Method of treating melanocortin-4 receptor-associated disorders in heterozygous carriers
Inventors
Tartaglia, Louis Anthony • Henderson, Bart • Van Der Ploeg, Leonardus H.T.
Assignees
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Publication Number
US-12655178-B2
Publication Date
2026-06-16
Expiration Date
Abstract
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).
Core Innovation
The patent discloses a method of treating a disorder in a subject who is a heterozygous carrier of a melanocortin-4 receptor (MC4R) mutation, where the disorder results from an attenuated response of MC4R to α-melanocortin stimulating hormone (α-MSH). The method comprises administering an effective amount of an MC4R agonist peptide containing a specified peptide motif [procedural detail omitted for safety], or a pharmaceutical salt thereof. Disclosed agonists include cyclic peptides and hydantoin-modified peptides.
The addressed disorders include obesity and metabolic syndrome associated with impaired MC4R signaling. Infusion of an MC4R agonist produces weight loss in MC4R+/- mice, whereas MC4R-/- mice show no significant weight loss. A planned study evaluates continuous subcutaneous infusion in obese patients with heterozygous MC4R mutations, assessing weight loss, safety, pharmacokinetics, and exploratory metabolic and behavioral endpoints.
Claims Coverage
The claims identify one independent claim comprising four claim elements directed to treating a disorder resulting from an attenuated MC4R response to α-MSH in a heterozygous MC4R mutation carrier.
Treatment by administration of an MC4R agonist
The method treats a disorder in a subject in need thereof by administering an effective amount of an agonist of the melanocortin-4 receptor (MC4R).
Peptide MC4R agonist containing a specified peptide motif
The MC4R agonist is a peptide containing a specified peptide motif [procedural detail omitted for safety], or a pharmaceutical salt thereof. Dependent claims specify agonist forms and exclude ACTH.
Heterozygous carrier of an MC4R mutation
The subject is a heterozygous carrier of an MC4R mutation.
Disorder resulting from attenuated MC4R response to α-MSH
The disorder results from an attenuated response of MC4R to α-melanocortin stimulating hormone (α-MSH).
The independent claim covers administering a peptide MC4R agonist, or a pharmaceutical salt thereof, to a heterozygous MC4R mutation carrier for a disorder resulting from an attenuated MC4R response to α-MSH. Dependent claims further specify the agonist structure and narrow the disorder to obesity and metabolic syndrome.
Stated Advantages
The specification identifies sustained weight loss and improvements in metabolic measures as potential benefits.
Infusion of an MC4R agonist produced weight loss in MC4R+/- mice, whereas MC4R-/- mice showed no significant weight loss.
Documented Applications
Treatment of a disorder resulting from an attenuated MC4R response to α-MSH in a heterozygous carrier of an MC4R mutation, including obesity and metabolic syndrome.
Peripheral administration of an MC4R peptide agonist, including continuous subcutaneous infusion.
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