Granted Patent B2

US 12,364,700 · App. 18/230,693 · Granted Jul 22, 2025

Inventors: Thomas Meinicke (Mittelbiberach, DE); Maximilian Von Eynatten (Wiesbaden, DE)

Assignee: Boehringer Ingelheim International GmbH

A61K31/522A61K9/00A61K9/0053A61K9/20A61K9/2018A61K31/155A61K45/06A61K31/50

Abstract

Claims (34)

1. A method for treating a type 2 diabetes patient having estimated glomerular filtration rate (eGFR) levels down to 30 mL/minute/1.73 m 2 , comprising administering to the patient an effective amount of linagliptin, or a pharmaceutically acceptable salt thereof, in combination with metformin, and optionally one or more further active agents selected from the group consisting of insulin and a sulfonylurea; wherein

the patient has both albuminuria and previous macrovascular disease.

2. The method of claim 1 , wherein the type 2 diabetes patient has an eGFR level down to 45 mL/minute/1.73 m 2 .

3. The method of claim 2 , wherein linagliptin and metformin are administered in a single pharmaceutical composition.

4. The method of claim 3 , wherein the linagliptin is present in the composition in a dosage strength of 2.5 mg; or of 5 mg.

5. The method of claim 4 , wherein the metformin is present in the composition in a dosage strength of 500 mg, 850 mg or 1000 mg in the form of immediate release metformin; or 500 mg, 750 mg, 1000 mg, 1500 mg or 2000 mg in the form of extended release metformin.

6. The method of claim 3 , wherein the pharmaceutical composition comprises 2.5 mg of linagliptin and 500 mg, 850 mg or 1000 mg of metformin in immediate release form, and optionally one or more pharmaceutically auxiliaries.

7. The method of claim 3 , wherein the pharmaceutical composition comprises 5 mg of linagliptin and 1000 mg of metformin in extended release form, and optionally one or more pharmaceutically auxiliaries, or

the pharmaceutical composition comprises 2.5 mg of linagliptin and 750 mg or 1000 mg of metformin in an extended release form, and optionally one or more pharmaceutically auxiliaries.

8. The method of claim 1 , wherein linagliptin is administered in a total oral daily dose of 5 mg.

9. The method of claim 1 , wherein linagliptin is administered in a total oral daily dose of 5 mg, wherein the 5 mg daily dose is administered as 2.5 mg linagliptin twice daily or 5 mg linagliptin once daily.

10. A method of treating a type 2 diabetes patient having eGFR level 30-44 mL/minute/1.73 m 2 , comprising administering to the patient an effective amount of linagliptin, or a pharmaceutically acceptable salt thereof, in combination with metformin,

wherein linagliptin and metformin are administered in a single oral dosage form comprising 2.5 mg linagliptin and 500 mg metformin, and optionally one or more pharmaceutically auxiliaries, and

wherein the single oral dosage form is administered orally twice daily to the patient, and wherein

the patient has both albuminuria and previous macrovascular disease.

11. The method of claim 1 , wherein the patient has an eGFR of 30-60 mL/minute/1.73 m 2 .

12. The method of claim 1 , wherein the patient has an eGFR of 45-59 mL/minute/1.73 m 2 .

13. The method of claim 1 , wherein the patient has an eGFR of 30-44 mL/minute/1.73 m 2 .

14. The method of claim 1 wherein the patient has:

renal impairment with an eGFR≥45-75 mL/min/1.73 m 2 with macro-albuminuria.

15. The method of claim 1 wherein the patient has:

i) albuminuria defined as urine albumin creatinine ratio (UACR)≥30 mg/g creatinine or ≥30 mg/l (milligram albumin per liter of urine) or ≥30 μg/min (microgram albumin per minute) or ≥30 mg/24 h (milligram albumin per 24 hours) and a previous macrovascular disease defined as one or more of a) to f):

a) previous myocardial infarction,

b) advanced coronary artery disease,

c) high-risk single-vessel coronary artery disease,

d) previous ischemic or haemorrhagic stroke,

e) presence of carotid artery disease,

f) presence of peripheral artery disease;

and/or

ii) impaired renal function defined by:

impaired renal function defined by MDRD formula with an eGFR [15 or] 30-45 mL/min/1.73 m 2 with any urine albumin creatinine ratio (UACR), or impaired renal function defined by MDRD formula with an eGFR≥45-75 mL/min/1.73 m 2 with an urine albumin creatinine ratio (UACR)>200 mg/g creatinine or >200 mg/l (milligram albumin per liter of urine) or >200 μg/min (microgram albumin per minute) or >200 mg/24 h (milligram albumin per 24 hours).

16. The method of claim 1 , further comprising administering to the patient an active substance that lowers blood pressure.

17. The method of claim 1 , further comprising administering to the patient an active substance that lowers the lipid level in the blood.

18. The method of claim 1 , further comprising administering aspirin to the patient.

Continuity (5)

References Cited (400)