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Tasigna (nilotinib) capsules
Detailed View: Safety Labeling Changes Approved By FDA Center for Drug Evaluation and Research (CDER)
- Avoid food 2 hours before and 1 hour after taking the dose (5.8)
5 WARNINGS AND PRECAUTIONS
5.2 QT Prolongation
- Before initiating Tasigna and periodically, test electrolyte, calcium and magnesium blood levels.
5.3 Sudden Deaths
- Sudden deaths have been reported in 0.3% of patients with CML treated with nilotinib in clinical studies of 5,661 patients.
5.4 Elevated Serum Lipase
- Tasigna can cause increases in serum lipase. Patients with a previous history of pancreatitismaybe at greater risk. If lipase elevations ...
- Tasigna may result in hepatotoxicity as measured by elevations in bilirubin, AST/ALT, and alkaline phosphatase. Monitor hepatic function tests monthly or as clinicallyindicated [see Warnings and Precautions (5.13)].
5.7 Drug Interactions
- Avoid administration of Tasigna with agents that are strong CYP3A4 inhibitors or anti-arrhythmic drugs (including, but not limited to amiodarone, disopyramide, procainamide, quinidine and sotalol) and other drugs that may prolong QT interval (including, but not limited to chloroquine, clarithromycin, haloperidol, methadone, moxifloxacin and pimozide) since nilotinib exposure will be increased. Should treatment with any of these agents be required, interrupt therapy with Tasigna.
5.8 Food Effects
- The bioavailability of nilotinib is increased with food, thus Tasigna must not be taken with food. No food should be consumed for at least 2 hours before and for at least 1 hour after the dose is taken. Also avoid grapefruit products and other foods that are known to inhibit CYP3A4 [see Boxed Warning, Drug Interactions (7.2) and Clinical Pharmacology (12.3)].
5.9 Hepatic Impairment
- Nilotinib exposure is increased in patients with impaired hepatic function. Use a lower starting dose for patients with mild to severe hepatic impairment (at baseline) and monitor the QT interval frequently [see Dosage and Administration (2.2) and Use in Specific Populations (8.7)].
17 PATIENT COUNSELING INFORMATION
- Tasigna doses should be taken twice daily approximately 12 hours apart. The capsules should be swallowed whole with water.
- If the patient missed a dose of Tasigna, the patient should take the next scheduled dose at its regular time. The patient should not take two doses at the same time.
- negative statement “do not take with food” changed to the positive statement “take Tasigna on an empty stomach”
Drugs that Affect Gastric pH
- Nilotinib has pH-dependent solubility, with decreased solubility at higher pH. Drugs such as proton pump inhibitors that inhibit gastric acid secretion to elevate the gastric pH may decrease the solubility of nilotinib and reduce its bioavailability. In healthy subjects, co-administration of a single 400 mg dose of Tasigna with multiple doses of esomeprazole (a proton pump inhibitor) at 40 mg daily decreased the nilotinib AUC by 34%. Increasing the dose of Tasigna when co-administered with such agents is not likely to compensate for the loss of exposure. Since proton pump inhibitors affect pH of the upper GI tract for an extended period, separation of doses may not eliminate the interaction. The concomitant use of proton pump inhibitors with Tasigna is not recommended.
- In healthy subjects, no significant change in nilotinib pharmacokinetics was observed when a single 400 mg dose of Tasigna was administered ten hours after and two hours before famotidine (an H2 blocker). Therefore, when the concurrent use of a H2 blocker is necessary, it may be administered approximately ten hours before and approximately two hours after the dose of Tasigna.
- Administration of an antacid (aluminum hydroxide/magnesium hydroxide/simethicone) to healthy subjects, two hours before or two hours after a single 400 mg dose of Tasigna did not alter nilotinib pharmacokinetics. Therefore, if necessary, an antacid may be administered approximately two hours before or approximately two hours after the dose of Tasigna.
What should I tell my doctor before starting Tasigna?
- Tell your doctor about all the medicines you take a medicine to block the amount of acid produced in the stomach (H2 blocker): Take these medicines about 10 hours before you take Tasigna, or about 2 hours after you take Tasigna.
- A dose reduction is recommended in patients with hepatic impairment.
WARNINGS AND PRECAUTIONS
- Nilotinib exposure is increased in patients with impaired hepatic function. A dose reduction is recommended for patients with mild to severe hepatic impairment and QT interval should be monitored closely.
Effects of Nilotinib on Drug Metabolizing Enzymes and Drug Transport Systems
- In vitro studies also suggest that nilotinib may induce CYP2B6, CYP2C8 and CYP2C9, and decrease the concentrations of drugs which are eliminated by these enzymes.
- Single-dose administration of Tasigna to healthy subjects did not change the pharmacokinetics and pharmacodynamics of warfarin. The ability of Tasigna to induce metabolism has not been determined in vivo
Drugs that Inhibit or Induce Cytochrome P450 3A4 Enzymes
- The administration of Tasigna with agents that are strong CYP3A4 inhibitors should be avoided. Concomitant use of Tasigna with medicinal products and herbal preparations that are potent inducers of CYP3A4 is likely to reduce exposure to nilotinib to a clinically relevant extent. Therefore, in patients receiving Tasigna, concomitant use of alternative therapeutic agents with less potential for CYP3A4 induction should be selected
Drugs that May Prolong the QT Interval
- The administration of Tasigna with agents that may prolong the QT interval such as anti-arrhythmic medicines should be avoided.
Who should not take Tasigna?
- Do not take if you have: low levels of potassium or magnesium in your blood or long QTc syndrome
During treatment with Tasigna, The tests will check (section updated)