Erlotinib is an oral anti cellular drug. It has been successfully launched both domestically and internationally and widely used in the treatment of malignant cells such as non-small cell lung diseases.

1、 Drug name

1. Common name: Erlotinib

2. Product Name: TARCEVA ®

2、 Indications

1. Non small cell lung cancer (NSCLC):

Frontline treatment for metastatic NSCLC with EGFR exon 19 deletion or exon 21 (L858R) mutation.

Second line or higher treatment after maintenance therapy or at least one chemotherapy regimen has progressed.

Limitations: Combination with platinum based chemotherapy is not recommended, and the safety and efficacy of other EGFR mutation patients have not been established.

2. Pancreatic cancer: first-line treatment of locally advanced or metastatic pancreatic cancer with gemcitabine.

3、 Specifications and characteristics

1. Tablets: 150mg.

2. Appearance: Thin film coated sheet.

4、 Main components

1. Active ingredient: Erlotinib (hydrochloride form).

2. Accessories: lactose monohydrate, hydroxypropyl methylcellulose, hydroxypropyl cellulose, magnesium stearate, etc.

5、 Usage and dosage

1. NSCLC: 150mg once daily, taken on an empty stomach (1 hour before or 2 hours after meals).

2. Pancreatic cancer: 100mg once a day in combination with gemcitabine, taken on an empty stomach.

3. Omission or vomiting: skip this dose and take the next dose at the original scheduled time.

6、 Dose adjustment

1. Interstitial lung disease (ILD): permanent discontinuation of medication after diagnosis.

2. Hepatotoxicity:

For patients without underlying liver damage: pause when ALT/AST>5 times ULN or bilirubin>3 times ULN, and stop medication if there is no improvement.

Individuals with underlying liver damage: pause when bilirubin or transaminase levels double from baseline.

Severe rash or diarrhea: pause or reduce dosage (decreasing by 50mg).

3. Drug interactions:

CYP3A4 strong inhibitors (such as ketoconazole): reduce dosage by 50mg.

CYP3A4 inducer (such as rifampicin): Increase to a maximum of 450mg.

7、 Medication precautions

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 combination therapy.

H2 receptor antagonists (such as ranitidine): TARCEVA should be taken 10 hours after H2 antagonist administration.

3. Antacids: Take them every few hours.

4. Smoking: Smoking can reduce blood drug concentration, which should be increased to a maximum of 300mg. After quitting smoking, the original dose should be restored.

8、 Medication for special populations

1. Pregnant women: May cause fetal malformation, non hormonal contraception should be used until one month after the last dose.

2. Breastfeeding period: Breastfeeding is prohibited during the treatment period and within 2 weeks after discontinuation of medication.

3. Children: Safety has not been established.

4. Liver dysfunction: requires close monitoring, and should be used with caution in patients with severe liver damage.

9、 Adverse reactions

1. Common (≥ 20%): rash (70%), diarrhea (42%), decreased appetite, fatigue, and difficulty breathing.

2. Serious adverse reactions:

ILD(1.1%)、 Liver failure, gastrointestinal perforation (0.4%), cerebrovascular accident (2.5% of pancreatic cancer patients).

10、 Contraindications

There are no clear contraindications.

11、 Drug interactions

1. CYP3A4 inhibitors/inducers: significantly affect blood drug concentration and require dosage adjustment.

2. Warfarin: increases bleeding risk, INR needs to be monitored.

3. Gastric acid regulator: reduces the absorption of erlotinib.

12、 Storage method

Store at 25 ° C (77 ° F) and allow short-term exposure to 15-30 ° C.

Erlotinibinformation