bosutinib (Rx)

Brand and Other Names:Bosulif
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 100mg
  • 400mg
  • 500mg

Chronic Myelogenous Leukemia

Newly-diagnosed chronic phase Philadelphia chromosome positive

  • Indicated for newly diagnosed chronic phase (CP) Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML)
  • 400 mg PO qDay with food
  • Continue until disease progression or unacceptable toxicity

Chronic, accelerated, or blast phase Philadelphia chromosome positive

  • Indicated for chronic, accelerated, or blast phase Ph+ CML in patients resistant to or intolerant to other therapies, including imatinib
  • 500 mg PO qDay with food
  • Continue until disease progression or unacceptable toxicity

Dose escalation

  • Consider escalating dose in patients with Ph+ CML who did not achieve or maintain a hematologic, cytogenetic, or molecular response and did not have Grade ≥3 adverse reactions at the initial dose
  • May increase dose by 100-mg/day increments; not to exceed 600 mg/day

Dosage Modifications

Renal impairment

  • Hemodialysis: Safety and efficacy not established
  • For patients who have declining renal function while on bosutinib who cannot tolerate the starting dose, follow dose adjustment recommendations for toxicity
  • Newly diagnosed chronic phase Ph+ CML
    • CrCl 30-50 mL/min: 300 mg PO qDay
    • CrCl <30 mL/min: 200 mg PO qDay
  • Chronic, accelerated, or blast phase Ph+ CML
    • CrCl 30-50 mL/min: 400 mg PO qDay
    • CrCl <30 mL/min: 300 mg PO qDay

Hepatic impairment

  • Mild to severe (Child-Pugh A to C): 200 mg PO qDay
  • There are no clinical data for efficacy at 200-mg/day

Hepatotoxicity

  • AST/ALT>5X ULN: Hold until recovery to ≤2.5X ULN; resume at 400 mg qDay thereafter; discontinue if recovery takes >4 weeks
  • AST/ALT ≥3X ULN concurrently with bilirubin elevations >2X ULN and alkaline phosphatase <2X ULN (Hy’s law case definition): Discontinue treatment

Diarrhea

  • Grade 3-4 (≥7 stools/day over baseline/pretreatment): Hold until recovery to Grade ≤1; may resume dose at 400 mg qDay

Other moderate or severe nonhematologic toxicities

  • Withhold until toxicity resolved, and then consider reducing dose by 100 mg/day
  • If clinically appropriate, consider re-escalating to the initial dose taken once daily
  • Doses <300 mg/day have been used in patients; however, efficacy has not been established

Myelosuppression

  • ANC <1000 x 106/L or platelets <50,000 x 106/L: Withhold until ANC ≥1000 x106/L and platelets ≥50,000 x106/L
  • Resume at same dose if recovery occurs within 2 weeks
  • If blood cell counts remain low for >2 weeks, reduce dose by 100 mg upon recovery and resume treatment
  • If cytopenia recurs, reduce dose by an additional 100 mg upon recovery and resume treatment
  • Doses <300 mg/day have been used in patients; however, efficacy has not been established

Dosing Considerations

Verify pregnancy status in females of reproductive potential prior to initiation

<18 years: Safety and efficacy not established

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Interactions

Interaction Checker

and bosutinib

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            Contraindicated (1)

            • lefamulin

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

            Serious - Use Alternative (93)

            • abametapir

              abametapir increases levels of bosutinib 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.

            • abiraterone

              abiraterone increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • amiodarone

              amiodarone increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              amiodarone increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • apalutamide

              apalutamide will decrease the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

            • aprepitant

              aprepitant increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • atazanavir

              atazanavir increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • atorvastatin

              atorvastatin increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • bicalutamide

              bicalutamide increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • bosentan

              bosentan decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85% .

            • carbamazepine

              carbamazepine decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85% .

