IP Library › Granted Patent US 9,200,054
Granted Patent B2
US 9,200,054 · App. 14/030,970 · Granted Dec 1, 2015

Somatostatin analogs with inhibitory activity to growth hormone release

Inventors: Murray Goodman (La Jolla, CA); Sandra Blaj Moore (London, GB)
Assignee: The Regents of the University of California
C07K14/6555A61K51/08A61K51/083
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Quick Facts
Patent No.
US 9,200,054
App. No.
14/030,970
Granted
Dec 1, 2015
Kind
B2
Abstract

Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.

Claims (16)

1. A method for reducing the release of growth hormone and/or thyroid stimulating hormone from the anterior pituitary of a subject, comprising administering an effective amount of a compound selected from any one of 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 (SEQ ID NO:1); 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Asp-NH 2 ; 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Thr-NH 2 ; 4-amino-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 ; and D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 , or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein administering the compound reduces the subject's blood levels of growth hormone in comparison to the subject's growth hormone level prior to receiving the compound.

3. The method of claim 2 , wherein the subject is a patient characterized by having elevated blood levels of growth hormone.

4. The method of claim 3 , where the subject has acromegaly.

5. The method of claim 1 , wherein administering the compound reduces the subject's blood levels of thyroid stimulating hormone (TSH) in comparison to the subject's TSH level prior to receiving the compound.

6. The method of claim 1 , wherein the compound is administered intravenously or subcutaneously.

7. A method for reducing the release of insulin and/or glucagon from the pancreas of a subject, comprising administering an effective amount of a compound selected from any one of 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 (SEQ ID NO:1); 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Asp-NH 2 ; 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Thr-NH 2 ; 4-amino-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 ; and D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 , or a pharmaceutically acceptable salt thereof.

8. The method of claim 7 , wherein administering the compound results in an increase in the subject's blood glucose levels in comparison to the subject's glucose level prior to receiving the compound.

9. The method of claim 7 , wherein the subject is a patient characterized by having hypoglycemia.

10. The method of claim 9 , wherein the subject has hypoglycemia from insulin treatment for diabetes mellitus.

11. The method of claim 7 , wherein the compound is administered intravenously or subcutaneously.

12. A method for reducing the activity and growth of a tumor in a subject, comprising administering an effective amount of a compound selected from any one of 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 (SEQ ID NO:1); 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Asp-NH 2 ; 4-amino-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-D-Thr-NH 2 ; 4-amino-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH 2 ; 4-amino-3-iodo-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 ; and D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH 2 , or a pharmaceutically acceptable salt thereof.

13. The method of claim 12 , wherein administering the compound results in a decrease in the secretory activity of the tumor in comparison to the secretory activity prior to administering the compound.

14. The method of claim 12 , wherein the tumor is a growth hormone-producing adenoma, TSH-producing adenoma, endocrine inactive adenoma, carcinoid, islet-cell carcinoma, a pancreatic hormone secreting tumor, or a gastrointestinal secreting tumor.

15. The method of claim 14 , wherein the tumor is a carcinoid.

16. The method of claim 12 , wherein the compound is administered intravenously or subcutaneously.

Assignments (1)
CONFIRMATORY LICENSE Recorded Nov 19, 2013
From: UNIVERSITY OF CALIFORNIA SAN DIEGO
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 031674/0213 →
Continuity (4)
Continuation 13077659 · Mar 31, 2011
Division 10568112
Provisional Application 60496942 · Aug 20, 2003
Related Publication 20140179598A1 · Jun 26, 2014