Tasigna (Nilotinib)
Tyrosine kinase inhibitor for Philadelphia chromosome-positive chronic myeloid leukemia
Quick Facts: Tasigna
Key Takeaways
- Tasigna (nilotinib) is a second-generation BCR-ABL tyrosine kinase inhibitor approved for treating Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in adults and children aged 2 years and older.
- Must be taken on an empty stomach — at least 2 hours after eating and 1 hour before the next meal — as food significantly increases absorption to potentially harmful levels.
- Carries a risk of QT prolongation and cardiovascular events including peripheral arterial occlusive disease; regular ECG monitoring and cardiovascular risk assessment are essential.
- Common side effects include rash, headache, nausea, fatigue, and blood count changes. Serious but less common side effects include pancreatitis, hepatotoxicity, and fluid retention.
- Treatment-free remission (TFR) may be possible for patients who achieve sustained deep molecular response under close medical supervision.
What Is Tasigna and What Is It Used For?
Tasigna contains the active substance nilotinib, a potent and selective second-generation tyrosine kinase inhibitor developed by Novartis. It was approved by the European Medicines Agency (EMA) and the U.S. Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia (CML) that is characterized by the Philadelphia chromosome — a genetic abnormality resulting from a translocation between chromosomes 9 and 22, creating the BCR-ABL fusion gene.
In patients with CML, this chromosomal change produces an abnormal protein (BCR-ABL tyrosine kinase) that sends continuous signals telling the body to produce excessive numbers of dysfunctional white blood cells. Nilotinib works by binding to and blocking the activity of this abnormal BCR-ABL protein, thereby halting the uncontrolled growth of leukemic cells. Unlike first-generation inhibitors, nilotinib demonstrates greater binding affinity and selectivity for BCR-ABL, making it effective in patients who have become resistant to or intolerant of imatinib therapy.
Tasigna is approved for use in both adults and pediatric patients (aged 2 years and older) in two distinct clinical scenarios: as first-line treatment for newly diagnosed Ph+ CML in the chronic phase, and as second-line treatment for patients who no longer benefit from prior therapy that included imatinib or who have experienced serious side effects requiring discontinuation of their prior treatment.
Monitoring During Treatment
Treatment with Tasigna requires regular and comprehensive monitoring. Your healthcare provider will schedule frequent blood tests to evaluate how well the medicine is working and to detect potential complications early. These tests will assess:
- Blood cell counts: White blood cells, red blood cells, and platelets are monitored to evaluate treatment response and detect cytopenias (low blood counts), which are common during treatment.
- Pancreatic and liver function: Levels of lipase, amylase, bilirubin, and liver enzymes (ALT, AST) are checked regularly, as nilotinib can affect these organs.
- Electrolytes: Potassium, magnesium, calcium, and phosphorus levels are monitored because electrolyte imbalances — particularly low potassium or magnesium — can increase the risk of cardiac arrhythmias.
- Metabolic parameters: Blood glucose and lipid levels (cholesterol, triglycerides) are assessed, as nilotinib can affect metabolic function.
- Cardiac function: Electrocardiograms (ECGs) are performed before starting treatment and periodically during therapy to monitor the QT interval and detect rhythm disturbances.
Your doctor will regularly evaluate your molecular and cytogenetic response to Tasigna to determine whether treatment should continue. In patients who achieve a sustained deep molecular response, your doctor may consider discontinuing treatment under close monitoring — a concept known as treatment-free remission (TFR). If your CML shows signs of returning after discontinuation, treatment with Tasigna can be restarted.
What Should You Know Before Taking Tasigna?
Contraindications
Do not take Tasigna if you are allergic to nilotinib or any of the other ingredients in this medicine. The inactive ingredients include lactose monohydrate, crospovidone, poloxamer 188, colloidal anhydrous silica, and magnesium stearate. The capsule shell contains gelatin, titanium dioxide (E171), and iron oxides (E172). If you suspect you may be allergic to any component, consult your doctor before taking Tasigna.
