XALKORI 250 mg
Crizotinib
What it does
Crizotinib is a medication that helps treat certain types of cancer by targeting specific proteins involved in the growth of cancer cells.
Commonly used for: lung cancer (non-small cell lung cancer), other cancers with specific genetic changes
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Answers come only from this medicine's registration record, BNF monograph and interaction data - not medical advice.
Medicine sourcing is available in Kenya only. We don't sell or dispense medicines - licensed pharmacies do.
Sourcing - Kenya onlyRegistration & product details
Source: South African Health Products Regulatory Authority · fetched 2026-04-15 21:20:59 · updated 2026-09-23 04:11:38
Drug Interactions
142Pharmacodynamic Warnings
Crizotinib appears in TABLE 6: Drugs that cause bradycardia
Crizotinib appears in TABLE 9: Drugs that prolong the QT interval
Severe (8)
Antipsychotics, Second Generation - increases exposure
Crizotinib is predicted to increase the exposure to antipsychotics, second generation (cariprazine). Avoid.
Crizotinib - increases exposure
Antifungals, azoles (itraconazole, ketoconazole, posaconazole, voriconazole) are predicted to increase the exposure to crizotinib. Avoid. Also see TABLE 9 p. 1519.
Crizotinib - increases exposure
Antifungals, azoles (itraconazole, ketoconazole, posaconazole, voriconazole) are predicted to increase the exposure to crizotinib. Avoid. Also see TABLE 9 p. 1519.
Crizotinib - decreases exposure
Mitotane is predicted to markedly decrease the exposure to crizotinib. Avoid.
Crizotinib - decreases exposure
St John's wort is predicted to decrease the exposure to crizotinib. Avoid.
Crizotinib - increases exposure
Grapefruitjuiceispredictedtoincreasetheexposureto crizotinib.Avoid.oTheoretical
Crizotinib - decreases exposure
Rifampicin is predicted to markedly decrease the exposure to crizotinib. Avoid.
Domperidone - increases exposure
Crizotinib is predicted to increase the exposure to domperidone. Avoid.
Moderate (35)
Alfentanil - increases exposure
Crizotinibispredictedtoincreasetheexposuretoopioids (alfentanil,buprenorphine,fentanyl,oxycodone).Monitorand adjustdose.oStudy →AlsoseeTABLE6p.1518
Amlodipine - increases exposure
Crizotinib is predicted to increase the exposure to calcium channel blockers (amlodipine, felodipine, lacidipine, lercanidipine, nicardipine, nifedipine, nimodipine). Monitor and adjust dose.
Antiarrhythmics - increases exposure
Crizotinibispredictedtoincreasetheexposureto antiarrhythmics(propafenone).Monitorandadjustdose. oStudy →AlsoseeTABLE6p.1518
Atorvastatin - increases exposure
Crizotinib is predicted to increase the exposure to statins (atorvastatin). Monitor and adjust dose.
Bosutinib - increases exposure
Crizotinib is predicted to increase the exposure to bosutinib. Avoid or adjust dose. Also see TABLE 9 p. 1519.
Unknown (99)
Abemaciclib - increases exposure
Crizotinib is predicted to increase the exposure to abemaciclib.
Acalabrutinib - increases exposure
Crizotinib is predicted to increase the exposure to acalabrutinib. Avoid or monitor.
Alphablockers - increases exposure
Crizotinibispredictedtoincreasetheexposuretoalpha blockers(tamsulosin).oTheoretical 1xidneppA|snoitcaretnI A1 com/codemedicalapps/ cal Applications)
Alprazolam - increases exposure
Crizotinib is predicted to increase the exposure to alprazolam.
Antihistamines,non-Sedating - increases exposure
Crizotinib is predicted to increase the exposure to antihistamines, non-sedating (mizolastine).
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact
About this medicine
Crizotinib is a medication that helps treat certain types of cancer by targeting specific proteins involved in the growth of cancer cells.
What it treats
- lung cancer (non-small cell lung cancer)
- other cancers with specific genetic changes
How it works
It works by blocking signals that help cancer cells grow and spread, effectively slowing down or stopping the cancer.
Who it's for
It is for patients with specific types of lung cancer or other cancers associated with certain genetic markers.
Cautions
- • Be cautious if taking drugs that slow down the heart rate.
- • Avoid medications that can affect heart rhythm.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Crizotinib
BNF-referencedCrizotinib is a targeted therapy classified as a tyrosine kinase inhibitor, primarily used for the treatment of advanced non-small cell lung cancer (NSCLC) that is positive for anaplastic lymphoma kinase (ALK) or ROS1 gene rearrangements. It functions by inhibiting specific receptor tyrosine kinases involved in cancer cell proliferation and survival, thus impeding tumor growth.
Indications
- Anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer
- ROS1-positive advanced non-small cell lung cancer
Dosage
Children: For pediatric dosing, please refer to the BNF for Children as specific pediatric doses are not provided in the BNF.
