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Brand Name :
Xospata
(Canada) [Available]Synonyms :
gilteritinib
Class :
Antineoplastics and Tyrosinase Kinase Inhibitor, FLT3 Inhibitor
Brand Name :
Xospata
(Canada) [Available]Synonyms :
gilteritinib
Class :
Antineoplastics and Tyrosinase Kinase Inhibitor, FLT3 Inhibitor
Dosage forms & StrengthsÂ
TabletÂ
40mg Â
120 mg orally each day, the response may get delayed Continue the dose for at least 6 months until the unacceptable toxicity or disease progression
Dose Adjustments
In case of adverse reactions
For PRES (posterior reversible encephalopathy syndrome), discontinue the treatment
If the QTc interval >500 milliseconds interrupt the treatment; start over at 80 mg when the QTc interval gets backs within 30 milliseconds
For pancreatitis, interrupt the treatment if the condition persists; start over the dose at 80 mg
Differentiation Syndrome
If differentiation syndrome is suspected, administer systemic corticosteroids, and start hemodynamic monitoring
Continue this process until symptoms are resolved for minimum 3 days
Interrupt dose if severe symptoms and signs persist for over 48 hours after initiating corticosteroids
Start over the previous dose if the symptoms improve
Hepatic or renal impairment
In the case of mild to moderate hepatic or renal impairment, the effect of meaningful pharmacokinetics is unknown
In case of severe hepatic or renal impairment, the effect of the drug is unknown
Safety and efficacy of gilteritinib are not found for pediatric dosing. Â
Refer to the adult dosingÂ
dronedarone and gilteritinib, when used in combination, increase the QTc interval
saquinavir and gilteritinib, when used in combination, increase the QTc interval
thioridazine and gilteritinib, when used in combination, increase the QTc interval
gilteritinib may enhance the QTc-prolonging effect of QT-prolonging Agents
gilteritinib may enhance the QTc-prolonging effect of QT-prolonging Agents
gilteritinib may enhance the QTc-prolonging effect of QT-prolonging Agents
gilteritinib may enhance the QTc-prolonging effect of QT-prolonging Agents
gilteritinib may enhance the QTc-prolonging effect of QT-prolonging Agents
gilteritinib: they may increase the QTc-prolonging effect of QTc-prolonging agents
gilteritinib: they may increase the QTc-prolonging effect of QTc-prolonging agents
gilteritinib: they may increase the QTc-prolonging effect of QTc-prolonging agents
gilteritinib: they may increase the QTc-prolonging effect of QTc-prolonging agents
gilteritinib: they may increase the QTc-prolonging effect of QTc-prolonging agents
gilteritinib: they may enhance the serum concentration of CYP2D6 Inhibitors
gilteritinib: they may enhance the serum concentration of CYP2D6 Inhibitors
gilteritinib: they may enhance the serum concentration of CYP2D6 Inhibitors
gilteritinib: they may enhance the serum concentration of CYP2D6 Inhibitors
gilteritinib: they may enhance the serum concentration of CYP2D6 Inhibitors
when both drugs are combined, there may be an increase in qtc interval  
may enhance the serum concentration of each other when it is combined
may enhance the serum concentration of each other when it is combined
may enhance the serum concentration of each other when it is combined
may enhance the serum concentration of each other when it is combined
may enhance the serum concentration of each other when it is combined
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
amiodarone and gilteritinib, when used in combination, increase the QTc interval
asenapine and gilteritinib, when used in combination, increase the QTc interval
clarithromycin increases the effect of gilteritinib by altering the intestinal/renal CYP3A4 enzyme metabolism
dofetilide and gilteritinib, when used in combination, increase the QTc interval
eribulin and gilteritinib, when used in combination, increase the QTc interval
fexinidazole and gilteritinib, when used in combination, increase the QTc interval
glasdegib and gilteritinib, when used in combination, increase the QTc interval
ibutilide and gilteritinib, when used in combination, increase the QTc interval
lapatinib and gilteritinib, when used in combination, increase the QTc interval
midostaurin and gilteritinib, when used in combination, increase the QTc interval
nilotinib and gilteritinib, when used in combination, increase the QTc interval
osimertinib and gilteritinib, when used in combination, increase the QTc interval
pentamidine and gilteritinib, when used in combination, increase the QTc interval
quinine and gilteritinib, when used in combination, increase the QTc interval
rifampin decreases the effect/level of gilteritinib
sevoflurane and gilteritinib, when used in combination, increase the QTc interval
tetrabenazine and gilteritinib, when used in combination, increase the QTc interval
vemurafenib and gilteritinib, when used in combination, increase the QTc interval
ziprasidone and gilteritinib, when used in combination, increase the QTc interval