            • carvedilol

              carvedilol increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • cimetidine

              cimetidine increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • clarithromycin

              clarithromycin increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

              clarithromycin increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • clotrimazole

              clotrimazole increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • clozapine

              clozapine increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • cobicistat

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

            • conivaptan

              conivaptan increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • crizotinib

              crizotinib increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • cyclosporine

              cyclosporine increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              cyclosporine increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • darunavir

              darunavir increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • desipramine

              desipramine increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • dexamethasone

              dexamethasone decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85% .

            • diltiazem

              diltiazem increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • dipyridamole

              dipyridamole increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • doxycycline

              doxycycline increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • dronedarone

              dronedarone increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              dronedarone increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • efavirenz

              efavirenz decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85% .

            • enzalutamide

              enzalutamide decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85% .

            • erythromycin base

              erythromycin base increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              erythromycin base increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              erythromycin ethylsuccinate increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • erythromycin lactobionate

              erythromycin lactobionate increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erythromycin stearate

              erythromycin stearate increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • eslicarbazepine acetate

              eslicarbazepine acetate will decrease the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%

              eslicarbazepine acetate decreases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • etravirine

              etravirine decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • famotidine

              famotidine will decrease the level or effect of bosutinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • fexinidazole

              fexinidazole and bosutinib 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 bosutinib 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.

            • fluconazole

              fluconazole increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • fosamprenavir

              fosamprenavir increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • fosphenytoin

              fosphenytoin decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • grapefruit

              grapefruit increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              grapefruit increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • haloperidol

              haloperidol increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • ibuprofen/famotidine

              ibuprofen/famotidine will decrease the level or effect of bosutinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • idelalisib

              idelalisib will increase the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates

            • imatinib

              imatinib increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • indinavir

              indinavir increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • isoniazid

              isoniazid increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • itraconazole

              itraconazole increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

              itraconazole increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • ivosidenib

              ivosidenib will decrease the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

            • ketoconazole

              ketoconazole increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

              ketoconazole increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • lapatinib

              lapatinib increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              lapatinib increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • lidocaine

              lidocaine increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • lonafarnib

              lonafarnib will increase the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.

            • lopinavir

              lopinavir increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

              lopinavir increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • lorlatinib

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

            • mefloquine

              mefloquine increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • metronidazole

              metronidazole increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • nafcillin

              nafcillin decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • nefazodone

              nefazodone increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • nelfinavir

              nelfinavir increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

              nelfinavir increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • nevirapine

              nevirapine decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • nicardipine

              nicardipine increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

              nicardipine increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • nilotinib

              nilotinib increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • nizatidine

              nizatidine will decrease the level or effect of bosutinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • oxcarbazepine

              oxcarbazepine decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • palifermin

              palifermin increases toxicity of bosutinib by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.

            • pentobarbital

              pentobarbital decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • phenobarbital

              phenobarbital decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • phenytoin

              phenytoin decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • posaconazole

              posaconazole increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • primidone

              primidone decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • progesterone, natural

              progesterone, natural increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • propafenone

              propafenone increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • propranolol

              propranolol increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • quinidine

              quinidine increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

              quinidine increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • ranolazine

              ranolazine increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • ribociclib

              ribociclib will increase the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • rifabutin

              rifabutin decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • rifampin

              rifampin decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • rifapentine

              rifapentine decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decreased bosutinib plasma concentration by ~85%.

            • ritonavir

              ritonavir increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

              ritonavir increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • saquinavir

              saquinavir increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

              saquinavir increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • sertraline

              sertraline increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • simvastatin

              simvastatin increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • sunitinib

              sunitinib increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • tacrolimus

              tacrolimus increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • tamoxifen

              tamoxifen increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • tetracycline

              tetracycline increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • tipranavir

              tipranavir increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • tolvaptan

              tolvaptan increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • tucatinib

              tucatinib will increase the level or effect of bosutinib 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.

