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      Drugs & Diseases

      osilodrostat (Rx)

      Brand and Other Names:Isturisa
      • Print

      Dosing & Uses

      AdultPediatric

      Dosage Forms & Strengths

      tablet

      • 1mg
      • 5mg
      • 10mg

      Cushing Disease

      Indicated for Cushing disease in adults for whom pituitary surgery is not an option or has not been curative

      Initial: 2 mg PO BID

      Titration

      • Initially, titrate by 1-2 mg BID, no more frequently than q2weeks based on rate of cortisol changes, individual tolerability, and improvement in Cushing disease signs and symptoms
      • If patient tolerates 10 mg PO BID and continues to have elevated 24-hr urine free cortisol (UFC) levels >ULN, titrate dosage further by 5 mg BID q2week
      • Monitor cortisol levels from at least two 24-hour UFC collections q1-2weeks until adequate clinical response maintained

      Maintenance

      • Individualize maintenance dose according to cortisol levels and signs/symptoms
      • Maintenance dosage varied from 2-7 mg BID in clinical trials
      • Maximum recommended maintenance dose: 30 mg BID
      • Once maintenance dose achieved, monitor cortisol levels at least every 1-2 months or as indicated

      Dosage Modifications

      Interruptions or modifications

      • Decrease or temporarily discontinue if UFC levels fall below target range, there is a rapid decrease in cortisol levels, and/or symptoms of hypocortisolism occur; if necessary, initiate glucocorticoid
      • Stop osilodrostat and administer exogenous glucocorticoid replacement therapy if serum or plasma cortisol levels are below target range and patients have symptoms of adrenal insufficiency
      • If treatment is interrupted, reinitiate at lower dose when cortisol levels are within target ranges and symptoms have resolved

      Renal impairment

      • No dose adjustment required
      • Caution in interpreting UFC levels with moderate-to-severe renal impairment, owing to reduced UFC excretion

      Hepatic impairment

      • Mild (Child-Pugh A): No dose adjustment required
      • Moderate (Child-Pugh B): Reduce initial dose to 1 mg BID
      • Severe (Child-Pugh C): Reduce initial dose to 1 mg qHS
      • May require more frequent adrenal function monitoring during dose titration in all patients with hepatic impairment

      Dosing Considerations

      Correct hypokalemia and hypomagnesemia before initiating

      Obtain baseline ECG; repeat ECG within 1 week after treatment initiation, and as clinically indicated thereafter

      Safety and efficacy not established

      Next:

      Interactions

      Interaction Checker

      and osilodrostat

      No Results

         activity indicator 
        No Interactions Found
        Interactions Found

        Contraindicated

          Serious - Use Alternative

            Significant - Monitor Closely

              Minor

                All Interactions Sort By:
                 activity indicator 

                Contraindicated (1)

                • lefamulin

                  lefamulin will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lefamulin is contraindicated with CYP3A substrates know to prolong the QT interval.

                Serious - Use Alternative (17)

                • abametapir

                  abametapir will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

                • adagrasib

                  adagrasib, osilodrostat. Either increases effects of the other by QTc interval. Avoid or Use Alternate Drug. Each drug prolongs the QTc interval, which may increased the risk of Torsade de pointes, other serious arryhthmias, and sudden death. If coadministration unavoidable, more frequent monitoring is recommended for such patients.

                • amisulpride

                  amisulpride and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • buprenorphine buccal

                  buprenorphine buccal and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • buprenorphine subdermal implant

                  buprenorphine subdermal implant and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • buprenorphine transdermal

                  buprenorphine transdermal and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • buprenorphine, long-acting injection

                  buprenorphine, long-acting injection and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • carbamazepine

                  carbamazepine will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                • ceritinib

                  ceritinib will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                • dofetilide

                  dofetilide and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • fexinidazole

                  fexinidazole and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels or prolong QT interval.

                  fexinidazole will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

                • fosphenytoin

                  fosphenytoin will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                • grapefruit

                  grapefruit will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                • mobocertinib

                  mobocertinib and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.

