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AssigneeRegeneron Pharmaceuticals, Inc.
InventorsAmy HAN, Jason Mastaitis, Xiang Zheng, Se Hyun Kim, Jean Yanolatos, Judith Altarejos, Mark Sleeman, Chester A. Metcalf, III, William Olson, Andrew J. Murphy, George D. Yancopoulos
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Described herein are protein-drug conjugates and compositions thereof that are useful, for example, for targeting glucagon-like peptide 1 receptor (GLP1R). In certain embodiments, provided are peptidomimetic payloads and linker-payloads and methods of making same. More specifically, GLP1 peptidomimetics, antibody-drug conjugates, and compositions which comprise anti-GLP1R antibodies and GLP1 peptidomimetic payloads and methods of treating GLP1R-associated conditions are provided.
A composition comprising an GLP1R agonist-tethered GDF8 antibody conjugate, or a pharmaceutically acceptable salt thereof, wherein the conjugate comprises
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A GLP1R agonist-tethered GDF8 antibody conjugate, or a pharmaceutically acceptable salt thereof, having a Formula (I):
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A compound, or a pharmaceutically acceptable salt thereof, having the structure of Formula (IV):
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A method for treating obesity by reducing body weight while maintaining or increasing lean body mass in a subject, comprising administering a therapeutically effective amount of a GLP-1 agonist-tethered GDF8 antibody conjugate of claim 26 to the subject in need thereof.
A method for treating obesity by reducing fat mass while maintaining or increasing lean body mass in a subject, comprising administering a therapeutically effective amount of a GLP-1 agonist-tethered GDF8 antibody conjugate of claim 26 to the subject in need thereof.
A method for treating Type 2 diabetes by improving glycemic control and maintaining or increasing lean body mass while reducing fat mass in a subject, comprising administering a therapeutically effective amount of a GLP-1 agonist-tethered GDF8 antibody conjugate of claim 26 to the subject in need thereof.
A method for treating obesity and Type 2 diabetes by improving glycemic control and maintaining or increasing lean body mass while reducing fat mass in a subject, comprising administering a therapeutically effective amount of a GLP-1 agonist-tethered GDF8 antibody conjugate of claim 26 to the subject in need thereof.
A method for treating obesity, diabetes, and/or liver diseases associated with increased fat mass in a subject, comprising administering a therapeutically effective amount of a GLP-1 agonist-tethered GDF8 antibody conjugate of claim 26 to the subject in need thereof.
A method for treating obesity, diabetes, and/or liver diseases associated with increased fat mass in a subject, comprising administering a therapeutically effective amount of a GLP-1 agonist-tethered GDF8 antibody conjugate of claim 26, together with one or more other therapeutic agents, to the subject in need thereof.
A method for treating a subject of metabolic syndrome by improving glycemic control, maintaining or increasing lean body mass while reducing fat mass in a subject, comprising administering a therapeutically effective amount of a GLP-1 agonist-tethered GDF8 antibody conjugate of claim 26 to the subject in need thereof.
A method for treating a subject of metabolic syndrome by improving glycemic control, maintaining or increasing lean body mass while reducing fat mass in a subject, comprising administering a therapeutically effective amount of a GLP-1 agonist-tethered GDF8 antibody conjugate of claim 26, together with one or more other therapeutic agents, to the subject in need thereof.
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A process for manufacturing a conjugate of GLP1R agonist tethered GDF8 antibody or antigen binding fragment thereof comprising a) covalently attaching a handle comprising a first reactive moiety for Click or Diels-Alder reaction, in the presence of microbial transglutaminase;
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A conjugate, or a pharmaceutically acceptable salt thereof, comprising an antigen-binding protein (BA) and a GLP1R agonist, wherein the BA specifically binds to and/or blocks the activity of GDF8 (SEQ ID NO:
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A process for conjugating a drug, a ligand, or a handle, site-specifically to an isolated antibody or antigen binding fragment thereof, wherein the site of conjugation is at Gln/Q55 of the light chain of the antibody, and wherein the site-specific conjugation is assisted by microbial transglutaminase (mTG).
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A compound of Formula (V):
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Dependencies are inferred from the claim text.