Tepotinib

Tepotinib, as the world's first MET inhibitor, was first approved for market by the Japanese Ministry of Health, Labour and Welfare (MHLW) on March 25, 2020. On February 3, 2021, the US Food and Drug Administration (FDA) accelerated the approval of Tepotinib for market.

The specification design of 225mg * 60Tablets for the Lucius version of Tepotinib takes into account multiple aspects such as patient medication needs. Patients should consult professional doctors or pharmacists for advice when choosing and using, and follow medical advice for standardized treatment.

Tepotinib is an orally administered selective MET tyrosine kinase inhibitor that selectively binds to MET and inhibits MET protein phosphorylation, blocking oncogenic MET receptor signaling caused by MET gene mutations and leading to tumor cell death.

1.Main components

Tepotinib

2.Adapt to the population

Tepotinib is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) harboring mesenchymal-epithelial transition (MET) exon 14 skipping alterations.

3.Medication for special populations

3.1Pregnancy

Tepotinib can cause fetal harm when administered to a pregnant woman. There are no available data on the use of Tepotinib in pregnant women. 

3.2Lactation

There are no data regarding the secretion of Tepotinib or its metabolites in human milk or its effects on the breastfed infant or milk production. Advise women not to breastfeed during treatment with Tepotinib and for one week after the final dose.

3.3Females and Males of Reproductive Potential

Advise females of reproductive potential to use effective contraception during Tepotinib treatment and for one week after the final dose.

Advise male patients with female partners of reproductive potential to use effective contraception during Tepotinib treatment and for one week after the final dose.

3.4Pediatric Use

The safety and efficacy of Tepotinib in pediatric patients have not been established.

3.5Geriatric Use

No clinically important differences in safety or efficacy were observed between patients aged 65 years or older and younger patients.

3.6Renal Impairment

No dosage modification is recommended in patients with mild or moderate renal impairment . The recommended dosage has not been established for patients with severe renal impairment.

3.7Hepatic Impairment

No dosage modification is recommended in patients with mild or moderate hepatic impairment. The pharmacokinetics and safety of Tepotinib in patients with severe hepatic impairment have not been studied.

4.Drug overdose

Drug overdose is not yet clear.

5.Drug storage

Store Tepotinib at 20°C-25°C (68°F-77°F); excursions permitted to 15°C-30°C (59°F-86°F).

Store in original package.  

6.Pharmacokinetics

The median Tmax of Tepotinib is 8 hours (range from 6 to 12 hours). The geometric mean (CV%) absolute bioavailability of Tepotinib in the fed state was 71.6% (10.8%) in healthy subjects. 

from FDA，2023.03