LONG-ACTING FATTY ACID-CONJUGATED GnRH DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
AssigneeNovel Pharma Inc.
InventorDong Kyu JIN
Life of this patent
Estimating the term…
Abstract
An aspect of the present disclosure pertains to a novel long-acting fatty acid-conjugated gonadotrophin-releasing hormone (GnRH) derivative and a pharmaceutical composition containing the same. A GnRH derivative of the present invention is expected to greatly contribute, through excellent bioavailability, increased half-life in blood, and remarkably high therapeutic effects on sex hormone-dependent disease, to the reduction in drug dosing frequency and dosage and the like in the treatment of sex hormone-dependent diseases. Particularly, the GnRH derivative can overcome the disadvantages of existing GnRH sustained-release preparations, which have the side effects of residual feeling and pain at the injection site.
Claims16
A pharmaceutical composition for preventing or treating a sex hormone-dependent disease, the pharmaceutical composition comprising:
- a long-acting fatty acid-conjugated gonadotropin-releasing hormone (GnRH) derivative in which the gonadotropin-releasing hormone (GnRH) derivative is conjugated with a fatty acid, or a pharmaceutically acceptable salt thereof as an active ingredient;
- and
- cyclodextrin,
- wherein the GnRH derivative comprises an amino acid sequence selected form the group consisting of SEQ ID NO:
- 2, and SEQ ID NOS:
- 4 to 11,
- wherein the fatty acid is a lauric acid, palmitic acid or arachidic acid,
- wherein a carboxyl group of the fatty acid of the GnRH derivative is conjugated through a peptide-bond to an amino terminus of the peptide portion of the GnRH derivative.
A method for preventing or treating a sex hormone-dependent disease, comprising administering a pharmaceutical composition to a patient in need thereof,
- wherein the pharmaceutical composition comprising:
- a long-acting fatty acid-conjugated gonadotropin-releasing hormone (GnRH) derivative in which the gonadotropin-releasing hormone (GnRH) derivative is conjugated with a fatty acid, or a pharmaceutically acceptable salt thereof as an active ingredient;
- and
- cyclodextrin,
- wherein the GnRH derivative comprises an amino acid sequence selected form the group consisting of SEQ ID NO:
- 2, and SEQ ID NOS:
- 4 to 11,
- wherein the fatty acid is a lauric acid, palmitic acid or arachidic acid,
- wherein a carboxyl group of the fatty acid of the GnRH derivative is conjugated through a peptide-bond to an amino terminus of the peptide portion of the GnRH derivative.
Dependencies are inferred from the claim text.