Warnings and Precautions
Before starting treatment with Tasigna, it is essential to discuss your complete medical history with your healthcare provider. You should inform your doctor if any of the following conditions apply to you:
- Cardiovascular disease: Previous heart attack, angina, stroke, peripheral arterial disease (claudication), or risk factors for cardiovascular disease such as hypertension, diabetes, or dyslipidemia. Nilotinib has been associated with serious cardiovascular events including peripheral arterial occlusive disease and ischemic heart disease.
- Heart rhythm disorders: Any disorder of cardiac function, particularly prolonged QT interval. Nilotinib can further prolong the QT interval, which in rare cases may lead to sudden cardiac death.
- Electrolyte imbalances: Low potassium (hypokalemia) or low magnesium (hypomagnesemia), which must be corrected before starting treatment as they increase the risk of QT prolongation.
- Liver or pancreatic disorders: Any pre-existing hepatic impairment or history of pancreatitis, as Tasigna can affect both organs.
- Previous gastrectomy: If you have had your entire stomach surgically removed (total gastrectomy), absorption of nilotinib may be altered.
- Hepatitis B infection: Current or past hepatitis B infection, as Tasigna may cause reactivation of the virus, which can be life-threatening. Patients will be screened for hepatitis B before treatment initiation.
- Fainting (syncope) or irregular heartbeat — may indicate a serious cardiac condition
- Chest pain, numbness or weakness, difficulty walking or speaking — possible signs of cardiovascular events
- Sudden rapid heartbeat, severe muscle weakness, paralysis, or seizures — potential signs of tumor lysis syndrome
- Pain, discoloration, or coldness in a limb — possible peripheral arterial occlusive disease
- Swollen feet or hands, general swelling, or rapid weight gain — signs of severe fluid retention
Children and Adolescents
Tasigna is approved for children and adolescents with CML aged 2 years and older. There is no experience with use in children under 2 years of age. For newly diagnosed CML, experience in children under 10 years is limited, and for second-line treatment (after prior therapy failure), there is limited experience in children under 6 years of age. Some children and adolescents taking Tasigna may experience slower growth than normal. Your child's growth will be monitored regularly throughout treatment by their healthcare team.
Food and Drink Interactions
Tasigna must not be taken with food. Food substantially increases the bioavailability of nilotinib — studies have shown that a high-fat meal can increase drug exposure by approximately 82%. This elevated absorption can raise blood levels of nilotinib to potentially dangerous concentrations, increasing the risk of side effects including QT prolongation. You should fast for at least 2 hours before taking Tasigna and wait at least 1 hour after taking it before eating.
Grapefruit and grapefruit juice must be avoided throughout treatment, as they inhibit the CYP3A4 enzyme system responsible for metabolizing nilotinib, which can significantly increase drug levels in the blood.
Pregnancy and Breastfeeding
Tasigna is not recommended during pregnancy unless absolutely necessary. Based on its mechanism of action and animal studies, nilotinib may cause harm to an unborn baby. Women of childbearing potential should use highly effective contraception during treatment and for at least two weeks after the last dose. If you discover you are pregnant while taking Tasigna, contact your doctor immediately to discuss the risks and benefits of continuing treatment.
Breastfeeding is not recommended during treatment with Tasigna and for two weeks after the last dose, as it is not known whether nilotinib passes into breast milk. Discuss feeding options with your healthcare provider.
Driving and Operating Machinery
If you experience side effects such as dizziness or visual disturbances after taking Tasigna that could affect your ability to drive safely or operate machinery, you should avoid these activities until the effects have resolved.
Tasigna capsules contain lactose (milk sugar). If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicine.
How Does Tasigna Interact with Other Drugs?
Nilotinib is primarily metabolized by the cytochrome P450 enzyme CYP3A4 and also inhibits several CYP enzymes and the P-glycoprotein transporter. This means Tasigna can both be affected by other medicines and alter the levels of other drugs in your body. It is critical to inform your doctor or pharmacist about all medicines you are taking, have recently taken, or plan to take.
