Dose and administration method
- Method of administration
- The recommended dose of Ceritinib is 750 mg orally once a day until disease progression or unacceptable Toxicity, give Ceritinib on an empty stomach, do not give it within 2 hours of a meal.
- The recommended dose has not been determined for patients with moderate to severe hepatic impairment.
- If you forget to take it, make up unless the next time of taking it is within 12 hours.
- Dosage specifications:
- Capsule, 150mg.
- Contraindications: None.
Warnings and Precautions
- Severe and persistent gastrointestinal toxicity Diarrhea, nausea, vomiting, or diarrhea occurred in 96% of the 255 patients treated with CERITINIB in Study 1 Abdominal pain includes 14% of patients with severe cases. Thirty-eight percent of the patients had diarrhea, nausea, vomiting or abdominal pain Whole dose. Monitor and treat patients with standard medical care, including antidiarrheals, antiemetics, or rehydration when instructed. According to not The severity of the benign drug reaction is as described in Table 1 without giving Ceritinib and resuming at a reduced dose.
- Liver toxicity: Drug-induced liver toxicity occurred in patients treated with CERITINIB. 27% of the 255 patients in Study 1 Alanine aminotransferase (ALT) rises greater than 5 times the upper limit of normal (ULN). One patient (0.4%) was Because of elevated transaminase and jaundice need to be permanently terminated. Monitor liver laboratory tests including ALT, aspartate aminotransferase (AST), and total bilirubin It is tested more frequently in patients with elevated transaminase once a month and when clinically indicated. According to adverse drug reaction
(Please read this notice carefully and take the medicine according to this notice or under the guidance of a doctor)
The severity of the response, as described in Table 1, withholding Ceritinib and reducing the dose to resume, or permanently discontinue Ceritinib.
- Interstitial lung disease (ILD)/pneumonia Severe, life-threatening, or fatal ILD/pneumonia may occur in patients treated with CERITINIB. In Study 1, pneumonia was reported in 4% of 255 patients treated with Ceritinib. In Study 1 3% Among them, CTCAE grade 3 or 4 ILD/pneumonia was reported, and 1 patient (0.4%) reported fatal ILD/pulmonary inflammation. In Study 1 1% of patients discontinued Ceritinib due to ILD/pneumonia. Monitor patients for pulmonary symptoms indicative of ILD/pneumonia. Exclude other potential causes of ILD/pneumonia, and Ceritinib is permanently discontinued in patients diagnosed with treatment-related ILD/pneumonia.
- Extended QT interval: Prolonged QTc interval occurred in patients treated with Ceritinib. 3% of the 255 patients in Study 1 The QTc interval experienced prolonged more than 60msec beyond the baseline. Across Ceritinib’s development plan, 1/304 Patients (less than 1%) who were treated with Ceritinib at doses ranging from 50 to 750 mg were found to have QTc More than 500msec and 3% of patients have QTc prolonged from baseline by more than 60msec. A pharmacokinetic scorem The analysis suggests that Ceritinib causes concentration-dependent QTc interval prolongation.
When possible, avoid ceritinib in patients with congenital long QT syndrome. Congestive heart Patients with visceral failure, bradyarrhythmia, electrolyte abnormalities, or patients with drugs known to prolong the QTc interval Monitor electrocardiograms (ECGs) and electrolytes regularly. QTc for at least 2 separate independent ECGs Patients with an interval greater than 500msec will not be given Ceritinib until the QTc interval is less than 481msec or recovery To baseline, if the QTc interval is greater than or equal to 481msec, then as described in Table 1 Repeat CERITINIB. When the patient develops QTc interval prolongation and torsion point [Torsadedepointes] or more Shaped ventricular tachycardia [polymorphicventriculartachycardia] or severe arrhythmia Permanently discontinue Ceritinib with a combination of signs/symptoms.
- High blood sugar
Patients receiving Ceritinib may develop hyperglycemia. In Study 1, CTCAE grade 3-4 hyperglycemia,
According to laboratory values, it occurred in 13% of 255 patients. In patients with diabetes or glucose intolerance
The risk of CTCAE grade 3-4 hyperglycemia increased 6-fold and the risk of corticosteroids increased 2-fold.
Monitor serum glucose levels when clinically instructed. When directed to start or optimize anti-hyperglycemic drugs. According to not
Severity of good drug reaction, withhold Ceritinib until hyperglycemia is properly controlled, then as described in Table 1
Reduce the dose and resume Ceritinib. If it cannot be treated with drugs to achieve proper blood glucose control, terminate permanently Ceritinib.
Bradycardia may occur in patients receiving Ceritinib. In Study 1, sinus bradycardia was determined
It means that the heart rate is less than 50 beats per minute, which was noted as a new discovery in 1% of 255 patients. In study 1 3%
The patient reported bradycardia.
Avoid using Ceritinib and other drugs known to cause bradycardia (eg, beta-blockers, non-
Dihydropyridine calcium channel blocker, clonidine [clonidine], combined with digoxin [digoxin]). regular
Monitor heart rate and blood pressure. In case of symptomatic bradycardia is not life-threatening, Ceritinib is not given until recovery
Return to asymptomatic bradycardia or to a heart rate of 60bpm or above, evaluate concurrent drug use, and adjust
The dose of ceritinib. If the drug is not identified at the same time, the life-threatening bradycardia is permanently terminated
Ceritinib; however, do not give Ceritinib if it is associated with concurrent medications known to cause bradycardia or hypotension
Until asymptomatic bradycardia is restored or the heart rate is 60bpm or above, and if the medication can be adjusted or end
Stop, as described in the table, resume Ceritinib at a reduced dose to asymptomatic bradycardia or to a heart rate of 60 bpm
Or more, with frequent monitoring.
- Embryo-fetal toxicity
According to its mechanism of action, Ceritinib may cause fetal harm when administered to pregnant women. In animal research
In the study, the maternal plasma exposure of rats and rabbits administered with Ceritinib during the organogenesis period was lower than the recommended human maximum dose.
The amount of 750 mg per day can cause skeletal abnormalities in rats and rabbits. Advise women of reproductive potential of the potential risk to the fetus
harm. Advise women of reproductive potential that Ceritinib is effective during treatment and at least 2 weeks after completion of treatment
Including: severe and persistent gastrointestinal toxicity, liver toxicity, interstitial lung disease/pneumonia, prolonged QT interval,
High blood sugar, bradycardia, etc.
Store at 25°C (77°F); going out is allowed 15°C to 30°C (59°F to 86°F).