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Osimertinib is an oral third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI).
Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, suitable for the following conditions:
1. Adjuvant treatment of early EGFR mutation-positive NSCLC: For adult patients after complete tumor resection, the presence of EGFR exon 19 deletion or exon 21L858R mutation must be confirmed by an FDA-approved test.
2. Locally advanced unresectable (stage III) EGFR mutation-positive NSCLC : Applicable to adult patients whose disease has not progressed after completing platinum-based chemotherapy and radiotherapy.
3. First-line treatment of EGFR mutation-positive metastatic NSCLC : Single agent or combined with pemetrexed and platinum-based chemotherapy for patients with locally advanced or metastatic disease.
4. Treated EGFRT790M mutation-positive metastatic NSCLC : For patients who have failed previous EGFRTKI treatment, the T790M mutation needs to be confirmed by an FDA-approved test.
Standard dose :80 mg orally once a day, on an empty stomach or after a meal.
Combination chemotherapy regimen : When combined with pemetrexed and platinum, 80 mg once daily until disease progression or intolerable toxicity.
Dose adjustment : The dose can be reduced to 40 mg once a day according to the severity of adverse reactions. Serious adverse reactions require permanent discontinuation of the drug.
Patients with dysphagia : Disperse the tablets in 60 mL of non-carbonated water, stir and drink immediately, then rinse the container with 120-240 mL of water.
Nasogastric tube administration : Disperse in 15mL of water, rinse the tube after administration through the NG tube.
Surgical management : Medication should be discontinued for at least 5 days before elective surgery and resumed at least 2 weeks after major surgery and after the wound has healed.
1. Monotherapy : Leukopenia (65% ), lymphopenia (64%), thrombocytopenia (53%), anemia (52%), diarrhea (47%), rash (46%), musculoskeletal pain (38%), nail toxicity (34%), stomatitis (24%), fatigue (21%).
2. Combined chemotherapy : Leukopenia (88%), thrombocytopenia (85%), neutropenia (85%), rash (49%), diarrhea (43%).
1. Interstitial lung disease/pneumonia : The incidence rate is 4% (single drug) to 56% (used after radiotherapy and chemotherapy), and the fatality rate is 0.4-0.7%. If dyspnea occurs, the drug must be discontinued immediately for evaluation.
2. QT interval prolongation : 1.1% of patients have QTc>500ms. Avoid coadministration with other QT prolonging drugs and monitor ECG and electrolytes regularly.
3. Cardiomyopathy :The incidence rate is 3.8% (single drug) to 9% (combination chemotherapy), manifested by decreased LVEF. Regular cardiac function monitoring is required during treatment.
4. Keratitis : The incidence rate is 0.6%. Eye inflammation and vision changes require ophthalmological evaluation.
5. Skin toxicity : Including erythema multiforme, Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), the drug needs to be permanently discontinued.
6. Aplastic anemia : The incidence rate is 0.06% and it may be fatal. Complete blood counts should be monitored before and after treatment.
7. Embryotoxicity : Contraindicated for pregnant women, and patients of childbearing age need to take effective contraceptive measures (during and 6 weeks after stopping the drug for women, and 4 months after stopping the drug for men).
1. Children : The safety and effectiveness have not been established.
2. Liver injury : No dose adjustment is required for mild to moderate cases, and no recommended dose for severe cases.
3. Renal injury :No adjustment is required for creatinine clearance ≥15mL/min, and there is no recommended dose for end-stage renal disease.
4. Lactation : Breastfeeding is prohibited during treatment and within 2 weeks of stopping the drug.
1. Strong CYP3A inducer (such as rifampicin): Avoid combined use. If combined use is necessary, the dose of osimertinib needs to be increased to 160 mg/day, and the original dose should be restored after stopping the induction agent for 3 weeks.
2. BCRP/P-gp substrate (such as rosuvastatin): Osimertinib may increase its exposure, and adverse reactions need to be monitored.