Major Interactions — Drugs to Avoid
The following medications should generally be avoided during treatment with Tasigna due to the risk of serious, potentially life-threatening interactions:
| Drug / Class | Used For | Interaction Risk |
|---|---|---|
| Ketoconazole, Itraconazole, Voriconazole | Antifungal infections | Strong CYP3A4 inhibitors — significantly increase nilotinib levels |
| Clarithromycin, Telithromycin | Bacterial infections | Strong CYP3A4 inhibitors — increase nilotinib exposure |
| Ritonavir | HIV (protease inhibitor) | Strong CYP3A4 inhibitor — markedly increases nilotinib levels |
| Carbamazepine, Phenobarbital, Phenytoin | Epilepsy | Strong CYP3A4 inducers — significantly reduce nilotinib efficacy |
| Rifampicin | Tuberculosis | Strong CYP3A4 inducer — markedly reduces nilotinib levels |
| St. John's Wort (Hypericum perforatum) | Mild depression and anxiety | CYP3A4 inducer — unpredictably reduces nilotinib levels |
| Astemizole, Terfenadine, Cisapride, Pimozid, Quinidine, Bepridil | Various (antihistamines, GI, antipsychotic, antiarrhythmic) | QT prolongation risk — combined with nilotinib may cause fatal arrhythmias |
| Ergot alkaloids (Ergotamine, Dihydroergotamine) | Migraine | CYP3A4 substrates — nilotinib may increase levels to toxic concentrations |
Moderate Interactions — Use with Caution
The following medications require dose adjustment or careful monitoring when used with Tasigna:
- Antiarrhythmics: Drugs that affect heart rhythm should be used with extreme caution due to additive QT prolongation risk.
- Statins (Lovastatin, Simvastatin): Nilotinib may increase statin levels, raising the risk of rhabdomyolysis (severe muscle breakdown) and kidney damage. Your doctor may need to switch to a different statin.
- Warfarin: Nilotinib may alter the metabolism of warfarin; closer INR monitoring is required.
- Midazolam, Alfentanil, Fentanyl: Nilotinib may increase levels of these sedatives and pain medications.
- Cyclosporine, Sirolimus, Tacrolimus: Immunosuppressant levels may be increased by nilotinib; dose adjustments and therapeutic drug monitoring may be necessary.
- Halofantrin, Chloroquine, Haloperidol, Methadone, Moxifloxacin: These drugs may have unwanted effects on heart rhythm when combined with nilotinib.
Antacid Interactions
Antacids and acid-suppressing medications can affect the absorption of nilotinib and must be taken at specific intervals:
- H2 blockers (e.g., ranitidine, famotidine): Should be taken approximately 10 hours before and approximately 2 hours after Tasigna.
- Antacids containing aluminum hydroxide, magnesium hydroxide, or simethicone: Should be taken approximately 2 hours before or approximately 2 hours after Tasigna.
Proton pump inhibitors (PPIs) should also be used with caution. If a new medication is prescribed while you are already taking Tasigna, always inform the prescribing physician that you are on nilotinib therapy.
What Is the Correct Dosage of Tasigna?
Always take Tasigna exactly as your doctor or pharmacist has instructed. The dosage depends on whether you are newly diagnosed or are being treated after prior therapy, and whether you are an adult or a child. Do not change your dose or stop taking Tasigna without consulting your doctor.
Adults
| Indication | Recommended Dose | How to Take |
|---|---|---|
| Newly diagnosed CML (chronic phase) | 600 mg per day | Two 150 mg capsules twice daily (300 mg every 12 hours) |
| CML resistant to or intolerant of prior therapy | 800 mg per day | Two 200 mg capsules twice daily (400 mg every 12 hours) |
Your doctor may prescribe a lower dose depending on your response to treatment, any side effects experienced, or other medical conditions. Dose reductions are common during the course of treatment and do not necessarily indicate treatment failure.
