Alectinib – Highly Selective ALK Tyrosine Kinase Inhibitor

Alectinib is a highly selective and potent oral inhibitor of the anaplastic lymphoma kinase (ALK) tyrosine kinase. The drug is specifically designed for targeted therapy of non-small cell lung cancer (NSCLC) driven by genetic rearrangement (fusion protein) of the ALK gene. Alectinib effectively blocks the phosphorylation of the ALK protein, which halts growth signaling within the cancer cell, leading to the cessation of cell division and triggering the processes of natural tumor death.

The mechanism of action of alectinib is distinguished by its ability to overcome the resistance that often arises with first-generation ALK inhibitors. One of the most important pharmacological features of the drug is its ability to penetrate the blood-brain barrier and remain in the central nervous system (CNS) without being actively expelled by P-glycoprotein. This makes alectinib the "gold standard" in treating patients with brain metastases, providing a high intracranial response rate and preventing the development of new CNS lesions. Compared to chemotherapy and earlier targeted drugs, alectinib demonstrates significantly higher progression-free survival and possesses a favorable safety profile, allowing patients to maintain a high quality of life during long-term treatment.

The drug is taken orally twice daily with food. Therapy requires mandatory laboratory confirmation of the tumor's ALK-positive status.

Wikipedia page
Alectinib

Indications

Alectinib is indicated as monotherapy for adult patients with the following confirmed diagnosis:

  • ALK-positive NSCLC: first-line therapy for advanced or metastatic non-small cell lung cancer.
  • Progression on Crizotinib: treatment of patients with ALK-positive NSCLC who have experienced disease progression on or intolerance to crizotinib therapy.
  • CNS Metastases: therapy for patients with existing or a high risk of developing secondary lesions in the brain during ALK-positive cancer.

Dosage and administration

The alectinib dosing regimen requires strict adherence to meal times to ensure optimal absorption of the drug.

  • Standard Dose: 600 mg (four 150 mg capsules) twice daily. The total daily dose is 1200 mg.
  • Administration Method: capsules should be taken with food, swallowed whole. It is highly recommended not to open or chew the capsules.
  • Missed Dose: if a dose is missed and there are less than 6 hours until the next dose, the missed dose should be skipped. If vomiting occurs after taking a dose, do not take an additional capsule.
  • Dose Adjustment: if toxicity develops, the dose is sequentially reduced to 450 mg or 300 mg twice daily.
  • Monitoring: regular monitoring of liver function (ALT, AST, bilirubin) every two weeks is necessary during the first months of treatment.

The use of alectinib is restricted in cases of hypersensitivity to its components and certain physiological conditions:

  • Hypersensitivity: known allergy to alectinib or any auxiliary substances in the capsule.
  • Pregnancy: the drug has fetotoxicity; use is prohibited, and effective contraception is required.
  • Lactation: breastfeeding should be discontinued during therapy and for one week after the last dose.
  • Severe Hepatic Impairment: requires extremely cautious use and adjustment of the starting dose.
  • Pediatric Use: efficacy and safety in patients under 18 years of age have not been established.

Alectinib is generally well-tolerated, but it may cause specific changes in various body systems:

  • General Symptoms: edema (peripheral edema of the face, eyelids, and extremities), fatigue, and muscle pain (myalgia).
  • Digestive System: constipation (one of the most common effects), nausea, diarrhea, and stomatitis.
  • Hepatobiliary System: increased levels of bilirubin and liver enzymes; in rare cases, liver injury may occur.
  • Cardiovascular System: slowing of the heart rate (bradycardia), requiring pulse monitoring.
  • Respiratory System: risk of developing interstitial lung disease or pneumonitis.
  • Photosensitivity: increased skin sensitivity to sunlight; patients are advised to use sunscreen.

Frequently Asked Questions

Alectinib is a highly selective and potent inhibitor of ALK (Anaplastic Lymphoma Kinase) tyrosine kinase. It is designed to block the activity of the abnormal ALK protein that drives cancer cells to grow and divide. By blocking this signal, alectinib slows tumor growth or causes the tumor to shrink.
One of the key features of alectinib is its ability to effectively cross the blood-brain barrier. This allows the medication to target metastases in the central nervous system, which is critical for patients with ALK-positive lung cancer, as this type of cancer frequently spreads to the brain.
Alectinib is taken twice daily (morning and evening). The capsules must be taken with food and swallowed whole. Taking it with a meal ensures the proper absorption of the active substance. It is important to avoid grapefruit and grapefruit juice during therapy, as they can interfere with the concentration of the medication in your blood.
Alectinib can cause an increase in creatine phosphokinase (CPK) levels, which indicates muscle tissue damage. If you experience unexplained muscle pain, weakness, or tenderness, you should inform your physician immediately. Blood tests may be required to monitor your muscle enzyme levels in such cases.
The medication can increase skin sensitivity to ultraviolet light (photosensitivity). During treatment and for at least 7 days after completion, it is recommended to avoid prolonged sun exposure, use broad-spectrum sunscreen with a high SPF, and wear protective clothing to prevent sunburn.

List of medicines by active substance

-6%
Alecnib 150 mg Everest
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Everest

Alecnib

Alectinib
150 mg 56 capsules
20225₴ 21573₴
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