                • primidone

                  primidone will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                • ribociclib

                  ribociclib and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • tucatinib

                  tucatinib will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

                Monitor Closely (194)

                • albuterol

                  osilodrostat and albuterol both increase QTc interval. Use Caution/Monitor.

                  albuterol and osilodrostat both increase QTc interval. Use Caution/Monitor. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • alfuzosin

                  osilodrostat and alfuzosin both increase QTc interval. Use Caution/Monitor.

                  alfuzosin and osilodrostat both increase QTc interval. Use Caution/Monitor. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • amiodarone

                  osilodrostat and amiodarone both increase QTc interval. Use Caution/Monitor.

                • amisulpride

                  osilodrostat and amisulpride both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended if coadministered.

                • amitriptyline

                  osilodrostat and amitriptyline both increase QTc interval. Use Caution/Monitor.

                • amobarbital

                  amobarbital will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • anagrelide

                  osilodrostat and anagrelide both increase QTc interval. Use Caution/Monitor.

                • apalutamide

                  apalutamide will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • apomorphine

                  osilodrostat and apomorphine both increase QTc interval. Use Caution/Monitor.

                • arformoterol

                  osilodrostat and arformoterol both increase QTc interval. Use Caution/Monitor.

                • aripiprazole

                  osilodrostat and aripiprazole both increase QTc interval. Use Caution/Monitor.

                • arsenic trioxide

                  osilodrostat and arsenic trioxide both increase QTc interval. Use Caution/Monitor.

                • artemether

                  osilodrostat and artemether both increase QTc interval. Use Caution/Monitor.

                • artemether/lumefantrine

                  osilodrostat and artemether/lumefantrine both increase QTc interval. Use Caution/Monitor.

                • asenapine

                  osilodrostat and asenapine both increase QTc interval. Use Caution/Monitor.

                • asenapine transdermal

                  asenapine transdermal and osilodrostat both increase QTc interval. Use Caution/Monitor. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • atazanavir

                  atazanavir will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • atomoxetine

                  osilodrostat and atomoxetine both increase QTc interval. Use Caution/Monitor.

                • azithromycin

                  osilodrostat and azithromycin both increase QTc interval. Use Caution/Monitor.

                • bedaquiline

                  osilodrostat and bedaquiline both increase QTc interval. Use Caution/Monitor.

                • bosentan

                  bosentan will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • bosutinib

                  osilodrostat and bosutinib both increase QTc interval. Use Caution/Monitor.

                • buprenorphine

                  osilodrostat and buprenorphine both increase QTc interval. Use Caution/Monitor.

                • butabarbital

                  butabarbital will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • butalbital

                  butalbital will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • capecitabine

                  osilodrostat and capecitabine both increase QTc interval. Use Caution/Monitor.

                • carbamazepine

                  carbamazepine will decrease the level or effect of osilodrostat by Other (see comment). Modify Therapy/Monitor Closely. Osilodrostat is a CYP3A4 and CYP2B6 subtrate. Monitor cortisol concentration and patient?s signs and symptoms during coadministration and discontinuation with strong CYP3A4 and/or CYP2B6 inducers. Adjust dose of osilodrostat if necessary.

                • ceritinib

                  osilodrostat and ceritinib both increase QTc interval. Use Caution/Monitor.

                • chloramphenicol

                  chloramphenicol will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • chloroquine

                  osilodrostat and chloroquine both increase QTc interval. Use Caution/Monitor.

                  chloroquine and osilodrostat both increase QTc interval. Use Caution/Monitor.

                • chlorpromazine

                  osilodrostat and chlorpromazine both increase QTc interval. Use Caution/Monitor.

                • ciprofloxacin

                  osilodrostat and ciprofloxacin both increase QTc interval. Use Caution/Monitor.

                • citalopram

                  osilodrostat and citalopram both increase QTc interval. Use Caution/Monitor.

                • clarithromycin

                  clarithromycin will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                  osilodrostat and clarithromycin both increase QTc interval. Use Caution/Monitor.

                • clofazimine

                  osilodrostat and clofazimine both increase QTc interval. Use Caution/Monitor.

                • clozapine

                  osilodrostat and clozapine both increase QTc interval. Use Caution/Monitor.

                • cobicistat

                  cobicistat will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • conivaptan

                  conivaptan will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • crizotinib

                  osilodrostat and crizotinib both increase QTc interval. Use Caution/Monitor.

                • dabrafenib

                  dabrafenib will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                  osilodrostat and dabrafenib both increase QTc interval. Use Caution/Monitor.

                • darunavir

                  darunavir will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • dasatinib

                  osilodrostat and dasatinib both increase QTc interval. Use Caution/Monitor.

