Therapeutic regimen

Abstract

The present invention relates to dosing regimen of a new antimalarial drug, as monotherapy or combination therapy.

1 . 2-amino-1-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)ethanone, or a pharmaceutically acceptable salt thereof, for use in preventing, treating malaria, or delaying the symptoms or ameliorating the conditions associated with malaria, wherein the compound is administered daily at a dose of about 200 mg to about 350 mg during 1 to 5 days, e.g. 1 to 3 days. 
     
     
         2 . The compound according to  claim 1 , wherein the compound is administered daily at a dose of about 200 mg, during 1 to 3 days, e.g. 1 or 2 days. 
     
     
         3 . The compound according to  claim 1 , wherein the compound is administered daily at a dose of about 400 mg, during 1 to 3 days, e.g. 1 or 2 days. 
     
     
         4 . The compound according to  claim 1 , wherein the compound is administered daily at a dose of about 800 mg, during 2 to 5 days, e.g. 2 or 3 days. 
     
     
         5 . 2-amino-1-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)ethanone, or a pharmaceutically acceptable salt thereof, for use in preventing, treating malaria, or delaying the symptoms or ameliorating the conditions associated with malaria, wherein the compound is administered with a second anti-malaria drug. 
     
     
         6 . The compound according to  claim 5 , wherein the compound is administered daily at a dose of about 200 mg to about 1000 mg during 1 to 5 days, e.g. 1 to 3 days. 
     
     
         7 . A method of preventing or treating malaria, or delaying the symptoms or ameliorating the conditions associated with malaria, in a subject in need thereof, comprising administering to said subject about 200 mg to 350 mg of 2-amino-1-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)ethanone, or a pharmaceutically acceptable salt thereof, delivered daily, during 1 to 5 days. 
     
     
         8 . The method according to  claim 7 , wherein said compound is administered at a dose of about 200 mg. 
     
     
         9 . The method according to  claim 7 , wherein said compound is administered daily at a dose of about 400 mg. 
     
     
         10 . The method according to  claim 7 , wherein said compound is administered daily at a dose of about 800 mg. 
     
     
         11 . A method of preventing or treating malaria, or delaying the symptoms or ameliorating the conditions associated with malaria, in a subject in need thereof, comprising administering to said subject about 200 mg to 1000 mg of 2-amino-1-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)ethanone, or a pharmaceutically acceptable salt thereof, in combination with a second anti-malaria drug. 
     
     
         12 . The method according to  claim 11 , wherein the second anti-malaria drug is lumefantrine. 
     
     
         13 . The method according to  claim 12 , wherein the lumefantrine is administered daily at a dose of about 400 mg to 1000 mg. 
     
     
         14 . A pharmaceutical combination comprising lumefantrine and a dose of about 200 mg to about 1000 mg of 2-amino-1-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)ethanone, or a pharmaceutically acceptable salt thereof. 
     
     
         15 . The pharmaceutical combination according to  claim 14 , comprising about 200 mg of 2-amino-1-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)ethanone, or a pharmaceutically acceptable salt thereof. 
     
     
         16 . The pharmaceutical combination according to  claim 14 , comprising about 400 mg of 2-amino-1-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)ethanone, or a pharmaceutically acceptable salt thereof. 
     
     
         17 . The pharmaceutical combination according to  claim 14 , comprising about 800 mg of 2-amino-1-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)ethanone, or a pharmaceutically acceptable salt thereof.