Generic
Osimertinib
11 brands available in the market
At a glance
Osimertinib is an EGFR tyrosine kinase inhibitor used for metastatic non-small cell lung cancer (NSCLC). It is effective in tumors with EGFR T790M, L858R and exon 19 deletion mutations.
Description
Osimertinib is a kinase inhibitor of EGFR that binds irreversibly to certain mutant forms of EGFR (T790M, L858R and exon 19 deletion). It produces pharmacologically active metabolites (AZ5104 and AZ7550) that exhibit anti-tumor activity against EGFR mutant tumors.
Indications
- Metastatic NSCLC with EGFR exon 19 deletions or exon 21 L858R mutations (first-line)
- EGFR T790M mutation-positive NSCLC (after progression on EGFR TKI therapy)
Therapeutic class
Cytotoxic Chemotherapy
Pharmacological class
EGFR Tyrosine Kinase Inhibitor
Pharmacology
Osimertinib binds to the ATP-binding site of EGFR to inhibit tyrosine kinase activity, preventing cancer cell growth and proliferation.
Mechanism of action
Treats NSCLC by inhibiting EGFR mutant cancer cell growth.
Dosage
Adult Dose (Oral):
- 80 mg once daily (with or without food)
- Continue until disease progression or unacceptable toxicity
Administration
- Swallow tablet whole; do not chew, crush or break
- Take at the same time each day
- May be taken with or without food
- For NG tube administration: Disperse in 15 ml non-carbonated water
Missed dose
If you miss a dose, skip it and take at next scheduled time; do not double the dose.
Side effects
Common Side Effects (≥20%):
- Diarrhea
- Rash
- Dry skin
- Nail toxicity
- Stomatitis
- Fatigue
- Decreased appetite
Serious: Interstitial Lung Disease/Pneumonitis (3.9%), QTc prolongation, Cardiomyopathy (1.4%)
Precautions & warnings
- Withhold if ILD/pneumonitis symptoms occur
- Monitor ECG in patients with QTc prolongation history
- Cardiomyopathy: Assess LVEF before and every 3 months
- Can cause fetal harm; use effective contraception (Females: 6 weeks after last dose; Males: 4 months after last dose)
Contraindications
No known contraindications.
Drug interactions
- Decreased exposure with strong CYP3A4 inducers (phenytoin, rifampicin, carbamazepine, St. John's Wort)
- Increased AUC and Cmax of rosuvastatin
- Decreased AUC and Cmax of simvastatin
- Increased exposure of BCRP substrates
Food interactions
Safety with alcohol not known; consult doctor.
Use in pregnancy
Use in Pregnancy: Osimertinib is highly unsafe during pregnancy; definite evidence of severe fetal harm. Do not use.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Osimertinib is probably unsafe during breastfeeding; do not breastfeed.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
Patients ≥65 years have higher incidence of Grade 3/4 adverse events and dose modifications.
Renal / hepatic impairment
Renal Impairment: Mild-severe (CrCl 15-89): No dose adjustment; ESRD (CrCl <15): No recommended dose.
Hepatic Impairment: Mild-moderate: No dose adjustment; Severe: No recommended dose.
Overdose effects
Limited information on overdose; symptomatic treatment.
Storage conditions
Store below 30°C; protect from moisture & light; safely discard expired medicine; keep out of reach of children.
Chemical structure
Osimertinib