Ceritinib(Zykadia)

Ceritinib is a drug developed and produced by Novartis in Switzerland for the treatment of specific types of lung cancer. It was approved for market by the US Food and Drug Administration (FDA) on April 29, 2014, becoming the second ALK inhibitor in the world.

Lucius version of Ceritinib is a generic version with a drug specification of 150mg * 50Capsules.

Ceritinib exerts inhibitory effects on cells expressing ALK fusion proteins such as EML4-ALK and NPM-ALK by suppressing the activity of ALK proteins, achieving the therapeutic effect of cancer treatment and overcoming patients' resistance to first generation ALK inhibitors to a certain extent.

1.Main components

Ceritinib

2.Adapt to the population

Select patients for treatment of metastatic NSCLC with Ceritinib based on the presence of ALK positivity in tumor specimens.

3.Medication for special populations

3.1Pregnancy

Ceritinib can cause fetal harm when administered to a pregnant woman. The limited available data on the use of Ceritinib in pregnant women are insufficient to inform a risk.

3.2Lactation

There are no data regarding the presence of Ceritinib or its metabolites in human milk, the effects of Ceritinib on the breastfed child or its effects on milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with Ceritinib and for 2 weeks following completion of therapy.

3.3Females and Males of Reproductive Potential

Advise females of reproductive potential to use effective contraception during treatment with Ceritinib and for 6 months following completion of therapy.

Based on the potential for genotoxicity, advise males with female partners of reproductive potential to use condoms during treatment with Ceritinib and for 3 months following completion of therapy.

3.4Pediatric Use

The safety and effectiveness of Ceritinib in pediatric patients have not been established.

3.5Geriatric Use

No overall differences in safety or effectiveness were observed between these subjects and younger subjects.

3.6Hepatic Impairment

For patients with severe hepatic impairment, reduce the dose of Ceritinib. No dose adjustment is recommended for patients with mild or moderate hepatic impairment.

4.Drug overdose

Drug overdose is not yet clear.

5.Drug storage

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

6.Pharmacokinetics

After a single oral administration of Ceritinib in patients, peak plasma levels (Cmax) of Ceritinib were achieved around 4 to 6 hours.

from FDA，2021.10