            • verapamil

              verapamil increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              verapamil increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • voriconazole

              voriconazole increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • voxelotor

              voxelotor will increase the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

            Monitor Closely (108)

            • aliskiren

              bosutinib increases levels of aliskiren by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • aluminum hydroxide

              aluminum hydroxide decreases levels of bosutinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Bosutinib displays pH-dependent solubility; may use short-acting antacids with administration separated by 2 hr.

            • amiodarone

              bosutinib increases levels of amiodarone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • arsenic trioxide

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

            • aspirin/citric acid/sodium bicarbonate

              aspirin/citric acid/sodium bicarbonate decreases levels of bosutinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Bosutinib displays pH-dependent solubility; may use short-acting antacids with administration separated by 2 hr.

            • atorvastatin

              bosutinib increases levels of atorvastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • bedaquiline

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

            • belzutifan

              belzutifan will decrease the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.

            • betrixaban

              bosutinib increases levels of betrixaban by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Decrease betrixaban dose to 80 mg PO once, then 40 mg PO qDay if coadministered with a P-gp inhibitor.

            • cabazitaxel

              bosutinib increases levels of cabazitaxel by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • calcium carbonate

              calcium carbonate decreases levels of bosutinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Bosutinib displays pH-dependent solubility; may use short-acting antacids with administration separated by 2 hr.

            • carvedilol

              bosutinib increases levels of carvedilol by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • cenobamate

              cenobamate will decrease the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

            • cetirizine

              bosutinib increases levels of cetirizine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • chlorpromazine

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

            • cimetidine

              bosutinib increases levels of cimetidine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • ciprofloxacin

              bosutinib increases levels of ciprofloxacin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • cisapride

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

            • crofelemer

              crofelemer increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.

            • dabrafenib

              dabrafenib will decrease the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

            • darunavir

              darunavir increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Strong CYP3A4 inhibitors increases bosutinib plasma concentration ~5-fold.

            • daunorubicin

              bosutinib increases levels of daunorubicin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • desloratadine

              bosutinib increases levels of desloratadine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • dexamethasone

              bosutinib increases levels of dexamethasone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • dexlansoprazole

              dexlansoprazole decreases levels of bosutinib by Other (see comment). Use Caution/Monitor. Comment: PPIs may decrease bosutinib concentration by ~45%; bosutinib displays pH-dependent solubility.

            • digoxin

              bosutinib increases levels of digoxin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • disopyramide

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

            • docetaxel

              bosutinib increases levels of docetaxel by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • dofetilide

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

            • doxorubicin

              bosutinib increases levels of doxorubicin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • duvelisib

              duvelisib will increase the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. will increase the level or effect of

            • elagolix

              elagolix will decrease the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

            • encorafenib

              encorafenib, bosutinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.

            • erythromycin base

              bosutinib increases levels of erythromycin base by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • erythromycin ethylsuccinate

              bosutinib increases levels of erythromycin ethylsuccinate by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • esomeprazole

              esomeprazole will decrease the level or effect of bosutinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Bosutinib displays pH dependent solubility

            • estradiol

              bosutinib increases levels of estradiol by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • etoposide

              bosutinib increases levels of etoposide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • fedratinib

              fedratinib will increase the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

            • fexofenadine

              bosutinib increases levels of fexofenadine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • fosamprenavir

              bosutinib increases levels of fosamprenavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • fostemsavir

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

            • goserelin

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

            • haloperidol

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

            • histrelin

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

            • hydrocortisone

              bosutinib increases levels of hydrocortisone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • ibutilide

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

            • idarubicin

              bosutinib increases levels of idarubicin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • iloperidone

              iloperidone increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.

            • indinavir

              bosutinib increases levels of indinavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • irinotecan

              bosutinib increases levels of irinotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • irinotecan liposomal

              bosutinib increases levels of irinotecan liposomal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • istradefylline

              istradefylline will increase the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

            • ivermectin

              bosutinib increases levels of ivermectin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lansoprazole

              lansoprazole decreases levels of bosutinib by Other (see comment). Use Caution/Monitor. Comment: PPIs may decrease bosutinib concentration by ~45%; bosutinib displays pH-dependent solubility.

