Afatinib – Targeted Therapy

Afatinib is a potent, highly selective, and irreversible blocker of the ErbB receptor family. As a targeted anti-tumor agent, it represents a significant advancement in the management of specific types of lung cancer.

The mechanism of action involves forming a strong covalent bond with the active sites of EGFR (ErbB1), HER2 (ErbB2), and ErbB4 receptors. Unlike first-generation reversible inhibitors, afatinib irreversibly shuts down signaling from these receptors, which are responsible for the growth, survival, and spread of tumor cells. This enables effective suppression of cancer cell proliferation, even in cases where tumors have developed resistance to other therapies. The drug is particularly effective in patients harboring specific mutations in the EGFR gene.

Administered orally in tablet form, afatinib allows for sustained therapy aimed at controlling tumor progression.

Wikipedia page
Afatinib

Indications

Afatinib is indicated for the treatment of adult patients in the following clinical scenarios:

  • EGFR-mutated NSCLC: as a first-line treatment for metastatic non-small cell lung cancer (NSCLC) with non-resistant EGFR mutations.
  • Squamous NSCLC: treatment of metastatic squamous NSCLC progressing on or after platinum-based chemotherapy.

Dosage and administration

Afatinib dosage is determined individually and may be adjusted by a physician based on patient tolerance.

  • Standard Dose: 40 mg once daily.
  • Maximum Dose: may be increased to 50 mg daily in specific clinical circumstances.
  • Administration Rules: must be taken on an empty stomach (at least 1 hour before or 3 hours after a meal).
  • Dose Modification: if severe adverse reactions occur, the dose may be temporarily reduced (to 30 mg or 20 mg) until symptoms stabilize.

The use of afatinib is restricted in the following cases:

  • Hypersensitivity: known allergic reactions to afatinib or any of its excipients.
  • Severe Hepatic or Renal Impairment: use is generally not recommended in patients with severely impaired organ function.
  • Pregnancy and Lactation: potential for fetal harm; breastfeeding is strictly prohibited during treatment.
  • Pediatric Use: safety and efficacy in patients under 18 years of age have not been established.

Afatinib therapy requires close medical monitoring due to the risk of the following reactions:

  • Dermatologic: skin rash (acneiform dermatitis), pruritus, dry skin, and paronychia (nail bed inflammation).
  • Gastrointestinal: diarrhea (very common; requires early management with loperamide), stomatitis, nausea, and decreased appetite.
  • Ocular: conjunctivitis and keratitis (rarely; requires immediate ophthalmological evaluation).
  • Respiratory: risk of interstitial lung disease (ILD) (rare but potentially serious).
  • Laboratory: elevation of liver enzymes and hypokalemia.

Frequently Asked Questions

Afatinib is a potent and selective irreversible blocker of the ErbB receptor family (including EGFR, HER2, and HER4). Unlike reversible inhibitors, it binds permanently to these receptors, completely shutting down the signaling pathways that drive cancer cell growth and division. This helps to suppress tumor progression for an extended period.
Afatinib is primarily indicated for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) with EGFR mutations. It may also be used to treat patients with squamous cell carcinoma of the lung that has progressed after platinum-based chemotherapy.
Food intake significantly affects the absorption of afatinib; taking the medication with a high-fat meal decreases its plasma concentration by more than 50%. To ensure optimal efficacy, tablets should be taken at least 1 hour before or 3 hours after a meal.
Diarrhea is a very common side effect. Patients are advised to keep loperamide on hand and start taking it at the first sign of loose stools. If a skin rash develops, it is important to avoid direct sunlight and use moisturizing agents. In cases of severe symptoms, a physician may temporarily interrupt treatment or reduce the dose.
Afatinib can cause keratitis (inflammation of the cornea), which may present as eye pain, tearing, or blurred vision. Patients who wear contact lenses should be particularly cautious. If any acute visual symptoms occur, an immediate consultation with an ophthalmologist is required.

List of medicines by active substance Afatinib

-14%
Afanat 40 mg Natco
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Natco

Afanat

Afatinib
40 mg 28 tablets
8350₴ 9669₴
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