Nilotinib STADA
Tyrosine kinase inhibitor for chronic myeloid leukemia (CML)
Quick Facts About Nilotinib STADA
Key Takeaways
- Second-generation TKI: Nilotinib is approximately 30 times more potent than imatinib against the BCR-ABL kinase in laboratory studies, offering an effective option for CML treatment
- Strict fasting requirement: Must be taken on an empty stomach — no food for 2 hours before and 1 hour after each dose to prevent dangerous increases in blood levels
- QT prolongation risk: Can cause serious heart rhythm changes; ECG monitoring is required before and during treatment
- Treatment-free remission possible: Some patients who achieve deep, sustained molecular responses may be able to discontinue treatment under careful medical supervision
- Regular monitoring essential: Blood counts, liver function, pancreatic enzymes, blood glucose, lipids, and ECG must be checked regularly throughout treatment
What Is Nilotinib STADA and What Is It Used For?
Nilotinib STADA is a targeted cancer medicine (tyrosine kinase inhibitor) used to treat Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in adults. It works by specifically blocking the BCR-ABL protein that causes leukemia cells to multiply uncontrollably.
Chronic myeloid leukemia (CML) is a type of blood cancer that originates in the bone marrow. In approximately 95% of CML patients, a genetic abnormality known as the Philadelphia chromosome is present. This chromosome results from a translocation between chromosomes 9 and 22, producing the BCR-ABL fusion gene. The BCR-ABL protein encoded by this gene is a constitutively active tyrosine kinase that drives the uncontrolled proliferation of white blood cells characteristic of CML.
Nilotinib belongs to a class of medicines called tyrosine kinase inhibitors (TKIs). It was developed as a second-generation TKI specifically designed to be more potent and selective than imatinib (the first TKI approved for CML). In preclinical studies, nilotinib demonstrated approximately 30-fold greater potency against the BCR-ABL kinase compared to imatinib, and it retains activity against many imatinib-resistant BCR-ABL mutations, with the notable exception of the T315I mutation.
Nilotinib STADA is a generic formulation of nilotinib, approved by the European Medicines Agency (EMA) as a bioequivalent alternative to the original branded product Tasigna (manufactured by Novartis). Generic medicines must meet the same rigorous standards of quality, safety, and efficacy as the originator product.
Approved Indications
Nilotinib STADA is approved for the treatment of:
- Newly diagnosed adult patients with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in the chronic phase
- Adult patients with chronic phase and accelerated phase Ph+ CML who are resistant to or intolerant of prior therapy, including imatinib
The effectiveness of nilotinib has been established in several landmark clinical trials. The ENESTnd (Evaluating Nilotinib Efficacy and Safety in Clinical Trials - Newly Diagnosed Patients) study demonstrated superior major molecular response (MMR) rates with nilotinib compared to imatinib at 12 months (44% vs. 22% for nilotinib 300 mg twice daily vs. imatinib 400 mg once daily). Long-term follow-up data from this trial confirmed sustained benefits, with fewer progressions to accelerated or blast phase CML.
Nilotinib binds to the inactive (DFG-out) conformation of the ABL kinase domain of the BCR-ABL protein. By occupying the ATP-binding site, it prevents the kinase from phosphorylating downstream signaling proteins, thereby halting the growth signals that drive CML cell proliferation. This highly targeted mechanism allows nilotinib to selectively attack cancer cells while largely sparing normal cells, although it also inhibits several other kinases including c-KIT, PDGFR, and DDR.
What Should You Know Before Taking Nilotinib STADA?
Before starting nilotinib, your doctor must check your heart rhythm (ECG), liver function, pancreatic enzymes, and blood counts. You must not take nilotinib if you have a severe heart rhythm disorder (long QT syndrome), severe liver impairment, or low potassium or magnesium levels.
Nilotinib is a powerful medicine that requires careful medical assessment before treatment can begin. Your prescribing physician, typically a hematologist or oncologist, will conduct a thorough evaluation to ensure that nilotinib is safe and appropriate for you. This evaluation includes a detailed medical history, physical examination, and several laboratory tests and investigations.