            • lenvatinib

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

            • lidocaine

              bosutinib increases levels of lidocaine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • loperamide

              bosutinib increases levels of loperamide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • loratadine

              bosutinib increases levels of loratadine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lovastatin

              bosutinib increases levels of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • magnesium oxide

              magnesium oxide decreases levels of bosutinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Bosutinib displays pH-dependent solubility; may use short-acting antacids with administration separated by 2 hr.

            • methadone

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

            • methotrexate

              bosutinib increases levels of methotrexate by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • mitomycin

              bosutinib increases levels of mitomycin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • mitotane

              mitotane decreases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.

            • nadolol

              bosutinib increases levels of nadolol by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nelfinavir

              bosutinib increases levels of nelfinavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nicardipine

              bosutinib increases levels of nicardipine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • olodaterol inhaled

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

            • omeprazole

              omeprazole decreases levels of bosutinib by Other (see comment). Use Caution/Monitor. Comment: PPIs may decrease bosutinib concentration by ~45%; bosutinib displays pH-dependent solubility.

            • ondansetron

              bosutinib increases levels of ondansetron by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • osilodrostat

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

            • oxaliplatin

              oxaliplatin and bosutinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Use of oxaliplatin with concomitant immunosuppressants or with impaired immune systems may increased risk for serious infections.

            • paclitaxel

              bosutinib increases levels of paclitaxel by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • paclitaxel protein bound

              bosutinib increases levels of paclitaxel protein bound by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • paliperidone

              bosutinib increases levels of paliperidone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • pantoprazole

              pantoprazole decreases levels of bosutinib by Other (see comment). Use Caution/Monitor. Comment: PPIs may decrease bosutinib concentration by ~45%; bosutinib displays pH-dependent solubility.

            • pazopanib

              bosutinib increases levels of pazopanib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • ponesimod

              ponesimod and bosutinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

            • pravastatin

              bosutinib increases levels of pravastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • procainamide

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

            • quinidine

              bosutinib increases levels of quinidine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

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

            • quinine

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

            • rabeprazole

              rabeprazole decreases levels of bosutinib by Other (see comment). Use Caution/Monitor. Comment: PPIs may decrease bosutinib concentration by ~45%; bosutinib displays pH-dependent solubility.

            • ranolazine

              bosutinib increases levels of ranolazine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • rifampin

              bosutinib increases levels of rifampin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • ritonavir

              bosutinib increases levels of ritonavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • rucaparib

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

            • saquinavir

              bosutinib increases levels of saquinavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • saxagliptin

              bosutinib increases levels of saxagliptin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • selpercatinib

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

            • siponimod

              siponimod and bosutinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

            • sirolimus

              bosutinib increases levels of sirolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • sitagliptin

              bosutinib increases levels of sitagliptin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • sodium zirconium cyclosilicate

              sodium zirconium cyclosilicate will decrease the level or effect of bosutinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Check specific recommendations for drugs that exhibit pH-dependent solubility that may affect their systemic exposure and efficacy. In general, administer drugs at least 2 hr before or after sodium zirconium cyclosilicate.

            • stiripentol

              stiripentol, bosutinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

            • tacrolimus

              bosutinib increases levels of tacrolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • tazemetostat

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

            • tecovirimat

              tecovirimat will decrease the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

            • temsirolimus

              bosutinib increases levels of temsirolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • teniposide

              bosutinib increases levels of teniposide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • tolvaptan

              bosutinib increases levels of tolvaptan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • vandetanib

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

            • verapamil

              bosutinib increases levels of verapamil by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • vinblastine

              bosutinib increases levels of vinblastine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • vincristine

              bosutinib increases levels of vincristine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • voclosporin

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

            • ziprasidone

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

            Minor (0)

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              Adverse Effects