                • degarelix

                  osilodrostat and degarelix both increase QTc interval. Use Caution/Monitor.

                • desflurane

                  osilodrostat and desflurane both increase QTc interval. Use Caution/Monitor.

                • desipramine

                  osilodrostat and desipramine both increase QTc interval. Use Caution/Monitor.

                • deutetrabenazine

                  osilodrostat and deutetrabenazine both increase QTc interval. Use Caution/Monitor. At the maximum recommended dose, deutetrabenazine does not prolong QT interval to a clinically relevant extent. Certain circumstances may increase risk of torsade de pointes and/or sudden death in association with drugs that prolong the QTc interval (eg, bradycardia, hypokalemia or hypomagnesemia, coadministration with other drugs that prolong QTc interval, presence of congenital QT prolongation).

                • disopyramide

                  osilodrostat and disopyramide both increase QTc interval. Use Caution/Monitor.

                • divalproex sodium

                  osilodrostat will decrease the level or effect of divalproex sodium by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

                • dofetilide

                  osilodrostat and dofetilide both increase QTc interval. Use Caution/Monitor.

                • dolasetron

                  osilodrostat and dolasetron both increase QTc interval. Use Caution/Monitor.

                • donepezil

                  osilodrostat and donepezil both increase QTc interval. Use Caution/Monitor.

                • doxepin

                  osilodrostat and doxepin both increase QTc interval. Use Caution/Monitor.

                • dronedarone

                  osilodrostat and dronedarone both increase QTc interval. Use Caution/Monitor.

                • droperidol

                  osilodrostat and droperidol both increase QTc interval. Use Caution/Monitor.

                • efavirenz

                  efavirenz will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                  osilodrostat and efavirenz both increase QTc interval. Use Caution/Monitor.

                • eliglustat

                  osilodrostat and eliglustat both increase QTc interval. Use Caution/Monitor.

                • encorafenib

                  osilodrostat and encorafenib both increase QTc interval. Use Caution/Monitor.

                • entrectinib

                  osilodrostat and entrectinib both increase QTc interval. Use Caution/Monitor.

                • enzalutamide

                  enzalutamide will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • eribulin

                  osilodrostat and eribulin both increase QTc interval. Use Caution/Monitor.

                • erythromycin base

                  osilodrostat and erythromycin base both increase QTc interval. Use Caution/Monitor.

                • erythromycin ethylsuccinate

                  osilodrostat and erythromycin ethylsuccinate both increase QTc interval. Use Caution/Monitor.

                • erythromycin lactobionate

                  osilodrostat and erythromycin lactobionate both increase QTc interval. Use Caution/Monitor.

                • erythromycin stearate

                  osilodrostat and erythromycin stearate both increase QTc interval. Use Caution/Monitor.

                • escitalopram

                  osilodrostat and escitalopram both increase QTc interval. Use Caution/Monitor.

                  escitalopram and osilodrostat both increase QTc interval. Use Caution/Monitor. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • etravirine

                  etravirine will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • ezogabine

                  osilodrostat and ezogabine both increase QTc interval. Use Caution/Monitor.

                • fingolimod

                  osilodrostat and fingolimod both increase QTc interval. Use Caution/Monitor.

                • flecainide

                  osilodrostat and flecainide both increase QTc interval. Use Caution/Monitor.

                • floxuridine

                  osilodrostat and floxuridine both increase QTc interval. Use Caution/Monitor.

                • fluconazole

                  osilodrostat and fluconazole both increase QTc interval. Use Caution/Monitor.

                • fluoxetine

                  osilodrostat and fluoxetine both increase QTc interval. Use Caution/Monitor.

                • fluphenazine

                  osilodrostat and fluphenazine both increase QTc interval. Use Caution/Monitor.

                • formoterol

                  osilodrostat and formoterol both increase QTc interval. Use Caution/Monitor.

                • foscarnet

                  osilodrostat and foscarnet both increase QTc interval. Use Caution/Monitor.

                • fosphenytoin

                  fosphenytoin will decrease the level or effect of osilodrostat by Other (see comment). Modify Therapy/Monitor Closely. Osilodrostat is a CYP3A4 and CYP2B6 subtrate. Monitor cortisol concentration and patient?s signs and symptoms during coadministration and discontinuation with strong CYP3A4 and/or CYP2B6 inducers. Adjust dose of osilodrostat if necessary.

