IP Library Granted Patent US 12,453,755
Granted Patent B2
US 12,453,755 · App. 18/422,177 · Granted Oct 28, 2025

GIP/GLP1 agonist compositions

Inventors: Vincent John Corvari (Carmel, IN); Christopher Sears Minie (Zionsville, IN); Dinesh Shyamdeo Mishra (Carmel, IN); Ken Kangyi Qian (Carmel, IN)
Assignee: ELI LILLY AND COMPANY
A61K38/16A61K9/0019A61K47/02A61K47/10A61M5/20
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 12,453,755
App. No.
18/422,177
Granted
Oct 28, 2025
Kind
B2
Abstract

A composition of tirzepatide, comprising an agent selected from NaCl and propylene glycol; and dibasic sodium phosphate is provided.

Claims (16)

1. A method of treating diabetes comprising administering to a human in need thereof an effective dose of a pharmaceutical composition comprising tirzepatide, or pharmaceutically acceptable salt thereof, at a concentration from about 5 mg/mL to about 30 mg/ml; dibasic sodium phosphate at a concentration from about 0.67 to about 2.68 mg/ml; NaCl at a concentration from about 6.2 mg/ml to about 9.5 mg/ml; and optionally comprising from about 3.0 mg/ml to about 7.0 mg/ml phenol.

2. A method of treating diabetes as claimed by claim 1 wherein the dose is administered using an automatic injection apparatus.

3. A method of treating diabetes as claimed by claim 2 wherein the dose is administered once weekly.

4. A method of treating diabetes comprising administering to a human in need thereof an effective dose of a pharmaceutical composition comprising tirzepatide, or a pharmaceutically acceptable salt thereof;

NaCl at a concentration from about 6.2 mg/mL to about 9.5 mg/mL; and

dibasic sodium phosphate.

5. A method as claimed by claim 4 , wherein the tirzepatide, or a pharmaceutically acceptable salt thereof, is at a concentration from about 5 mg/ml to about 30 mg/mL.

6. A method as claimed by claim 5 wherein the dibasic sodium phosphate is at a concentration from about 1 mg/ml to about 3 mg/mL.

7. A method as claimed by claim 4 wherein the dibasic sodium phosphate is at a concentration from about 0.67 mg/ml to about 2.68 mg/mL.

8. A method as claimed by claim 7 wherein the dibasic sodium phosphate concentration is about 1.34 mg/mL.

9. A method as claimed by claim 8 wherein tirzepatide, or a pharmaceutically acceptable salt thereof, is at a concentration selected from the group consisting of 5 mg/ml, 10 mg/ml, 15 mg/mL, 20 mg/mL, 25 mg/mL, and 30 mg/mL.

10. A method as claimed by claim 5 wherein the NaCl concentration is from about 7.0 mg/ml to about 9.0 mg/mL.

11. A method as claimed by claim 10 wherein the NaCl concentration is about 8.2 mg/mL.

12. A method as claimed by claim 11 wherein the concentration of tirzepatide, or a pharmaceutically acceptable salt thereof, is selected from the group consisting of 5 mg/ml, 10 mg/mL, 15 mg/mL, 20 mg/mL, 25 mg/mL, and 30 mg/mL.

