Method of treating melanocortin-4 receptor-associated disorders in heterozygous carriers
Inventors
Tartaglia, Louis Anthony • Henderson, Bart • Van Der Ploeg, Leonardus H. T.
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-10954268-B2
Publication Date
2021-03-23
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 disclosed invention relates to methods of treating obesity and metabolic syndrome by administering an agonist of the melanocortin-4 receptor (MC4R) to a subject in need thereof. The subject is defined as a heterozygous carrier of an MC4R mutation, and the administration is carried out with an effective amount of the MC4R agonist.
The disclosure provides a mechanistic rationale grounded in the leptin-melanocortin pathway and MC4R signaling. It describes obesity and metabolic syndrome as being associated with an attenuated MC4R response to alpha-melanocortin stimulating hormone (α-MSH), and proposes that restoring MC4R signaling yields sustained weight loss and metabolic improvements.
The specification further defines treatment-related terms and describes MC4R agonist embodiments including peptide agonists with specific sequences, together with associated chemical forms such as salts, hydrates, solvates, and prodrugs. It also includes hydantoin moiety-containing compounds defined by Formula (IV), Formula (V), Formula (VI), Formula (VII), and Formula (VIII).
Claims Coverage
The claim coverage includes two independent treatment claims. The inventive coverage centers on the subject genotype, being a heterozygous carrier of an MC4R mutation, and administering an effective amount of an MC4R agonist for two disease areas.
Treating obesity in a heterozygous MC4R mutation carrier
Administering an effective amount of an agonist of the melanocortin-4 receptor (MC4R), wherein the subject is a heterozygous carrier of an MC4R mutation.
Treating metabolic syndrome in a heterozygous MC4R mutation carrier
Administering an effective amount of an agonist of the melanocortin-4 receptor (MC4R), wherein the subject is a heterozygous carrier of an MC4R mutation.
Overall, the claims are directed to administering MC4R agonists at an effective amount to heterozygous carriers of an MC4R mutation for treating obesity and metabolic syndrome. Dependent claims further narrow the MC4R agonist embodiments to specific peptide sequences and may attribute the obesity or metabolic syndrome to an attenuated MC4R response to α-MSH, including embodiments limited to a human subject.
Stated Advantages
Restoring MC4R signaling yields sustained weight loss and metabolic improvements.
Documented Applications
Treating obesity in a subject in need thereof by administering an effective amount of an MC4R agonist to a heterozygous carrier of an MC4R mutation.
Treating metabolic syndrome in a subject in need thereof by administering an effective amount of an MC4R agonist to a heterozygous carrier of an MC4R mutation.
Interested in licensing this patent?