Contraindications
You must not take Nilotinib STADA if you:
- Are allergic to nilotinib or any of the other ingredients in this medicine
- Have hypokalemia (low potassium levels) or hypomagnesemia (low magnesium levels) that has not been corrected
- Have long QT syndrome or a family history of long QT syndrome
- Are currently taking medicines known to significantly prolong the QT interval (such as amiodarone, disopyramide, procainamide, quinidine, sotalol, or certain antibiotics and antifungals)
- Have severe hepatic (liver) impairment
Warnings and Precautions
Several important warnings apply to nilotinib treatment. Your medical team will monitor you closely for these potential risks:
Nilotinib carries a boxed warning for QT prolongation, which can lead to potentially fatal ventricular arrhythmias including torsade de pointes. Sudden deaths have been reported in patients receiving nilotinib. An ECG must be performed before starting treatment, at 7 days, periodically thereafter, and after any dose adjustment. Electrolyte abnormalities (hypokalemia, hypomagnesemia) must be corrected before initiating therapy and monitored throughout treatment.
Cardiovascular events: Nilotinib has been associated with an increased risk of cardiovascular events, including peripheral arterial occlusive disease (PAOD), ischemic heart disease, and ischemic cerebrovascular events. Patients should be assessed for cardiovascular risk factors before and during treatment. Risk factors include diabetes, hypertension, hyperlipidemia, and smoking. Patients should be advised to maintain a healthy lifestyle and manage modifiable risk factors.
Hepatotoxicity: Nilotinib can cause elevations in liver enzymes (ALT, AST, bilirubin, and alkaline phosphatase). Liver function tests should be performed monthly or as clinically indicated. Dose modifications or discontinuation may be required for significant elevations.
Pancreatitis: Cases of pancreatitis, including fatal cases, have been reported. Serum lipase levels should be monitored periodically. If lipase elevation is accompanied by abdominal symptoms, nilotinib should be interrupted, and pancreatitis should be ruled out.
Myelosuppression: Nilotinib can cause neutropenia, thrombocytopenia, and anemia. Complete blood counts should be performed every 2 weeks for the first 2 months, then monthly thereafter. Dose adjustments may be necessary for grade 3 or 4 cytopenias.
Tumor lysis syndrome: Patients with high tumor burden may be at risk of tumor lysis syndrome. Adequate hydration and correction of uric acid levels should be ensured before starting treatment.
Pregnancy and Breastfeeding
Nilotinib may cause harm to an unborn baby. Based on findings from animal studies and its mechanism of action, nilotinib is expected to cause fetal harm when administered to a pregnant woman. Women of childbearing potential must use highly effective contraception during treatment and for at least 2 weeks after the last dose.
It is not known whether nilotinib passes into breast milk. Because of the potential for serious adverse reactions in nursing infants, breastfeeding must be discontinued during treatment and for at least 2 weeks after the last dose.
Male patients taking nilotinib should be aware of potential effects on fertility. While specific data in humans are limited, animal studies have shown effects on reproductive organs. Men should discuss fertility preservation options with their healthcare team before starting treatment.
Elderly Patients
No overall differences in safety or efficacy have been observed between patients aged 65 years and older and younger patients in clinical trials. However, elderly patients may be more susceptible to certain adverse effects, particularly cardiovascular events and QT prolongation, due to age-related changes in cardiac function and higher prevalence of comorbidities. Careful monitoring and dose adjustments may be required.
How Does Nilotinib STADA Interact with Other Drugs?
Nilotinib has significant drug interactions, especially with medicines that affect the CYP3A4 liver enzyme or prolong the QT interval. Strong CYP3A4 inhibitors can dangerously increase nilotinib levels, while CYP3A4 inducers can reduce its effectiveness. Grapefruit and St John's wort must be avoided.