                • fostemsavir

                  osilodrostat and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.

                • gadoterate meglumine

                  osilodrostat and gadoterate meglumine both increase QTc interval. Use Caution/Monitor.

                • gemifloxacin

                  osilodrostat and gemifloxacin both increase QTc interval. Use Caution/Monitor.

                • gemtuzumab

                  osilodrostat and gemtuzumab both increase QTc interval. Use Caution/Monitor.

                • gilteritinib

                  gilteritinib and osilodrostat both increase QTc interval. Use Caution/Monitor. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval

                • glasdegib

                  osilodrostat and glasdegib both increase QTc interval. Use Caution/Monitor.

                • goserelin

                  osilodrostat and goserelin both increase QTc interval. Use Caution/Monitor.

                • granisetron

                  osilodrostat and granisetron both increase QTc interval. Use Caution/Monitor.

                • haloperidol

                  osilodrostat and haloperidol both increase QTc interval. Use Caution/Monitor.

                • hydroxychloroquine sulfate

                  osilodrostat and hydroxychloroquine sulfate both increase QTc interval. Use Caution/Monitor.

                  hydroxychloroquine sulfate and osilodrostat both increase QTc interval. Use Caution/Monitor.

                • hydroxyzine

                  osilodrostat and hydroxyzine both increase QTc interval. Use Caution/Monitor.

                • ibutilide

                  osilodrostat and ibutilide both increase QTc interval. Use Caution/Monitor.

                • idelalisib

                  idelalisib will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • iloperidone

                  osilodrostat and iloperidone both increase QTc interval. Use Caution/Monitor.

                • indacaterol, inhaled

                  osilodrostat and indacaterol, inhaled both increase QTc interval. Use Caution/Monitor.

                • indinavir

                  indinavir will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • inotuzumab

                  osilodrostat and inotuzumab both increase QTc interval. Use Caution/Monitor.

                • isoflurane

                  osilodrostat and isoflurane both increase QTc interval. Use Caution/Monitor.

                • isoniazid

                  isoniazid will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • itraconazole

                  itraconazole will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                  osilodrostat and itraconazole both increase QTc interval. Use Caution/Monitor.

                • ivosidenib

                  ivosidenib will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                  osilodrostat and ivosidenib both increase QTc interval. Use Caution/Monitor.

                • ketoconazole

                  ketoconazole will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • lapatinib

                  osilodrostat and lapatinib both increase QTc interval. Use Caution/Monitor.

                • lefamulin

                  osilodrostat and lefamulin both increase QTc interval. Use Caution/Monitor.

                • lenacapavir

                  lenacapavir will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.

                • lenvatinib

                  osilodrostat and lenvatinib both increase QTc interval. Use Caution/Monitor.

                • leuprolide

                  osilodrostat and leuprolide both increase QTc interval. Use Caution/Monitor.

                • levalbuterol

                  osilodrostat and levalbuterol both increase QTc interval. Use Caution/Monitor.

                • levofloxacin

                  osilodrostat and levofloxacin both increase QTc interval. Use Caution/Monitor.

                • levoketoconazole

                  levoketoconazole will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • lithium

                  osilodrostat and lithium both increase QTc interval. Use Caution/Monitor.

                • lofexidine

                  osilodrostat and lofexidine both increase QTc interval. Use Caution/Monitor.

                • loperamide

                  osilodrostat and loperamide both increase QTc interval. Use Caution/Monitor.

                • lopinavir

                  lopinavir will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                  osilodrostat and lopinavir both increase QTc interval. Use Caution/Monitor.

                • lorlatinib

                  lorlatinib will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • lumacaftor/ivacaftor

                  lumacaftor/ivacaftor will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • macimorelin

                  osilodrostat and macimorelin both increase QTc interval. Use Caution/Monitor.

                • mefloquine

                  osilodrostat and mefloquine both increase QTc interval. Use Caution/Monitor.

                • methadone

                  osilodrostat and methadone both increase QTc interval. Use Caution/Monitor.

                • midostaurin

                  osilodrostat and midostaurin both increase QTc interval. Use Caution/Monitor.

                • mifepristone

                  mifepristone will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                  osilodrostat and mifepristone both increase QTc interval. Use Caution/Monitor.