              >10%

              Newly diagnosed CP CML

              • All grades
                • Creatinine increased (94%)
                • Hemoglobin decreased (89%)
                • Lymphocyte count decreased (84%)
                • Diarrhea (75%)
                • Platelet count decreased (68%)
                • Serum glutamic-pyruvic transaminase (SGPT)/ALT increased (68%)
                • Glucose increased (57%)
                • Serum glutamic-oxaloacetic transaminase (SGOT)/AST increased (56%)
                • Calcium decreased (55%)
                • Phosphorus decreased (54%)
                • Lipase increased (53%)
                • WBC decreased (50%)
                • Hepatic dysfunction (45%)
                • ANC decreased (42%)
                • Alkaline phosphatase increased (41%)
                • Rash (40%)
                • Abdominal pain (39%)
                • Nausea (37%)
                • Creatine kinase increased (36%)
                • Fatigue (33%)
                • Amylase increased (32%)
                • Respiratory tract infection (27%)
                • Headache (22%)
                • Vomiting (21%)
                • Arthralgia (18%)
                • Pyrexia (17%)
                • Edema (15%)
                • Constipation (13%)
                • Back pain (12%)
                • Pruritus (11%)
                • Cough (11%)
                • Dyspnea (11%)
                • Decreased appetite (11%)
              • Grade 3 or 4
                • SGPT/ALT increased (26%)
                • Hepatic dysfunction (27%)
                • Lipase increased (19%)
                • Platelet count (14%)
                • SGOT/AST increased (13%)
                • Lymphocyte count (12%)
                • Pruritus (11%)
                • Hypertension (11%)

              Imatinib-resistant or -intolerant Ph+ CP, AP, and BP CML

              • All grades
                • Hemoglobin decreased (89-97%)
                • Creatinine increased (87-95%)
                • Diarrhea (76-85%)
                • Lymphocyte decreased (79-82%)
                • Platelet count decreased (66-80%)
                • ANC decreased (50-66%)
                • SGPT/ALT increased (39-58%)
                • WBC decreased (51-57%)
                • Calcium decreased (45-55%)
                • SGOT/AST increased (37-50%)
                • Abdominal pain (36-49%)
                • Urate increased (43-46%)
                • Rash (42-48%)
                • Nausea (47-48%)
                • Vomiting (38-43%)
                • Glucose increased (39-42%)
                • Phosphorus decreased (33-41%)
                • Alkaline phosphatase increased (39%)
                • Fatigue (27-35%)
                • Lipase increased (19-32%)
                • Hepatic dysfunction (21-29%)
                • Potassium decreased (22-29%)
                • Magnesium increased (18-27%)
                • Respiratory tract infection (17-27%)
                • Potassium increased (19-25%)
                • Pyrexia (25-37%)
                • Cough (224%)
                • Sodium decreased (18-27%)
                • Sodium increased (11-23%)
                • Total bilirubin increased (16-22%)
                • Headache (18-21%)
                • Dyspnea (12-20%)
                • Edema (17-19%)
                • Arthralgia (15-19%)
                • Pneumonia (10-18%)
                • Constipation (15-17%)
                • Decreased appetite (14%)
                • Pleural effusion (9-14%)
                • Dizziness (11-14%)
                • Back pain (8-14%)
                • Chest pain (8-12%)
                • Pruritis (7-12%)
                • Hypertension (8-11%)
                • Influenza (3-11%)
              • Grade 3 or 4
                • Platelet count decreased (26-57%)
                • ANC decreased (16-39%)
                • Hemoglobin decreased (13-38%)
                • WBC decreased (7-27%)
                • Lymphocyte (14-21%)
                • Lipase increased (6-12%)
                • Pneumonia (4-12%)
                • Hepatic dysfunction (10-11%)
                • SGPT/ALT increased (6-11%)

