Tepotinib

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

1. Drug name

1. Generic name : Tepotinib (Tepotinib)

2. Trade name : TEPMET KO®

2. Indications

It is used to treat adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors contain the MET exon 14 skipping mutation . This indication received accelerated approval based on overall response rate and duration of response, and further verification of clinical benefit is required.

3. Specifications and properties

1. Specifications : 225mg/tablet

2. Properties : Film-coated tablets

4. Main ingredients

1. Active ingredient :Tepotinibhydrochloridehydrate (tepotinib hydrochloride hydrate)

2. Excipient :Mannitol, microcrystalline cellulose, crospovidone, etc.

5. Usage and dosage

1. Recommended dosage of : 450mg (2 tablets) once a day, take with food.

2. How to take : Swallow the tablet whole. Do not chew, crush or break it.

3. Treatment of missed doses : If you miss a dose, you can take it within 8 hours; otherwise, skip it and take the medicine as originally planned the next day.

4. Vomiting treatment : There is no need to take another dose after vomiting. Take the next dose according to the planned time.

VI. Dose adjustment of

1. Adjust the dose according to the severity of adverse reactions:

(1). First dose reduction of : 225mg (1 tablet) once a day.

(2). Permanent discontinuation of : when the 225mg dose cannot be tolerated.

2. Key adjustments :

(1) Interstitial lung disease (ILD) : Suspend if suspected, permanently discontinue if confirmed.

(2). Hepatotoxic : suspend or reduce dosage according to the degree of ALT/AST elevation.

7. Medication precautions

1. Dietary requirements : Need to be taken with food to improve absorption.

2. Drug interactions :

Avoid combined use of : strong CYP3A inhibitors/P-gp inhibitors (such as ketoconazole), strong CYP3A inducers (such as rifampicin).

3. Use P-gp substrate (such as digoxin) with caution, the dose may need to be adjusted.

8. Medication for special groups

1. Pregnancy/breastfeeding : It has embryo-fetal toxicity and requires contraception until 1 week after stopping the drug; it is contraindicated during lactation.

2. Hepatic/renal insufficiency : No dose adjustment is required for mild to moderate symptoms, and insufficient data for severe symptoms.

3. Elderly : No dose adjustment is required (79% of patients in clinical trials are ≥65 years old).

9. Adverse reactions

1. Common (≥20%) :

Edema, fatigue, nausea, diarrhea, musculoskeletal pain, and dyspnea.

2. Serious adverse reactions :

ILD/pneumonitis (2.2%, possibly fatal), hepatotoxicity (4.2% ≥Grade 3 ALT/AST elevation).

10. Contraindications

There are no clear contraindications.

11. Storage method

Conditions : 20°C-25°C (15°C-30°C allowed), stored in original packaging.