Ceritinib

What is Ceritinib?

• Ceritinib (Zykadia) is a kinase inhibitor used to treat people with non-small cell lung cancer (NSCLC).

What are the uses of this medicine?

Ceritinib (Zykadia) is used to treat people with non-small cell lung cancer (NSCLC) that:

• is caused by a defect in a gene called anaplastic lymphoma kinase (ALK), and
• has spread to other parts of the body

How does this medicine work?

• Ceritinib (se ri' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against anaplastic lymphoma kinase (ALK) that is rearranged and mutated in selected cancers including approximately 5% of non-small cell lung cancer (NSCLC). The mutated, rearranged ALK promotes unregulated cell growth and proliferation and is overexpressed in some cancer cells.
• Ceritinib has been found to inhibit mutated ALK in cell culture and in several clinical trials was found to induce objective responses in a proportion of patients with advanced ALK-positive NSCLC.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Avoid concurrent use of Zykadia with strong CYP3A inhibitors(eg: ketoconazole) or inducers(eg: rifampin). If concurrent use of a strong CYP3A inhibitor is unavoidable, dose reduce Zykadia.
• Avoid coadministration of Zykadia with sensitive CYP3A substrates(eg: midazolam).
• Avoid coadministration of Zykadia with CYP2C9 substrates(eg: warfarin) for which minimal concentration changes may lead to serious toxicities.
• Avoid coadministration of Zykadia with other products with a known potential to prolong the QTc interval.
• Avoid coadministration of Zykadia with other products known to cause bradycardia.

Is this medicine FDA approved?

• Ceritinib received accelerated approval for use crizotinib-refractory, ALK-positive NSCLC in the United States in 2014.

How should this medicine be used?

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

Recommended Dosage:

• The recommended dosage of Zykadia is 450 mg orally once daily with food until disease progression or unacceptable toxicity.

Dosage Modification for Strong CYP3A Inhibitors

• Avoid concurrent use of strong CYP3A inhibitors during treatment with Zykadia
• If concurrent use of a strong CYP3A inhibitor is unavoidable, reduce the Zykadia dose by approximately one-third, rounded to the nearest multiple of the 150 mg dosage strength.

Dosage Modification for Patients With Severe Hepatic Impairment

• For patients with severe hepatic impairment (Child-Pugh C), reduce the Zykadia dose by approximately one-third, rounded to the nearest multiple of the 150 mg dosage strength.

Administration

• Take Zykadia exactly as your healthcare provider tells you. Do not change your dose or stop taking Zykadia unless your healthcare provider tells you to.
• Take Zykadia one time a day.
• Take Zykadia with food.
• If you vomit after taking Zykadia, do not take an additional dose. Continue with the next scheduled dose.
• If you miss a dose of Zykadia, take it as soon as you remember. If your next dose is due within 12 hours, then skip the missed dose. Just take the next dose at your regular time.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 150 mg
• Tablets: 150 mg

This medicine is available in fallowing brand namesː

• Zykadia

What side effects can this medication cause?

The most common side effects of this medicine include:

• stomach and intestinal (gastrointestinal) problems.
• tiredness, decreased appetite, and weight loss

Zykadia may cause serious side effects, including:

• Stomach and intestinal (gastrointestinal) problems
• Liver problems
• High blood sugar (hyperglycemia)
• Inflammation of the pancreas (pancreatitis)

What special precautions should I follow?

• You should not drink grapefruit juice or eat grapefruit during treatment with Zykadia. It may make the amount of Zykadia in your blood increase to a harmful level.
• Zykadia can cause gastrointestinal adverse reactions. If severe or intolerable, withhold if not responsive to antiemetics or antidiarrheals; upon improvement, resume Zykadia at a reduced dose.
• Zykadia can cause hepatotoxicity. Monitor liver laboratory tests at least monthly. Withhold then dose reduce, or permanently discontinue Zykadia.
• Severe, life-threatening, or fatal interstitial lung diseases (ILD)/pneumonitis occurred in patients treated with Zykadia. Permanently discontinue Zykadia in patients diagnosed with treatment-related interstitial lung disease (ILD)/pneumonitis.
• Zykadia can cause QTc interval prolongation. Monitor electrocardiograms and electrolytes in patients with congestive heart failure, bradyarrhythmias, electrolyte abnormalities, or those who are taking medications that are known to prolong the QTc interval. Withhold then dose reduce, or permanently discontinue Zykadia.
• Zykadia can cause hyperglycemia. Monitor fasting glucose prior to treatment and periodically thereafter. Initiate or optimize anti-hyperglycemic medications as indicated. Withhold, then dose reduce, or permanently discontinue Zykadia.
• Zykadia can cause bradycardia. Monitor heart rate and blood pressure regularly. Withhold, then dose reduce, or permanently discontinue Zykadia.
• Elevations of lipase and/or amylase and pancreatitis can occur. Monitor lipase and amylase prior to treatment and periodically thereafter as clinically indicated. Withhold, then dose reduce Zykadia.
• Zykadia can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

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

Can this medicine be used in children?

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

What are the active and inactive ingredients in this medicine?

• Active ingredient: ceritinib
• Inactive ingredients capsules: colloidal silicon dioxide, low-substituted hydroxypropyl cellulose, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate. Capsule shell contains FD&C Blue # 2, gelatin, and titanium dioxide.
• Inactive ingredients tablets:
• Tablet core: colloidal silicon dioxide, croscarmellose sodium, low-substituted hydroxypropyl cellulose, magnesium stearate, microcrystalline cellulose and povidone. Tablet coating: FD&C Blue # 2 aluminum lake, hypromellose, polyethylene glycol 4000, talc, and titanium dioxide.

Who manufactures and distributes this medicine?

• Distributed by: Novartis Pharmaceuticals Corporation, East Hanover, New Jersey

What should I know about storage and disposal of this medication?

• Store Zykadia at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep Zykadia and all medicines out of the reach of children.

• Dailymed label info on Ceritinib
• FDA Ceritinib

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