Capmatinib – Selective MET Tyrosine Kinase Inhibitor

Capmatinib is a highly selective and potent oral inhibitor of the MET receptor tyrosine kinase (hepatocyte growth factor receptor). The drug was specifically developed for the targeted therapy of non-small cell lung cancer (NSCLC) associated with genetic alterations in the MET signaling pathway. Its primary mechanism of action involves blocking MET phosphorylation, which prevents the activation of downstream signaling pathways (such as MAPK, PI3K/AKT, and STAT3) responsible for abnormal growth, survival, and metastasis of tumor cells.

Capmatinib holds particular significance for patients with a MET exon 14 skipping mutation (METex14). This mutation leads to the loss of a regulatory domain in the protein, causing its constant activation and uncontrolled cell proliferation. Capmatinib effectively suppresses this process, demonstrating high antitumor activity even in patients previously treated with chemotherapy or immunotherapy. Clinical studies also confirm its ability to cross the blood-brain barrier, allowing for the control of brain metastases. The drug represents a breakthrough in precision oncology, enabling an aggressive form of lung cancer to be managed as a controlled chronic condition.

The drug is taken orally twice daily. Therapy requires mandatory molecular-genetic testing of the tumor to confirm the presence of a MET mutation.

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Capmatinib

Indications

Capmatinib is indicated for the treatment of adult patients with the following diagnosis:

  • Metastatic NSCLC: non-small cell lung cancer with a confirmed MET exon 14 skipping mutation (METex14).
  • Lines of Therapy: the drug can be used both as first-line therapy (previously untreated patients) and after prior treatment.
  • Special Cases: effective in the presence of central nervous system metastatic disease.

Dosage and administration

The capmatinib dosing regimen is designed to maintain constant blockade of MET receptors.

  • Standard Dose: 400 mg twice daily (two 200 mg tablets in the morning and evening).
  • Administration Method: tablets are taken orally whole, regardless of food. Do not break or chew the tablets.
  • Missed Dose: if a dose is missed by more than 8 hours, skip the dose and take the next one as scheduled.
  • Dose Adjustment: if intolerable toxicity occurs, the dose is reduced to 300 mg or 200 mg twice daily. If 200 mg is not tolerated, therapy is discontinued.
  • Monitoring: regular monitoring of lung function and liver enzymes is required.

The use of capmatinib involves certain medical precautions:

  • Hypersensitivity: known allergy to capmatinib or any excipients.
  • Pregnancy: the drug has fetotoxic potential; patients of childbearing age must use effective contraception during treatment and for one week after.
  • Lactation: breastfeeding is prohibited during therapy and for 7 days after the final dose.
  • Drug Interactions: avoid concomitant use with strong CYP3A inducers (e.g., rifampin, St. John's wort), as they significantly reduce drug concentrations.

The side effects of capmatinib are specific to this class of tyrosine kinase inhibitors:

  • Edema: peripheral edema (the most frequent symptom), typically affecting the lower limbs and hands.
  • Digestive System: nausea, vomiting, diarrhea, and decreased appetite.
  • Hepatotoxicity: increased ALT and AST levels, requiring regular biochemical blood analysis.
  • Pulmonology: risk of developing interstitial lung disease (ILD) or pneumonitis, requiring immediate cessation of treatment if dyspnea appears.
  • General Symptoms: fatigue, weakness, and increased blood creatinine levels.

Frequently Asked Questions

Capmatinib is a targeted therapy that acts as a potent and selective inhibitor of the mesenchymal-epithelial transition (MET) receptor. In certain cancer cells, the MET receptor is constitutively active, driving the tumor to grow and spread uncontrollably. Capmatinib blocks this receptor, interrupting growth signals and promoting cancer cell death.
Capmatinib is indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) harboring a specific genetic alteration—MET exon 14 skipping mutations (METex14). Testing for this biomarker is mandatory before initiating therapy, as the drug specifically targets this mechanism of disease progression.
The standard dose of capmatinib is taken twice daily (morning and evening) at approximately the same time. The tablets can be taken with or without food and must be swallowed whole. If vomiting occurs within one hour of taking a dose, do not take an additional dose; wait until the next scheduled time.
Peripheral edema (most commonly swelling of the ankles or feet) is a very common side effect of capmatinib. You should report any swelling to your doctor. Depending on the severity, management may include the use of compression stockings, dietary salt restriction, or a temporary dose reduction.
Capmatinib can cause serious lung inflammation (pneumonitis) and elevations in liver enzymes. If you develop new or worsening shortness of breath, cough, or fever, contact your physician immediately. Additionally, regular blood tests will be conducted during therapy to monitor your liver function.

List of medicines by active substance

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Capmaxen 200 mg Everest
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Everest

Capmaxen

Capmatinib
200 mg 56 tablets
29663₴ 32360₴
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