13. A method as claimed by claim 1 wherein the pharmaceutical composition has a is pH of 6.5 to 7.5.

14. A method of treating diabetes comprising administering to a human in need thereof an effective dose of a pharmaceutical composition comprising: (a) tirzepatide, or pharmaceutically acceptable salt thereof, at a concentration from about 5 mg/ml to about 30 mg/mL; (b) dibasic sodium phosphate, at a concentration of about 1.34 mg/ml; and (c) NaCl, at a concentration of about 8.2 mg/ml; and wherein the composition has a pH of 6.5 to 7.5.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 25, 2024
From: CORVARI, VINCENT JOHN; MINIE, CHRISTOPHER SEARS; MISHRA, DINESH SHYANDEO; QIAN, KEN KANGYI
To: ELI LILLY AND COMPANY
Reel/Frame 066244/0031 →
Continuity (4)
Continuation 17741067 · May 10, 2022
Continuation 16441329 · Jun 14, 2019
Provisional Application 62688632 · Jun 22, 2018
Related Publication 20240226229A1 · Jul 11, 2024
References Cited (61)
US 7084243B2 · Glaesner et al. · 2006 [cited by applicant]
US 7498308B2 · Glaesner et al. · 2009 [cited by applicant]
US 8114833B2 · Pedersen et al. · 2012 [cited by applicant]
US 8734394B2 · Adams et al. · 2014 [cited by applicant]
US 9474780B2 · Bokvist et al. · 2016 [cited by applicant]
US 11357820B2 · Corvari et al. · 2022 [cited by applicant]
US 20090232807A1 · Glaesner et al. · 2009 [cited by applicant]
US 20100196405A1 · Ng · 2010 [cited by applicant]
US 20120329708A1 · DiMarchi et al. · 2012 [cited by applicant]
US 20170136092A1 · Arnold et al. · 2017 [cited by applicant]
CN 103893744B · 2017 [cited by applicant]
EP 0619322A2 · 1994 [cited by applicant]
WO 2003002136A2 · 2003 [cited by applicant]
WO 2004105790A1 · 2004 [cited by applicant]
WO 2006051103A2 · 2006 [cited by applicant]
WO 2006051110A2 · 2006 [cited by applicant]
WO 2008019147A2 · 2008 [cited by applicant]
WO 2011094337 · 2011 [cited by applicant]
WO 2013164483A1 · 2013 [cited by applicant]
WO 2014005858A1 · 2014 [cited by applicant]
WO 2014166836A1 · 2014 [cited by applicant]
WO 2014202780A1 · 2014 [cited by applicant]
WO 2015022400A1 · 2015 [cited by applicant]
WO 2015071355A1 · 2015 [cited by applicant]
WO 2015104311A1 · 2015 [cited by applicant]
WO 2018103868A1 · 2018 [cited by applicant]
Chandra Mohan, Buffers, A guide for the preparation and use of buffers in biological systems, Calbiochem, 38 pages, EMD booklet 2014. [cited by applicant]
Product Description of Phosphate Buffered Saline, Smartbuffers, Medicago AB, 2 pages, 2010. [cited by applicant]
Phosphate Buffered Saline—Cold Harbor Protocols, 1 page, 2006. [cited by applicant]
Lachman, The Theory and Practice of Industrial Pharmacy, Varghese Publishing House, 11987, p. 190-193. [cited by applicant]
Aulton, The Science of Dosage Form Design, Pharmaceutics, Second Edition, 2002, p. 317. [cited by applicant]
Disodium Hydrogen Phosphate, Monograph, 2 pages. [cited by applicant]
Bydureon Prescribing Information, 2018, 49 pages. [cited by applicant]
Chabenne et al, J Diabetes Sci Technol, 2010, 4, 6, p. 1322-1331. [cited by applicant]
Selinsky, Membrane Protein Protocols, Methods in Molecular Biology, 2003, 228, 3 pages. [cited by applicant]
Larsen et al, Diabetes, 2001, 50, 11, p. 2530-3539. [cited by applicant]
Norregaard, et al, Diabetes Obes Metabl, 2018, 20 p. 60-68. [cited by applicant]
Frokjaer et al, Pharmaceutical Formulation Development of Peptides, 2000, pp. 124, 125, 150, 151. [cited by applicant]
Swarbrick, Encylopedia of Pharmaceutical Technology, vol. 1, 3rd Edition, 2007, p. 1266-1278. [cited by applicant]
Gibson, Pharmaceutical Preformulation and Formulation, 2009, 2nd ed, p. 325-328. [cited by applicant]
FDA Highlights of Prescribing Information Ozempic, 2017, 44 pages. [cited by applicant]
FDA Highlights of Prescribing Information Victoza, 2017, 40 pages. [cited by applicant]
Rowe, et al., Handbook of Pharmaceutical Excipients, 2009, 6th ed, p. 637-639. [cited by applicant]
Nema, et al., Pharmaceutical Dosage Forms, Formulation and Packaging, vol. 1, p. 232-237. [cited by applicant]
SO, Improving Patient Compliance with Biopharmaceuticals by Reducing Injection-Associated Pain, Journal of Mucopolysaccharidosis and Rare Diseases, 2015, p. 15-18. [cited by applicant]
Coskun et al, Molecular Metabolism, 2018, 18, 3-14. [cited by applicant]
Cleland et al, Formulation and Delivery of Proteins and Peptides, 1994, Chapter 1, 19 pages. [cited by applicant]
Saxenda—Prescribing Information, 2014, 40 pages. [cited by applicant]
Yu et al, Advanceed Drug Del Rev, 2018, 130, 113-130. [cited by applicant]
Tresiba Prescribing Instructions, 2018, 35 pages. [cited by applicant]
Egrifta Prescribing Instructions, 2015, 21 pages. [cited by applicant]
Wang and Hanson, Jo Parenteral Science and Technology, 1988, 42, 2S, S4-S25. [cited by applicant]
Chang et al., Lypophilized Biologics and Vaccines, Lypophilized Biologics, 2016, p. 93-119. [cited by applicant]
Arturk et al, Jo of Diabetes Science and Technology, 2024, p. 1-5. [cited by applicant]
EP Opposition of EP3810201—Preliminary Opinion, 2025, 9 pages. [cited by applicant]
Fransson, J., & Espander-Jansson, A. (1996). Local tolerance of subcutaneous injections. [cited by applicant]
Williamson, A.; Hoggart,(2005)Pain: A review of three commonly used pain rating scales. [cited by applicant]
Millican, R.L., et al, Diabetes, Suppl., Abstract Book, A363 1504-P 65 [cited by applicant]
Laursen, T., Hansen, B., & Fisker, S. (2006). Pain perception after subcutaneous injections of media containing different buffers. [cited by applicant]
Troy, Editor, (2006) [cited by applicant]
Saha, J. K., Xia, J., Millican, R., Grondin, J. M., Glaesner, W., & Jakubowski, J. A. (2007). DPP-4 Resistant Glucagon-Like Peptide-1 Analog LY548806: A Novel Agent for Control of Acute Hyperglycemia. [cited by applicant]
Cited By (1)
US 12,629,404