may enhance the immunosuppressive effect of immunosuppressants
QTc interval increases on taking gilteritinib and lenvatinib together. Avoid or take an alternate drug
increases the serum concentration of BCRP/ABCG2 substrates
increases the serum concentration of BCRP/ABCG2 substrates
increases the serum concentration of BCRP/ABCG2 substrates
both lapatinib and gilteritinib increase the QTc interval
CYP3A strong enhancers of the small intestine may reduce the bioavailability of gilteritinib 
when used together, entrectinib and gilteritinib both increase the QTc interval
when used together, encorafenib and gilteritinib both increase the QTc interval
midostaurin and gilteritinib, when used simultaneously, increase the QTc level
midostaurin and gilteritinib, when used simultaneously, increase the QTc level
It may enhance QTc interval when combined with pentamidine
it increases the QT-c prolonging effect of gilteritinib
it increases the QT-c prolonging effect of gilteritinib
the concentration of BCRP/ABCG2 substrates in serum is increased by gilteritinib
it increases the serum level of CYP3A4 substrate on combined with gilteritinib
the CYP3A4 substrate serum concentration is increased by erdafitinib
it increases the QT-c prolonging effect of gilteritinib
it increases the QT-c prolonging effect of gilteritinib
it increases the QT-c prolonging effect with gilteritinib
it increases the QT-c prolonging effect with gilteritinib
it increases the QT-c prolonging effect with gilteritinib
it increases the concentration of OCT1 substrates in the serum
It may enhance the serum concentration when combined with CYP3A4 Inhibitors (Moderate)
It may enhance the serum concentration when combined with CYP3A4 Inhibitors (Moderate)
It may enhance the serum concentration when combined with CYP3A4 Inhibitors (Moderate)
It may enhance the serum concentration when combined with CYP3A4 Inhibitors (Moderate)
It may enhance the serum concentration when combined with CYP3A4 Inhibitors (Moderate)
It may enhance the risk of QTc prolongation when combined with moexipril
it may enhance the metabolism when combined with oxcarbazepine
gilteritinib: they may enhance the serum concentration of CYP3A inhibitors
gilteritinib: they may enhance the serum concentration of CYP3A inhibitors
gilteritinib: they may enhance the serum concentration of CYP3A inhibitors
gilteritinib: they may enhance the serum concentration of CYP3A inhibitors
gilteritinib: they may enhance the serum concentration of CYP3A inhibitors
when both drugs are combined, there may be a decreased metabolism of etoposide   
when both drugs are combined, there may be a decreased metabolism of vinblastine  
when both drugs are combined, there may be an increased risk or severity of QTC prolongation  
it increases the concentration of P-Glycoprotein or ABCB1 substrates in serum
may enhance the serum concentration of BCRP/ABCG2 Substrates
Actions and Spectrum:Â
Actions:Â
By inhibiting the activity of FLT3) FMS-like tyrosine kinase 3), gilteritinib helps prevent the proliferation of leukemia cells and promotes apoptosis or programmed cell death. gilteritinib also inhibits the activity of other tyrosine kinases, such as AXL and MER, which can contribute to AML cell survival.Â
Spectrum:Â
The spectrum of gilteritinib activity is primarily limited to AML patients with FLT3 mutations. It is ineffective for treating other types of leukemia or solid tumors. The drug has a relatively good safety profile, with the most common side effects including nausea, diarrhea, fatigue, and abnormal liver function tests.Â
Frequency defined:Â Â
>10%Â
Myalgia/arthralgia Â
Increased transaminases Â
Fatigue/malaise Â
Fever Â
Dyspnea Â
Edema Â
Non-infectious diarrhea Â
Rash Â
Pneumonia Â
Constipation Â
Nausea Â
Stomatitis Â
Cough Â
PneumoniaÂ
Hypotension Â
Headache Â
Dizziness Â
Vomiting Â
Renal impairment Â
Abdominal pain Â
Increased transaminases Â
Decreased appetite Â
Sepsis Â
Insomnia Â
Sepsis Â
Dyspnea Â
Dysgeusia Â
Increased bilirubin  Â
1-10%Â
Hypertension Â
HypotensionÂ
HypertensionÂ
Myalgia/arthralgiaÂ
Increased bilirubinÂ
FeverÂ
Fatigue/malaiseÂ
Renal impairmentÂ
StomatitisÂ
Non-infectious diarrheaÂ
RashÂ
EdemaÂ
Decreased appetiteÂ
Abdominal painÂ
HeadacheÂ
Nausea Â
<1%Â
ConstipationÂ
InsomniaÂ
DizzinessÂ
CoughÂ
Black-Box Warning:Â
Differentiation syndromeÂ
Symptoms of differentiation syndrome may include fever, dyspnea (shortness of breath), hypoxia (low oxygen levels), pulmonary infiltrates (abnormalities on chest X-ray), pleural or pericardial effusions (fluid accumulation around the lungs or heart), rapid weight gain or peripheral edema (swelling), hypotension (low blood pressure), or renal dysfunction (abnormal kidney function). Â
If differentiation syndrome is suspected, immediate medical attention is necessary. Treatment typically involves initiating corticosteroid therapy and monitoring the patient’s hemodynamics until symptoms resolve. Other supportive measures such as oxygen therapy, diuretics, or fluid management may also be necessary.
