35results about "Melanocyte-stimulating hormone" patented technology

The present invention provides methods of using non-naturally occurring melanocortin analogs to increase body weight and / or increase food consumption in a subject having a kidney disease and / or a liver disease (e.g., chronic kidney disease, renal failure, non-alcoholic fatty liver disease (NAFLD)). Also provided are methods of stimulating appetite in a subject via administration of a non-naturally occurring melanocortin analogue. The non-naturally occurring melanocortin analogs may be present in pharmaceutical compositions and delivered via parenteral administration (e.g., subcutaneous injection). The methods improve appetite, increase food consumption, increase body weight, muscle mass, and / or fat mass in the subject.

The present technology comprises stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin analogs. In some embodiments, the non-naturally occurring melanocortin analogs may be agonists or antagonists of the melanocortin 5 receptor (MC5R) with sub-micromolar or low-nanomolar binding activity. In some embodiments, the present technology comprises a pharmaceutical composition having a pH of about 4.0 to about 6.5, comprising a non-naturally occurring melanocortin analog having at least one cationic amino acid residue, an osmolyte, a pH adjusting agent, and a buffer.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

A linker for linking a therapeutic agent to another moiety, such as the Fc region of an antibody. A linker having two or more maleimide functional groups capable of undergoing a nucleophilic conjugate addition reaction. A method for increasing the duration of action of a therapeutic agent by conjugating it to a novel linker and the Fc region of an antibody. An antibody-drug conjugate having an increased duration of action over the drug alone.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor and full or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.

The present technology comprises pharmaceutical compositions of non-naturally occurring melanocortin analogs formulated for oral administration. The non-naturally occurring melanocortin analogs may be agonists or antagonists of the melanocortin 4 receptor (MC4R) and / or the melanocortin 3 receptor (MC3R) with sub-micromolar or low-nanomolar binding activity, or may be agonists of the melanocortin 1 receptor (MC1R) with sub-micromolar or low-nanomolar binding activity.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor and full or partial agonists of the melanocortin 4 receptor with sub-micromolar and / or low-nanomolar binding activity.

Provided herein are non-naturally occurring melanocortin analogs or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof and compositions comprising the same. The melanocortin analogs are agonists or antagonists of melanocortin 3 and / or 4 receptors with sub-micromolar or low-nanomolar binding activity.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full or partial antagonists of the melanocortin 3 receptor with sub-micromolar or low-nanomolar binding activity. Some of the non-naturally occurring melanocortin analogs may also be full or partial antagonists or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.

Provided herein are methods of treating, preventing, or reducing one or more symptoms or conditions associated with metabolic dysfunction, such as obesity, in a subject in need thereof using a non-naturally occurring melanocortin analog. In some embodiments, the non-naturally occurring melanocortin analog is administered orally. In some embodiments, the method comprises suppressing appetite in a subject in need thereof using a non-naturally occurring melanocortin analog in accordance with the present technology.

The disclosure relates to compositions and methods comprising MSH analogs and cell therapy.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may exhibit (i) full MC4R antagonism and full, partial, or no MC3R agonism; (ii) partial MC4R antagonism and no MC3R activity; or (iii) full MC4R agonism and full MC3R antagonism with sub-micromolar or low-nanomolar binding activity.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full or partial antagonists of the melanocortin 3 receptor with sub-micromolar or low-nanomolar binding activity. Some of the non-naturally occurring melanocortin analogs may also be full or partial antagonists or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor and full or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.

Provided herein are non-naturally occurring melanocortin analogs that selectively bind at least a portion of a melanocortin receptor The melanocortin receptor may be a melanocortin 3 receptor (MC3R) or a melanocortin 4 receptor (MC4R). The non-naturally occurring melanocortin analogs may have a dissociation constant (Kd) value for a melanocortin receptor or one or more amino acids thereof that is less than that of a conventional melanocortin analog.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

Provided herein are non-naturally occurring melanocortin analogs or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof and compositions comprising the same. The melanocortin analogs are agonists or antagonists of melanocortin 3 and / or 4 receptors with sub-micromolar or low-nanomolar binding activity.

