Ceritinib

About Ceritinib

• Ceritinib, is a prescription-only medication utilized for treating non-small cell lung cancer (NSCLC). 
• The FDA approved Ceritinib capsules on April 29, 2014. The approval was granted following an analysis of findings from a clinical trial involving 376 individuals diagnosed with advanced or metastatic non-small cell lung cancer (NSCLC) positive for ALK. 
• The research indicated that ceritinib exhibited a notable enhancement in progression-free survival and objective response rates when contrasted with the outcomes observed with chemotherapy.
• Ceritinib acts as both a substrate and a potent inhibitor of the enzyme CYP3A4, making it susceptible to interactions with medications that share an affinity for this enzyme. 
• The therapeutic impact of ceritinib is achieved through the inhibition of autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and the proliferation of ALK-dependent cancer cells.
• There are two generic versions of Ceritinib available in India, which are Noxalk and Spexib. Noxalk is manufactured by Natco Pharma Ltd., while Spexib is marketed by Novartis India Ltd. Both Noxalk and Spexib are available in 150mg capsules and are used to treat non-small cell lung cancer

Strength: 

The Ceritinib capsules comes in 150 mg.

Recommended Dosage:

• The prescribed dosage for Ceritinib is 750 mg taken orally once a day, continuing until disease progression or if intolerable side effects arise. 
• It is advisable to consume Ceritinib at least 1 hour before or 2 hours after a meal. 
• In case a dose is overlooked, it should be compensated unless the subsequent dose is scheduled within the next 12 hours. 
• If vomiting occurs during the treatment, refrain from administering an extra dose and proceed with the next scheduled Ceritinib dose.

Important: 

Discontinue Ceritinib for patients who cannot tolerate 300 mg daily. Avoid using strong CYP3A inhibitors concurrently with Ceritinib. If simultaneous use of a strong CYP3A inhibitor is inevitable, reduce the Ceritinib dose by about one-third, rounded to the nearest multiple of the 150 mg dosage strength. Upon discontinuation of a strong CYP3A inhibitor, resume the Ceritinib dose taken before initiating the strong CYP3A4 inhibitor.

Warnings & Precaution:

• Ceritinib, a kinase inhibitor indicated for metastatic non-small cell lung cancer (NSCLC) with anaplastic lymphoma kinase (ALK) positivity, demands a thorough understanding of potential risks and careful patient management. 
• Gastrointestinal toxicity, a serious concern, may require dose adjustments in response to symptoms such as diarrhea, nausea, vomiting, or abdominal pain, with vigilance for responsiveness to antiemetics or antidiarrheals. 
• Regular monthly monitoring of liver function is imperative due to the associated risk of hepatotoxicity, with appropriate actions taken based on laboratory test results. Patients diagnosed with interstitial lung disease (ILD)/pneumonitis should permanently discontinue Ceritinib. 
• Moreover, the drug’s potential to cause QT interval prolongation, hyperglycemia, bradycardia, and pancreatitis necessitates diligent monitoring and potential dose adjustments. 
• Female patients of reproductive potential must be thoroughly informed about the potential harm to a fetus and the critical need for effective contraception. 
• Prudent consideration, active monitoring, and timely interventions are essential components of ensuring the safe and effective use of Ceritinib in clinical practice.

Common Ceritinib Side Effects:

• Diarrhea (most common)
• Nausea and vomiting
• Loss of appetite
• Constipation
• Fatigue
• Rash
• Muscle and joint pain
• Headache
• Vision changes

Use in Specific Population

• Ceritinib, a kinase inhibitor with potential fetal harm, is cautioned for use in pregnant women. Animal studies and the drug’s mechanism of action support the risk of fetal harm when administered to pregnant individuals. 
• Although data on the presence of ceritinib or its metabolites in human milk, its effects on breastfed infants, or milk production are not available, caution is advised due to the potential for serious adverse reactions. 
• Female patients are advised against breastfeeding during Ceritinib treatment and for two weeks following therapy completion. 
• It is reiterated that Ceritinib can cause fetal harm in pregnant women. Females of reproductive potential should use effective contraception during Ceritinib treatment and for six months after therapy completion. 
• For males with female partners of reproductive potential, the use of condoms is recommended during Ceritinib treatment and for three months after therapy completion, considering the drug’s potential for genotoxicity. 
• The safety and effectiveness of Ceritinib in pediatric patients have not been established, and its use in this population is not recommended. 
• Additionally, caution is advised in patients with hepatic impairment, as Ceritinib is primarily eliminated via the liver, and dose adjustment is not recommended for those with mild hepatic impairment. 
• However, no recommended dose has been determined for patients with moderate to severe hepatic impairment.

Storage and Handling

• Keep Ceritinib at a temperature of 25°C (77°F). Excursions within the range of 15°C to 30°C (59°F to 86°F) are permitted.
• Do not freeze the medicine. 
• Keep the medicine away from pets and children. 

Check Prescribing Information