Contraindication/Caution:Â
Contraindication:Â
Pregnancy consideration: The drug is toxic and unsafe for pregnant women and the developing fetus.Â
Breastfeeding warnings: No data available regarding the excretion of gilteritinib in breast milk. Hence, potential adverse effects and potential benefits should be compared and considered.Â
Pregnancy category:Â
Â
Pharmacology:Â
gilteritinib is a small-molecule drug that targets the FLT3 receptor tyrosine kinase. It is approved by the U.S. Food and Drug Administration (FDA) for treating adult patients with relapsed or refractory acute myeloid leukemia (AML) with an FLT3 mutation.Â
FLT3 is a protein often mutated in AML, leading to uncontrolled growth and survival of leukemic cells. gilteritinib works by binding to and inhibiting the activity of FLT3, thereby preventing the growth and proliferation of leukemic cells.Â
Pharmacodynamics:Â
The pharmacodynamics of gilteritinib are primarily related to its inhibition of the FLT3 receptor tyrosine kinase. FLT3 is a protein that plays a key role in the growth and survival of leukemic cells in AML, particularly in patients with FLT3 mutations.Â
gilteritinib selectively binds to the ATP-binding site of FLT3 and inhibits its activity, inhibiting downstream signaling pathways involved in cell proliferation, differentiation, and survival.Â
Pharmacokinetics:Â
gilteritinib is a small-molecule drug used to treat acute myeloid leukemia (AML) with a specific genetic mutation called FLT3. The pharmacokinetics of gilteritinib refers to how the drug is absorbed, distributed, metabolized, and eliminated in the body.Â
AbsorptionÂ
gilteritinib is administered orally and is rapidly absorbed into the bloodstream. The maximum plasma concentration (Cmax) of gilteritinib is achieved within 2 hours after oral administration.Â
DistributionÂ
gilteritinib has a high distribution volume, indicating that it is extensively distributed throughout the body. The drug is highly bound to plasma proteins, mainly to albumin.Â
MetabolismÂ
gilteritinib is metabolized primarily in the liver by the cytochrome P450 enzyme system, mainly by the CYP3A4 enzyme. The primary metabolite of gilteritinib is M5, which has a similar pharmacological activity to the parent drug.Â
Elimination/ExcretionÂ
gilteritinib and its metabolites are eliminated mainly through feces. Approximately 84% of the dose is excreted in the feces and 5% in the urine. The elimination half-life of gilteritinib is approximately 113 hours.Â
Administration:Â
gilteritinib is available in the form of oral tablets and is administered by mouth. The recommended dose of gilteritinib for adult patients with FLT3 mutation-positive relapsed or refractory acute myeloid leukemia (AML) is 120 mg once daily with or without food until disease progression or unacceptable toxicity.Â
If a dose is missed, patients take the missed dose as soon as possible on the same day and should not take an additional dose to make up for the missed dose. gilteritinib tablets should be swallowed whole with water and not crushed, chewed, or broken. Patients should not consume grapefruit or grapefruit juice while taking gilteritinib, as this may increase the exposure to the drug and increase the risk of side effects.Â
Patient information leafletÂ
Generic Name: gilteritinib (Rx)Â
Pronounced: GIL-te-RI-ti-nibÂ
Why do we use gilteritinib?Â
The primary use of gilteritinib is for treating adult patients who have relapsed or refractory acute myeloid leukemia (AML) with a specific genetic mutation called FLT3. FLT3 mutations occur in about 25-30% of AML cases and are associated with a poor prognosis. gilteritinib is a tyrosine kinase inhibitor that works by blocking the activity of FLT3, which can slow down the growth and division of leukemia cells and potentially lead to their death.
In addition to its primary use in treating FLT3-mutated AML, gilteritinib has also been studied in other types of cancer, including solid tumors with FLT3 mutations. gilteritinib is being evaluated in clinical trials as a potential treatment for a variety of other cancers, including acute lymphoblastic leukemia (ALL), myelodysplastic syndromes (MDS), and myeloproliferative neoplasms (MPN).Â
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