gilteritinib (Rx)

Brand and Other Names:Xospata
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 40mg

Acute Myeloid Leukemia

Indicated for treatment of patients who have relapsed or refractory acute myeloid leukemia (AML) with a FMS-like tyrosine kinase 3 (FLT3) mutation

120 mg PO qDay

Response may be delayed

Continue for at least 6 months for a clinical response or until disease progression or unacceptable toxicity

Dosage Modifications

Dosage modifications for adverse reactions

  • Posterior reversible encephalopathy syndrome (PRES): Discontinue treatment
  • QTc interval >500 msec: Interrupt treatment; resume at 80 mg when QTc interval returns to within 30 msec of baseline or ≤480 msec
  • QTc interval increased by >30 msec on ECG on Day 8 of Cycle 1: Confirm ECG on Day 9; if confirmed, consider reducing dose to 80 mg
  • Pancreatitis: Interrupt treatment until pancreatitis resolved; resume at 80 mg
  • Other Grade ≥3 drug-related toxicity: Interrupt until toxicity resolves or improves to Grade 1; resume at 80 mg
  • Differentiation syndrome
    • If suspected, administer systemic corticosteroids and initiate hemodynamic monitoring until symptoms resolve for at least 3 days
    • Interrupt dose if severe signs and/or symptoms persist for >48 hr after initiation of corticosteroids
    • Resume when signs and symptoms improve to Grade ≤2

Renal or hepatic impairment

  • Mild or moderate ([CrCl 30-80 mL/min] or [Child-Pugh Class A or B]): No clinically meaningful effects on the pharmacokinetics of gilteritinib
  • Severe ([CrCl <30 mL/min] or [Child-Pugh C]): Unknown

Dosing Considerations

Assess blood cell counts and chemistries prior to initiation, at least qWeek for the first month, once every other week for the second month, and once monthly thereafter

Perform ECG prior to initiation of treatment, on Days 8 and 15 of Cycle 1, and prior to the next 2 subsequent cycles

Patient selection

  • Select patients based on presence of FLT3 mutation in blood or bone marrow
  • Information on FDA-approved tests for FLT3 mutation detection in AML is available at http://www.fda.gov/CompanionDiagnostics

Safey and efficacy not established

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Interactions

Interaction Checker

and gilteritinib

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              Serious - Use Alternative (48)

              • abametapir

                abametapir will increase the level or effect of gilteritinib 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.

              • apalutamide

                apalutamide will decrease the level or effect of gilteritinib by Other (see comment). Avoid or Use Alternate Drug. Gilteritinib is a P-gp and CYP3A4 substrates. Coadministration of gilteritinib with a combined P-gp and strong CYP3A inducer decreases gilteritinib exposure and efficacy.

              • artemether

                artemether and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • artemether/lumefantrine

                artemether/lumefantrine and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • atazanavir

                atazanavir will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • bedaquiline

                bedaquiline and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • carbamazepine

                carbamazepine will decrease the level or effect of gilteritinib by Other (see comment). Avoid or Use Alternate Drug. Gilteritinib is a P-gp and CYP3A4 substrates. Coadministration of gilteritinib with a combined P-gp and strong CYP3A inducer decreases gilteritinib exposure and efficacy.

              • ceritinib

                ceritinib and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • chloramphenicol

                chloramphenicol will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • chloroquine

                chloroquine and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • citalopram

                gilteritinib will decrease the level or effect of citalopram by Other (see comment). Avoid or Use Alternate Drug. Coadministration of gilteritinib with drugs that inhibit 5HT2B or sigma nonspecific receptors. Avoid use of these drugs with gilteritinib unless coadministration is necessary.

                citalopram and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • clarithromycin

                clarithromycin will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • cobicistat

                cobicistat will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • conivaptan

                conivaptan will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • crizotinib

                crizotinib and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • darunavir

                darunavir will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • desflurane

                desflurane and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • encorafenib

                encorafenib and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • entrectinib

                entrectinib and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • erdafitinib

                erdafitinib will increase the level or effect of gilteritinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If coadministration unavoidable, separate administration by at least 6 hr before or after administration of P-gp substrates with narrow therapeutic index.

              • escitalopram

                gilteritinib will decrease the level or effect of escitalopram by Other (see comment). Avoid or Use Alternate Drug. Coadministration of gilteritinib with drugs that inhibit 5HT2B or sigma nonspecific receptors. Avoid use of these drugs with gilteritinib unless coadministration is necessary.

