Tepotinib is an oral kinase inhibitor that primarily acts on MET receptor tyrosine kinase.

1、 Drug name

1. Common name: Tepotinib

2. Product Name: TEPMETKO ®

2、 Indications

Used for the treatment of metastatic non-small cell lung cancer (NSCLC) in adult patients with MET exon 14 skipping mutation in the tumor.

3、 Specifications and characteristics

1. Specification: 225mg per tablet (calculated as tepotinib).

2. Appearance: Thin film coated sheet.

4、 Main components

1. Active ingredient: Terbotinib hydrochloride hydrate (equivalent to 225mg Terbotinib).

2. Accessories: mannitol, microcrystalline cellulose, cross-linked polyvinylpyrrolidone, magnesium stearate, colloidal silica, etc.

3. Coating ingredients: Hydroxypropyl methylcellulose, titanium dioxide, lactose, polyethylene glycol, triacetin, iron oxide red, etc.

5、 Usage and dosage

1. Recommended dose: 450mg (2 tablets) once daily, taken with meals.

2. Usage: Swallow the whole tablet, do not chew, crush or break it open.

3. Course of treatment: Continue medication until disease progression or intolerable toxicity occurs.

6、 Dose adjustment

1. First dose reduction: 225mg (1 tablet) once daily.

2. Permanent discontinuation: If unable to tolerate 225mg once daily.

3. Specific adjustment basis:

(1) ILD/pneumonia: If suspected, medication will be temporarily suspended; if diagnosed, medication will be permanently discontinued.

(2) Hepatotoxicity: Suspend or discontinue medication based on the degree of elevation of ALT/AST/total bilirubin.

4. Other adverse reactions: Adjust dosage or discontinue medication based on severity (grades 2-4).

7、 Medication precautions

1. After meals: Improve bioavailability.

2. Missed medication: If it is more than 8 hours before the next medication, it can be taken again, otherwise it will be skipped.

3. Vomiting: After vomiting, there is no need to take the next dose according to the original plan.

8、 Medication for special populations

1. Pregnant women: There is a risk of fetal malformation and effective contraception is necessary.

2. Breastfeeding period: It is not recommended to breastfeed during the treatment period and within one week after the last dose.

3. Elderly: No need to adjust dosage

4. Liver/kidney dysfunction: Mild to moderate without adjustment, severe with insufficient data.

9、 Adverse reactions

1. Common (≥ 20%):

Edema, fatigue, nausea, diarrhea, musculoskeletal pain, and difficulty breathing.

2. Serious adverse reactions:

(1) ILD/pneumonia (2.2%, fatal).

(2) Hepatotoxicity (13% ALT/AST elevation, 0.2% liver failure leading to death).

(3) Laboratory abnormalities: decreased lymphocytes, hypoalbuminemia, hyponatremia, elevated GGT/ALT/AST, etc.

10、 Contraindications

There are no clear contraindications.

11、 Drug interactions

1. Avoid using in combination:

Strong CYP3A inhibitors or inducers.

2. P-gp inhibitor

P-gp substrates with narrow therapeutic window (such as digoxin and dabigatran).

Monitoring is required: When used in combination with P-gp substrates, the dosage of the latter may need to be adjusted.

Twelve storage methods

1. Keep in its original packaging, away from light and moisture.

2. Temperature: 20 ° C-25 ° C (15 ° C-30 ° C allowed).

3. Do not touch children.

Tepotinibinformation