              1-10%

              Pulmonary hypertension

              Acute kidney injury

              Renal impairment

              Renal failure

              Dysgeusia

              Myalgia

              Dehydration

              Electrocardiogram QT prolonged

              Bronchitis

              Drug hypersensitivity

              Pain

              Gastritis

              Pancreatitis

              Gastrointestinal hemorrhage

              Hypothyroidism

              Tinnitus

              Pericardial effusion

              Newly diagnosed CP CML

              • Grade 3 or 4
                • Diarrhea (9%)
                • ANC decreased (9%)
                • Hemoglobin decreased (9%)
                • Phosphorus decreased (9%)
                • WBC decreased (6%)
                • Hypertension (5%)
                • Amylase increased (3.4%)
                • Glucose increased (3%)
                • Creatinine kinase increased (3%)
                • Rash (2%)
                • Abdominal pain (2%)
                • Calcium decreased (1.5%)
                • Creatinine increased (1.1%)
                • Vomiting (1%)
                • Dyspnea (1%)
                • Arthralgia (1%)
                • Headache (1%)
                • Respiratory tract infection (1%)
                • Pyrexia (1%)
                • Fatigue (1%)

              Imatinib-resistant or -intolerant Ph+ CP, AP, and BP CML

              • All grades
                • Chest pain (8%)
              • Grade 3 or 4
                • Diarrhea (4-10%)
                • Rash (5-9%)
                • Phosphorus decreased (7-8%)
                • Abdominal pain (2-7%)
                • Fatigue (3-6%)
                • SGOT/AST increased (3.5-5%)
                • Pleural effusion (4%)
                • Vomiting (3%)
                • Hypertension (3%)
                • Pyrexia (1-3%)
                • Total bilirubin increased (0.7-2.8%)
                • Dyspnea (2%)
                • Nausea (1-2%)
                • Chest pain (1%)
                • Headache (1%)
                • Back pain (1%)
                • Decreased appetite (<1%)
                • Constipation (<1%)
                • Edema (<1%)
                • Influenza (<1%)
                • Pruritis (<1%)
                • Respiratory tract infection (<1%)
                • Arthralgia (<1%)

              <1%

              Febrile neutropenia

              Pericarditis

              Hyperthyroidism

              Acute pulmonary edema (eg, acute pulmonary edema, pulmonary edema)

              Erythema multiforme

              Newly diagnosed CP CML

              • Grade 3 or 4
                • Decreased appetite
                • Back pain
                • Pruritis

              Postmarketing Reports

              Thrombotic microangiopathy

              Stevens Johnson syndrome

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              Warnings

              Contraindications

              Hypersensitivity

              Cautions

              Diarrhea, nausea, vomiting, and abdominal pain may occur; monitor and manage patients using standards of care, including antidiarrheals, antiemetics, and fluid replacement

              Thrombocytopenia, anemia, and neutropenia occur with treatment; perform CBC weekly for first month and then monthly thereafter, or as clinically indicated

              Fluid retention may occur and manifest as pericardial effusion, pleural effusion, pulmonary edema, and/or peripheral edema

              Cardiac failure and left ventricular dysfunction have been reported in patients taking; monitor for signs and symptoms consistent with cardiac failure and treat as clinically indicated; interrupt, dose reduce, or discontinue as necessary

              Decline in glomerular filtration rate reported in patients receiving therapy, which in turn increases bosutinib exposure in patients; use caution in patients with moderate renal impairment; dosage adjustment recommended

              Fetal harm may occur when administered to pregnant females

              Hepatic toxicity

              • Elevated ALT, AST, and/or bilirubin may occur; perform monthly hepatic enzyme tests for first 3 months during treatment, and then as clinically indicated
              • Median time to onset of increased ALT and AST was 35 and 33 days; median duration for each was 21 days
              • Perform hepatic enzyme tests monthly for the first 3 months of treatment and as clinically indicated; in patients with transaminase elevations, monitor liver enzymes more frequently

              Drug interaction overview

              • CYP3A4 substrate
              • Strong or moderate CYP3A4 inhibitors
                • Avoid coadministration
                • Strong or moderate CYP3A4 inhibitors increase bosutinib Cmax and AUC, which may increase the risk of toxicities
              • Strong CYP3A4 inducers
                • Avoid coadministration
                • Strong CYP3A4 inducers decrease bosutinib Cmax and AUC, which may reduce efficacy
              • Proton pump inhibitors (PPI)
                • Use short-acting antacids or H2-blockers as an alternant; separate dosing by >2 hr from bosutinib dosing
                • PPIs decrease bosutinib Cmax and AUC, which may reduce efficacy
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              Pregnancy & Lactation

