Methods for treating disorders or diseases associated with hyperlipidemia and hypercholesterolemia while minimizing side-effects

• US 9,364,470 B2
• Filed: 12/04/2015
• Issued: 06/14/2016
• Est. Priority Date: 03/05/2004
• Status: Active Grant

• Current Assignee: Trustees Of The University Of Pennsylvania (University of Pennsylvania)
• Original Assignee: Trustees Of The University Of Pennsylvania (University of Pennsylvania)
• Inventors: Rader, Daniel J.
• Primary Examiner(s): Weddington, Kevin E
• Application Number:
  US14/959,756
• Publication Number:
  US 20160081994A1
• Time in Patent Office: 193 Days
• Field of Search: 514/321, 514/325, 514/252.03, 514/255.03
• US Class Current: 1/1
• CPC Class Codes: A61K 31/21 Esters, e.g. nitroglycerine, selenocyanates
• CPC Class Codes: A61K 31/405 Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/4468 having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
• CPC Class Codes: A61K 31/52 Purines, e.g. adenine
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.

Claims

1. A method of treating a subject suffering from hyperlipidemia or hypercholesterolemia, the method comprising administering to the subject an effective amount of an MTP inhibitor, wherein said administration comprises at least three step-wise, increasing dose levels of the MTP inhibitor, wherein a first dose level is from about 0.02 to about 0.059 mg/kg/day, a second dose level is from about 0.06 to about 0.19 mg/kg/day, and a third dose level is from about 0.2 to about 0.59 mg/kg/day;

and wherein the MTP inhibitor is represented by;

2. The method of claim 1, wherein administering increasing dose levels further comprises a maximum dose level of about 50 to about 75 mg/day.