Pricing
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Erinlar is indicated for:
Pharmacology
Ceritinib is a kinase inhibitor. In biochemical or cellular assays, at clinically relevant concentrations, it was found to act on ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR) and ROS1. Of these, Ceritinib is most active against ALK. In in vitro and in vivo assays, it blocked autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and the proliferation of ALK dependent cancer cells.
Absorption: After a single oral dose in patients, peak plasma levels (Cmax) of Ceritinib were reached at about 4 to 6 hours. AUC and Cmax rose in proportion to the dose over 50 to 750 mg under fasted conditions. The absolute bioavailability of Ceritinib has not been determined.
Distribution: Ceritinib is 97% bound to human plasma proteins, and this does not depend on the drug concentration. The apparent volume of distribution is 4230 L after a single 750 mg fasted dose in patients. Ceritinib also distributes slightly more into red blood cells than into plasma, with a mean in vitro blood-to-plasma ratio of 1.35.
Elimination: After a single 750 mg fasted dose, the geometric mean apparent plasma terminal half life (t½) of Ceritinib in patients was 41 hours. Its PK is nonlinear over time. The geometric mean apparent clearance was lower at steady-state (33.2 L/h) after 750 mg daily dosing than after a single 750 mg dose (88.5 L/h).
Metabolism: In vitro studies showed that CYP3A was the major enzyme involved in the metabolic clearance of Ceritinib. After a single 750 mg radiolabeled oral dose under fasted conditions, the parent compound was the main circulating component in human plasma (82%).
Excretion: After a single 750 mg radiolabeled oral dose under fasted conditions, 92.3% of the dose was recovered in the feces (68% of it as unchanged parent compound), while 1.3% of the dose was recovered in the urine.
Dosage Reference
Reference Information Only
Dosages shown are general references from official sources. Always consult your doctor or pharmacist for personalized dosing.
Adults:
Doctors choose Ceritinib for metastatic NSCLC based on whether ALK positivity is found in tumor specimens. The recommended dose is 450 mg by mouth once daily with food, and treatment continues until the disease progresses or the toxicity becomes unacceptable. If you miss a dose of Ceritinib, make it up, unless the next dose is due within 12 hours. If vomiting happens during treatment, don't take an extra dose. Just continue with the next scheduled dose. Or, as directed by the registered physician.
Side Effects
Gastrointestinal adverse reactions, hepatotoxicity, interstitial lung disease/pneumonitis, QT interval prolongation, hyperglycemia, bradycardia, pancreatitis.
Cautions & Contraindications
Warnings & Precautions
Gastrointestinal Adverse Reactions Severe gastrointestinal toxicity occurred in patients who took Ceritinib 750 mg under fasted conditions. Across clinical studies, diarrhea, nausea, vomiting or abdominal pain occurred in 95% of 925 patients, and severe cases (Grade 3 or 4) occurred in 14% of patients on Ceritinib. These symptoms led to dose interruptions or reductions in 36% of patients, and to stopping treatment in 1.6%. Patients should be monitored and managed with standard care, including antidiarrheals, antiemetics or fluid replacement, as indicated. Depending on how severe the reaction is, Ceritinib should be withheld and then restarted at a reduced dose. Hepatotoxicity Drug-induced hepatotoxicity occurred in patients treated with Ceritinib. Across clinical studies of 925 patients, alanine aminotransferase (ALT) rose to more than 5 times the upper limit of normal (ULN) in 28%, and aspartate aminotransferase (AST) rose to more than 5 times ULN in 16%. ALT above 3 times the ULN together with total bilirubin above 2 times the ULN, with alkaline phosphatase below 2 times the ULN, occurred in 0.3% of patients. About 1.0% of patients had to stop permanently because of hepatotoxicity. Liver tests, including ALT, AST and total bilirubin, should be checked once a month and as clinically indicated, and more often in patients who develop transaminase elevations. Depending on severity, Ceritinib should be withheld and restarted at a reduced dose, or stopped permanently. Interstitial Lung Disease (ILD)/Pneumonitis Severe, life-threatening or fatal ILD/pneumonitis occurred in patients treated with Ceritinib. Across clinical studies, it was reported in 2.4% of 925 patients. National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) Grade 3 or 4 ILD/pneumonitis was reported in 1.3% of patients, and fatal events in 0.2%. Ten patients (1.1%) stopped Ceritinib because of ILD/pneumonitis. Patients should be monitored for lung symptoms that point to ILD/pneumonitis. QT Interval Prolongation QTc interval prolongation, which may raise the risk of ventricular tachyarrhythmia (e.g., torsades de pointes) or sudden death, occurred in patients treated with Ceritinib. Across clinical studies, 6% of 919 patients with at least one ECG assessment after baseline had a QTc increase of more than 60 msec over baseline. About 1.3% of patients taking Ceritinib 750 mg fasted had a QTc greater than 500 msec. Where possible, Ceritinib should be avoided in patients with congenital long QT syndrome. Electrocardiograms (ECGs) and electrolytes should be checked from time to time in patients with congestive heart failure, bradyarrhythmias or electrolyte abnormalities, and in those taking medicines known to prolong the QTc interval. Hyperglycemia Hyperglycemia occurred in patients receiving Ceritinib. Across clinical studies, CTCAE Grade 3 or 4 hyperglycemia, based on laboratory