Nilotinib is primarily metabolized by the cytochrome P450 enzyme CYP3A4 in the liver and is also an inhibitor of CYP3A4, CYP2C8, CYP2C9, CYP2D6, and UGT1A1. It is also a substrate and inhibitor of the efflux transporter P-glycoprotein (P-gp). These pharmacokinetic properties mean that nilotinib has a significant potential for drug interactions, which must be carefully managed by the prescribing physician.
Additionally, because nilotinib can prolong the QT interval, combining it with other QT-prolonging medicines increases the risk of serious cardiac arrhythmias. Your doctor should review all your current medicines, including over-the-counter products and herbal supplements, before starting nilotinib.
Major Interactions
| Interacting Drug / Class | Mechanism | Clinical Effect | Recommendation |
|---|---|---|---|
| Ketoconazole, Itraconazole, Voriconazole | Strong CYP3A4 inhibitors | Up to 3-fold increase in nilotinib exposure | Avoid concomitant use; consider alternative antifungals |
| Clarithromycin, Telithromycin | Strong CYP3A4 inhibitors | Significantly increased nilotinib levels | Avoid; use azithromycin as alternative |
| Ritonavir, Nelfinavir (HIV protease inhibitors) | Strong CYP3A4 inhibitors | Significantly increased nilotinib levels and QT risk | Avoid concomitant use if possible |
| Rifampicin, Rifabutin | Strong CYP3A4 inducers | Up to 80% reduction in nilotinib exposure | Avoid; loss of therapeutic efficacy |
| Phenytoin, Carbamazepine, Phenobarbital | Strong CYP3A4 inducers | Substantially reduced nilotinib levels | Avoid; use alternative anticonvulsants |
| QT-prolonging medicines (amiodarone, sotalol, haloperidol) | Additive QT prolongation | Increased risk of torsade de pointes and sudden death | Contraindicated; avoid concomitant use |
| Grapefruit, Seville oranges, starfruit | CYP3A4 inhibition in gut wall | Increased nilotinib absorption and blood levels | Must be completely avoided |
| St John's wort (Hypericum perforatum) | CYP3A4 induction | Unpredictably reduced nilotinib levels | Contraindicated; must not be used |
Minor Interactions
| Interacting Drug / Class | Mechanism | Recommendation |
|---|---|---|
| Warfarin | Nilotinib inhibits CYP2C9; may increase warfarin levels | Monitor INR closely; consider LMWH alternative |
| Midazolam | Nilotinib inhibits CYP3A4; increases midazolam exposure by ~30% | Use lower doses of CYP3A4 substrates |
| Proton pump inhibitors (omeprazole, lansoprazole) | Reduced gastric acid may alter nilotinib solubility | Separate dosing; PPIs are generally acceptable |
| Antacids (aluminum, magnesium hydroxide) | May affect nilotinib absorption | Separate by at least 2 hours |
| Metformin | Nilotinib may affect glucose metabolism | Monitor blood glucose closely |
What Is the Correct Dosage of Nilotinib STADA?
The standard adult dose of nilotinib is 300 mg twice daily for newly diagnosed CML, or 400 mg twice daily for resistant/intolerant CML. Each dose must be taken on an empty stomach, approximately 12 hours apart. The capsules should be swallowed whole with water.
The dosage of nilotinib is determined by your treating hematologist based on your specific clinical situation, including whether you are newly diagnosed or have been previously treated, the phase of your CML, your response to treatment, and your overall health status. Nilotinib STADA 50 mg capsules allow for flexible dose adjustments when needed.
Adults
Newly Diagnosed Chronic Phase CML
Recommended dose: 300 mg (six 50 mg capsules) taken orally twice daily, approximately 12 hours apart.
Administration: Must be taken on an empty stomach. No food should be consumed for at least 2 hours before and at least 1 hour after each dose. The capsules should be swallowed whole with water.
Alternative for swallowing difficulties: For patients who cannot swallow capsules, the contents may be dispersed in one teaspoon of applesauce and taken immediately. No food should be consumed for at least 2 hours before and at least 1 hour after taking the medicine.
Resistant or Intolerant Chronic Phase or Accelerated Phase CML
Recommended dose: 400 mg (eight 50 mg capsules) taken orally twice daily, approximately 12 hours apart.
