Methods for treating diabetes and reducing body weight
Inventors
Fineman, Mark • MacConell, Leigh • Taylor, Kristin
Assignees
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Publication Number
US-8329648-B2
Publication Date
2012-12-11
Expiration Date
Abstract
Methods for reducing body weight, altering body composition, treating diabetes, reducing HbA1c and reducing average daily blood glucose by the use of exendins, exendin agonists or exendin analog agonists are provided.
Core Innovation
The invention relates to chronic treatment of diabetes in a human in need thereof using pharmaceutical compositions that include biocompatible poly(lactide-co-glycolide) copolymer and exendin-4 or an exendin analog. The treatment is carried out to achieve a mean steady state plasma concentration of the exendin-4 or the exendin-4 analog at least 170 pg/ml for at least one month.
In the context of reducing diabetes-related parameters, the compositions are administered to reduce one or more of HbA1C, fasting plasma glucose, and body weight. The method maintains an exposure level of exendin-4 or the exendin analog at a mean steady state concentration of at least 170 pg/ml for at least one month.
For type 2 diabetes, the invention further specifies a once weekly administration approach using a pharmaceutical composition comprising 5% (w/w) exendin-4, 2% (w/w) sucrose, and 93% (w/w) poly(lactide-co-glycolide) copolymer. The method targets a mean steady state plasma concentration of exendin-4 of 170 pg/ml to 350 pg/ml for at least one month.
The invention also characterizes exendin analogs by amino acid sequence selections, including sequences identified as SEQ ID NOs: 2 and 9-142. The described framework links the selection of exendin-4 or exendin analog with sustained mean steady state plasma exposure to support chronic diabetes treatment and reduction of specified clinical parameters.
Claims Coverage
The independent claims center on administering exendin-4 or an exendin analog with a biocompatible poly(lactide-co-glycolide) copolymer to achieve a specified mean steady state plasma concentration level for at least one month, with additional constraints for clinical outcome targets and for a specific once weekly type 2 diabetes formulation and concentration range. In total, the claims emphasize three core inventive aspects: sustained mean steady state exposure, diabetes indication/clinical outcome targeting, and a defined once-weekly formulation and dosing schedule.
Biocompatible poly(lactide-co-glycolide) copolymer with exendin-4 or exendin analog for mean steady state exposure
Administering to the human an effective amount of a pharmaceutical composition comprising a biocompatible poly(lactide-co-glycolide) copolymer and exendin-4 or an exendin analog to achieve a mean steady state plasma concentration of the exendin-4 or the exendin-4 analog at least 170 pg/ml for at least one month in the human to treat diabetes.
Reducing HbA1C, fasting plasma glucose, and body weight using mean steady state exendin exposure
Reducing one or more of HbA1C, fasting plasma glucose, and body weight in a human by administering to the human an effective amount of a pharmaceutical composition comprising a biocompatible poly(lactide-co-glycolide) copolymer and exendin-4 or an exendin analog in an amount to achieve a mean steady state concentration of exendin-4 or the exendin-4 analog of at least 170 pg/ml for at least one month to reduce one or more of HbA1C, fasting plasma glucose, and body weight.
Once weekly type 2 diabetes treatment with a specified composition and concentration range
Administering once weekly to the human an effective amount of a pharmaceutical composition comprising 5% (w/w) exendin-4, 2% (w/w) sucrose, and 93% (w/w) poly(lactide-co-glycolide) copolymer to achieve a mean steady state plasma concentration of exendin-4 at 170 pg/ml to 350 pg/ml for at least one month in the human to treat Type 2 diabetes.
Overall, the claim coverage is focused on chronic diabetes treatment through sustained mean steady state plasma concentration of exendin-4 or an exendin analog (at least 170 pg/ml for at least one month) provided by pharmaceutical compositions containing a biocompatible poly(lactide-co-glycolide) copolymer, with further claim-level refinement to reduce HbA1C and/or fasting plasma glucose and body weight and to define an explicit once weekly type 2 diabetes formulation and concentration range.
Stated Advantages
Achieves a mean steady state plasma concentration of exendin-4 or the exendin analog at least 170 pg/ml for at least one month.
Treats diabetes in a human in need thereof.
Reduces one or more of HbA1C, fasting plasma glucose, and body weight.
Provides once-weekly treatment for type 2 diabetes with a specified mean steady state plasma concentration range of exendin-4.
Documented Applications
Treating diabetes in a human by administering exendin-4 or an exendin analog with a biocompatible poly(lactide-co-glycolide) copolymer to achieve sustained mean steady state plasma concentration.
Reducing one or more of HbA1C, fasting plasma glucose, and body weight in a human using exendin-4 or an exendin analog with a biocompatible poly(lactide-co-glycolide) copolymer and achieving mean steady state concentration of at least 170 pg/ml for at least one month.
Treating type 2 diabetes in a human using a once-weekly pharmaceutical composition comprising 5% (w/w) exendin-4, 2% (w/w) sucrose, and 93% (w/w) poly(lactide-co-glycolide) copolymer to achieve a mean steady state plasma concentration of exendin-4 at 170 pg/ml to 350 pg/ml for at least one month.
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