A61K47/65

Biologically active compound conjugated to a stapled or stitched peptide

The invention relates to improvements in drug delivery and more particularly to the use of Cell Penetrating Agents (CPA's) or Cell Penetrating Peptides (CPP's) which have been stabilized by, for example: i) stapling two amino acids to form Stapled CPP's (StaP's) or ii) stitching three or more amino acids to form stitched CPP's (StiP's). These stabilized CPP's are conjugated to a drug or Biologically Active Compound (BAC) directly or via a Bi-Functional Linker (BFL) so that the BAC can be carried through a cell membrane by the CPP. The resulting molecules are referred to as Drug Carrying Cell Penetrating Molecules (DCCPM's). The preferred BAC is an electrically low charge carrying oligonucleotide such as a phosphorodiamidate morpholino oligonucleotide (PMO). The invention also relates to a method of facilitating the uptake of a BAC into a cell, the use of a DCCPM in the treatment of a disease requiring alteration of an endogenous or exogenous gene, a method of improving the bioavailability of a drug or BAC, a method of introducing a drug or BAC to a site which is refractory to the drug or BAC in its native state, a method of treating a subject comprising administering the DCCPM's of the invention and to a pharmaceutical composition comprising the DCCPM and one or more pharmaceutically acceptable excipients.

Noncrushable pill formulations

Non-crushable pill formulations and methods of using the formulations are disclosed. A non-crushable pill formulation for preventing unintended use of a drug, comprising a polymer, the polymer forming a polymer backbone of the complex; cross-linkers, the cross-linkers connecting the polymer backbone through covalently bonding to form at least one inner cavity within the complex; and the drug, the drug being trapped either covalently or non-covalently in the at least one inner cavity within the complex, wherein the drug is protected from releasing outside of the complex.

Noncrushable pill formulations

Non-crushable pill formulations and methods of using the formulations are disclosed. A non-crushable pill formulation for preventing unintended use of a drug, comprising a polymer, the polymer forming a polymer backbone of the complex; cross-linkers, the cross-linkers connecting the polymer backbone through covalently bonding to form at least one inner cavity within the complex; and the drug, the drug being trapped either covalently or non-covalently in the at least one inner cavity within the complex, wherein the drug is protected from releasing outside of the complex.

Anti-ASGR1 antibody TLR8 agonist comprising conjugates and uses thereof

The disclosure provides conjugates of anti-ASGR1 antibodies or antigen binding fragments thereof to a myeloid cell agonist, compositions comprising the conjugates, and methods of treating liver viral infections with the conjugates. The disclosure also provides for anti-ASGR1 antibodies or antigen binding fragments thereof and methods for using the antibodies or antigen binding fragments thereof in treating liver viral infections.

Anti-ASGR1 antibody TLR8 agonist comprising conjugates and uses thereof

The disclosure provides conjugates of anti-ASGR1 antibodies or antigen binding fragments thereof to a myeloid cell agonist, compositions comprising the conjugates, and methods of treating liver viral infections with the conjugates. The disclosure also provides for anti-ASGR1 antibodies or antigen binding fragments thereof and methods for using the antibodies or antigen binding fragments thereof in treating liver viral infections.

MATRIPTASE AND U-PLASMINOGEN ACTIVATOR SUBSTRATES AND OTHER CLEAVABLE MOIETIES AND METHOS OF USE THEREOF

The invention relates generally to polypeptides that include a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator (uPA), to activatable antibodies and other larger molecules that include the cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator, and to methods of making and using these polypeptides that include a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator in a variety of therapeutic, diagnostic and prophylactic indications.

MATRIPTASE AND U-PLASMINOGEN ACTIVATOR SUBSTRATES AND OTHER CLEAVABLE MOIETIES AND METHOS OF USE THEREOF

The invention relates generally to polypeptides that include a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator (uPA), to activatable antibodies and other larger molecules that include the cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator, and to methods of making and using these polypeptides that include a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator in a variety of therapeutic, diagnostic and prophylactic indications.

AN EXTRACELLULAR VESICLE
20220409739 · 2022-12-29 ·

The present invention relates to compositions for the delivery of molecules such as a peptide, a nucleic acid and/or a small molecule drug. In particular, the present invention relates to an extracellular vesicle (EV) loaded with a peptide, a nucleic acid and/or a small molecule drug, along with methods of producing said EV.

AN EXTRACELLULAR VESICLE
20220409739 · 2022-12-29 ·

The present invention relates to compositions for the delivery of molecules such as a peptide, a nucleic acid and/or a small molecule drug. In particular, the present invention relates to an extracellular vesicle (EV) loaded with a peptide, a nucleic acid and/or a small molecule drug, along with methods of producing said EV.

PEPTIDE-MHC II PROTEIN CONSTRUCTS AND USES THEREOF

Compositions comprising an MHC ligand peptide covalently attached to an MHC class II molecule are provided herein. In some compositions, the MHC ligand peptide is covalently attached to the MHC class II molecule by a peptide linker, wherein the MHC ligand peptide or the peptide linker comprises a first cysteine, wherein the MHC class II a chain or a portion thereof or the MHC class II β chain or a portion thereof comprises a second cysteine, and wherein the first cysteine and the second cysteine form a disulfide bond such that the MHC ligand peptide is bound in a peptide-binding groove formed by the MHC class II a chain or the portion thereof and the MHC class II β chain or the portion thereof. Also provided are nucleic acids encoding such compositions and methods for using such compositions to elicit an immune response in a subject.