Administration: Same fasting requirements as above apply.
| Indication | Dose | Frequency | Daily Total |
|---|---|---|---|
| Newly diagnosed CP-CML | 300 mg | Twice daily (every 12 hours) | 600 mg/day |
| Resistant/intolerant CP or AP-CML | 400 mg | Twice daily (every 12 hours) | 800 mg/day |
Children
Nilotinib STADA 50 mg capsules can be used in pediatric patients. Nilotinib is approved by the EMA for children and adolescents with newly diagnosed Ph+ CML in the chronic phase and for those with chronic phase Ph+ CML who are resistant to or intolerant of prior therapy. The recommended dose for pediatric patients is 230 mg/m² twice daily, rounded to the nearest 50 mg dose (maximum single dose 400 mg). The 50 mg capsule strength is particularly useful for achieving accurate pediatric dosing. Your child's doctor will calculate the appropriate dose based on body surface area.
Elderly
No specific dose adjustments are recommended solely based on age. However, elderly patients are more likely to have reduced hepatic and renal function, and they may have a higher prevalence of cardiac conditions that predispose to QT prolongation. Therefore, more frequent monitoring may be warranted, and dose adjustments should follow the same guidelines for managing adverse events as in younger adults. Careful cardiovascular risk assessment is particularly important in this population.
Missed Dose
If you miss a dose of nilotinib, do not take a double dose to make up for the missed one. Simply skip the missed dose and take your next dose at the regularly scheduled time. It is important to maintain the approximately 12-hour interval between doses. Consistent adherence to the dosing schedule is critical for achieving optimal treatment outcomes in CML. If you frequently miss doses, speak with your healthcare team about strategies to improve adherence.
Overdose
In the event of an overdose, the patient should be observed and appropriate supportive treatment given. There is no specific antidote for nilotinib. Overdose cases have been reported in clinical trials, with events including thrombocytopenia, vomiting, and drowsiness. Given the risk of QT prolongation, cardiac monitoring with serial ECGs is essential after an overdose. If overdose is suspected, contact a poison control center or emergency medical services immediately.
What Are the Side Effects of Nilotinib STADA?
The most common side effects of nilotinib include rash, itching, headache, nausea, fatigue, and muscle pain. More serious but less common side effects include QT prolongation, liver problems, pancreatitis, cardiovascular events, and low blood cell counts. Most side effects are manageable with dose adjustments and supportive care.
Like all medicines, Nilotinib STADA can cause side effects, although not everybody gets them. Understanding the potential side effects and their frequency can help you and your healthcare team identify and manage them promptly. It is important to report any new or worsening symptoms to your doctor, even if they seem minor, as early intervention can prevent more serious complications.
The side effects listed below are based on data from clinical trials (including the pivotal ENESTnd and ENACT studies) and post-marketing surveillance reports submitted to the EMA and FDA.
Very Common
- Rash (various types of skin eruptions)
- Pruritus (itching)
- Headache
- Nausea
- Fatigue and asthenia (weakness)
- Alopecia (hair thinning)
- Myalgia (muscle pain)
- Upper respiratory tract infections (nasopharyngitis)
- Neutropenia (low neutrophil count)
- Thrombocytopenia (low platelet count)
- Anemia (low red blood cell count)
Common
- Abdominal pain (upper and lower)
- Constipation or diarrhea
- Vomiting
- Arthralgia (joint pain)
- Bone pain and muscle spasms
- Peripheral edema (swelling in limbs)
- Dizziness
- Insomnia
- Dry skin and night sweats
- Elevated lipase and amylase (pancreatic enzymes)
- Elevated liver enzymes (ALT, AST, bilirubin)
- Hyperglycemia (elevated blood sugar)
- Hypercholesterolemia and hypertriglyceridemia
- QT prolongation on ECG
- Decreased appetite
Uncommon
- Pancreatitis (inflammation of the pancreas)
- Hepatotoxicity (serious liver damage)
- Peripheral arterial occlusive disease (PAOD)
- Ischemic heart disease (angina, myocardial infarction)
- Ischemic cerebrovascular events (stroke, TIA)
- Pleural effusion (fluid around the lungs)
- Pericardial effusion (fluid around the heart)
- Gastrointestinal hemorrhage
- Hyperkalemia or hypokalemia
- Diabetes mellitus
Rare
- Sudden cardiac death (associated with QT prolongation)
- Torsade de pointes (dangerous heart arrhythmia)
- Tumor lysis syndrome
- Hepatic failure
- Stevens-Johnson syndrome (severe skin reaction)
- Erythema multiforme
- Papilledema (swelling of the optic disc)
Contact your doctor or go to the emergency department immediately if you experience: chest pain or palpitations; sudden difficulty breathing; sudden severe abdominal pain; yellowing of the skin or eyes (jaundice); sudden numbness, weakness, or difficulty speaking (possible stroke); or severe skin reactions with blistering. These may indicate serious, potentially life-threatening side effects that require urgent treatment.
