Abstract: A long-acting conjugate of a triple agonist which has activities to all of glucagon, GLP-1, and GIP receptors and uses thereof.

Abstract: Disclosed is a protein complex, comprising a physiologically active polypeptide, a dimeric protein and a non-peptidyl polymer having three functional ends (3-arm), with the linkage of both the physiologically active polypeptide and the dimeric protein to the 3-arm non-peptidyl polymer via respective covalent bonds. The protein complex guarantees the long acting activity and biostability of a physiologically active polypeptide. Having the ability to maintain the bioactivity of physiologically active polypeptides or peptides highly and to significantly improve the serum half life of the polypeptides or peptides, the protein complex can be applied to the development of sustained release formulations of various physiologically active polypeptide drugs. Also, it utilizes raw materials including the physiologically active polypeptides without significant loss, thereby increasing the production yield. Further, it can be easily purified.

Abstract: A sustained release preparation of a human growth hormone conjugate is disclosed. The sustained release preparation contains a sustained release human growth hormone (hGH) conjugate resulting from conjugation between an immunoglobulin Fc region and a human growth hormone (hGH) as an active peptide; a buffer solution; a nonionic surfactant; and a sugar alcohol. A freeze dried preparation and a liquid preparation including the sustained release human growth hormone conjugate, a production method for the freeze dried preparation, a method of reconstituting the freeze dried preparation, and a kit containing the freeze dried preparation and a reconstituting solution are also disclosed.

Abstract: The present invention relates to a sustained type human growth hormone conjugate preparation comprising: a sustained type human growth hormone (hGH) conjugate resulting from conjugation between the immunoglobulin Fc region and a human growth hormone (hGH) constituting a bioactive peptide; a buffer solution; a nonionic surfactant; and a sugar alcohol. More specifically, the present invention relates to a sustained type human growth hormone conjugate freeze dried preparation and liquid preparation, to a production method for the freeze dried preparation, to a method of reconstituting the freeze dried preparation, and to a kit comprising the freeze dried preparation and a reconstituting solution.

Abstract: The present invention relates to a liquid formulation of long-acting insulin conjugate, comprising a pharmaceutically effective amount of a long-acting insulin conjugate, wherein a physiologically active peptide, which is an insulin, is linked to an immunoglobulin Fc region; and an albumin-free stabilizer, wherein the stabilizer comprises a buffer, a sugar alcohol, a non-ionic surfactant, and an isotonic agent, and a method for preparing the formulation. For preventing microbial contamination in multiple uses, a preservative can be added to the formulation. The liquid formulation of the present invention does not comprise a human serum albumin and potentially hazardous factors to body, and thus it has excellent storage stability for insulin conjugate without a risk of viral infection.

Abstract: A long-acting conjugate of a triple agonist which has activities to all of glucagon, GLP-1, and GIP receptors and uses thereof.

Abstract: The present invention relates to a conjugate in which an immunoglobulin Fc region is linked to therapeutic enzymes through a non-peptide polymer linkage moiety, and more specifically, to a conjugate in which a non-peptide polymer linkage moiety is specifically linked to an immunoglobulin Fc, a method of preparing the same, and a composition comprising the same.

Abstract: The present invention relates to insulin and/or an insulin analogue conjugate, and a use thereof, wherein the insulin and/or insulin analogue have improved in vivo durability and stability by linking the same with an Fc region of immunoglobulin. The insulin and/or an insulin analogue conjugate of the present invention show an in vivo activity similar to that of insulin. In addition, the insulin and/or insulin analogue conjugate of the present invention are long-acting formulations of insulin and/or the analogue thereof, in which serum half-life is remarkably increased, and therefore, the present invention provides remarkable insulin and/or an insulin analogue conjugate, which do not induce hypoglycemia, a drawback of insulin treatment.

Abstract: The present invention relates to a novel glucagon derivative peptide, and a composition for preventing or treating hypoglycemia containing the novel glucagon derivative peptide as an active ingredient. The glucagon derivative according to the present invention has improved physical properties due to the change in isoelectric point (pI) while being capable of maintaining an activity on glucagon receptors, and thus can improve patient compliance when used as a hypoglycemic agent, and is also suitable for administration in combination with other anti-obesity agents. Accordingly, the glucagon derivative according to the present invention can be effectively used for the prevention and treatment of hypoglycemia and obesity.

Abstract: An insulin conjugate having improved in vivo duration and stability is provided. The conjugate is prepared by covalently linking insulin with an immunoglobulin Fc region via a non-peptidyl polymer, a long-acting formulation comprising the same, and a preparation method thereof. The insulin conjugate of the present invention maintains in vivo activity of the peptide at a relatively high level and remarkably increases the serum half-life thereof, thereby greatly improving drug compliance upon insulin treatment.