Children and Adolescents
The dose for children and adolescents is calculated based on body weight and height (body surface area). Your doctor will determine the appropriate dose and instruct you on which capsule strength and how many capsules to give your child. The total daily dose for children must not exceed 800 mg. The 50 mg capsules are primarily designed for flexible pediatric dosing.
Elderly Patients (65 Years and Older)
The same dosing recommendations apply to elderly patients as to other adults. No specific dose adjustment is required based on age alone, though elderly patients may be more susceptible to certain side effects such as cardiovascular events and should be monitored accordingly.
How to Take Tasigna
Administration Instructions
- Take the capsules twice daily, approximately every 12 hours
- Take at least 2 hours after any food
- Wait at least 1 hour before eating again
- Swallow capsules whole with a glass of water
- Do not eat food when taking the capsules
- Do not open the capsules unless you cannot swallow them
- If unable to swallow: mix the contents of each capsule with 1 teaspoon of applesauce and take immediately. Do not use more than 1 teaspoon per capsule and do not mix with anything other than applesauce.
- Take Tasigna at the same time each day to maintain consistent blood levels
Missed Dose
If you miss a dose of Tasigna, simply take your next scheduled dose at the regular time. Do not take a double dose to make up for a forgotten capsule. Taking extra doses could increase the risk of serious side effects, particularly those affecting the heart.
Overdose
If you take more Tasigna than prescribed, or if someone else accidentally takes your capsules, contact your doctor or go to the nearest emergency department immediately. Bring the medicine packaging and this information with you. Medical treatment may be necessary, and symptoms of overdose may include pronounced QT prolongation and exacerbation of known side effects.
Stopping Treatment
Do not stop taking Tasigna unless your doctor tells you to do so. Stopping treatment without medical advice can lead to disease progression, which may have life-threatening consequences. If your doctor recommends discontinuation based on achieving sustained deep molecular response (treatment-free remission), you will be closely monitored with regular molecular testing before, during, and after stopping treatment. If your CML shows signs of returning, your doctor may instruct you to restart Tasigna.
What Are the Side Effects of Tasigna?
Most side effects of Tasigna are mild to moderate and generally resolve within the first few days to weeks of treatment. However, some side effects can be serious and require immediate medical attention. Always report any new or worsening symptoms to your healthcare provider.
Very Common
- Rash, itching
- Headache
- Nausea, vomiting
- Diarrhea, constipation
- Fatigue (lack of energy)
- Muscle pain, bone pain, back pain, limb pain
- Hair loss
- Upper respiratory infections (sore throat, runny nose, sneezing)
- Low blood cell counts (red blood cells, platelets) or hemoglobin
- Elevated lipase levels (pancreatic function marker)
- Elevated bilirubin and ALT levels (liver function markers)
- Slowed growth in children and adolescents
Common
- Abdominal pain, bloating, flatulence
- Pneumonia, bronchitis, flu-like symptoms, sore throat
- Dry skin, acne, decreased skin sensitivity
- Weight loss or weight gain
- Insomnia, depression, anxiety
- Night sweats, excessive sweating
- Nosebleeds
- Gout (painful, swollen joints)
- Erectile dysfunction
- Ear pain, tinnitus (ringing in ears)
- Hemorrhoids, heavy menstrual periods
- Conjunctivitis, eye irritation, red eyes
- High blood pressure, flushing
- Peripheral arterial occlusive disease (leg pain from reduced blood flow)
- Shortness of breath
- Mouth ulcers with gum inflammation (stomatitis)
- Elevated creatinine, amylase, liver enzymes
- Low white blood cell count (leukopenia, neutropenia)
- Low magnesium, potassium, sodium, calcium, or phosphorus
- Elevated blood lipids (cholesterol) and uric acid
Uncommon
- Allergic hypersensitivity reactions
