IP Library Granted Patent US 12,365,716
Granted Patent B2
US 12,365,716 · App. 18/057,398 · Granted Jul 22, 2025

Incretin analogs and uses thereof

Inventors: Jorge Alsina-Fernandez (Indianapolis, IN); Tamer Coskun (Carmel, IN); Lili Guo (Carmel, IN); Hongchang Qu (Carmel, IN)
Assignee: ELI LILLY AND COMPANY
C07K14/605A61K38/00
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 12,365,716
App. No.
18/057,398
Granted
Jul 22, 2025
Kind
B2
Abstract

Incretin analogs are provided that have activity at each of the GIP, GLP-1 and glucagon receptors. The incretin analogs have structural features resulting in balanced activity and extended duration of action at each of these receptors. Methods also are provided for treating diseases such as diabetes mellitus, dyslipidemia, fatty liver disease, metabolic syndrome, non-alcoholic steatohepatitis and obesity.

Claims (17)

1. A method of treating a disease selected from the group consisting of diabetes mellitus, obesity, fatty liver disease, non-alcoholic steatohepatitis, dyslipidemia and metabolic syndrome, the method comprising a step of:

administering to an individual in need thereof an effective amount of an incretin analog having a formula of SEQ ID NO: 17, or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the disease is obesity.

3. The method of claim 1 , wherein the disease is type II diabetes mellitus.

4. The method of claim 1 , wherein the disease is fatty liver disease.

5. The method of claim 1 , wherein the disease is non-alcoholic steatohepatitis.

6. The method of claim 1 , wherein the disease is dyslipidemia.

7. The method of claim 1 , wherein the disease is metabolic syndrome.

8. A method of treating a disease selected from the group consisting of diabetes mellitus, obesity, fatty liver disease, non-alcoholic steatohepatitis, dyslipidemia and metabolic syndrome, the method comprising a step of:

a administering to an individual in need thereof an effective amount of an incretin analog having a formula of:

or a pharmaceutically acceptable salt thereof.

9. The method of claim 8 , wherein the disease is obesity.

10. The method of claim 8 , wherein the disease is type II diabetes mellitus.

11. The method of claim 8 , wherein the disease is fatty liver disease.

12. The method of claim 8 , wherein the disease is non-alcoholic steatohepatitis.

13. The method of claim 8 , wherein the disease is dyslipidemia.

14. The method of claim 8 , wherein the disease is metabolic syndrome.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 3, 2025
From: ALSINA-FERNANDEZ, JORGE; COSKUN, TAMER; GUO, LILI; QU, HONGCHANG
To: ELI LILLY AND COMPANY
Reel/Frame 070383/0466 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 22, 2022
From: ALSINA-FERNANDEZ, JORGE; COSKUN, TAMER; GUO, LILI; QU, HONGCHANG
To: ELI LILLY AND COMPANY
Reel/Frame 061850/0343 →
Continuity (3)
Continuation 16768960
Provisional Application 62608613 · Dec 21, 2017
Related Publication 20230203121A1 · Jun 29, 2023
References Cited (17)
US 10400020B2 · Oh et al. · 2019 [cited by applicant]
US 11542313B2 · Alsina-Fernandez · 2023 [cited by examiner]
WO 2010108937A3 · 2010 [cited by applicant]
WO 2014049610A2 · 2014 [cited by applicant]
WO 2015067715A2 · 2015 [cited by applicant]
WO 2015067716A1 · 2015 [cited by applicant]
WO 2016198624A1 · 2016 [cited by applicant]
WO 2017116204A1 · 2017 [cited by applicant]
WO WO2019125938A1 · 2019 [cited by examiner]
Nørregaard, P. K., Deryabina, M. A., Tofteng Shelton, P., Fog, J. U., Daugaard, J. R., Eriksson, P. O., . . . & Jessen, L. (2018). A novel GIP analogue, ZP 4165, enhances glucagon-like peptide-1-induced body weight loss… [cited by applicant]
Bachem, Peptides in Diabetes, Peptide Trends, Oct. 2017. [cited by applicant]
Coskun T, Sloop KW, Loghin C, Alsina-Fernandez J, Urva S, Bokvist KB, Cui X, Briere DA, Cabrera O, Roell WC, et al. 2018 LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellit… [cited by applicant]
Frias, J. P., Nauck, M. A., Van, J., Kutner, M. E., Cui, X., Benson, C., . . . & Haupt, A. (2018). Efficacy and safety of LY3298176, a novel dual GIP and GLP-1 receptor agonist, in patients with type 2 diabetes: a rando… [cited by applicant]
International Searching Authority, International Search Report for PCT/US2018/065605, Dated Mar. 27,. [cited by applicant]
International Searching Authority, Written Opinion for PCT/US2018/065605, Dated Mar. 27, 2019. [cited by applicant]
Jensen, L., Helleberg, H., Roffel, A., van Lier, J. J., Bjørnsdottir, I., Pedersen, P. J., . . . & Pedersen, M. L. (2017). Absorption, metabolism and excretion of the GLP-1 analogue semaglutide in humans and nonclinical… [cited by applicant]
Betts J. M. and Russell R. B (2003) Amino Acid Properties and Consequences of Substitutions. In MR Barnes and IC Gray (Eds.) Bioinformatics for Geneticists pp. 289-316. [cited by applicant]