oligo-guanidinium dendrimers G12 and G18. These designed and synthesized dendrimers exhibit antimicrobial activities as well as biofilm disrupting activity against various pathogens such as Gram-negative bacteria, Gram-positive bacteria, and fungi. The application of these dendrimers are very broad, which includes application to pharmaceutical compounds that are covalently or non-covalently complexed. These combinations are important in helping the body reach the proper immune balance required for maximized function and/or optimal health.
POLYETHYLENIMINE NANOPARTICLES AND METHODS OF USING SAME
Disclosed herein are nanoparticle compositions containing that may be created by functionalizing polyethylenimine (PEI) with fatty acids and carboxylate terminated poly(ethylene glycol) (PEG). The disclosed compositions may be delivered to an individual in need thereof via delivery into blood circulation, where the nanoparticle compositions show an exceptionally high specificity to the pulmonary microvascular endothelium with minimal targeting of other cell types in the lung, to provide delivery of therapeutic agents such as stabilized nucleic acids. Methods of using the compositions are also disclosed.
POLYETHYLENIMINE NANOPARTICLES AND METHODS OF USING SAME
Disclosed herein are nanoparticle compositions containing that may be created by functionalizing polyethylenimine (PEI) with fatty acids and carboxylate terminated poly(ethylene glycol) (PEG). The disclosed compositions may be delivered to an individual in need thereof via delivery into blood circulation, where the nanoparticle compositions show an exceptionally high specificity to the pulmonary microvascular endothelium with minimal targeting of other cell types in the lung, to provide delivery of therapeutic agents such as stabilized nucleic acids. Methods of using the compositions are also disclosed.
Pharmaceutical compositions for basic or neutral, low molecular weight compounds
The present invention provides novel, solid or liquid pharmaceutical preparations comprising a basic or neutral, low molecular weight active pharmaceutical ingredient and the polymer Eudragit® EPO, optionally together with additional pharmaceutically acceptable excipients. The present preparations are for oral or topical administration.
TERTIARY AMINE PHARMACEUTICAL COMPOSITION AND INDUSTRIALIZED BATCH PREPARATION METHOD THEREOF
A tertiary amine pharmaceutical composition includes a drug having a tertiary amine structure, a biocompatible polymer material, and a quaternary ammonium salt impurity. The pharmaceutical composition is obtained by dissolving or dispersing the drug in a halogenated hydrocarbon or a mixed solvent mainly containing halogenated hydrocarbon or a solution containing halogenated hydrocarbon. The quaternary ammonium salt impurity is generated from reacting the drug having the tertiary amine structure with the halogenated hydrocarbon. The pharmaceutical composition comprises 40 wt % to 80 wt % of the biocompatible polymer material, and 20 wt % to 60 wt % of the drug with the tertiary amine structure. The content of the quaternary ammonium salt impurity is less than 0.05 wt %, the content of the halogenated hydrocarbon in the composition is less than 1.5 wt %, and the quaternary ammonium salt impurity does not increase or increases slowly during storage, which complies with requirements of pharmaceutical regulations.
NANOPARTICLE COMPOSITIONS CONTAINING SUGAR FUNCTIONALIZED NUCLEIC ACID CARRIERS
Nanoparticle compositions for delivery of nucleic acids to subjects including carriers comprising sugar functionalized nucleic acid carriers, and therapeutic or immunogenic nucleic acid agents enclosed within the delivery molecules are described. Methods for treating or preventing diseases or conditions in a subject by administering the nanoparticle compositions that provide immune responses and synergistic therapeutic or preventive effects are provided.
PLGA-modified polyethylenimine self-assembly nanotechnology for nucleic acid and drug delivery
Embodiments of the invention concern copolymers and nanoparticles for use as delivery agents for one or more agents for therapy for a medical condition of humans and animals. Some of embodiments of the invention provide new reagents for biomedical research in cell culture, animal models and plants, for example. The copolymers comprise PLGA and PEI and, in some embodiments, also comprise 1-(3-aminopropyl)-4-methylpiperazine (APMP), Fc binding peptide and/or antibody. In certain embodiments, APMP-PLGA-PEI, Fc binding peptide/antibody-PLGA-PEI or Fc binding peptide/antibody-APMP-PLGA-PEI nanoparticles comprising one or more therapeutic agents are delivered to an individual in need thereof or used for biomedical research in cell cultures, animal models and plants.