Many of the common side effects of nilotinib are manageable and may improve over time as your body adjusts to the medicine. Your healthcare team can provide supportive measures to help manage symptoms. For example, skin rashes may respond to topical corticosteroids or antihistamines, and nausea can often be managed with anti-emetic medications taken before the nilotinib dose.
Dose adjustments, temporary treatment interruptions, or in some cases permanent discontinuation may be necessary depending on the severity and type of side effect. Your doctor will follow specific guidelines for managing each type of adverse event, balancing the need to maintain effective CML treatment against the risk of continued toxicity.
How Should You Store Nilotinib STADA?
Store Nilotinib STADA capsules at room temperature below 30°C (86°F) in the original packaging to protect from moisture. Keep out of the sight and reach of children. Do not use after the expiry date printed on the package.
Proper storage of your medicine is essential to ensure that it remains effective and safe throughout the course of your treatment. Nilotinib capsules should be stored under the following conditions:
- Temperature: Store below 30°C (86°F). Do not refrigerate or freeze.
- Protection from moisture: Keep the capsules in the original blister packaging until you are ready to take them. Do not transfer to a pill box or other container that does not protect against moisture.
- Protection from light: Store in the original carton to protect from light exposure.
- Keep out of reach: Store in a secure location out of the sight and reach of children. Nilotinib is a potent anticancer medicine and accidental ingestion by children can cause serious harm.
- Expiry date: Do not use this medicine after the expiry date stated on the carton and blister. The expiry date refers to the last day of that month.
Do not dispose of medicines in household waste or wastewater. Ask your pharmacist how to dispose of medicines you no longer use. Nilotinib is classified as a cytotoxic agent, and special disposal procedures may be required in your country to prevent environmental contamination.
What Does Nilotinib STADA Contain?
Each Nilotinib STADA hard capsule contains 50 mg of nilotinib (as nilotinib hydrochloride monohydrate) as the active ingredient, along with several inactive excipients necessary for capsule formulation.
Understanding what your medicine contains can be important, particularly if you have allergies or intolerances to certain ingredients. The full composition of Nilotinib STADA 50 mg hard capsules is as follows:
Active substance: Each hard capsule contains nilotinib hydrochloride monohydrate equivalent to 50 mg nilotinib.
Other ingredients (excipients):
- Capsule contents: Lactose monohydrate, crospovidone, poloxamer 188, colloidal anhydrous silica, magnesium stearate
- Capsule shell: Gelatin, titanium dioxide (E171), iron oxide red (E172), iron oxide yellow (E172)
- Printing ink: Shellac, iron oxide black (E172), propylene glycol, ammonium hydroxide
Nilotinib STADA capsules contain lactose monohydrate. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicine. The amount of lactose per capsule is small, but patients with rare hereditary conditions of galactose intolerance, total lactase deficiency, or glucose-galactose malabsorption should not take this medicine.