- Chest pain, dry mouth, breast enlargement in men
- Herpes virus infection, skin abscess, skin wart
- Memory loss, restless legs syndrome
- Gastritis, intestinal inflammation (enterocolitis)
- Urinary incontinence, frequent urination
- Psoriasis, skin cysts, skin discoloration
- Heart attack (myocardial infarction), heart failure
- Pericarditis (chest pain behind breastbone)
- Blood clot in a vein (deep vein thrombosis)
- Pleural effusion, pulmonary edema, interstitial lung disease
- Hypertensive crisis
- Claudication (painful legs when walking)
- Atherosclerosis (fat deposits in arteries)
- Low blood sugar, dehydration
- Tremor, peripheral neuropathy (numbness/tingling in extremities)
- Facial nerve paralysis
- Eye hemorrhage, conjunctival hemorrhage
- Sepsis (blood poisoning)
- Tooth sensitivity, gum inflammation (gingivitis)
Rare
- Hand-foot syndrome (redness and peeling of palms and soles)
- Mouth warts
- Thyroiditis (inflammation of the thyroid gland)
- Mood disturbances or depression
- Secondary hyperparathyroidism
- Cerebral artery stenosis (narrowing of brain arteries)
- Brain swelling (cerebral edema)
- Optic neuritis (blurred vision, vision loss)
- Cardiac dysfunction (reduced ejection fraction)
- Low or high insulin levels
- Sudden death (reported in uncommon frequency)
- Signs of heart problems: chest pain, irregular heartbeat, fainting, blue discoloration of lips or skin
- Signs of blocked arteries: leg pain or cramps during walking, slow-healing wounds, cold or pale extremities
- Signs of pancreatitis: severe upper abdominal pain
- Signs of liver problems: yellowing of skin/eyes, dark urine, loss of appetite
- Signs of serious infection: fever, easy bruising or bleeding, severe or frequent infections
- Signs of blood clots: swelling and pain in a limb
- Signs of stroke: weakness/paralysis in face, arms, or legs, difficulty speaking, severe headache
How Should You Store Tasigna?
Proper storage of Tasigna is important to ensure the medicine remains effective and safe throughout its shelf life. Follow these storage guidelines:
- Store at no more than 30°C (86°F)
- Keep in the original packaging to protect from moisture
- Keep out of the sight and reach of children
- Do not use after the expiry date (EXP) printed on the carton and blister — the expiry date refers to the last day of that month
- Do not use if the packaging is damaged or shows signs of tampering
Do not dispose of medicines via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures help protect the environment.
What Does Tasigna Contain?
Each Tasigna capsule contains nilotinib as the active substance in the form of nilotinib hydrochloride monohydrate. The capsules are available in three strengths:
| Strength | Appearance | Imprint | Pack Sizes |
|---|---|---|---|
| 50 mg | Red/light yellow capsule | NVR/ABL (black) | 120 capsules (3 × 40) |
| 150 mg | Red capsule | NVR/BCR (black) | 28, 40, 112, 120, or 392 capsules |
| 200 mg | Light yellow capsule | NVR/TKI (red) | 28, 40, 112, 120, or 392 capsules |
Inactive ingredients (all strengths): Lactose monohydrate, crospovidone type A, poloxamer 188, colloidal anhydrous silica, magnesium stearate. The capsule shell contains gelatin, titanium dioxide (E171), and iron oxides (E172). Printing ink contains shellack (E904) and iron oxide (E172). Not all pack sizes may be marketed in all countries.
Tasigna is manufactured by Novartis Pharmaceutical Manufacturing LLC (Ljubljana, Slovenia), Novartis Farmacéutica SA (Barcelona, Spain), Lek d.d. (Lendava, Slovenia), and Novartis Pharma GmbH (Nürnberg, Germany). The marketing authorization holder is Novartis Europharm Limited, Dublin, Ireland.
Frequently Asked Questions About Tasigna
Tasigna (nilotinib) is used to treat Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML), a type of blood cancer. It is approved for both newly diagnosed adult and pediatric patients (aged 2 years and older) and for patients whose CML has not responded to or who cannot tolerate prior treatment with imatinib. Tasigna works by blocking the abnormal BCR-ABL protein that drives the uncontrolled growth of leukemic cells.