                • mirtazapine

                  osilodrostat and mirtazapine both increase QTc interval. Use Caution/Monitor.

                • mitotane

                  mitotane will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • moxifloxacin

                  osilodrostat and moxifloxacin both increase QTc interval. Use Caution/Monitor.

                • nafcillin

                  nafcillin will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • nefazodone

                  nefazodone will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • nelfinavir

                  nelfinavir will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • nevirapine

                  nevirapine will decrease the level or effect of osilodrostat by affecting hepatic enzyme CYP2B6 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP2B6 inducers. Adjust dose of osilodrostat if necessary.

                • nilotinib

                  osilodrostat and nilotinib both increase QTc interval. Use Caution/Monitor.

                • nortriptyline

                  osilodrostat and nortriptyline both increase QTc interval. Use Caution/Monitor.

                • ofloxacin

                  osilodrostat and ofloxacin both increase QTc interval. Use Caution/Monitor.

                • olanzapine

                  osilodrostat and olanzapine both increase QTc interval. Use Caution/Monitor.

                • olodaterol inhaled

                  osilodrostat and olodaterol inhaled both increase QTc interval. Use Caution/Monitor.

                • ondansetron

                  osilodrostat and ondansetron both increase QTc interval. Use Caution/Monitor.

                • osimertinib

                  osilodrostat and osimertinib both increase QTc interval. Use Caution/Monitor.

                • oxaliplatin

                  osilodrostat and oxaliplatin both increase QTc interval. Use Caution/Monitor.

                • ozanimod

                  ozanimod and osilodrostat both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.

                • paliperidone

                  osilodrostat and paliperidone both increase QTc interval. Use Caution/Monitor.

                • panobinostat

                  osilodrostat and panobinostat both increase QTc interval. Use Caution/Monitor.

                • pasireotide

                  osilodrostat and pasireotide both increase QTc interval. Use Caution/Monitor.

                • pazopanib

                  osilodrostat and pazopanib both increase QTc interval. Use Caution/Monitor.

                • pentamidine

                  osilodrostat and pentamidine both increase QTc interval. Use Caution/Monitor.

                • pentobarbital

                  pentobarbital will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • phenobarbital

                  phenobarbital will decrease the level or effect of osilodrostat by Other (see comment). Modify Therapy/Monitor Closely. Osilodrostat is a CYP3A4 and CYP2B6 subtrate. Monitor cortisol concentration and patient?s signs and symptoms during coadministration and discontinuation with strong CYP3A4 and/or CYP2B6 inducers. Adjust dose of osilodrostat if necessary.

                • phenytoin

                  phenytoin will decrease the level or effect of osilodrostat by Other (see comment). Modify Therapy/Monitor Closely. Osilodrostat is a CYP3A4 and CYP2B6 subtrate. Monitor cortisol concentration and patient?s signs and symptoms during coadministration and discontinuation with strong CYP3A4 and/or CYP2B6 inducers. Adjust dose of osilodrostat if necessary.

                • pimavanserin

                  osilodrostat and pimavanserin both increase QTc interval. Use Caution/Monitor.

                • pimozide

                  osilodrostat and pimozide both increase QTc interval. Use Caution/Monitor.

                • pitolisant

                  osilodrostat and pitolisant both increase QTc interval. Use Caution/Monitor.

                • posaconazole

                  posaconazole will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • primaquine

                  osilodrostat and primaquine both increase QTc interval. Use Caution/Monitor.

                • primidone

                  primidone will decrease the level or effect of osilodrostat by Other (see comment). Modify Therapy/Monitor Closely. Osilodrostat is a CYP3A4 and CYP2B6 subtrate. Monitor cortisol concentration and patient?s signs and symptoms during coadministration and discontinuation with strong CYP3A4 and/or CYP2B6 inducers. Adjust dose of osilodrostat if necessary.

                • procainamide

                  osilodrostat and procainamide both increase QTc interval. Use Caution/Monitor.

                • propofol

                  osilodrostat and propofol both increase QTc interval. Use Caution/Monitor.

                • quetiapine

                  osilodrostat and quetiapine both increase QTc interval. Use Caution/Monitor.

                • quinidine

                  osilodrostat and quinidine both increase QTc interval. Use Caution/Monitor.

                • quinine

                  osilodrostat and quinine both increase QTc interval. Use Caution/Monitor.

