Tagrisso Osimertinib Mesylate Tablets

1. Indications and Usage
Locally Advanced or Metastatic Non-Small Cell Lung Cancer (NSCLC):
Osimertinib is indicated for the treatment of patients with locally advanced or metastatic NSCLC whose tumors have specific sensitizing EGFR mutations (exon 19 deletions or exon 21 L858R mutations).
Metastatic NSCLC with EGFR T790M Mutation:
Indicated for the treatment of patients with metastatic NSCLC whose tumors have the T790M mutation, as detected by an FDA-approved test.
2. Dosage and Administration
Recommended Dosage:
Dose: 80 mg orally once daily.
Administration: Can be taken with or without food. If a dose is missed, it may be taken as soon as possible unless the next dose is due within 12 hours.
Dose Modifications:
Reduce dose to 40 mg once daily for certain adverse reactions (e.g., ILD, QTc prolongation, severe skin toxicity).
3. Mechanism of Action
EGFR TKI:
Osimertinib is an irreversible tyrosine kinase inhibitor of both EGFR sensitizing mutations (e.g., exon 19 del, L858R) and the T790M resistance mutation.
Physiological Effect:
It inhibits the phosphorylation of EGFR and downstream signaling pathways (such as PI3K/AKT and MAPK), thereby inhibiting tumor cell proliferation and inducing apoptosis.
4. Safety and Warnings
Interstitial Lung Disease (ILD):
Severe, fatal, or life-threatening ILD has been reported. Permanently discontinue in patients who develop ILD.
QTc Interval Prolongation:
Osimertinib can prolong the QTc interval. Avoid use in patients with congenital long QT syndrome. Monitor ECG and electrolytes periodically.
Embryo-Fetal Toxicity:
May cause fetal harm. Advise females of reproductive potential to use effective contraception during treatment and for at least 6 weeks after the final dose.
5. Adverse Reactions
Most Common:
Diarrhea, rash, fatigue, decreased appetite, dry skin, nail toxicity (paronychia), cough, and nausea.
Serious Adverse Events:
ILD/pneumonitis, QTc prolongation, cardiomyopathy, and keratitis.
6. Drug Interactions
Strong CYP3A4 Inducers:
Avoid concomitant use with strong CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine, St. John’s wort) as they may significantly decrease osimertinib exposure.
BCRP Substrates:
Osimertinib is a BCRP inhibitor. Monitor patients for potential toxicity when used with BCRP substrates (e.g., rosuvastatin).
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Osimertinib Mesylate.
Storage:
Store at room temperature (20°C to 25°C or 68°F to 77°F). Keep in original package to protect from moisture.