Afatinib Dimaleate

Afatinib Dimaleate is an orally administered tyrosine kinase inhibitor (TKI) that irreversibly blocks EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) pathways to inhibit tumor proliferation in non-small cell lung cancer (NSCLC).

First-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) possessing non-resistant EGFR mutations (Exon 19 deletions or Exon 21 L858R substitutions), and previously treated metastatic squamous NSCLC progressing after platinum-based chemotherapy.

Tyrosine Kinase Inhibitor

Irreversible ErbB Family Blocker

Afatinib covalently binds to EGFR, HER2, and HER4, irreversibly inhibiting tyrosine kinase autophosphorylation and downregulating ErbB signaling in cancer cells.

Irreversible inhibition of ErbB family receptor tyrosine kinases halts downstream signaling cascades, resulting in cell cycle arrest and inhibition of tumor growth.

Recommended dose: 40 mg orally once daily. Severe renal impairment (eGFR 15 to 29 mL/min/1.73 m²): 30 mg orally once daily.

Administer orally once daily on an empty stomach at least 1 hour before or 2 hours after a meal with a glass of water.

Take the missed dose as soon as remembered if >12 hours remain before the next scheduled dose. If <12 hours remain, skip the missed dose.

Common to severe: Diarrhea, bullous/exfoliative skin disorders, rash, paronychia, stomatitis, decreased appetite, keratitis, elevated liver enzymes, and interstitial lung disease (ILD).

Withhold or reduce dose for severe or prolonged Grade ≥2 diarrhea, cutaneous reactions, suspected interstitial lung disease (ILD), hepatic toxicity, or keratitis.

Known hypersensitivity to Afatinib or any component of the formulation.

P-gp inhibitors (e.g., ketoconazole, erythromycin, verapamil) increase afatinib exposure. P-gp inducers (e.g., rifampin, carbamazepine, St. John's wort) decrease afatinib exposure.

Food significantly decreases the absorption and AUC of afatinib. Must be taken on an empty stomach.

Pregnancy Category D. Can cause fetal harm when administered to a pregnant woman. Females of reproductive potential must use effective contraception.

Pregnancy Category: D — always consult a doctor before taking during pregnancy.

Do not breastfeed during treatment with Afatinib and for 2 weeks after the final dose.

Safety and effectiveness in pediatric patients have not been established.

No overall differences in effectiveness were observed between elderly and younger patients, but elderly patients may experience higher rates of adverse reactions like severe diarrhea.

Dose adjustment to 30 mg daily in severe renal impairment (eGFR 15–29 mL/min/1.73 m²). Discontinue in severe hepatic impairment.

Overdose can lead to nausea, vomiting, asthenia, dizziness, headache, abdominal pain, and elevated amylase levels. Supportive management is indicated.

Store below 30°C in a dry and cool place, away from sunlight. Keep out of reach of children.

Afatinib Dimaleate (C24H25ClFN5O3 · 2C4H4O4)

Question: What type of drug is Afatinib Dimaleate? Answer: Afatinib is a targeted tyrosine kinase inhibitor (TKI) used primarily to treat EGFR mutation-positive metastatic non-small cell lung cancer (NSCLC). Question: How should Afatinib be taken? Answer: It should be taken orally once daily on an empty stomach, at least 1 hour before or 2 hours after a meal. Question: What should be done if severe diarrhea occurs during treatment? Answer: Anti-diarrheal medication should be initiated at the first sign of diarrhea, along with fluid hydration. If diarrhea is prolonged or severe, consult a physician as dose reduction or withholding treatment may be required. Question: Can Afatinib be taken during pregnancy or breastfeeding? Answer: No, it can cause fetal harm. Breastfeeding is contraindicated during treatment and for at least 2 weeks after the final dose.