Ceritinib

Ceritinib is a prescription medication used to treat non-small cell lung cancer (NSCLC).

Ceritinib belongs to a group of drugs called anaplastic lymphoma kinase (ALK) inhibitor. These work by blocking proteins that promote the development of cancerous cells.

This medication comes in capsule form and is taken once a day, without food.

Common side effects of ceritinib include diarrhea, nausea, vomiting, and abdominal pain.

Ceritinib can also cause blurred vision. Do not drive or operate heavy machinery until you know how ceritinib affects you.

Lung cancer is cancer that forms in the cells of the lungs. Some patients have ALK-positive lung cancer. ALK is a protein that is involved in the division of cells, including cancer cells. Some patients have a change (or mutation) in the ALK protein that causes cancer cells to divide more rapidly.

ALK testing is done to see whether treatment with ceritinib is likely to be effective. If testing is not done, treatment with ceritinib is not likely to be effective.

Ceritinib is approved for the treatment of ALK-positive metastatic non-small cell lung cancer (NSCLC) in patients in whom cancer has progressed or is resistant to treatment with crizotinib. It is specifically designed to target the ALK protein. By binding to the ALK protein, ceritinib prevents the growth of cancer cells.

Ceritinib is a prescription medication 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 (advanced), and
• who have taken the medicine crizotinib, but their NSCLC worsened or they cannot tolerate taking crizotinib

This medication treats tumors that are anaplastic lymphoma kinase (ALK)-positive which is detected by an FDA-approved test. 

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Ceritinib may be found in some form under the following brand names:

• Zykadia

Serious side effects have been reported with ceritinib. See the “Ceritinib Precautions” section.

• diarrhea
• nausea
• vomiting
• constipation
• abdominal pain
• fatigue
• decreased appetite
• elevated liver enzymes

This is not a complete list of ceritinib side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• medications that block a protein in the body (CYPA4) such as some macrolide antibiotics (clarithromycin, telithromycin), some HIV protease inhibitors (indinavir, nelfinavir, ritonavir, saquinavir), some HCV protease inhibitors (boceprevir, telaprevir), some azole antifungals (ketoconazole, itraconazole, posaconazole, voriconazole), conivaptan (Vaprisol), delavirdine (Rescriptor), and nefazodone
• medications that increase the activity of the enzyme CYP3A4 such as carbamazepine (Tegretol, Equetro, Carbatrol), phenobarbital, phenytoin (Dilantin), rifampin (Rifadin), St John's wort, and nimodipine (Nimotop)
• medications that use the enzyme CYP3A4 such as alfentanil (Alfenta), cyclosporine (Neoral, Gengraf, Sandimmune), dihydroergotamine (Migranal), ergotamine (Cafergot), fentanyl (Abstral, Fentora, Onsolis, Actiq), pimozide (Orap), quinidine (Cardioquin, Duraquin, Quinact), sirolimus (Rapamune), and tacrolimus (Prograf).
• medications that use the enzyme CYP2C9 such as phenytoin (Dilantin) and warfarin (Coumadin, Jantoven).

This is not a complete list of ceritinib drug interactions. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with ceritinib including the following:

• Stomach and intestinal (gastrointestinal) problems. Ceritinib causes stomach and intestinal problems in most people, including diarrhea, nausea, vomiting, and stomach-area pain. These problems can sometimes be severe. Follow your healthcare provider’s instructions about taking medicines to help these symptoms. Call your healthcare provider for advice if your symptoms are severe or do not go away.

Ceritinib can cause drowsiness. Do not drive or operate heavy machinery until you know how ceritinib affects you.

Do not take ceritinib if you are allergic to ceritinib or to any of its ingredients.

Grapefruit and grapefruit juice may interact with ceritinib and may make the amount of ceritinib in your blood increase to a harmful level. This can lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Before taking ceritinib, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to ceritinib or to any of its ingredients
• have liver problems

• have diabetes or high blood sugar
• have heart problems, including a condition called long QT syndrome
• are pregnant or plan to become pregnant. Ceritinib may harm your unborn baby. Women who are able to become pregnant should use an effective method of birth control during treatment with ceritinib and for at least 2 weeks after stopping ceritinib. Talk to your healthcare provider about birth control methods that may be right for you.
• are breastfeeding or plan to breastfeed. It is not known if ceritinib passes into your breast milk. You should not breastfeed if you take ceritinib.

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Ceritinib falls into category D. In animal studies, pregnant animals were given this medication and had some babies born with problems.

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if ceritinib crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using ceritinib.

Take ceritinib exactly as prescribed.

Ceritinib comes in capsule form and is taken once every day. Take on an empty stomach. Do not eat for 2 hours before and do not eat for 2hours after taking Ceritinib.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses of ceritinib at the same time.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

• other medications you are taking
• certain side effects

The recommended dose of ceritinib for the treatment of non-small cell lung cancer is 750 mg once daily.

If you take too much ceritinib, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

• Store ceritinib at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep this and all medicines out of the reach of children.
• Patients can take anti-emetic and anti-diarrheal medications if they experience nausea and diarrhea. Advise patients to contact their healthcare provider for severe or stomach/intestine symptoms that do not stop.