              Pregnancy

              No data are available in pregnant women to inform the drug-associated risk; however, fetal harm may occur when administered to pregnant women based on mechanism of action and findings from animal studies

              Verify pregnancy status in females of reproductive potential prior to starting treatment

              Animal data

              • In rats and rabbits, oral administration of bosutinib during organogenesis caused adverse developmental outcomes, including structural abnormalities, embryofetal mortality, and alterations to growth at maternal exposures (AUC) as low as 1.2 times the human exposure at a 500-mg/day dose
              • Advise pregnant women of the potential risk to a fetus

              Contraception

              • Based on findings from animal studies, fetal harm may occur when administered to pregnant females
              • Females of reproductive potential: Use effective contraception during treatment and for at least 2 weeks after the last dose

              Infertility

              • Risk of infertility in females or males of reproductive potential has not been studied in humans
              • Based on findings from animal studies, reduced fertility may occur in females and males of reproductive potential

              Lactation

              No data are available regarding presence of bosutinib or its metabolites in human milk or its effects on a breastfed child or on milk production

              Bosutinib is present in the milk of lactating rats

              Owing to the potential for serious adverse reactions in a nursing child, breastfeeding is not recommended during treatment and for at least 2 weeks after the last dose

              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

              Tyrosine kinase inhibitor; Inhibits Bcr-Abl kinase that promotes CML; also inhibits SRc-family kinases including Src, Lyn, and Hck

              Bosutinib inhibited 16 of 18 imatinib-resistant forms of Bcr-Abl expressed in murine myeloid cell lines, but did not inhibit T315I and V299L mutant cells

              Absorption

              Absolute bioavailability: 34% (healthy volunteers with food)

              Peak plasma time (500-mg dose with food): 6 hr

              Peak plasma concentration

              • Multiple 400-mg doses: 146 ng/mL
              • Multiple 500-mg doses: 200 ng/mL

              AUC

              • Multiple 400-mg doses: 2720 ng•hr/mL
              • Multiple 500-mg doses: 3650 ng•hr/mL

              Effect of food

              • Bosutinib administered with a high-fat meal (800-1000 total calories) increased Cmax by 1.8-fold and increased AUC by 1.7-fold

              Distribution

              Protein bound: 94% (in vivo); 96% (ex vivo)

              Vd: 6,080 L

              P-gp substrate and inhibitor

              Metabolism

              Metabolized by in liver primarily by CYP3A4

              Metabolites (inactive): Oxydechlorinated (M2) bosutinib (19% of parent exposure) and N-desmethylated (M5) bosutinib (25% of parent exposure), with bosutinib N-oxide (M6) as a minor circulating metabolite

              Elimination

              Half-life

              • Single 120-mg IV: 33.5 hr
              • Single oral dose: 22.5 hr

              Clearance

              • Single 120-mg IV: 63.6 L/hr
              • Single oral dose: 189 L/hr

              Excretion: Feces (91.3%); urine (3%)

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              Administration

              Oral Administration

              Take with food

              Swallow tablet whole; do not chew, crush, or cut

              Consider procedures for proper disposal of drug

              Avoid touching or handling crushed or broken tablets

              Take antacids or H2-blockers at least 2 hr before or 2 hr after bosutinib

              Missed dose

              • Missed dose >12 hr: Skip dose and take the usual prescribed dose on the following day: do not take 2 doses at one time

              Storage

              Tablets: Store at 20-25ºC (68-7ºF)

              Discard any unused products or waste materials in accordance with local requirements, or drug take back programs

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              Bosulif oral
              -
              500 mg tablet
              Bosulif oral
              -
              100 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              bosutinib oral

              BOSUTINIB - ORAL

              (boe-SUE-ti-nib)

              COMMON BRAND NAME(S): Bosulif

              USES: Bosutinib is used to treat a certain type of blood cancer (chronic myelogenous leukemia-CML). It works by slowing or stopping the growth of cancer cells.

              HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking bosutinib and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with food as directed by your doctor, usually once daily. Swallow the medication whole. Do not crush, chew, or split the tablets. Avoid handling or touching crushed or broken tablets.The dosage is based on your medical condition and response to treatment. Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.Use this medication regularly to get the most benefit from it. Remember to use it at the same time each dayMedications which reduce or block stomach acid (such as proton pump inhibitors/PPIs, H2 blockers, antacids) may reduce the absorption of bosutinib, making it work less well. Do not take PPIs (such as omeprazole, lansoprazole) while using this medication. If you take antacids or H2 blockers (such as famotidine, ranitidine), take these medications at least 2 hours before or after bosutinib.Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.

              SIDE EFFECTS: Nausea, vomiting, stomach/abdominal pain, loss of appetite, cough, joint pain, headache, or dizziness may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Diarrhea is a common side effect. Drink plenty of fluids as directed by your doctor to reduce your risk of dehydration. Your doctor may prescribe anti-diarrhea medication (such as loperamide) to control your symptoms. Tell your doctor right away if you develop severe or persistent diarrhea, signs of dehydration (such as extreme thirst, dizziness, decreased urination).People using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.This medication decreases bone marrow function, an effect that may lead to a low number of blood cells such as red cells, white cells, and platelets. This effect can cause anemia, decrease your body's ability to fight an infection, or cause easy bruising/bleeding. Tell your doctor right away if you develop any of the following unlikely symptoms: unusual tiredness, pale skin, signs of infection (such as fever, chills, persistent sore throat), easy bleeding/bruising.Tell your doctor right away if you have any serious side effects, including: severe stomach/abdominal pain, yellowing eyes/skin, dark urine, swelling hands/ankles/feet, sudden weight gain, signs of kidney problems (such as change in the amount of urine).Get medical help right away if you have any very serious side effects, including: chest pain, shortness of breath.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.Bosutinib can commonly cause a mild rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe allergic reaction. Get medical help right away if you develop any rash.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Before taking bosutinib, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease.This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis). Alcohol may also increase the risk of serious liver problems.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose). Wash your hands well to prevent the spread of infection.To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while taking bosutinib. Bosutinib may harm an unborn baby. Your doctor should order a pregnancy test before you start this medication. Ask about reliable forms of birth control while using this medication and for 2 weeks after stopping treatment. If you become pregnant, talk to your doctor right away about the risks and benefits of this medication.It is unknown if this medication passes into breast milk. Because of the possible risk to the infant, breast-feeding is not recommended while using this drug and for 2 weeks after stopping treatment. Consult your doctor before breast-feeding.

              DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: drugs that reduce stomach acid (for example, antacids, H2 blockers such as famotidine/ranitidine, proton pump inhibitors such as omeprazole).Other medications can affect the removal of bosutinib from your body, which may affect how bosutinib works. Examples include azole antifungals (such as ketoconazole, itraconazole), boceprevir, macrolide antibiotics (such as clarithromycin), nefazodone, HIV protease inhibitors (such as indinavir, nelfinavir, ritonavir), rifamycins (such as rifabutin), St. John's wort, drugs used to treat seizures (such as carbamazepine, phenytoin), telaprevir, telithromycin, among others.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

              NOTES: Do not share this medication with others.Laboratory and/or medical tests (such as kidney/liver function, complete blood count) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

              MISSED DOSE: If you miss a dose, take it as soon as you remember if it is within 12 hours of your scheduled dose. If it is more than 12 hours after your scheduled dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

              STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

              MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

              Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Formulary

              FormularyPatient Discounts

              Adding plans allows you to compare formulary status to other drugs in the same class.

              To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

              Adding plans allows you to:

              • View the formulary and any restrictions for each plan.
              • Manage and view all your plans together – even plans in different states.
              • 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.

              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
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.