              • fexinidazole

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

              • fluoxetine

                gilteritinib will decrease the level or effect of fluoxetine by Other (see comment). Avoid or Use Alternate Drug. Coadministration of gilteritinib with drugs that inhibit 5HT2B or sigma nonspecific receptors. Avoid use of these drugs with gilteritinib unless coadministration is necessary.

              • fluvoxamine

                gilteritinib will increase the level or effect of fluvoxamine by Other (see comment). Avoid or Use Alternate Drug. Coadministrationwith drugs that inhibit 5HT2B or sigma nonspecific receptors. Avoid use of these drugs with gilteritinib unless coadministration is necessary

              • fosphenytoin

                fosphenytoin will decrease the level or effect of gilteritinib by Other (see comment). Avoid or Use Alternate Drug. Gilteritinib is a P-gp and CYP3A4 substrates. Coadministration of gilteritinib with a combined P-gp and strong CYP3A inducer decreases gilteritinib exposure and efficacy.

              • grapefruit

                grapefruit will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • idelalisib

                idelalisib will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • indinavir

                indinavir will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • isoniazid

                isoniazid will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • itraconazole

                itraconazole will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects.

              • ketoconazole

                ketoconazole will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • lefamulin

                lefamulin and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

              • lopinavir

                lopinavir will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • mifepristone

                mifepristone will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • nefazodone

                nefazodone will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • nelfinavir

                nelfinavir will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • paroxetine

                gilteritinib will decrease the level or effect of paroxetine by Other (see comment). Avoid or Use Alternate Drug. Coadministration of gilteritinib with drugs that inhibit 5HT2B or sigma nonspecific receptors. Avoid use of these drugs with gilteritinib unless coadministration is necessary.

              • phenobarbital

                phenobarbital will decrease the level or effect of gilteritinib by Other (see comment). Avoid or Use Alternate Drug. Gilteritinib is a P-gp and CYP3A4 substrates. Coadministration of gilteritinib with a combined P-gp and strong CYP3A inducer decreases gilteritinib exposure and efficacy.

              • phenytoin

                phenytoin will decrease the level or effect of gilteritinib by Other (see comment). Avoid or Use Alternate Drug. Gilteritinib is a P-gp and CYP3A4 substrates. Coadministration of gilteritinib with a combined P-gp and strong CYP3A inducer decreases gilteritinib exposure and efficacy.

              • posaconazole

                posaconazole will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • rifampin

                rifampin will decrease the level or effect of gilteritinib by Other (see comment). Avoid or Use Alternate Drug. Gilteritinib is a P-gp and CYP3A4 substrates. Coadministration of gilteritinib with a combined P-gp and strong CYP3A inducer decreases gilteritinib exposure and efficacy.

              • ritonavir

                ritonavir will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • saquinavir

                saquinavir will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • sertraline

                gilteritinib will decrease the level or effect of sertraline by Other (see comment). Avoid or Use Alternate Drug. Coadministration of gilteritinib with drugs that inhibit 5HT2B or sigma nonspecific receptors. Avoid use of these drugs with gilteritinib unless coadministration is necessary.

              • St John's Wort

                St John's Wort will decrease the level or effect of gilteritinib by Other (see comment). Avoid or Use Alternate Drug. Gilteritinib is a P-gp and CYP3A4 substrates. Coadministration of gilteritinib with a combined P-gp and strong CYP3A inducer decreases gilteritinib exposure and efficacy.

              • stiripentol

                stiripentol will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • tipranavir

                tipranavir will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              • voriconazole

                voriconazole will increase the level or effect of gilteritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternatives to any strong CYP3A4 inhibitor when coadministered with gilteritinib. If such a combination cannot be avoided, closely monitor for gilteritinib-related adverse effects. Interrupt and reduce gilteritinib dosage in patients with serious or life-threatening toxicity.

              Monitor Closely (17)

              • albuterol

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

              • alfuzosin

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

              • apomorphine

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

              • arformoterol

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

              • aripiprazole

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

              • atomoxetine

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

              • clozapine

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

              • dasatinib

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

              • degarelix

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

              • deutetrabenazine

                deutetrabenazine and gilteritinib both increase QTc interval. Use Caution/Monitor.

              • dolasetron

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

              • donepezil

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

              • doxepin

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

              • efavirenz

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

              • fostemsavir

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

              • osilodrostat

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

              • siponimod

                siponimod and gilteritinib 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.

