66 results about "Agonist peptide" patented technology

The present application provides protease-resistant Glucagon-Like Peptide 1 (eGLP-1) peptides, and also provides protease-resistant dual agonist peptides against GLP-1R and GIPR, methods of making such peptides, as well as compositions comprising protease-resistant peptides and methods of treatment utilizing such peptides.

Described herein is a method of treating a disease or condition, for example, obesity, weight gain, or diabetes, comprising administering to a subject in need thereof a glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and a glucagon-like peptide 1 receptor (GLP-1R) agonist. Further described herein are pharmaceutical compositions comprising a GIPR antagonist and a GLP-1R agonist, which may be useful in the treatment of a disease or condition, for example, obesity, weight gain, or diabetes.

A pharmaceutical composition comprises a GPCR agonist fusion protein in which a GPCR agonist peptide is covalently coupled to albumin via a linker in a manner that is resistant to a retro-Michael addition. Advantageously, compositions presented herein avoid decoupling of the agonist form the albumin while retaining the agonist in a steric relationship to the albumin that allows for effective binding and activation of the GPCR while also enabling gp60-mediated transcytosis and FcRn-mediated albumin recycling. These properties enable ultra-low dosages for the GPCR agonist fusion protein to give a therapeutic effect while substantially reducing or even entirely avoiding adverse effects otherwise commonly associated with unbound agonists. Such retro-Michael resistant composition is generally achieved by conformational modification of the albumin, resulting in stereoselective coupling of the linker to the albumin.

A pharmaceutical composition comprises a GPCR agonist fusion protein wherein the GPCR agonist peptide is covalently conjugated to an albumin via a linker in a manner that is resistant to a reverse Michael addition. Advantageously, the compositions presented herein avoid uncoupling of the agonist to the albumin while maintaining the agonist and the albumin in a spatial relationship that allows efficient binding and activation of the GPCR while also enabling gp60-mediated endocytosis transport and FcRn-mediated albumin recirculation. These characteristics enable ultra-low doses of GPCR agonist fusion proteins to produce therapeutic effects while significantly reducing or even completely avoiding side effects that would otherwise be typically associated with unbound agonists. Such reverse Michael resistant compositions are typically achieved by conformationally modifying an albumin, resulting in a stereoselective coupling of a linker to the albumin.

Described herein is a method of treating a disease or condition, for example, obesity, weight gain, or diabetes, comprising administering to a subject in need thereof a glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and a glucagon-like peptide 1 receptor (GLP-1R) agonist. Further described herein are pharmaceutical compositions comprising a GIPR antagonist and a GLP-1R agonist, which may be useful in the treatment of a disease or condition, for example, obesity, weight gain, or diabetes.

The invention discloses a circRNA nano delivery system capable of reversing nucleus pulposus progenitor cell senescence and a preparation method and application of the circRNA nano delivery system. The circRNA nano delivery system comprises: a) Klotho circRNA, and b) a liposome, and the liposome comprises a vascular peptide vasculotide, an ionizable lipid molecule, a phospholipid, a PEG lipid, and a steroid. The invention also provides application of the circRNA nano delivery system capable of reversing nucleus pulposus progenitor cell senescence in preparation of drugs for treating intervertebral disc degeneration. The invention provides liposome particles (Vas-Klotho-LNP) which have targeted NPPCs and wrap circRNA, Klotho circRNA is efficiently introduced into the NPPCs through Tie2 agonist peptide, so that rejuvenation of the NPPCs is promoted, ECM synthesis is promoted, and regeneration and repair of intervertebral discs are synergistically promoted in vivo and in vitro.

