Tepotinib

MET inhibitors
MET inhibitors
High alert
An error with this medicine can cause serious harm: double checks and protocols are used.
Pregnancy: avoid
Avoid in pregnancy. Tepotinib may harm the fetus: a pregnancy test is done first, contraception is used during treatment and for a week after, and breastfeeding is stopped.

An oral MET inhibitor taken with food for lung cancer with MET exon 14 skipping. Oedema, lung inflammation and liver injury are key risks.

Updated Nov 12, 2026

Quick facts

Group: MET inhibitors
Target: MET (hepatocyte growth factor receptor) tyrosine kinase
Key effects: Peripheral oedema · Nausea · Fatigue
Monitor: MET exon 14 test before starting · Liver tests
ATC: L01EP02

No doses: the clinician sets them by the current guideline.

Mechanism of action

MET (hepatocyte growth factor receptor) tyrosine kinaseTepotinib

The crystal shows tepotinib in the ATP site of human MET kinase.

Target in 3D: MET (hepatocyte growth factor receptor) tyrosine kinase. PDB structure 4R1V (RCSB PDB, public domain). View the structure at RCSB PDB

Tepotinib selectively blocks the ATP site of the MET kinase. In tumours with MET exon 14 skipping, MET is not degraded and drives growth continuously; tepotinib shuts down that signal and the tumour shrinks.

Tepotinib binds the ATP site of MET
Continuous MET signalling stops
MET-driven lung cancer shrinks

Indications

Metastatic non-small cell lung cancer with a MET exon 14 skipping alteration. Lung cancer →

Adverse effects

Common

Peripheral oedema
Nausea, diarrhoea, constipation, vomiting
Fatigue, decreased appetite, abdominal pain
Muscle, joint or bone pain
Rash, itching, dizziness, headache

Contraindications

Hypersensitivity to tepotinib

Key interactions

Prescription and over-the-counter drugs, vitamins and herbal products: Several interact; the list is reviewed and doses or monitoring adjusted.

What is monitored

MET exon 14 test before starting
Liver tests
Amylase and lipase
New cough, fever or breathlessness; limb swelling

Administration and safety

Oral tablets with food, swallowed whole; if needed, dispersed only in still water (not crushed) and drunk at once.
Can be given by nasogastric tube following the instructions.
If vomiting follows a dose, no extra dose is taken.

Pregnancy and breastfeeding

Avoid in pregnancy. Tepotinib may harm the fetus: a pregnancy test is done first, contraception is used during treatment and for a week after, and breastfeeding is stopped.

Nursing care

Teach to report cough, fever or breathlessness at once.
Monitor limb swelling and weight.
Teach the signs of liver injury and pancreatitis.
Contraception during treatment and for a week after; breastfeeding is stopped.

Pharmacokinetics

Absorption: Oral tablets once a day with food; can be dispersed in water for people who cannot swallow tablets.

Test yourself

Think of the answer, then tap the question to see it.

How is tepotinib taken relative to food?

With food.

What is the target of tepotinib?

The MET receptor tyrosine kinase.

Which lung complication must be reported at once?

Interstitial lung disease or pneumonitis (new cough, fever, breathlessness).

Add to my cards (3)

Connections

← Back to the class: MET inhibitors

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Tepotinib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2024); Tepotinib Hydrochloride - NCI (National Cancer Institute, 2024); RCSB PDB - 4R1V: Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors (RCSB Protein Data Bank, 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.