Methods for treating disorders or diseases associated with hyperlipidemia and hypercholesterolemia while minimizing side-effects
First Claim
1. A method of treating a subject suffering from hyperlipidemia or hypercholesterolemia, the method comprising orally administering to the subject an effective amount of an MTP inhibitor, wherein said administration comprises three step-wise, increasing dose levels of the MTP inhibitor, wherein each dose level is 50% of the immediately following dose level, wherein the third dose level is about 0.2 to about 0.59 mg/kg/day, and wherein the MTP inhibitor is N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4′
- -(trifluoromethyl)[1,1′
-biphenyl]-2-yl] carbonyl] amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide, methanesulfonate; and
wherein each dose level is administered about 1 to about 12 weeks.
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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.
115 Citations
20 Claims
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1. A method of treating a subject suffering from hyperlipidemia or hypercholesterolemia, the method comprising orally administering to the subject an effective amount of an MTP inhibitor, wherein said administration comprises three step-wise, increasing dose levels of the MTP inhibitor, wherein each dose level is 50% of the immediately following dose level, wherein the third dose level is about 0.2 to about 0.59 mg/kg/day, and wherein the MTP inhibitor is N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4′
- -(trifluoromethyl)[1,1′
-biphenyl]-2-yl] carbonyl] amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide, methanesulfonate; and
wherein each dose level is administered about 1 to about 12 weeks. - View Dependent Claims (2, 3, 4, 5, 6, 7)
- -(trifluoromethyl)[1,1′
-
8. 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 each dose level is 50% of the immediately following dose level, wherein the second dose level is about 0.06 mg/kg/day to about 0.19 mg/kg/day, wherein the MTP inhibitor is N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4′
- -(trifluoromethyl)[l,r-biphenyl]-2-yl] carbonyl] amino]-l-piperidinyl]butyl]-9H-fluorene-9-carboxamide, methanesulfonate, and wherein each dose level is administered about 1 to about 12 weeks.
- View Dependent Claims (9, 10, 11, 12, 13, 14)
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15. 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 three step-wise, increasing dose levels of the MTP inhibitor, wherein each dose level is no more than 50% of the immediately following dose level, and wherein the first dose level is about 0.02 to about 0.059 mg/kg/day, the second dose level is about 0.06 mg/kg/day to about 0.19 mg/kg/day, and the third dose level is about 0.2 to about 0.59 mg/kg/day;
- wherein the MTP inhibitor is N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4′
-(trifluoromethyl)[l,r-biphenyl]-2-yl] carbonyl] amino]-l-piperidinyl]butyl]-9H-fluorene-9-carboxamide, methanesulfonate; and
wherein each dose level is administered about 1 to about 12 weeks. - View Dependent Claims (16, 17, 18, 19, 20)
- wherein the MTP inhibitor is N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4′
Specification