              Minor (0)

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                Adverse Effects

                >10%

                Myalgia/arthralgia (42%)

                Increased transaminases (41%)

                Fatigue/malaise (40%)

                Fever (35%)

                Dyspnea (34%)

                Edema (34%)

                Noninfectious diarrhea (34%)

                Rash (30%)

                Pneumonia (30%)

                Constipation (27%)

                Nausea (27%)

                Stomatitis (26%)

                Cough (25%)

                Pneumonia, Grade 3 or 4 (23%)

                Hypotension (21%)

                Headache (21%)

                Dizziness (20%)

                Vomiting (20%)

                Renal impairment (19%)

                Abdominal pain (17%)

                Increased transaminases, Grade 3 or 4 (16%)

                Decreased appetite (15%)

                Sepsis (15%)

                Insomnia (14%)

                Sepsis, Grade 3 or 4 (14%)

                Dyspnea, Grade 3 or 4 (12%)

                Dysgeusia (11%)

                Increased bilirubin (11%)

                1-10%

                Hypertension (10%)

                Hypotension, Grade 3 or 4 (7%)

                Hypertension, Grade 3 or 4 (6%)

                Myalgia/arthralgia, Grade 3 or 4 (5%)

                Increased bilirubin, Grade 3 or 4 (5%)

                Fever, Grade 3 or 4 (5%)

                Fatigue/malaise, Grade 3 or 4 (5%)

                Renal impairment, Grade 3 or 4 (4%)

                Stomatitis, Grade 3 or 4 (4%)

                Noninfectious diarrhea, Grade 3 or 4 (3%)

                Rash, Grade 3 or 4 (3%)

                Edema, Grade 3 or 4 (2%)

                Decreased appetite, Grade 3 or 4 (2%)

                Abdominal pain, Grade 3 or 4 (2%)

                Headache, Grade 3 or 4 (1%)

                Nausea, Grade 3 or 4 (1%)

                <1%

                Constipation, Grade 3 or 4

                Insomnia, Grade 3 or 4

                Dizziness, Grade 3 or 4

                Cough, Grade 3 or 4

                Postmarketing Reports

                Differentiation syndrome

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                Warnings

                Black Box Warnings

                Differentiation syndrome

                • Symptoms of differentiation syndrome may occur, which can be fatal or life-threatening
                • Symptoms may include fever, dyspnea, hypoxia, pulmonary infiltrates, pleural or pericardial effusions, rapid weight gain or peripheral edema, hypotension, or renal dysfunction
                • If differentiation syndrome suspected, initiate corticosteroid therapy and hemodynamic monitoring until symptom resolution

                Contraindications

                Hypersensitivity to gilteritinib or any of the excipients

                Cautions

                Rare reports of posterior reversible encephalopathy syndrome (PRES) with symptoms including seizure and altered mental status; symptoms resolved after discontinuing treatment; a diagnosis of PRES requires confirmation by brain imaging, preferably magnetic resonance imaging (MRI); discontinue therapy in patients who develop PRES

                Associated with prolonged QT interval cardiac ventricular repolarization; in clinical trials, 1% were found to have a QTc interval >500 msec and 7% of patients had an increase from baseline QTc >60 msec; interrupt and reduce dosage in patients who have a QTcF >500 msec

                Hypokalemia or hypomagnesemia may increase QT prolongation risk; correct electrolyte abnormalities before initiating and during administration

                In clinical trials, rare reports of pancreatitis noted; interrupt and reduce dose in patients who develop pancreatitis

                Embryo-fetal harm may occur when administered to pregnant women (see Pregnancy)

                Differentiation syndrome

                • Differentiation syndrome reported (see Black Box Warnings)
                • If differentiation syndrome suspected, initiate dexamethasone 10 mg IV every 12 hours (or an equivalent dose of an alternative oral or IV corticosteroid) and hemodynamic monitoring until improvement
                • Taper corticosteroids after resolution of symptoms and administer corticosteroids for a minimum of 3 days; symptoms of differentiation syndrome may recur with premature discontinuation of corticosteroid treatment
                • If severe signs and/or symptoms persist for more than 48 hours after initiation of corticosteroids, interrupt therapy until signs and symptoms are no longer severe