Abstract: Provided is a conjugate in which an immunoglobulin Fc region is linked to an iduronate-2-sulfatase enzyme through a non-peptide polymer linker moiety. Further, provided are a conjugate, a method for preparing the same, and a composition including the same in which a non-peptide polymer linker moiety is specifically linked to an immunoglobulin Fc.

Abstract: A method for preparing a conjugate by linking a physiologically active polypeptide, a non-peptidyl polymer linker, and an immunoglobulin constant region via a covalent bond are disclosed. The method enables an efficient preparation of a physiologically active polypeptide conjugate, in which a salt is used in a coupling reaction to improve the problem of low production yield during preparation of the physiologically active polypeptide conjugate.

Abstract: An insulin analog with an improved in vitro effect compared with native insulin, a pharmaceutical composition for treating diabetes containing the insulin analog as an active ingredient, and a method for treating diabetes using the insulin analog or the pharmaceutical composition are described. A nucleic acid encoding the insulin analog, an expression vector including the nucleic acid, a transformant introduced with the expression vector, and a method of producing the insulin analog from the transformant are also described.

Abstract: The present invention relates to a novel peptide of a glucagon derivative and a composition for preventing or treating obesity comprising the peptide as an active ingredient. The glucagon derivative according to the present invention shows a more excellent activating effect with regard to both glucagon-like peptide-1 receptors and glucagon receptors compared to native glucagon, and thus can be widely used as an effective agent for treating obesity.

Abstract: The present invention relates to an insulin analog conjugate and use thereof.

Abstract: Provided is a complex composition, of which positional isomers are minimized by using a N-terminus of an immunoglobulin Fc region as a binding site when the immunoglobulin Fc region is used as a carrier. Also provided are a protein complex which is prepared by N-terminal-specific binding of immunoglobulin Fc region, thereby prolonging blood half-life of the physiologically active polypeptide, maintaining in vivo potency at a high level, and having no risk of immune responses, a preparation method thereof, and a pharmaceutical composition including the same for improving in vivo duration and stability of the physiologically active polypeptide. The protein complex may be usefully applied to the development of long-acting formulations of various physiologically active polypeptide drugs.

Abstract: Disclosed are a composition for preventing or treating diabetes, disbesity or diabetic complications, containing an oxyntomodulin analog as an active ingredient and a method for treating diabetes, diabesity or diabetic complications, including administering a pharmaceutically effective amount of an oxyntomodulin analog to a subject. The oxyntomodulin analog shows a greater activity to activate a GLP-1 receptor and a glucagon receptor, than native oxyntomodulin. The oxyntomodulin analog induces an expansion of beta-cells and increases insulin secretion, thereby reducing blood glucose levels that were increased due to a high-calorie and high-fat diet. The oxyntomodulin analog induces decreases in a body weight and appetite to improve insulin sensitivity and is useful in maintaining normal blood glucose levels.

Abstract: The present invention relates to a novel peptide of a glucagon derivative and a composition for preventing or treating obesity comprising the peptide as an active ingredient. The glucagon derivative according to the present invention shows a more excellent activating effect with regard to both glucagon-like peptide-1 receptors and glucagon receptors compared to native glucagon, and thus can be widely used as an effective agent for treating obesity.

Abstract: The present invention relates to a composition for preventing or treating hyperlipidemia, fatty liver disease or arteriosclerosis, comprising an oxyntomodulin derivative as an active ingredient. The oxyntomodulin derivative has a high ability to activate GLP-1 receptor and glucagon receptor compared to native oxyntomodulin and has the effects of reducing the blood total cholesterol, low-density cholesterol and triglyceride levels that were increased by high-fat diet, and increasing high-density cholesterol levels and the high-density cholesterol/low-density cholesterol ratio. Thus, the oxyntomodulin derivative can be effectively used for the treatment of hyperlipidemia and related diseases.

Abstract: Provided is a long-acting pharmaceutical composition containing a conjugate comprising a physiologically active polypeptide linked to an immunoglobulin Fc fragment, wherein the composition contains a monomeric conjugate comprising one molecule of the physiologically active polypeptide linked to a single immunoglobulin Fc fragment, and optionally contains a multimeric conjugate comprising two or more molecules of the same physiologically active polypeptide linked to a single immunoglobulin Fc fragment, provided that the molar ratio of the monomeric conjugate to the multimeric conjugate in the composition is at least 19; a physiologically active polypeptide monomer-immunoglobulin Fc fragment conjugate that comprises a physiologically active polypeptide monomer linked via a non-peptidyl linker to an immunoglobulin Fc fragment, wherein the physiologically active polypeptide is linked via the non-peptidyl linker to the immunoglobulin Fc fragment in a monomeric form.