About

Osimertinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) specifically designed to target both EGFR-sensitizing mutations (Ex19del, L858R) and the EGFR T790M resistance mutation. This dual targeting makes it highly effective in treating non-small cell lung cancer (NSCLC) patients who have developed resistance to earlier generation EGFR TKIs, as well as in the first-line setting for patients with common EGFR mutations.

Osimertinib is administered orally and is primarily metabolized by CYP3A4 and flavin-containing monooxygenase 3 (FMO3). Its selective action minimizes off-target effects while providing robust anti-tumor activity. Due to its cardiac and pulmonary side effect profile, careful monitoring of cardiac function (QTc interval) and respiratory symptoms is essential throughout treatment.

Uses

First-line treatment for metastatic NSCLC with EGFR Exon 19 deletions or Exon 21 L858R mutations.
Treatment of metastatic NSCLC with EGFR T790M mutation, after progression on prior EGFR TKI therapy.
Adjuvant therapy after tumor resection in NSCLC patients with EGFR mutations.
Used in specific cases of advanced NSCLC with certain EGFR mutations.

Directions For Use

Take orally once daily, with or without food. Swallow the tablet whole with water.

Benefits

Effective against EGFR T790M resistance mutation.
Improves progression-free survival in NSCLC.
Can cross the blood-brain barrier, treating brain metastases.
Offers a targeted therapy option for NSCLC.
Available as a convenient oral tablet.
May improve overall survival in certain patient populations.

Side Effects

Diarrhea
Rash
Dry skin
Nail disorders (paronychia)
Stomatitis
Fatigue
Decreased appetite
QTc prolongation
Interstitial lung disease (ILD)
Cardiomyopathy
Anemia
Thrombocytopenia

Safety Measures

Alcohol - Limit alcohol intake as it may exacerbate gastrointestinal side effects or liver enzyme elevations.
Pregnancy - Contraindicated in pregnancy due to potential for fetal harm. Use effective contraception.
Breastfeeding - Not recommended during breastfeeding due to potential excretion into breast milk and harm to the infant.
Liver - Use with caution in patients with hepatic impairment; dose adjustments may be necessary due to liver metabolism.
Kidney - Generally safe in mild to moderate renal impairment. No specific dose adjustment usually required for severe impairment, but monitor closely.
Lung - Monitor closely for signs of interstitial lung disease (ILD) or pneumonitis; discontinue if ILD is confirmed.

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