Frequently Asked Questions About Nilotinib STADA
Nilotinib STADA is used to treat Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in adult patients. It may be prescribed for newly diagnosed patients in the chronic phase, or for patients with chronic or accelerated phase CML who are resistant to or intolerant of prior therapy including imatinib. It works by blocking the BCR-ABL tyrosine kinase that drives CML cell growth. It is also used in pediatric patients at a dose calculated by body surface area.
Nilotinib must be taken on an empty stomach because food significantly increases its absorption and blood levels. A high-fat meal can increase nilotinib exposure by approximately 82%. Higher-than-intended blood levels increase the risk of QT prolongation, a serious heart rhythm disturbance that can potentially be life-threatening. You should not eat for at least 2 hours before and 1 hour after taking your dose. Only water is permitted during the fasting period.
The most serious side effects include QT prolongation (which can cause sudden cardiac death), hepatotoxicity (liver damage that can progress to liver failure), pancreatitis (including rare fatal cases), and cardiovascular events including peripheral arterial occlusive disease, heart attacks, and strokes. Myelosuppression (low blood counts) is also common and may increase the risk of infections or bleeding. Regular monitoring of ECG, liver function, pancreatic enzymes, and blood counts is essential to detect and manage these risks early.
Nilotinib STADA is a generic version of the original branded product Tasigna (manufactured by Novartis). Both contain the same active ingredient, nilotinib, and have been shown to be bioequivalent, meaning they deliver the same amount of active drug into the bloodstream. Generic medicines must meet the same quality, safety, and efficacy standards as the original product and are approved by regulatory agencies such as the European Medicines Agency (EMA). Nilotinib STADA is typically available at a lower cost while offering the same therapeutic benefit.
Treatment-free remission (TFR) is possible for some patients, but the decision to stop nilotinib must only be made by your specialist hematologist. To be considered for TFR, you typically need to have achieved and maintained a deep molecular response (MR4 or better, meaning BCR-ABL levels less than 0.01%) for at least 2 years. After stopping, you will need very frequent molecular monitoring (monthly for the first year, then every 6–12 weeks). Approximately 50–60% of patients who attempt TFR maintain their response, while others may need to restart treatment. Never stop taking nilotinib without medical guidance.
If you have difficulty swallowing capsules, you may open the capsule and sprinkle the contents into one teaspoon of applesauce (apple puree). The mixture should be swallowed immediately and not stored for later use. Do not use any liquid or food other than applesauce to mix with the capsule contents. The same fasting requirements apply: no food for 2 hours before and 1 hour after taking the medicine. Speak with your pharmacist or doctor if you continue to have difficulty.
References
- European Medicines Agency (EMA). Nilotinib STADA — Summary of Product Characteristics. Available at: www.ema.europa.eu
- Saglio G, Kim DW, Issaragrisil S, et al. Nilotinib versus imatinib for newly diagnosed chronic myeloid leukemia. New England Journal of Medicine. 2010;362(24):2251-2259. doi:10.1056/NEJMoa0912614
- 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.
- National Comprehensive Cancer Network (NCCN). Clinical Practice Guidelines in Oncology: Chronic Myeloid Leukemia. Version 1.2026.
- Hochhaus A, Baccarani M, Silver RT, et al. European LeukemiaNet 2020 recommendations for treating chronic myeloid leukemia. Leukemia. 2020;34(4):966-984.
- U.S. Food and Drug Administration (FDA). Tasigna (nilotinib) prescribing information. Reference ID: 5063780.
- World Health Organization (WHO). WHO Model List of Essential Medicines — 23rd List (2023). Geneva: WHO; 2023.
- Cortes JE, Kantarjian H, Shah NP, et al. Ponatinib in refractory Philadelphia chromosome-positive leukemias. New England Journal of Medicine. 2012;367(22):2075-2088.
- Etienne G, Guilhot J, Rea D, et al. Long-term follow-up of the French Stop Imatinib (STIM1) study in patients with chronic myeloid leukemia. Journal of Clinical Oncology. 2017;35(3):298-305.
- British National Formulary (BNF). Nilotinib. National Institute for Health and Care Excellence (NICE). Available at: bnf.nice.org.uk
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