                • ranolazine

                  osilodrostat and ranolazine both increase QTc interval. Use Caution/Monitor.

                • ribociclib

                  osilodrostat and ribociclib both increase QTc interval. Use Caution/Monitor.

                  ribociclib will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

                • rifabutin

                  rifabutin will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • rifampin

                  rifampin will decrease the level or effect of osilodrostat by Other (see comment). Use Caution/Monitor. Osilodrostat is a CYP3A4 and CYP2B6 subtrate. Monitor cortisol concentration and patient?s signs and symptoms during coadministration and discontinuation with strong CYP3A4 and/or CYP2B6 inducers. Adjust dose of osilodrostat if necessary.

                  rifampin will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

                • rifapentine

                  rifapentine will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • rilpivirine

                  osilodrostat and rilpivirine both increase QTc interval. Use Caution/Monitor.

                • risperidone

                  osilodrostat and risperidone both increase QTc interval. Use Caution/Monitor.

                • ritonavir

                  ritonavir will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • romidepsin

                  osilodrostat and romidepsin both increase QTc interval. Use Caution/Monitor.

                • rucaparib

                  rucaparib will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

                • salmeterol

                  osilodrostat and salmeterol both increase QTc interval. Use Caution/Monitor.

                • saquinavir

                  saquinavir will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                  osilodrostat and saquinavir both increase QTc interval. Use Caution/Monitor.

                • secobarbital

                  secobarbital will decrease the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor cortisol concentration and patient?s signs and symptoms during coadministration or discontinuation with strong CYP3A4 inducers. Adjust dose of osilodrostat if necessary.

                • selpercatinib

                  selpercatinib and osilodrostat both increase QTc interval. Use Caution/Monitor.

                • sertraline

                  osilodrostat and sertraline both increase QTc interval. Use Caution/Monitor.

                • siponimod

                  osilodrostat and siponimod both increase QTc interval. Use Caution/Monitor.

                • solifenacin

                  osilodrostat and solifenacin both increase QTc interval. Use Caution/Monitor.

                • sorafenib

                  osilodrostat and sorafenib both increase QTc interval. Use Caution/Monitor.

                • sotalol

                  osilodrostat and sotalol both increase QTc interval. Use Caution/Monitor.

                • stiripentol

                  stiripentol, osilodrostat. Other (see comment). Modify Therapy/Monitor Closely. Comment: Stiripentol is both an inhibitor and inducer of CYP2B6, and CYP3A4. Osilodrostat is a CYP3A4 and CYP2B6 subtrate. Monitor cortisol concentration and patient?s signs and symptoms during coadministration and discontinuation with stiripentol. Adjust dose of osilodrostat if necessary.

                • sunitinib

                  osilodrostat and sunitinib both increase QTc interval. Use Caution/Monitor.

                • tacrolimus

                  osilodrostat and tacrolimus both increase QTc interval. Use Caution/Monitor.

                • telavancin

                  osilodrostat and telavancin both increase QTc interval. Use Caution/Monitor.

                • terbutaline

                  osilodrostat and terbutaline both increase QTc interval. Use Caution/Monitor.

                • tetrabenazine

                  osilodrostat and tetrabenazine both increase QTc interval. Use Caution/Monitor.

                • theophylline

                  osilodrostat will increase the level or effect of theophylline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

                • thioridazine

                  osilodrostat and thioridazine both increase QTc interval. Use Caution/Monitor.

                • tipranavir

                  tipranavir will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                • tizanidine

                  osilodrostat will increase the level or effect of tizanidine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

                • toremifene

                  osilodrostat and toremifene both increase QTc interval. Use Caution/Monitor.

                • trazodone

                  osilodrostat and trazodone both increase QTc interval. Use Caution/Monitor.

                • triclabendazole

                  osilodrostat and triclabendazole both increase QTc interval. Use Caution/Monitor.

                • triptorelin

                  osilodrostat and triptorelin both increase QTc interval. Use Caution/Monitor.

                • valbenazine

                  valbenazine and osilodrostat both increase QTc interval. Use Caution/Monitor.

                • valproic acid

                  osilodrostat will decrease the level or effect of valproic acid by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

                • vandetanib

                  osilodrostat and vandetanib both increase QTc interval. Use Caution/Monitor.

                • vardenafil

                  osilodrostat and vardenafil both increase QTc interval. Use Caution/Monitor.