values, occurred in 13% of 925 patients. Fasting serum glucose should be checked before Ceritinib is started and periodically after that, as clinically indicated. Depending on severity, Ceritinib should be withheld until the hyperglycemia is well controlled, and then restarted at a reduced dose. Bradycardia Bradycardia occurred in patients receiving Ceritinib. Across clinical studies, sinus bradycardia (a heart rate of less than 50 beats per minute, bpm) was a new finding in 1% of 925 patients, and bradycardia was reported as an adverse drug reaction in 1%. No patient had to stop treatment, and 0.1% needed an interruption followed by a dose reduction. To the extent possible, Ceritinib should be avoided together with other agents known to cause bradycardia (e.g., beta-blockers, nondihydropyridine calcium channel blockers, clonidine and digoxin). Heart rate and blood pressure should be checked regularly. If bradycardia causes symptoms but is not life threatening, Ceritinib should be withheld until the patient has no symptoms or the heart rate is 60 bpm or above, the other medicines being used should be reviewed, and the Ceritinib dose adjusted. Pancreatitis Pancreatitis occurred in patients receiving Ceritinib. In clinical studies it occurred in less than 1% of patients, including one death. CTCAE Grade 3 or 4 elevations of amylase occurred in 7% of patients, and Grade 3 or 4 elevations of lipase in 14%. Lipase and amylase should be checked before Ceritinib is started and periodically after that, as clinically indicated. Depending on how abnormal the laboratory results are, Ceritinib should be withheld and restarted at a reduced dose. Embryo-Fetal Toxicity Based on how it works and on findings in animal studies, Ceritinib can harm the fetus when given to a pregnant woman. Pregnant women should be told about the possible risk to the fetus. Females who could become pregnant should be advised to use effective contraception during treatment with Ceritinib and for 6 months after therapy ends. Because of the potential for genotoxicity, males with female partners who could become pregnant should be advised to use condoms during treatment and for 3 months after therapy ends.
Contraindications
Ceritinib must not be given to anyone who is known to be hypersensitive to Ceritinib or to any other component of the product.
Pregnancy & Breastfeeding
Ceritinib can harm an unborn baby when it is given to a pregnant woman. If a woman uses it during pregnancy, or becomes pregnant while she is taking it, she should be told about the possible danger to the baby.
There are no data on whether Ceritinib or its metabolites pass into human milk. Nor is there any information on what it does to a breastfed infant or to milk production. Ceritinib can cause serious adverse reactions, including gastrointestinal adverse reactions, hepatotoxicity, pneumonitis, bradycardia and pancreatitis. Because of this, a woman should be advised not to breastfeed during treatment with Ceritinib and for 2 weeks after she completes therapy.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Use in Special Populations
Ceritinib can cause harm to the unborn baby when a pregnant woman takes it. Women who could become pregnant should use effective contraception while on Ceritinib and for 6 months after the treatment ends.
For men, there is a possible risk of genotoxicity. So men whose female partners could become pregnant should use condoms during treatment with Ceritinib and for 3 months after finishing it.
Pediatric use: The safety and effectiveness of Ceritinib in children have not been established.
Geriatric use: Clinical studies of Ceritinib included 925 patients. Of these, 18% were 65 years or older and 5% were 75 years or older. Doctors saw no overall differences in safety or effectiveness between these older patients and the younger ones.
Hepatic impairment: In patients with severe hepatic impairment (Child-Pugh C), the Ceritinib dose should be reduced by about one-third, rounded to the nearest multiple of the 150 mg strength. No dose adjustment is recommended for mild (Child-Pugh A) or moderate (Child-Pugh B) hepatic impairment.
Storage
Keep Ceritinib in a cool, dry place where the temperature stays below 30°C, and away from sunlight. Make sure children can't reach it.
Drug Interactions
Common questions about Erinlar 150 mg
What is Erinlar 150 mg Capsule?
Erinlar 150 mg Capsule is a medicine that contains Ceritinib. It is made by Genvio Pharma Ltd.
What is Erinlar used for?
Erinlar is used for: Cancer.
What are the side effects of Erinlar?
Gastrointestinal adverse reactions, hepatotoxicity, interstitial lung disease/pneumonitis, QT interval prolongation, hyperglycemia, bradycardia, pancreatitis.
Can I take Erinlar during pregnancy or while breastfeeding?
Ceritinib can harm an unborn baby when it is given to a pregnant woman. If a woman uses it during pregnancy, or becomes pregnant while she is taking it, she should be told about the possible danger to the baby. Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
How should I store Erinlar?
Keep Ceritinib in a cool, dry place where the temperature stays below 30°C, and away from sunlight. Make sure children can't reach it.
Can I take other medicines with Erinlar?
Some medicines can interact with Ceritinib, for example: Midazolam, St. John's Wort, Ketoconazole, Carbamazepine, Telithromycin, Ritonavir. Tell your doctor or pharmacist about every medicine you take.
Is there a cheaper medicine with the same ingredient?
Erinlar is already among the lowest-priced brands of Ceritinib at this strength.
Do I need a prescription for Erinlar?
Erinlar is a prescription (Rx) medicine. Take it as your doctor advises.