                Drug interactions overview

                • Gilteritinib is a CYP3A and P-gp substrate; it potentially inhibits breast cancer resistance protein (BCRP) and organic cation transporter 1 (OCT1) transporter
                • Combined P-gp and strong CYP3A inducers
                  • Coadministration with a combined P-gp and strong CYP3A inducer decreases gilteritinib exposure which may decrease efficacy
                  • Avoid use with combined P-gp and strong CYP3A inducers
                • Strong CYP3A inhibitors
                  • Coadministration with a strong CYP3A inhibitor increases gilteritinib exposure
                  • Consider alternative therapies that are not strong CYP3A inhibitors; if concomitant use is necessary, closely monitor for adverse reactions of gilteritinib
                  • Interrupt and reduce dose in patients with serious or life-threatening toxicity
                • Drugs that target 5HT2B receptor or sigma nonspecific receptor
                  • Coadministration with drugs that target 5HT2B receptors or sigma nonspecific receptors (eg, escitalopram, fluoxetine, sertraline) may reduce effects of these drugs
                  • Avoid use of these drugs unless clinically necessary
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                Pregnancy

                Pregnancy

                Based on findings from animal studies and its mechanism of action, fetal harm may occur when administered to pregnant women

                No data available on use in pregnant women to inform a drug-associated risk of adverse developmental outcomes

                Advise pregnant women of potential fetal risks

                Pregnancy testing recommended for females of reproductive potential within 7 days before initiating treatment

                Animal studies

                • In animal reproduction studies, administration to pregnant rats during organogenesis caused adverse developmental outcomes including embryo-fetal lethality, suppressed fetal growth, and teratogenicity at maternal exposures ~0.4 times the AUC in patients receiving the recommended dose

                Contraception

                • Females of reproductive potential: Use effective contraception during treatment and for ≥6 months after last dose
                • Males: Males with partners of reproductive potential should use effective contraception during treatment and for ≥4 months

                Lactation

                No data on presence of gilteritinib and/or its metabolites in human milk, effects on the breastfed child, or effects on milk production

                Following administration to lactating rats, milk concentrations of radioactivity were higher than radioactivity in maternal plasma at 4 and 24 hr post-dose

                In animal studies, gilteritinib and/or its metabolite(s) were distributed to tissues in infant rats via the milk

                Advise lactating women not to breastfeed during treatment and for 2 months after 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

                Small molecule that inhibits multiple receptor tyrosine kinases, including FMS-like tyrosine kinase 3 (FLT3)

                Demonstrates ability to inhibit FLT3 receptor signaling and proliferation in cells exogenously expressing FLT3 including FLT3-ITD, tyrosine kinase domain mutations (TKD) FLT3-D835Y and FLT3-ITD-D835Y, and induces apoptosis in leukemic cells expressing FLT3-ITD

                Absorption

                Peak plasma concentration (steady-state): 374 ng/mL

                Peak plasma time (fasted state): 4-6 hr

                AUC: 6943 ng·hr/mL

                Steady-state plasma levels reached: Within 15 days

                Effect of food (single 40-mg dose in healthy adults)

                • Peak plasma concentration decreased by 26% and AUC decreased by <10% when coadministered with a high-fat meal compared to a fasted state
                • Median peak plasma time delayed by 2 hr when administered with a high-fat meal

                Distribution

                Vd: 1092 L (central); 1100 L (peripheral)

                Protein bound: ~94%

                Metabolism

                Primarily metabolized via CYP3A4

                At steady state, primary metabolites include M17 (formed via N-dealkylation and oxidation), M16 and M10 (both formed via N-dealkylation)

                None of these metabolites exceeded 10% of overall parent exposure

                Elimination

                Half-life: 113 hr

                Clearance: 14.85 L/hr

                Excretion (single-dose): Feces (64.5%)

                Excretion (total-dose): Urine (16.4% [unchanged drug and metabolites])

                Pharmacogenomics

                Patient selection are based on presence of FLT3 mutation in blood or bone marrow

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                Administration

                Oral Administration

                Administer with or without food

                Swallow whole; do not break or crush

                Administer at same time each day

                Missed dose

                • Administer as soon as possible on the same day, and at least 12 hr prior to next scheduled dose; resume normal schedule the following day
                • Do not administer 2 doses within 12 hr

                Storage

                Store at 20-25°C (68-77°F); excursions permitted between 15-30°C (59-86°F)

                Keep in original container

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                Images

                BRAND FORM. UNIT PRICE PILL IMAGE
                Xospata oral
                -
                40 mg tablet

                Copyright © 2010 First DataBank, Inc.

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                Patient Handout

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