Adults: The recommended adult dose is 250 mg taken orally twice daily. In cases of moderate to severe hepatic impairment, the dose may need to be adjusted based on individual safety and tolerability.
Mechanism of action
Crizotinib targets and inhibits anaplastic lymphoma kinase (ALK), hepatocyte growth factor receptor (HGFR, c-MET), and ROS1 (c-ros) by preventing their phosphorylation. This inhibition leads to the formation of inactive protein conformations, reducing cell proliferation and promoting apoptosis in cells harboring ALK-positive mutations, such as those with EML4-ALK fusion proteins.
Pharmacodynamics
Clinical studies have shown that crizotinib can lead to significant antitumor activity in patients with ALK-positive NSCLC, with a 6-month progression-free survival rate of around 72%. Its effectiveness is particularly notable in patients with specific genetic mutations, where it has demonstrated improved overall survival rates compared to untreated counterparts. However, the drug may be associated with adverse effects including hepatotoxicity and interstitial lung disease.
Pharmacokinetics
Crizotinib is administered orally, with a half-life that allows for twice-daily dosing. It is extensively metabolized by the liver, primarily via CYP3A4, and its pharmacokinetics can be significantly affected by concomitant medications that induce or inhibit this enzyme. The presence of liver or renal impairment may necessitate dosage adjustments.
Contra-indications
- Hypersensitivity to crizotinib or any of its components
- Severe hepatic impairment
Adverse effects
- Nausea
- Vomiting
- Diarrhea
- Fatigue
- Visual disturbances
- Cardiac failure
- Pulmonary edema
- Interstitial lung disease
- Hepatotoxicity
- QT interval prolongation
- Bradycardia
- Neutropenia
- Gastrointestinal perforation
Interactions
- Increased exposure when used with azole antifungals (itraconazole, ketoconazole, posaconazole, voriconazole)
- Increased exposure when used with second-generation antipsychotics
- Increased exposure when used with domperidone
- Decreased exposure when used with mitotane
- Decreased exposure when used with rifampicin
- Increased exposure when used with propafenone
- Increased exposure when used with midazolam
- Decreased exposure when used with St. John's Wort
- Increased exposure when used with grapefruit juice
Precautions
- Monitor for signs and symptoms of cardiac failure
- Regularly monitor ECG and electrolytes
- Use with caution in patients with moderate to severe hepatic impairment
- Monitor for gastrointestinal perforation
- Assess risk of QT interval prolongation
Pregnancy
Avoid, as there is evidence of toxicity in animal studies.
Breast-feeding
Avoid, as there is no available information on excretion in human milk.
Storage
Store at room temperature, away from moisture and heat.
Formulations
- Crizotinib 250 mg tablets
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Crizotinib
PubChem CID 11626560Molecular formula: C21H22Cl2FN5O
Mechanism of action
Crizotinib is a tyrosine kinase receptor inhibitor that targets anaplastic lymphoma kinase (ALK), hepatocyte growth factor receptor (HGFR, c-MET), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON). When activated, ALK inhibits apoptosis and promotes cell proliferation, and ALK-gene translocations can lead to the expression of oncogenic fusion proteins. A small portion of non-small cell lung cancer (NSCLC) patients have ALK-positive tumors. Most of these cases are characterized by the fusion of ALK with the chimeric protein echinoderm microtubule-associated protein-like 4 (EML4), resulting in increased kinase activity. Crizotinib inhibits ALK by inhibiting its phosphorylation and creating an inactive protein conformation. This ultimately lowers the proliferation of cells carrying this genetic mutation and tumour survivability. _In vitro_ assays on tumor cell lines demonstrated that crizotinib inhibits ALK, ROS1, and c-Met phosphorylation in a concentration-dependent manner. _In vivo_ studies in mice with tumor xenografts that expressed EML4- or nucleophosmin (NPM)-ALK fusion proteins or c-Met showed that crizotinib has antitumor activity.
Pharmacodynamics
In a phase I study, 37 patients with a variety of solid-tumor cancers refractory to therapy received 50 to 300 mg of crizotinib daily or twice daily. In this group, two patients with non-small cell lung cancer (NSCLC) exhibiting echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) mutations responded to therapy; therefore, following studies focused on patients with advanced ALK-positive disease. In this group of patients, the 6-month progression-free survival among crizotinib users was approximately 72%. When compared to ALK mutation-positive patients that did not receive crizotinib, ALK mutation-positive patients treated with crizotinib had a higher two-year overall survival rate (54% vs 36%). The use of crizotinib may lead to hepatotoxicity, interstitial lung disease (ILD), pneumonitis, QT interval prolongation, bradycardia, severe visual loss, embryo-fetal toxicity and gastrointestinal toxicity in pediatric and young adult patients with anaplastic large cell lymphoma (ALCL) or pediatric patients with inflammatory myofibroblastic tumor (IMT).
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
This drug in other countries
The same active ingredient registered across other registries we cover - including different brands.