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Other brands with the same active ingredient
These brands contain the same active ingredient (Crizotinib). Same strength and form. Confirm the switch with your doctor or pharmacist.
Indications & Uses
Crizocent 250 is indicated for:
Pharmacology
Crizotinib inhibits several receptor tyrosine kinases, including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros) and Recepteur d'Origine Nantais (RON). Translocations can affect the ALK gene and lead to oncogenic fusion proteins. When ALK fusion proteins form, the gene's expression and signaling are activated and dysregulated, which can add to increased cell proliferation and survival in tumors that express these proteins. Cell-based assays using tumor cell lines showed concentration-dependent inhibition of ALK, ROS1 and c-Met phosphorylation. The drug also showed antitumor activity in mice bearing tumor xenografts that expressed echinoderm microtubule-associated protein-like 4 (EML4)- or nucleophosmin (NPM)-ALK fusion proteins or c-Met.
Absorption
After a single oral dose, crizotinib was absorbed with a median time to peak concentration of 4 to 6 hours. With 250 mg twice daily, steady state was reached within 15 days and stayed stable, with a median accumulation ratio of 4.8. Steady state systemic exposure (C.min and AUC) appeared to rise more than in proportion to the dose across the range of 200 to 300 mg twice daily. Mean absolute bioavailability was 43% (range: 32% to 66%) after a single 250 mg oral dose. A high-fat meal reduced AUCinf and Cmax by approximately 14%.
Distribution
The geometric mean volume of distribution (Vss) was 1772 L after an intravenous 50 mg dose, which points to extensive distribution from the plasma into tissues. Binding to human plasma proteins in vitro is 91% and doesn't depend on drug concentration. Studies done in vitro also suggested that crizotinib is a substrate for P-glycoprotein (P-gp). The blood-to-plasma concentration ratio is approximately 1.
Metabolism
Crizotinib is mainly metabolized by CYP3A4/5, according to in vitro studies. The primary metabolic pathways in humans were oxidation of the piperidine ring to crizotinib lactam and O-dealkylation, followed by Phase 2 conjugation of the O-dealkylated metabolites.
Elimination
Following single doses, the mean apparent plasma terminal half-life was 42 hours in patients. Healthy subjects were given a single 250 mg radiolabeled dose, and 63% of it was recovered in feces and 22% in urine. Unchanged crizotinib made up approximately 53% of the dose in feces and 2.3% in urine. The mean apparent clearance (CL/F) was lower at steady state (60 L/hr) after 250 mg twice daily than after a single 250 mg oral dose (100 L/hr). This was likely due to auto inhibition of CYP3A by crizotinib after multiple dosing.
Dosage Reference
Reference Information Only
Dosages shown are general references from official sources. Always consult your doctor or pharmacist for personalized dosing.
Adults:
Recommended dose: the adult dose of Crizotinib is 250 mg taken by mouth, twice daily.
Geriatric use: no differences in safety or efficacy were seen between older and younger patients. That said, the clinical studies of Crizotinib in patients with ROS1-positive metastatic NSCLC did not include enough patients aged 65 years and older to tell whether they respond differently from younger patients.
Pediatric dose: the safety and effectiveness of Crizotinib in pediatric patients have not been established.
Renal impairment: patients with severe renal impairment (creatinine clearance <30 mL/min) who do not need dialysis should take 250 mg by mouth once daily. No change to the starting dose is needed for patients with mild (ClCr 60 to 89 mL/min) or moderate (ClCr 30 to 59 mL/min) renal impairment, based on a population pharmacokinetic analysis.
Hepatic impairment: use caution in patients with hepatic impairment.
Side Effects
Crizotinib most often causes vision disorders, nausea, diarrhea, vomiting, edema, constipation, raised transaminases, fatigue, decreased appetite, upper respiratory infection, dizziness and neuropathy. Each of these was reported in 25% or more of people taking the medicine.
Cautions & Contraindications
Warnings & Precautions
Hepatotoxicity: Patients should have their liver tested at regular intervals. Crizotinib should be suspended temporarily, the dose reduced, or the medicine stopped permanently. Interstitial lung disease (ILD)/Pneumonitis: Crizotinib should be stopped permanently in patients who develop ILD or pneumonitis. QT interval prolongation: Electrocardiograms and electrolytes should be monitored in patients who have a history of QTc prolongation or a tendency towards it, and in those taking medicines that prolong the QT interval. Crizotinib should be suspended temporarily, the dose reduced, or the medicine stopped permanently. Bradycardia: Crizotinib can cause bradycardia, so heart rate and blood pressure should be checked regularly. Crizotinib should be suspended temporarily, the dose reduced, or the medicine stopped permanently. Severe visual loss: An ophthalmological evaluation should be done. Crizotinib should be discontinued if severe visual loss occurs. Embryo-fetal toxicity: Crizotinib can cause harm to the fetus. Females who could become pregnant should be told about the possible risk to a fetus and advised to use effective contraception.
Pregnancy & Breastfeeding
Crizotinib can harm an unborn baby, going by how the medicine works in the body. There are no data on its use during pregnancy. Women who could become pregnant should be told about the possible risk to a baby and should use effective contraception.
It isn't known whether Crizotinib passes into human milk, what it does to a breastfed infant, or whether it affects milk production. Because breastfed infants could have adverse reactions, patients should not breastfeed during treatment with Crizotinib and for 45 days after the final dose.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Storage
Store Crizotinib below 30°C, and keep it away from light and moisture. Keep it out of the reach of children.
Drug Interactions
Common questions about Crizocent 250 250 mg
What is Crizocent 250 250 mg Capsule?
Crizocent 250 250 mg Capsule is a medicine that contains Crizotinib. It is made by Incepta Pharmaceuticals Ltd. It belongs to the Targeted Cancer Therapy group of medicines.
What is Crizocent 250 used for?
Crizocent 250 is used for: Cancer.
What are the side effects of Crizocent 250?
Crizotinib most often causes vision disorders, nausea, diarrhea, vomiting, edema, constipation, raised transaminases, fatigue, decreased appetite, upper respiratory infection, dizziness and neuropathy. Each of these was reported in 25% or more of people taking the medicine.
Can I take Crizocent 250 during pregnancy or while breastfeeding?
Crizotinib can harm an unborn baby, going by how the medicine works in the body. There are no data on its use during pregnancy. Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
How should I store Crizocent 250?
Store Crizotinib below 30°C, and keep it away from light and moisture. Keep it out of the reach of children.
Can I take other medicines with Crizocent 250?
Some medicines can interact with Crizotinib, for example: Cyclosporine, Carbamazepine, Clarithromycin, Fentanyl, Itraconazole, Telithromycin. Tell your doctor or pharmacist about every medicine you take.
Do I need a prescription for Crizocent 250?
Crizocent 250 is a prescription (Rx) medicine. Take it as your doctor advises.