A pharmaceutical composition comprises a GPCR agonist fusion protein in which a GPCR agonist peptide is covalently coupled to albumin via a linker in a manner that is resistant to a retro-Michael addition. Advantageously, compositions presented herein avoid decoupling of the agonist form the albumin while retaining the agonist in a steric relationship to the albumin that allows for effective binding and activation of the GPCR while also enabling gp60-mediated transcytosis and FcRn-mediated albumin recycling. These properties enable ultra-low dosages for the GPCR agonist fusion protein to give a therapeutic effect while substantially reducing or even entirely avoiding adverse effects otherwise commonly associated with unbound agonists. Moreover, these properties also enable transport of the GPCR agonist fusion protein across the blood brain barrier and therefore allow treatment of neural disorders.

Disclosed herein are antibodies, agonist peptides, and dual agonist peptides. Further disclosed herein are antibody conjugates comprising the antibodies, agonist peptides, and / or dual agonist peptides disclosed herein. In some embodiments, the antibodies or antibody conjugates of the invention may be used to treat metabolic diseases.

The invention provides low-dose formulations of guanylate cyclase-C (“GCC”) agonist peptides and methods for their use. The formulations of the invention can be administered either alone or in combination with one or more additional therapeutic agents, preferably an inhibitor of cGMP-dependent phosphodiesterase or a laxative.

Provided are novel compounds for GIPR, GLP-1R and GCGR. Specifically, provided are GLP-1R / GIPR / GCGR triagonists peptides, and conjugates comprising an Fc fragment and GLP-1R / GIPR / GCGR triagonists peptides. Pharmaceutical compositions comprising these compounds,as well as uses thereof in treating metabolic conditions and disorders, such as diabetes mellitus, type 2 diabetes, obesity, metabolic dysfunction-associated fatty liver disease (MAFLD), non-alcoholic fatty liver disease (NAFLD), metabolic dysfunction-associated steatohepatitis (MASH), and non-alcoholic steatohepatitis (NASH) are also provided.

To provide GLP-1R agonistic peptides with reduced GLP-1R agonistic activity, fusion molecules comprising the same and pharmaceutical compositions.SOLUTION: The invention provides a GLP-1R agonistic peptide whose GLP-1R agonistic activity is about 9- to about 531-fold reduced as compared to the GLP-1R agonistic activity of native GLP-1 of a specific sequence. The invention also provides a nucleic acid molecule encoding GLP-1R agonistic peptide with reduced GLP-1R agonistic activity, a pharmaceutical composition comprising a GLP-1R agonistic peptide with reduced GLP-1R agonistic activity and combinations thereof. The pharmaceutical composition is for treating obesity, overweight, metabolic syndrome, diabetes, diabetic retinopathy, hyperglycemia, dyslipidemia, non-alcoholic steatohepatitis (NASH) and / or atherosclerosis.SELECTED DRAWING: None

The present invention relates to methods of treatment using acylated compounds and peptide hormones having dual agonist activity for the GLP-1 (glucagon-like peptide 1) and GLP-2 5 (glucagon-like peptide 2) receptors. In particular, the present invention relates to the administration of a dual GLP-1 / GLP-2 agonist peptide and amylin for modulating body weight and preventing or treating obesity and related conditions.

The present disclosure provides GIP receptor agonist peptide compounds suitable for once per day dosing (QD), said peptide compounds having an activating action on GIP receptors and use of the GIP receptor agonist peptide as a medicament for the treatment and / or prevention of emesis, or a symptom or condition associated with emesis while having an improved profile.

This disclosure relates to the field of GLP-1R and GCGR agonists, formulations, and methods of using the same, including but not limited to dual agonist peptides of any of SEQ ID NOS. 1-10 or 12-27 conjugated to a non-ionic glycolipid surfactant.

The present application provides protease resistant glucagon-like peptide 1 (eGLP-1) peptides, as well as protease resistant dual agonist peptides directed against GLP-1R and GIPR, methods of making these peptides, as well as compositions comprising the protease resistant peptides and methods of treatment utilizing these peptides.

