50 results about "Insulinotropin" patented technology

The present invention provides methods of administering an insulinotropic peptide in an amount effective to treat a disorder or condition while reducing nausea side effect by administering to a subject in need thereof an insulinotropic peptide conjugated to albumin. The present invention also provides methods of selecting a subject for administration of a conjugated insulinotropic peptide. Exemplary disorders or conditions treatable with an insulinotropic peptide include obesity and type II diabetes.

The present invention relates generally to the novel use of incretin compounds (ICs) and amylinomimetic compounds to treat, prevent, or ameliorate a variety of metabolic conditions or diseases.

Embodiments of the invention provide shaped masses comprising one or more drugs such as proteins or polypeptides and methods for forming such shaped masses. One embodiment provides a shaped mass comprising a drug such as a protein or polypeptide having a biological activity in the body of a mammal. The shaped mass is formed by compression of a precursor material comprising the drug wherein an amount of biologically active drug in the mass is a preserved above a minimum level. Drugs which may be incorporated into the shaped mass may include one or more glucose regulating proteins such as insulin, incretins; and immunoglobulins such as TNF-inhibiting antibodies or interleukin neutralizing antibodies. Embodiments of the shaped mass may be incorporated into a tissue penetrating member which is inserted into the intestinal wall allowing for the oral delivery of proteins and peptides which would otherwise be degraded in the intestinal tract.

The present invention relates to drug fusions and conjugates that have improved serum half lives. These fusions and conjugates comprise immunoglobulin (antibody) single variable domains and insulinotropic and/or incretin and/or gut peptide molecules. The invention further relates to uses, formulations, compositions and devices comprising such drug fusions and conjugates. The invention also relates to compositions which comprise more than one insulinotropic and/or incretin and/or gut peptide molecules present as part of a fusion or conjugate and to uses and formulations thereof.

The invention relates to a fusion protein. The fusion protein sequentially contains exendin-4, a connecting peptide and a human IgG2 Fc mutant from an N end to a C end. The invention also relates to a preparation method for the fusion protein. The fusion protein can be highly expressed in a mannalian cell, and a purification process is simple and favorable for further preparing the fusion proteins in large scale. The fusion protein provided by the invention has the bioactivity of natural exendin-4 and the advantage of longer serum half-life period, and can stimulate the secretion of insulin, suppress the release of glucagons after food intake and be used for treating various diabete.

The invention relates to a marine oligosaccharide compound with type II diabetes resisting activity, which is a compound which is formed by following steps: taking D-polymannose aldehydic oligosaccharide which comes from sea and contains carboxyl in each oligosaccharide ring, reacting with dilute alkali and chromium salt solution and introducing trivalent chromium ions which is closely relative tothe generation and the development of diabetes into oligosaccharide molecules. A pharmacological experiment proves that the product has remarkable effect on accelerating insulin secretion, is not influenced by amylin and has effects on lightening glucose load, improving blood-lipoid metabolism, insulin sensitivity and certain kidney protection and lightening pancreatic injury for type II diabetesrats and mouse. The product of the invention comes from marine natural species, has the advantages of good security, unique structure, low molecular weight, high chromium binding ratio, good oral absorption effect, and the like, can play a hypoglycemic role in a plurality of links and has favorable market application prospect on the aspect of preventing and treating type II diabetes.

The invention provides a novel biological activity determination method of exendin-4-HAS Byetalog. The basic principle of the method is that a GLP-1R (Glucagon-Like Peptide-1R) and a cAMP (cyclic Adenosine Monophosphate) response element (CER) report gene carrier are used for co-transfection of a CHO-K1 cell, and the steps of pressurization, sieving and monoclonal separation and cultivation are carried out to obtain a stable monoclonal cell strain CHOglplr/crec14. After the GLP-1R is combined with a ligand, a series of signal transduction is carried out to stimulate the expression of CRE reporter gene luciferase, and the activity of the Byetalog is quantified by detecting the change of the expression of the luciferase after the Byetalog stimulates. The specific detection steps are as follows: 6000 CHOglplr/crec14 cells are placed on each pore of a 96-pore plate to be cultured for 16-18 hours; the Byetalog with different concentrations is added to stimulate the cells for 6 hours; the activity of the luciferase is detected. The method is simple to operate, sensitive in reaction and small in variability, and has very important meaning to quality control and clinical application of the Byetalog.

