Crizotinib – ALK and ROS1 Inhibitor Therapy

Crizotinib is a highly selective oral receptor tyrosine kinase inhibitor that represents a breakthrough in personalized oncology. The drug belongs to the category of targeted therapies and is specifically designed to treat tumors whose growth is driven by specific genetic alterations. Crizotinib blocks signaling pathways within cancer cells, inhibiting their division and inducing cell death.

The mechanism of action of crizotinib involves the inhibition of anaplastic lymphoma kinase (ALK), proto-oncogene ROS1, and hepatocyte growth factor receptor (HGFR, c-Met). In ALK-positive patients, a genetic rearrangement occurs, leading to the fusion of the ALK gene with the EML4 gene, creating an abnormal protein that constantly stimulates tumor growth. Crizotinib selectively binds to the ATP-binding pocket of these enzymes, effectively "switching off" the molecular growth switch. This leads to a significant reduction in tumor mass and disease stabilization, even in advanced stages where traditional chemotherapy proves ineffective.

The drug is available in oral capsule form, allowing patients to undergo treatment in an outpatient setting under the regular supervision of a physician.

Wikipedia page
Crizotinib

Indications

Crizotinib is indicated for the treatment of adult patients with advanced or metastatic cancers harboring a specific biomarker:

  • ALK-positive NSCLC: first-line therapy or subsequent treatment of non-small cell lung cancer with a confirmed ALK gene translocation.
  • ROS1-positive NSCLC: treatment of metastatic non-small cell lung cancer in patients whose tumors harbor a ROS1 gene rearrangement.
  • Genetic Testing: the drug should only be prescribed after mandatory confirmation of these genetic abnormalities using certified diagnostic methods (FISH or IHC).

Dosage and administration

The dosing regimen for crizotinib is standardized but may be adjusted based on the patient's individual tolerance to the medication.

  • Standard Dose: the recommended dose is 250 mg twice daily (total daily dose of 500 mg).
  • Administration Method: capsules should be swallowed whole, with or without food. Do not crush, dissolve, or open the capsules.
  • Missed Dose: if the next dose is due in less than 6 hours, the missed dose should be skipped.
  • Dose Adjustment: in case of severe adverse reactions, the dose may be tapered to 200 mg twice daily, and then to 250 mg once daily.
  • Monitoring: regular monitoring of complete blood counts, liver enzyme levels, and ECG monitoring of the QT interval is required during therapy.

The use of crizotinib requires caution and is excluded in the presence of the following factors:

  • Hypersensitivity: allergic reactions to crizotinib or any excipients within the capsule.
  • Hepatic Impairment: severe liver insufficiency (the drug is extensively metabolized in the liver).
  • Pregnancy and Lactation: due to the risk of severe fetal toxicity, therapy is contraindicated during pregnancy; breastfeeding must be discontinued.
  • Cardiovascular Conditions: presence of congenital long QT syndrome or severe bradycardia.
  • Drug Interactions: concomitant use of strong CYP3A4 inducers or inhibitors (e.g., St. John's wort, rifampicin, ketoconazole) is prohibited.

Crizotinib therapy may be accompanied by several characteristic adverse reactions:

  • Visual Disturbances: the most common effect, manifesting as light flashes, double vision, or blurred vision (usually at the start of treatment).
  • Hepatotoxicity: elevation of transaminase levels (ALT, AST), requiring strict laboratory monitoring.
  • GI Disorders: nausea, vomiting, diarrhea or constipation, and decreased appetite.
  • Pulmonology: risk of developing interstitial lung disease or pneumonitis (requires immediate discontinuation of the drug).
  • Neurology and Heart: peripheral neuropathy, dizziness, edema, and QT interval prolongation.
  • Hematology: development of neutropenia and leukopenia, increasing the risk of infections.

Frequently Asked Questions

Crizotinib is a targeted therapy belonging to the class of receptor tyrosine kinase inhibitors. It works by blocking specific abnormal proteins, such as ALK (anaplastic lymphoma kinase), ROS1, and MET. These proteins signal cancer cells to divide and grow uncontrollably. By inhibiting these pathways, crizotinib slows down tumor progression and can lead to tumor shrinkage.
The primary indication is locally advanced or metastatic non-small cell lung cancer (NSCLC) that tests positive for ALK or ROS1 gene rearrangements. Before starting therapy, patients must undergo a genetic test to confirm the presence of these specific biomarkers, as the drug is effective only in these cases.
Visual disturbances are among the most common side effects of crizotinib. Patients may experience light flashes, blurred vision, double vision, or "floaters." These symptoms typically occur early in the course of treatment. Any changes in vision should be reported to a healthcare provider, especially if they impair the ability to drive or operate machinery.
The medication can cause QTc interval prolongation on an ECG and a slow heart rate (bradycardia), making periodic cardiac monitoring essential. Additionally, elevated liver enzymes can occur, indicating potential liver stress. A physician will regularly order blood tests and ECGs to adjust the dose or temporarily pause treatment if necessary.
Capsules are taken twice daily, with or without food, and should be swallowed whole. It is vital to avoid grapefruit and grapefruit juice during treatment, as they can significantly increase the drug's concentration in the body, raising the risk of severe side effects.

List of medicines by active substance

-7%
Xalkori 250 mg Pfizer
View
Pfizer
250 mg 60 capsules
58427₴ 62921₴
-6%
Crizocent 250 250 mg Incepta Pharmaceuticals
View
Incepta Pharmaceuticals
250 mg 60 capsules
15461₴ 16404₴
-10%
Lucicriz 250 mg Lucius
View
Lucius
250 mg 60 capsules
20225₴ 22472₴
-9%
Alkixen 250 mg Everest
View
Everest
250 mg 60 capsules
18427₴ 20225₴
-53%
Crikzo 250 mg Hetero
View
Hetero
250 mg 30 capsules
10112₴ 21528₴
✅ All products loaded (5)

Contact us

Choose a convenient way to contact

We work daily from 9:00 to 20:00