Provided is dual target agonist peptides, and more specifically to a series of dual target agonists that can simultaneously activate the human Glucagon like peptide-1 (GLP-1) receptor and the human glucose dependent insulinotropic polypeptide (GIP) receptor, as well as its pharmaceutical salts and pharmaceutical compositions. The peptides have dual agonist effect and can be used for the treatment of diabetes, obesity and other related diseases.

The present disclosure relates to a pharmaceutical formulation suitable for sublingual administration for use in the treatment of obesity, type II diabetes, or related diseases. The pharmaceutical formula comprises 5 to 10 milligrams of glucagon-like peptide-1 receptor agonist peptide (GLP-1 RA-P) which is dissolved in 1.5 to 2.0 milliliters of a buffer solution, and the pH (Potential of Hydrogen) value of the pharmaceutical formula is 5.5 to 7.5. The disclosure also discloses a method for treating obesity, type II diabetes, or related diseases. The method comprises administering the pharmaceutical formulation of the present disclosure to a subject in a sublingual administration, and allowing the pharmaceutical formulation to be continuously located sublingually of the subject for 5-10 minutes, where the pharmaceutical formulation has a bioavailability for GLP-1 RA-P of 2-10% compared to the administration to the subject through subcutaneous injection.

Hydrochloride salt forms of synthetic C-terminal peptide analogs of C5a, which are response selective agonists of C5aR-bearing antigen presenting cells. Methods of inducing an immune response in a subject by administering such peptide analogs alone or in combination with other active agents are also disclosed.

The present invention relates to GIP / GLP1 agonist compositions. The present invention is a GIP / GLP1 co-agonist peptide pharmaceutical composition for subcutaneous injection. The composition comprises tirzepatide, NaCl, and disodium hydrogen phosphate. The composition provides commercially acceptable shelf-life stability, use-life stability, and an acceptable patient injection site experience. An alternative composition comprises tirzepatide, propylene glycol, and disodium hydrogen phosphate, which also provides acceptable shelf-life stability.

Peptides that exhibit amylin and calcitonin receptor agonist activity (DACRAs) are provided as well as prodrug derivatives thereof. Analogs having enhanced agonist selectivity for the calcitonin receptor relative to amylin are also provided as well as conjugates of the DACRA peptides with incretin peptides. Pharmaceutical compositions comprising such peptide analogs and therapeutic methods of using such peptide analogs are also provided.

The present invention relates to a GIP / GLP1 agonist composition. The present invention relates to a GIP / GLP1 co-agonist peptide pharmaceutical composition for subcutaneous injection. The composition is prepared from tilpotide, NaCl and disodium hydrogen phosphate. The compositions provide commercially acceptable shelf-life stability, shelf-life stability, and are related to acceptable patient injection site experiences. Alternatively, the composition comprises tirpotide, propylene glycol, and disodium hydrogen phosphate, which also provides acceptable shelf life stability.

The present invention relates to immunoglobulins, such as immunoconjugates, comprising an ActRII receptor antibody and a GLP-1 agonist molecule, such as a GLP-1 agonist peptide. Such constructs are useful in the treatment of numerous diseases and disorders, including metabolic disorders such as obesity, diabetes, and others.

This invention belongs to the field of peptide medicine, specifically relating to a compound as a TGF-β receptor agonist peptide and its uses. The amino acid sequence of the peptide is shown in SEQ ID No. 1. The peptide of this invention has a significant agonistic effect on the TGF-β receptor and can be used in the preparation of drugs for the prevention and / or treatment of TGF-β-related diseases, particularly for the prevention of hair loss and / or the promotion of hair growth.

GLP-1 and glucagon dual agonists disclosed herein have improved biological stability, including proteolytic stability, and duration of action. The peptides can be administered about once a week.

