Pharmaceutical composition, methods for treating and uses thereof

Inactive Publication Date: 2014-10-09
BOEHRINGER INGELHEIM INT GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0214]The terms “prophylactically treating”, “preventivally treating” and “preventing” are used interchangeably an

Problems solved by technology

The use of a number of anti-diabetes agents is restricted in patients with renal impairment.
Metformin is

Method used

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  • Pharmaceutical composition, methods for treating and uses thereof
  • Pharmaceutical composition, methods for treating and uses thereof
  • Pharmaceutical composition, methods for treating and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Example

Example 1

Empagliflozin in Patients with Type 2 Diabetes Mellitus (T2DM) and Renal Impairment (RI)

[0354]A Phase III trial investigated the efficacy and safety of empagliflozin (EMPA) as add-on to existing therapy for 52 weeks in patients with T2DM and RI. Patients with mild RI (eGFR [MDRD equation]≧60 to 2; n=290; mean age 62.6 years; mean BMI 31.5 kg / m2) received EMPA 10 or 25 mg qd or placebo (PBO). Patients with moderate RI (eGFR ≧30 to 2; n=374; mean age 64.9 years; mean BMI 30.2 kg / m2) received EMPA 25 mg qd or PBO. The primary endpoint was change from baseline in HbA1c at week 24. Exploratory endpoints included changes from baseline in fasting plasma glucose (FPG), weight and blood pressure (BP) at week 24 (FIG. 1).

[0355]EMPA significantly reduced HbA1c vs PBO at week 24. Further analyses showed significant reductions in FPG, weight and BP. At week 24, adverse events (AEs) were reported by 79.6%, 75.4% and 72.7% of all patients (including an exploratory group with severe RI [n=...

Example

Example 2

Mixed Effects Modeling to Quantify the Effect of Empagliflozin Exposure on the Renal Glucose Threshold in Patients with Type 2 Diabetes Mellitus

[0358]Empagliflozin, a selective and potent SGLT2 inhibitor, reduces renal glucose reabsorption by lowering the renal threshold for glucose (RTG) leading to increased urinary glucose excretion (UGE) and decreased plasma glucose (PG) in patients with type 2 diabetes mellitus (T2DM). This analysis aimed to quantify the impact of empagliflozin on RTG by characterizing the relationship between empagliflozin exposure and UGE in patients with T2DM using nonlinear mixed-effects modeling.

[0359]A pharmacokinetic (PK)-pharmacodynamic (PD) model was developed using UGE, PG, PK and estimated glomerular filtration rate (eGFR) data from three Phase I / II trials (N=223; placebo, empagliflozin 1 to 100 mg once daily [QD]). The model assumed that when PG>RTG, UGE increased with increasing PG and eGFR; and when PGRTG slight glucose leakage into urine ...

Example

Example 3

Pharmacokinetics and Pharmacodynamics of Empagliflozin in Subjects with Renal Impairment

[0361]Subjects. Male and female subjects aged 18 to 75 years weighing at least 45 kg (females only) and with a body mass index (BMI) of 18 to 34 kg / m2 were eligible for inclusion in this study. Participants with normal renal function (eGFR >90 mL / min / 1.73 m2; control) were required to have T2DM. Patients with mild renal impairment (eGFR 60-89 mL / min / 1.73 m2), moderate renal impairment (eGFR 30-59 mL / min / 1.73 m2), severe renal impairment (eGFR 2) or renal failure / ESRD (requiring dialysis) did not need to have T2DM. eGFR was calculated using the Modification of Diet in Renal Disease (MDRD) formula: 186×serum creatinine−1.154×age−0.203×[0.742 if female].

[0362]Subjects were excluded from the study if they had recently participated in a study (multiple-dose: within 2 months; single-dose: within 1 month), were abusing alcohol (males >60 g / day; females >40 g / day) or drugs, had donated >100 mL b...

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Abstract

The present invention relates to certain SGLT-2 inhibitors for treating and/or preventing metabolic disorders, such as type 1 or type 2 diabetes mellitus or pre-diabetes, in patients with renal impairment or chronic kidney disease (CKD).

Description

TECHNICAL FIELD OF THE INVENTION[0001]The present invention relates to certain SGLT-2 inhibitors for treating and / or preventing metabolic disorders, such as type 2 or type 1 diabetes mellitus or pre-diabetes, in patients with renal impairment or chronic kidney disease (CDK).BACKGROUND OF THE INVENTION[0002]Diabetes is a major public health problem, with a prevalence that is expected to reach 552 million people worldwide by 2030. Type 2 diabetes mellitus (T2DM) accounts for 90% of all diabetes cases. Most medications for the treatment of T2DM act through insulin-dependent mechanisms; the progressive loss of beta-cell function that is characteristic of T2DM means that most patients with T2DM ultimately require multiple therapies to maintain glycemic control.[0003]Nephropathy is a well-established complication of poor glycemic control in patients with diabetes. An estimated 10-36% of patients with T2DM have some degree of renal impairment and chronic kidney disease (CKD) is present in ...

Claims

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Application Information

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IPC IPC(8): A61K31/7034
CPCA61K31/7034A61K9/2018A61K9/2866A61K31/7048A61P13/12A61P3/08A61P3/10
Inventor BROEDL, ULI CHRISTIANMACHA, SREERAJVON EYNATTEN, MAXIMILIANWOERLE, HANS-JUERGEN
Owner BOEHRINGER INGELHEIM INT GMBH
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