A recombinant protein comprising multiple multi-peptide sets includes first through fifth sequencing primers and first through fourth multi-peptide regions. The first multi-peptide region is between the first and the second sequencing primers. The second multi-peptide region is between the second and the third sequencing primers. The third multi-peptide region is between the third and the fourth sequencing primers. The fourth multi-peptide region is between the fourth and the fifth sequencing primers. In each of the multi-peptide regions, multiple functional peptides can be inserted, and manufacturing thereof can be done through expression of the recombinant protein, thereby significantly enhancing the concentrations of the functional peptides. With the combination of peptide having different functions, the recombinant protein product can provide more complete and more comprehensive functionality. This application also discloses a pharmaceutical composition comprising the recombinant protein and a method for preparing the recombinant protein.

A method of treating a disorder in a subject. The method comprises administering to said subject an effective amount of an agonist of the melanocortin-4 receptor (MC4R). The subject is a heterozygous carrier of an MC4R mutation, and the disorder results from an attenuated response of MC4R to α-melanocortin stimulating hormone (α-MSH).

Provided herein are stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin antagonist analogs. The non-naturally occurring melanocortin antagonist analog comprises a sequence of Formula (I) Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may selectively bind the melanocortin 3 receptor and / or the melanocortin 4 receptor over the melanocortin 1, melanocortin 2, and melanocortin 5 receptors. In some embodiments, the non-naturally occurring melanocortin analogs are antagonists of melanocortin 3 and / or 4 receptors with sub-micromolar or low-nanomolar binding activity.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. In some embodiments, the non-naturally occurring melanocortin analogs may be agonists of melanocortin 1 which have sub-micromolar or low-nanomolar binding activity. The non-naturally occurring melanocortin analogs may be present in a composition that is formulated for delivery to a subject in need thereof.

Methods are provided for increasing body weight and / or food consumption in subjects with kidney disease and / or liver disease (e.g., chronic kidney disease, renal failure, nonalcoholic fatty liver disease (NAFLD)) using a non-naturally occurring melanocortin analog. Methods are also provided for stimulating a subject's appetite by administering a non-naturally occurring melanocortin analog. The non-naturally occurring melanocortin analog can be present in a pharmaceutical composition and can be delivered via parenteral administration (e.g., subcutaneous injection). The methods improve a subject's appetite, increase food consumption, and increase body weight, muscle mass, and / or fat mass.

Provided herein are non-naturally occurring melanocortin analogs. The non-naturally occurring melanocortin analogs of the present technology may be useful in treating, preventing, reducing, or otherwise ameliorating one or more disorders associated with the melanocortin system. In some embodiments, the non-naturally occurring melanocortin analog is administered orally to a subject in need thereof.

Provided are methods of increasing body weight of and / or increasing food consumption in a subject having a kidney disease and / or a liver disease (e.g., chronic kidney disease, renal failure, nonalcoholic fatty liver disease (NAFLD)) using non-naturally occurring melanocortin analogs. Also provided are methods of stimulating appetite in the subject via administration of non-naturally occurring melanocortin analogs. The non-naturally occurring melanocortin analog may be present in a pharmaceutical composition and delivered via parenteral administration (e.g., subcutaneous injection). The methods improve appetite, increase food consumption, increase body weight, muscle mass, and / or fat mass of the subject.

Provided are methods of increasing body weight of and / or increasing food consumption in a metabolically unchallenged subject using non-naturally occurring melanocortin analogs. Also provided are methods of stimulating appetite in a subject via administration of non-naturally occurring melanocortin analogs. The non-naturally occurring melanocortin analog can be present in a pharmaceutical composition and delivered via parenteral administration (e.g., subcutaneous injection). The methods improve appetite, increase food consumption, increase body weight, muscle mass, and / or fat mass of the subject.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

Provided herein are stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin agonist analogs. The non-naturally occurring melanocortin agonist analog comprises a sequence of Formula (I): Ac-Nle-c[Glu-Pro-p(F)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

Provided herein are pharmaceutical compositions of non-naturally occurring melanocortin agonist analogs formulated for oral administration. The non-naturally occurring melanocortin agonist analog comprises a sequence of Formula (I): Ac-Nle-c[Glu-Pro-p(F)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.