Methods of reducing small, dense LDL particles
Inventors
Karpf, David • Krauss, Ronald M. • CHOI, YUN-JUNG • Wang, Xueyan • Gregoire, Francine M.
Assignees
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Publication Number
US-11007162-B2
Publication Date
2021-05-18
Expiration Date
Abstract
The present invention provides methods for increasing LDL particle size.
Core Innovation
The invention relates to a method of changing the LDL particle size pattern in a human having LDL particle size pattern I or B. The method comprises identification of the human as having LDL particle size pattern I or B and administration of a therapeutically effective amount of a compound of the formula or a salt thereof. By performing these steps, the LDL particle size pattern of the human is changed from pattern I to pattern A, or from pattern B to pattern I or A.
The treatment is described as shifting LDL particle distribution toward pattern A and altering the distribution from pattern I to A or from pattern B to I/A. The document further describes a decrease in small dense LDL, including reduced LDL-III and LDL-IV, and associated changes in lipid biomarkers. These biomarker changes are described as lower ApoB-100, LDL-cholesterol, and triglycerides, and increased HDL.
The therapeutic compound is described as a PPARδ agonist, with embodiments including Formula I and related structures such as Compound II, including salts, prodrugs, and isomers. The document also mentions GW501516 and L-165,041 among described entities. The partial content summary further states that clinical studies show increased predominant LDL diameter and shift toward pattern A.
Claims Coverage
The independent claim recites three main inventive features: identifying a human as having LDL particle size pattern I or B, administering a therapeutically effective amount of a compound of the formula or a salt thereof, and changing the LDL particle size pattern from I or B to A, or from B to I or A. Dependent claims refine the patient population, post-administration pattern identification, and optional statin co-administration including atorvastatin.
Identifying a human as having LDL particle size pattern I or B
The method comprises identifying the human as having LDL particle size pattern I or B.
Administering a therapeutically effective formula compound or salt
The method comprises administering to the human a therapeutically effective amount of a compound of the formula or a salt thereof.
Changing LDL particle size pattern from I/B to A (or I/A)
Administering the therapeutically effective amount thereby changes the LDL particle size pattern of the human from pattern I to pattern A, or from pattern B to pattern I or A.
Selecting a human with LDL particle size pattern B before administration
The method further includes identifying the human as having LDL particle size pattern B prior to administering the compound.
Identifying the post-administration LDL particle size pattern as I
The method further includes, after administering the compound, identifying the human as having LDL particle size pattern I.
Administering a statin
The method includes administering a statin to a human.
Using atorvastatin as the statin
The method of the statin refinement is carried out using atorvastatin.
Treating a human with diabetes
The method is directed to a human who has diabetes.
Overall, the claim set covers changing LDL particle size patterns by identifying humans with LDL pattern I or B and administering a therapeutically effective formula compound or salt to achieve a shift to pattern A and/or pattern I/A, with dependent refinements covering pattern B pre-selection, pattern I post-identification, diabetes, and optional statin co-administration including atorvastatin.
Stated Advantages
Changing the LDL particle size pattern of the human from pattern I to pattern A, or from pattern B to pattern I or A.
Decreasing small dense LDL, including reduced LDL-III and LDL-IV.
Improving lipid biomarkers by lowering ApoB-100, LDL-cholesterol, and triglycerides and increasing HDL.
Documented Applications
Treatment of a human with LDL particle size pattern I or B to change the LDL particle size pattern to pattern A, or from pattern B to pattern I or A.
Use of the method in patient groups described as having metabolic syndrome, diabetes, insulin resistance, atherosclerosis, or dyslipidemia.
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