Gilteritinib

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1] Associate Editor(s)-in-Chief:

Adult Indications and Dosage

Plasma Concentration

• After 15 days, the plasma concentration becomes steady
  • Maximum Concentration: 374 ng/mL
  • AUC: 6943 ng.h/mL
• The Data is different in people who are fasting
  • The Maximum Concentration decreased by 26%
  • AUC decreased by 10%

Excretion

• About 64.5% of the administered dose is excreted in the feces
• About 16.4% of the administered dose goes through the urine

Distribution

• Central Volume of Distribution is approximately 1092 L
• Peripheral Volume of Distribution is approximately 1100 L

Pediatric Indications and Dosage

• There is limited information on the indications and dosage of the drug Gilteritinib on children.

Contraidications

• Hypersensitivity under any ingredient in Gilteritinib

Adverse Reactions

Differentiation Syndrome

• May result in some "life-threatening symptoms" known as differentiation syndrome
  • Contact doctor immediately if any of these symptoms occur:
  • Fever, cough rash, rapid weight gain, vertigo, urination problems, joint swelling, difficulty breathing, chest pain, or joint pain

Side Effects

• If persists, call a doctor:
  • joint/muscle pain, severe tiredness, acute vomiting and nausea, diarrhea, mouth sores, loss in taste/ appetite, headache or insomnia
• More Serious
  • Seizures, difference in heartbeat, persisting pain in the abdomen region that could spread to the back

Drug Interactions

• There is limited information on the drug interactions with Gilteritinib

IV Compatibility

• There is limited information about Gilteritinib's compatibility with IV transfusions

Pharmacology

• Inhibited the receptor tyrosine kinase which regulates FLT3 in acute myeloid luekemia

Trials

• Phase 1 and 2:
  • Complete response: 41%
  • Overall Response Rate: 52%
  • Duration of Response(Median): 20 weeks
  • Overall Survival(Median): 31 weeks

• Phase 3:
  • Complete Remission
  • Complete Remission with limited blood recovery: 21% of patients

Clinical Studies

• The medicinal value of Gilteritinib was analyzed from five clinical trials
• Results:
  • Elimination was through feces
  • Exposure to the drug (effectiveness) was similar with and without fasting
  • Administering Gilteritinib with itraconazole(strong P-gylcoprotein and CYP3A4 inhibitor) or rifampicin(strong P-glycoprotein and CYP3A inducer) lowered the effectiveness of the drug and altered its structure
  • Administering Gilteritinib with midazolam(CYP3A4 substrate) did not alter the effectiveness
  • Hepatic impairment(liver impairment) does not affect the unbound exposure of the drug

How is it Supplied

• The authorized dose for patients on Gilteritinib is 120 mg but may go up to 200 mg is the response from the patient is dissatisfactory

Precautions with Alcohol

There is limited information on Alcohol-Gilteritinib interactions. Talk to your doctor for further instruction on consuming alcohol with Gilteritinib.

Brand Names

• Xospata

Names of Drugs that Look Alike

• There is limited information on Gilteritinib look-alike drugs

Price

Contraindicated Medications

{{MedCondContrAbs |MedCond = NameOfTheContraindication|Drug1|Drug2|Drug3}}