The invention provides a fusion protein of Exendin-4 and mutational human serum albumin and a preparation method of the fusion protein, belonging to the technical field of long-acting recombined fusion protein drugs. The invention relates to the fusion protein of Exendin-4 and human serum albumin (HSA) in which the 410-site is mutated to A (Ala alanine) from R (Arg arginine). The fusion protein comprises two polypeptide zones, wherein zone I is composed of two Exendin-4 repetitive sequences, and zone II is site-mutation human serum albumin (HSA); the zone I is directly connected with the N-terminal of the zone II by the C-terminal of the zone I without adding any connecting peptides therebetween; and the structure of the fusion protein is: (Exendin-4)2-HSA (R410A). Compared with Exendin-4 and (Exendin-4)2-HAS, (Exendin-4)2-HSA (R410A) fusion protein provided by the invention has the characteristic of longer-lasting effect in vivo, and can be used for preparing long-lasting preparation of non-insulin-dependent diabetes.

The invention discloses a GLP-1 and GIP co-agonist compound. A series of human glucose-dependent insulinotropic polypeptide (GIP) based dual agonist compound and a pharmaceutical composition with available pharmaceutical salt is provided. The compound has dual agonist effects on human glucagon-like peptide-1 (GIP-1) receptors and human GIP receptors, and can be used for treating related diseases such as non-insulin dependent diabetes mellitus, insulin-dependent diabetes mellitus and obesity.

The invention relates to a novel glucagon analogue and application thereof. Compared with wild-type human GLP1, the novel glucagon analogue has a longer half-life period and a better insulin secretionpromotion activity, and a strong long-acting blood glucose reducing effect.

The invention relates to an HSA (Human Serum Albumin) long-acting fusion protein and a rapid assembly, separation and purification method thereof. The fusion protein comprises two polypeptide regions, wherein the first region is formed by a repetitive sequence of Exendin-4, the second region is formed by a sequence of the HSA, the C-end of the first region is connected with the N-end of the second region via glycine and serine, or the N-end of the first region is connected with the C-end of the second region via glycine and serine. The Exendin-4 is repeated for once to 4 times, and the repetitive sequence of the Exendin-4 is directly connected via glycine and serine. By adopting a Bglbrick method by the invention, an arbitrary number of Exendin-4 can be arbitrarily added on the N-end or C-end of the HSA, then high-purity fusion protein is acquired through expression and purification.

The invention belongs to the field of genetic engineering and biopharmaceuticals, and discloses a recombinant expression method of a Brevinin-2GUb polypeptide, wherein the method comprises the steps:(1) inserting a Brevinin-2GUb gene into pET32-series vectors containing thioredoxin, histone labels and enterokinase digestion sites, to obtain recombinant expression vectors; (2) transforming the recombinant expression vectors into escherichia coli to obtain recombinant expression engineering strains; (3) carrying out inducible expression on the engineering strains, centrifuging to collect bacteria, crushing, centrifuging to obtain a supernatant, and carrying out nickel ion affinity chromatography on the supernatant to obtain a fusion protein; and (4) dialysing the fusion protein with an enterokinase digestion buffer, then cutting the fusion protein by enterokinase, carrying out nickel ion affinity chromatography, then concentrating to obtain the target polypeptide without labels. The polypeptide can significantly promote insulin secretion activity in INS-1 cells at low concentration, and can be used for preparing hypoglycemic polypeptide drugs.

The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

The invention belongs to the technical field of medicines and discloses a medicinal composition for treating diabetes and preventing and treating diabetic complications and pharmaceutic use thereof. The medicinal composition consists of a chemical medicinal and a Chinese medicine extract and particularly consists of Glinide insulin secretagogue and cinnamon extract. The medicinal composition disclosed by the invention has remarkable treatment effect on diabetes, can effectively control the occurrence of diabetic complications, is low in adverse reaction, safer and more reliable than chemical medicine used alone and can reduce the dose of Glinide insulin secretagogue.

The invention relates to configurational isomers 4-hydroxyisoleucine, and to lactones, pharmaceutically acceptable salts, and prodrugs thereof, to processes for their preparation, and to pharmaceutical compositions comprising the same. The isomers of the invention exhibit insulinotropic activity and thus may be useful for the prevention and treatment of disorders of carbohydrate or lipid metabolism, including diabetes mellitus (type 1 and type 2 diabetes), pre-diabetes, and Metabolic Syndrome.

The present invention relates to a method of treating an incretin related disease such as diabetes, obesity and the like by delivery of long chain fatty acid to the colon by bypassing the upper digestive tract.

Insulin dimers conjugated to peptides having at least one incretin activity are disclosed.