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Erlotinib is an oral anti-cellular drug. It has been successfully marketed both at home and abroad, and is widely used in the treatment of malignant cells such as non-small cell lung disease.
1. Generic name: Erlotinib
2. Trade name: TARCEVA®
1. Non-small cell lung cancer (NSCLC) :
First-line treatment of metastatic NSCLC with EGFR exon 19 deletion or exon 21 (L858R) mutation.
Maintenance therapy or second-line or above treatment after progression on at least one chemotherapy regimen.
Restrictions on : It is not recommended to be used in combination with platinum-containing chemotherapy. The safety and efficacy of other patients with EGFR mutations have not been established.
2. Pancreatic cancer : combined with gemcitabine in the first-line treatment of locally advanced or metastatic pancreatic cancer.
1. Tablet : 150mg.
2. Characteristics : film-coated tablets.
1. Active ingredient: erlotinib (hydrochloride form).
2. Excipients: lactose monohydrate, hypromellose, hydroxypropylcellulose, magnesium stearate, etc.
1. NSCLC : 150mg once a day, take on an empty stomach (1 hour before a meal or 2 hours after a meal).
2. Pancreatic cancer : 100 mg once a day combined with gemcitabine, taken on an empty stomach.
3. Missing a dose or vomiting : Skip the dose and take the next dose at the originally planned time.
1. Interstitial lung disease (ILD) : permanently discontinue the drug after diagnosis.
2. Hepatotoxicity :
For patients without underlying liver damage: suspend when ALT/AST>5 times ULN or bilirubin>3 times ULN, discontinue if no improvement occurs.
For patients with basic liver damage: pause when bilirubin or transaminase doubles from baseline.
Severe rash or diarrhea : suspend or reduce the dose (in 50 mg increments).
3. Drug interactions :
Strong inhibitors of CYP3A4 (such as ketoconazole): reduce the dosage by 50 mg.
CYP3A4 inducers (such as rifampicin): increase to a maximum of 450 mg.
1. Medication time : It must be taken on an empty stomach and avoid taking it with food.
2. Gastric acid regulator :
Proton pump inhibitors (such as omeprazole): avoid combined use.
H2 receptor antagonists (such as ranitidine): TARCEVA needs to be taken 10 hours after the administration of H2 antagonists.
3. Antacids: Take them several hours apart.
4. Smoking : Smoking will reduce the blood concentration of the drug, so it needs to be increased to a maximum of 300mg, and the original dose can be restored after quitting smoking.
1. Pregnant women : It can cause fetal malformation, so you need to use non-hormonal contraception until 1 month after the last dose.
2. Breastfeeding : Breastfeeding is prohibited during treatment and within 2 weeks after stopping the drug.
3. Children : safety has not been established.
4. Liver insufficiency : Close monitoring is required, and patients with severe liver damage should use with caution.
1. Common (≥20%) : rash (70%), diarrhea (42%), loss of appetite, fatigue, dyspnea.
2. Serious adverse reactions :
ILD (1.1%), liver failure, gastrointestinal perforation (0.4%), cerebrovascular accident (2.5% in patients with pancreatic cancer).
There are no clear contraindications.
1. CYP3A4 inhibitor/inducer : Significantly affects blood drug concentration, the dose needs to be adjusted.
2. Warfarin : Increases the risk of bleeding and requires monitoring of INR.
3. Gastric acid regulator : Reduces the absorption of erlotinib.
Store at 25°C (77°F), allow short-term exposure to 15-30°C.