Food significantly increases the absorption of nilotinib, which can raise blood levels of the drug to potentially dangerous concentrations. A high-fat meal can increase drug exposure by approximately 82%. This elevated absorption increases the risk of side effects, particularly QT prolongation (a dangerous change in heart rhythm). To ensure safe and effective therapy, you must fast for at least 2 hours before taking Tasigna and wait at least 1 hour before eating afterward.
In certain patients who have achieved a sustained deep molecular response (typically at least MR4.5 maintained for at least 2 years), your doctor may consider treatment-free remission (TFR). This involves carefully monitored discontinuation of Tasigna with regular molecular testing. Approximately half of eligible patients can successfully maintain remission without treatment. However, if CML shows signs of returning, Tasigna is promptly restarted. You should never stop taking Tasigna on your own without your doctor's guidance, as this could lead to disease progression.
Yes, Tasigna can affect the heart in several ways. It can cause QT prolongation (a change in the electrical activity of the heart), which in rare cases may lead to serious arrhythmias or sudden death. Nilotinib has also been associated with cardiovascular events including peripheral arterial occlusive disease, ischemic heart disease (heart attacks), and ischemic cerebrovascular events (strokes). Your doctor will perform ECGs before and during treatment and assess your cardiovascular risk factors. Report any chest pain, irregular heartbeat, leg pain during walking, or difficulty breathing immediately.
Both Tasigna (nilotinib) and Gleevec (imatinib) are BCR-ABL tyrosine kinase inhibitors used to treat CML. However, nilotinib is a second-generation TKI that was specifically designed to have greater potency and selectivity for BCR-ABL than imatinib. Clinical studies (ENESTnd) have shown that nilotinib achieves faster and deeper molecular responses compared to imatinib as first-line therapy. Nilotinib is effective against many BCR-ABL mutations that cause imatinib resistance, though it is not active against the T315I mutation. The side effect profiles differ: imatinib is more associated with fluid retention and muscle cramps, while nilotinib carries higher cardiovascular risk.
Yes, but timing is critical. Antacids containing aluminum hydroxide, magnesium hydroxide, or simethicone should be taken approximately 2 hours before or 2 hours after Tasigna. H2 blockers (such as ranitidine or famotidine) should be taken approximately 10 hours before and 2 hours after Tasigna. These medications can alter the acidity of the stomach and affect how nilotinib is absorbed. Always consult your doctor or pharmacist before combining any acid-reducing medication with Tasigna.
References
- European Medicines Agency (EMA). Tasigna (nilotinib) — Summary of Product Characteristics. Last updated 2025. Available at: ema.europa.eu/en/medicines/human/EPAR/tasigna
- U.S. Food and Drug Administration (FDA). Tasigna (nilotinib) Prescribing Information. Novartis Pharmaceuticals Corporation. Available at: FDA Label
- Hochhaus A, Saglio G, Hughes TP, et al. Long-term benefits and risks of frontline nilotinib vs imatinib for chronic myeloid leukemia in chronic phase: 5-year update of the randomized ENESTnd trial. Leukemia. 2016;30(5):1044-1054. doi:10.1038/leu.2016.5
- National Comprehensive Cancer Network (NCCN). Clinical Practice Guidelines in Oncology: Chronic Myeloid Leukemia. Version 1.2025.
- World Health Organization (WHO). WHO Model List of Essential Medicines — 23rd List, 2023. Geneva: WHO; 2023.
- Hochhaus A, Baccarani M, Silver RT, et al. European LeukemiaNet 2020 recommendations for treating chronic myeloid leukemia. Leukemia. 2020;34(4):966-984. doi:10.1038/s41375-020-0776-2
- British National Formulary (BNF). Nilotinib. Available at: bnf.nice.org.uk/drugs/nilotinib
Editorial Team
This article has been written and reviewed by the iMedic Medical Editorial Team, which includes board-certified specialists in clinical pharmacology, hematology, and oncology. All content follows the GRADE evidence framework and adheres to international guidelines from the EMA, FDA, WHO, and NCCN.
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