Medicament

Abstract

A medicament for treating a patient in need of pemafibrate therapy, the medicament comprising the step of avoiding or suspending concomitant use of pemafibrate, a salt thereof, or a solvate of any of these as an active ingredient in order to suppress an increase in plasma concentration of pemafibrate when the treatment is combined with a medicament containing an OATP1B inhibitor, or the step of reducing the dose of pemafibrate, a salt thereof, or a solvate of any of these.

1 - 9 : (canceled) 
     
     
         10 : A pharmaceutical kit comprising:
 (A) pemafibrate, a salt thereof, or a solvate thereof (pemafibrate); and   (B) an instruction to administer the pemafibrate concomitantly with an OATP1B inhibitor or a CYP inhibitor to a patient, wherein if the patient's plasma concentration of pemafibrate during the concomitant administration increases relative to the plasma concentration of pemafibrate in the patient when pemafibrate is administered without the OATP1B inhibitor and without the CYP inhibitor, then either (i) or (ii):   (i) stop concomitant administration of pemafibrate and the OATP1B inhibitor or the CYP inhibitor; or   (ii) continue concomitant administration of pemafibrate and the OATP1B inhibitor or the CYP inhibitor, with a dose of pemafibrate sufficiently reduced to suppress the increase in plasma concentration of pemafibrate in the patient.   
     
     
         11 : The pharmaceutical kit according to  claim 10 , wherein the pemafibrate, a salt thereof, or a solvate thereof is pemafibrate. 
     
     
         12 : The pharmaceutical kit according to  claim 10 , wherein the OATP1B inhibitor is one or more drugs selected from the group consisting of clarithromycin, rifampicin, cyclosporine, a combination agent of lopinavir and ritonavir, a combination agent of atazanavir and ritonavir, a combination agent of dalnavir and ritonavir, clopidogrel, eltronbopag, a combination agent of saquinavir and ritonavir, a combination agent of tipranavir and ritonavir, and gemfibrozil. 
     
     
         13 : (canceled) 
     
     
         14 : The pharmaceutical kit according to  claim 10 , instructing to reduce the dose of pemafibrate, compared with the dose when the pemafibrate is administered alone, to ½ or less. 
     
     
         15 : The pharmaceutical kit according to  claim 10 , instructing to reduce the dose of pemafibrate to 0.1 to 0.2 mg per day. 
     
     
         16 : The pharmaceutical kit according to  claim 10 , instructing to administer pemafibrate twice per day. 
     
     
         17 : The pharmaceutical kit according to  claim 10 , wherein the instruction is a package insert, a package label, or a user manual. 
     
     
         18 - 34 : (canceled) 
     
     
         35 : The pharmaceutical kit according to  claim 10 , wherein the CYP inhibitor is a drug that inhibits CYP3A. 
     
     
         36 : The pharmaceutical kit according to  claim 35 , wherein the drug that inhibits CYP3A is one or more drugs selected from the group consisting of clarithromycin, cyclosporine, cobicistat, indinavir, itraconazole, ritonavir, telaprevir, voriconazole, nelfinavir, saquinavir, boceprevir, conivaptan, ketoconazole, a combination agent of lopinavir and ritonavir, mibefradil, nefazodone, posaconazole, telithromycin, fluconazole, amprenavir, aprepitant, atazanavir, ciprofloxacin, crizotinib, a combination agent of darnavir and ritonavir, diltiazem, erythromycin, fosamprenavir, imatinib, istradefylline, miconazole, tofisopam, casopitant, dronedarone, and verapamil. 
     
     
         37 : The pharmaceutical kit according to  claim 10 , wherein the CYP inhibitor is a drug that inhibits CYP2C8. 
     
     
         38 : The pharmaceutical kit according to  claim 37 , wherein the drug that inhibits CYP2C8 is one or more drugs selected from the group consisting of gemfibrozil, clopidogrel, cyclosporine, deferasirox, and teriflunomide. 
     
     
         39 : The pharmaceutical kit according to  claim 10 , wherein the CYP inhibitor is a drug that inhibits CYP2C9. 
     
     
         40 : The pharmaceutical kit according to  claim 39 , wherein the drug that inhibits CYP2C9 is one or more drugs selected from the group consisting of a fluorouracil derivative, carmofur, sulfaphenazole, amiodarone, bucolome, cyclosporine, fluconazole, miconazole, and oxandrolone. 
     
     
         41 - 50 : (canceled) 
     
     
         51 : A method of treating a patient in need of with pemafibrate therapy with the concomitant administration of an OATP1B inhibitor where the pemafibrate plasma concentration becomes excessive, comprising:
 administering pemafibrate, a salt thereof, or a solvate thereof (pemafibrate) concomitantly with an OATP1B inhibitor to the patient, and   if the patient's plasma concentration of pemafibrate during the concomitant administration increases relative to the plasma concentration of pemafibrate in the patient when pemafibrate is administered without the OATP1B inhibitor, then either (i) or (ii):   (i) stopping concomitant administration of pemafibrate and the OATP1B inhibitor; or   (ii) continuing concomitant administration of pemafibrate and the OATP1B inhibitor, with a dose of pemafibrate sufficiently reduced to suppress the increase in plasma concentration of pemafibrate in the patient.   
     
     
         52 - 54 : (canceled) 
     
     
         55 : A method of treating a patient with pemafibrate therapy with the concomitant administration of a CYP inhibitor where the pemafibrate plasma concentration becomes excessive, comprising:
 administering pemafibrate, a salt thereof, or a solvate thereof (pemafibrate) concomitantly with a CYP inhibitor to the patient, and   if the patient's plasma concentration of pemafibrate during the concomitant administration increases relative to the plasma concentration of pemafibrate in the patient when pemafibrate is administered without the CYP inhibitor, then either (i) or (ii):   (i) stopping concomitant administration of pemafibrate and the CYP inhibitor, or   (ii) continuing concomitant administration of pemafibrate and the CYP inhibitor, with a dose of pemafibrate sufficiently reduced to suppress the increase in plasma concentration of pemafibrate in the patient.   
     
     
         56 - 58 : (canceled) 
     
     
         59 : The method of  claim 51 , wherein the dose of pemafibrate sufficiently reduced to suppress the increase in plasma concentration of pemafibrate in the patient is a dose that is ½ or less the dose when the pemafibrate is administered alone. 
     
     
         60 : The method of  claim 51 , wherein the dose of pemafibrate sufficiently reduced to suppress the increase in plasma concentration of pemafibrate in the patient is a dose that is 0.1 to 0.2 mg per day. 
     
     
         61 : The method of  claim 55 , wherein the dose of pemafibrate sufficiently reduced to suppress the increase in plasma concentration of pemafibrate in the patient is a dose that is ½ or less the dose when the pemafibrate is administered alone. 
     
     
         62 : The method of  claim 55 , wherein the dose of pemafibrate sufficiently reduced to suppress the increase in plasma concentration of pemafibrate in the patient is a dose that is 0.1 to 0.2 mg per day.