.jpeg)
{{ variable.name }}
Gilteritinib is an oral small molecule tyrosine kinase inhibitor that exerts anti-tumor effects by selectively inhibiting the activity of FMS-like tyrosine kinase 3 (FLT3). Its mechanism of action includes blocking FLT3 receptor signaling, inhibiting leukemia cell proliferation and inducing apoptosis.
1. Common name: Gilteritinib (Gilteritinib)
2. Trade name: XOSPATA®
3. English name: G ilteritinib Tablets
Geritinib is suitable for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) who have FMS-like tyrosine kinase 3 (FLT3) mutations confirmed by FDA-approved testing methods.
This product is a tablet with a specification of 40mg.
Each tablet contains 40 mg of the active ingredient (free base) of geritinib. Inactive ingredients include: mannitol, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, magnesium stearate, hypromellose, talc, polyethylene glycol, titanium dioxide, and iron oxide¹¹.
1. The recommended starting dose is 120 mg once a day (i.e. 3 40 mg tablets) orally.
2. It can be taken with food or on an empty stomach.
3. The tablet should be swallowed whole and should not be broken, crushed or chewed.
Dose adjustment is mainly based on the severity of adverse reactions. For QTc intervals greater than 500 milliseconds, it is recommended to interrupt administration and resume administration at a dose of 80 mg after the QTc interval returns to within 30 milliseconds of baseline or ≤480 milliseconds. For pancreatitis, it is recommended to interrupt dosing until pancreatitis resolves and then resume dosing at 80 mg. For other treatment-related toxicities of grade 3 or above, it is recommended to interrupt administration until the toxicity is relieved or improved to grade 1, and then resume administration at a dose of 80 mg. If posterior reversible encephalopathy syndrome (PRES) occurs, the drug should be permanently discontinued.
1. Medication time: Take once a day at a roughly fixed time. It can be taken with food or on an empty stomach.
2. Treatment of missed doses: If you miss a dose, you should take it as soon as possible on the same day, and ensure that there is at least 12 hours between the next dose. Return to normal medication the next day. Do not take two doses within 12 hours.
3. How to take the medicine: Swallow the tablet whole and do not break it, crush it or chew it.
4. Monitoring requirements: Before starting treatment and during treatment, blood routine, blood biochemistry (including creatine phosphokinase) and electrocardiogram (ECG) need to be monitored regularly, and hypokalemia or hypomagnesemia should be corrected.
5. Others: Be alert to symptoms of reversible posterior encephalopathy syndrome (such as epilepsy, mental status changes), QT interval prolongation (such as dizziness, syncope), and pancreatitis (such as severe persistent abdominal pain).
1. Pregnant women: Based on animal research and mechanism of action, it may cause harm to the fetus, and pregnant women should be informed of the potential risks.
2. Breastfeeding women: It is recommended not to breastfeed during treatment and for at least 2 months after the last dose.
3. Women and men of childbearing potential: Female patients should use effective contraceptive measures during treatment and for at least 6 months after the last dose. Male patients with a female partner of childbearing potential should use effective contraception during treatment and for at least 4 months after the last dose.
4. Elderly people (≥65 years old): No overall difference in effectiveness or safety was observed.
5. Hepatic insufficiency: Patients with mild to moderate hepatic insufficiency do not need to adjust the dose. The effects in patients with severe hepatic impairment are unknown.
6. Renal insufficiency: Patients with mild to moderate renal insufficiency do not need to adjust the dose. The effects in patients with severe renal impairment are unknown.
7. Children: Safety and effectiveness have not been established.
1. The most common (≥20%) adverse reactions include:Myalgia/arthralgia, elevated transaminases, fatigue/malaise, fever, non-infectious diarrhea, dyspnea, edema, rash, pneumonia, nausea, stomatitis, cough, headache, hypotension, dizziness and vomiting.
2. Common serious adverse reactions (≥5%) include:Pneumonitis, sepsis, fever and dyspnea.
3. Other adverse reactions of clinical concern include: QT interval prolongation, heart failure, pericardial effusion, pericarditis, differentiation syndrome, allergic reaction⁶ and reversible posterior encephalopathy syndrome.
4. Common laboratory abnormalities (>20%) include: Elevated creatinine, hyperglycemia, hypertriglyceridemia, elevated alanine aminotransferase (ALT), elevated aspartate aminotransferase (AST), elevated alkaline phosphatase, hypocalcemia, hypoalbuminemia, elevated creatine kinase, hypophosphatemia, hypokalemia and hyponatremia.
It is prohibited for those who are allergic to giritinib or any excipients. Anaphylaxis has been observed in clinical trials.
1. P-gp and strong CYP3A inducers: Combined use will reduce the exposure of giritinib and may reduce the efficacy, so combined use should be avoided.
2. Strong CYP3A inhibitors: Coadministration will increase the exposure of giritinib, and alternative treatments should be considered. If coadministration is necessary, patients should be monitored more frequently for adverse reactions, and dose interruptions and adjustments should be made for serious or life-threatening toxicities.
3. Drugs that act on 5HT2B receptors or σ non-specific receptors (such as escitalopram, fluoxetine, sertraline): Giritinib may reduce the efficacy of these drugs, and their combined use should be avoided unless they are considered critical to patient care.
12. Storage method
Store at room temperature between 20°C and 25°C (68°F and 77°F), short-distance transport permitted between 15°C and 30°C (59°F and 86°F). Keep medicines in their original containers.