                • vemurafenib

                  osilodrostat and vemurafenib both increase QTc interval. Use Caution/Monitor.

                • voclosporin

                  voclosporin, osilodrostat. Either increases effects of the other by QTc interval. Use Caution/Monitor.

                • voriconazole

                  voriconazole will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of osilodrostat, a CYP3A4 substrate, by half when coadministered with a strong CYP3A4 inhibitor.

                  osilodrostat and voriconazole both increase QTc interval. Use Caution/Monitor.

                • vorinostat

                  osilodrostat and vorinostat both increase QTc interval. Use Caution/Monitor.

                • ziprasidone

                  osilodrostat and ziprasidone both increase QTc interval. Use Caution/Monitor.

                Minor (4)

                • acetazolamide

                  acetazolamide will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

                • anastrozole

                  anastrozole will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

                • cyclophosphamide

                  cyclophosphamide will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

                • larotrectinib

                  larotrectinib will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

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                Adverse Effects

                >10%

                Adrenal insufficiency (43.1%)

                Fatigue (38.7%)

                Nausea (37.2%)

                Headache (30.7%)

                Edema (21.2%)

                Nasopharyngitis (19.7%)

                Vomiting (19%)

                Arthralgia (17.5%)

                Back pain (15.3%)

                Rash (15.3%)

                Diarrhea (14.6%)

                Blood corticotrophin increased (13.9%)

                Dizziness (13.9%)

                Abdominal pain (13.1%)

                Hypokalemia (12.4%)

                Myalgia (12.4%)

                Decreased appetite (11.7%)

                Hormone level abnormal (11.7%)

                Hypotension (11.7%)

                Urinary tract infection (11.7%)

                Blood testosterone increased (10.9%)

                Pyrexia (10.9%)

                Anemia (10.2%)

                Cough (10.2%)

                Hypertension (10.2%)

                Influenza (10.2%)

                1-10%

                Hirsutism (9.5%)

                Acne (8.8%)

                Dyspepsia (8%)

                Insomnia (8%)

                Anxiety (7.3%)

                Depression (7.3%)

                Gastroenteritis (7.3%)

                Malaise (6.6%)

                Tachycardia (6.6%)

                Alopecia (5.8%)

                Transaminases increased (4.4%)

                ECG QT prolongation (3.6%)

                Syncope (1.5%)

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                Warnings

                Contraindications

                None

                Cautions

                Hypocortisolism

                • Osilodrostat lowers cortisol levels and can lead to hypocortisolism and sometimes life-threatening adrenal insufficiency
                • Lowering of cortisol can cause nausea, vomiting, fatigue, abdominal pain, loss of appetite, dizziness; significant lowering may result in hypotension, abnormal electrolyte levels, and hypoglycemia
                • Can occur at any time during treatment; evaluate for precipitating causes of hypocortisolism (eg, infection, physical stress)
                • Monitor 24-hr urine free cortisol (UFC), serum or plasma cortisol, and signs/symptoms
                • Decrease or temporarily discontinue osilodrostat if UFC levels fall below target range, there is a rapid decrease in cortisol levels, and/or symptoms of hypocortisolism occur
                • Stop osilodrostat and administer exogenous glucocorticoid replacement therapy if serum or plasma cortisol levels are below target range and patients have symptoms of adrenal insufficiency
                • Reinitiate at lower dose when urine free, serum, or plasma cortisol levels are within target range, and/or patient symptoms have resolved
                • After discontinuation, cortisol suppression may persist beyond the 4 hr drug half-life

                QTc prolongation

                • Associated with dose-dependent QT interval prolongation (maximum mean estimated QTcF increase of up to 5.3 ms at 30 mg), which may cause cardiac arrhythmias
                • Obtain baseline ECG with QTc interval measurement before initiating and monitor QTc interval thereafter
                • Correct hypokalemia and/or hypomagnesemia before initiating and monitor periodically during treatment; correct electrolyte abnormalities if indicated
                • Consider temporary discontinuation if QTc interval >480 ms
                • Caution with risk factors for QT prolongation, (eg, congenital long QT syndrome, CHF, bradyarrhythmias, uncorrected electrolyte abnormalities, other drugs known to prolong QT) and consider more frequent ECG monitoring