A pharmaceutical composition comprises a GPCR agonist fusion protein in which a GPCR agonist peptide is covalently coupled to albumin via a linker in a manner that is resistant to a retro-Michael addition. Advantageously, compositions presented herein avoid decoupling of the agonist form the albumin while retaining the agonist in a steric relationship to the albumin that allows for effective binding and activation of the GPCR while also enabling gp60-mediated transcytosis and FcRn-mediated albumin recycling. These properties enable ultra-low dosages for the GPCR agonist fusion protein to give a therapeutic effect while substantially reducing or even entirely avoiding adverse effects otherwise commonly associated with unbound agonists. Moreover, these properties also enable transport of the GPCR agonist fusion protein across the blood brain barrier and therefore allow treatment of neural disorders.

To provide fusion proteins with optimized GLP-1R agonist / FGF21 compound activity ratio.SOLUTION: The invention relates to a fusion protein comprising a glucagon-like peptide 1 receptor 5 (GLP-1R) agonistic peptide and a variant of human fibroblast growth factor 21 (FGF21). The invention further relates, in particular to the use of a fusion protein comprising a GLP-1R agonistic peptide and a variant of FGF21 as a medicament for treating obesity, overweight, metabolic syndrome, diabetes, diabetic retinopathy, hyper glycemia, dyslipidemia, non-alcoholic steatohepatitis (NASH) and / or atherosclerosis in a subject. The invention further relates to pharmaceutical compositions comprising a fusion protein comprising a GLP-1R agonistic peptide and a variant of FGF21.SELECTED DRAWING: None

G protein-coupled receptor (GPCR) agonist peptides and their use are described. Also described are vectors for expressing the GPCR agonist peptides and method for treating a disease or disorder with the GPCR agonist peptides.

To provide a GIP receptor agonist peptide compound having an activating action on a GIP receptor.SOLUTION: To provide a new peptide compound containing an amino acid sequence represented by a specific sequence and having activation action on a GIP receptor, and to provide use of the peptide compound as a medicine.SELECTED DRAWING: None

A pharmaceutical composition comprises a GPCR agonist fusion protein wherein the GPCR agonist peptide is covalently conjugated to an albumin via a linker in a manner that is resistant to a reverse Michael addition. Advantageously, the compositions presented herein avoid uncoupling of the agonist to the albumin while maintaining the agonist and the albumin in a spatial relationship that allows efficient binding and activation of the GPCR while also enabling gp60-mediated endocytosis transport and FcRn-mediated albumin recirculation. These characteristics enable ultra-low doses of GPCR agonist fusion proteins to produce therapeutic effects while significantly reducing or even completely avoiding side effects that would otherwise be typically associated with unbound agonists. In addition, these properties also enable GPCR agonist fusion proteins to transport across the blood-brain barrier, and thus allow for the treatment of neurological disorders.

The present invention relates generally to novel multi-agonist peptides useful as agents for the treatment and prevention of metabolic diseases and disorders, for example, diseases and disorders that can be ameliorated by controlling weight loss, plasma glucose and lipid levels, insulin levels and / or insulin secretion, positive myodynamia, reducing catabolism, slowing gastric emptying, and preventing neurodegeneration. Such conditions and disorders include, but are not limited to, control of food intake, weight loss, energy metabolism, plasma glucose levels, insulin levels and / or insulin secretion, positive myodynamia, reduction of catabolism, slowing of gastric emptying, obesity, diabetes and diabetes-related conditions, liver fat-related inflammation and injury. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular diseases, dietetic disorders, and rare obesity genetic diseases such as Prallard-Willi Syndrome, intensive care, insulin resistance and related disorders such as polycystic ovarian Syndrome, obesity, any type of diabetes, including type 1, type 2 and gestational diabetes, as well as diabetes mellitus, such as diabetes mellitus, diabetes mellitus, diabetes mellitus, diabetes mellitus, and diabetes mellitus. And CNS disorders such as prevention of neurodegeneration, depression, alcohol addiction, Alzheimer's disease and Parkinson's disease, and non-alcoholic steatohepatitis (NASH).