                Elevated adrenal hormone precursors and androgens

                • Osilodrostat blocks cortisol synthesis and may increase circulating levels of cortisol and aldosterone precursors (11-deoxy cortisol and 11-deoxycorticosterone) and androgens
                • Elevated 11-deoxycorticosterone levels may activate mineralocorticoid receptors and cause hypokalemia, edema, and hypertension
                • Correct hypokalemia before initiating
                • Monitor for hypokalemia, worsening hypertension, and edema
                • Treat osilodrostat-induced hypokalemia with IV or oral potassium supplementation based on event severity; if hypokalemia persists despite potassium supplementation, consider adding mineralocorticoid antagonists; osilodrostat dose reduction or discontinuation may be necessary
                • Accumulation of androgens may lead to hirsutism, hypertrichosis, and acne (in females)

                Drug interaction overview

                • Strong CYP3A4 inhibitors
                  • Osilodrostat is a substrate of CYP3A4 substrate (major)
                  • Reduce osilodrostat dose by 50% if coadministered with strong CYP3A4 inhibitors
                • Strong CYP3A4 and/or CYP2B6 inducers
                  • Osilodrostat is a substrate of CYP3A4 (major) and CYP2B6 (moderate)
                  • Coadministration with strong CYP3A4 and/or CYP2B6 inducers may decrease osilodrostat concentration and reduce efficacy
                  • Discontinuation of strong CYP3A4 and/or CYP2B6 inducers while using osilodrostat may increase osilodrostat concentration and the related adverse effects
                • CYP1A2 and CYP2C19 substrates
                  • Osilodrostat showed inhibition potential on CYP1A2 and CYP2C19 in clinical studies
                  • Caution if coadministered with CYP1A2 or CYP2C19 substrates with a narrow therapeutic index
                • QTc prolonging drugs
                  • Osilodrostat is associated with dose-dependent QT interval prolongation
                  • Caution if coadministered with other drugs known to prolong QT interval
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                Pregnancy & Lactation

                Pregnancy

                Data are not available regarding use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

                There are risks to the mother and fetus associated with active Cushing syndrome during pregnancy

                Clinical considerations

                • Active Cushing syndrome during pregnancy associated with increased risk of maternal and fetal morbidity and mortality (including gestational diabetes, gestational hypertension, preeclampsia, maternal death, miscarriage, fetal loss, preterm birth)

                Animal data

                • No adverse developmental outcomes observed in reproduction studies in pregnant rats and rabbits when exposed during organogenesis at doses that produced maternal exposures of 7 and 0.5 times the 30-mg BID maximum clinical dose, by AUC
                • In rabbits, exposures associated with maternal toxicity at 7 times the maximum clinical dose resulted in decreased fetal viability
                • No adverse developmental outcomes were observed in a prenatal and postnatal development study with administration to pregnant rats from organogenesis through lactation at 8 times the 30-mg BID maximum clinical dose

                Lactation

                Data are not available regarding presence in human or animal milk, effects on breastfed infants, or effects on milk production

                Because of potential for serious adverse effects (eg, adrenal insufficiency), do not breastfeed during treatment and for at least 1 week after discontinuing drug

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

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                Pharmacology

                Mechanism of Action

                Orally administered steroidogenesis inhibitor of 11-beta-hydroxylase, an enzyme that catalyzes the final step of cortisol synthesis in the adrenal cortex

                Absorption

                Peak plasma time: 1 hr

                Distribution

                Protein bound: 36.4%

                Vd: 100 L

                Metabolism

                Multiple CYP enzymes (ie, CYP3A4, CYP2B6, CYP2D6) and UDP-glucuronosyltransferases contribute to metabolism

                No single enzyme contributes >25% to total clearance

                Metabolites are not expected to contribute to the pharmacological effect

                Elimination

                Half-life: 4 hr

                Excretion: 90.6% urine (5.2% as unchanged); 1.58% feces

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                Administration

                Oral Administration

                May take with or without food

                Missed dose: Take next dose at the regularly scheduled time

                Storage

                Store at room temperature of 68-77ºF (20-25ºC); excursions permitted to 15-30ºC (59-86ºF)

                Protect from moisture

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                Images

                No images available for this drug.
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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

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                Create Your List of Plans

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                • Compare formulary status to other drugs in the same class.
                • Access your plan list on any device – mobile or desktop.

                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                View explanations for tiers and restrictions
                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
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                ST Step Therapy
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