Ceritinib – Oral

Ceritinib is an antineoplastic agent that works by destroying and preventing the growth of cancerous cells.

Overview

Ceritinib is a prescription only-drug that is used to treat patients with metastatic non-small cell lung cancer.

Metastatic cancer is cancer that has already spread to other parts of the body. Non-small cell lung cancer forms when there is a defect in the gene named anaplastic lymphoma kinase. Lung cancer is cancer that starts in the trachea, the lung tissue or the bronchus. This type of cancer is formed in any part of the airways or lungs (the body’s breathing system).

Lung cancer is the third most common type of cancer in the United States. Around four in ten cases of lung cancer are in people over the age of 75. It is prevalent in both men and women and can be triggered by a range of lifestyle factors. At least 80% of cases of lung cancer take place in patients that smoke. However, the disease can also be caused by other factors, such as exposure to chemicals in the workplace, exposure to radon gas, a family history of lung cancer or other lung diseases, as well as a weak immune system.

Non-small cell lung cancer is one of two types of lung cancer and is the most common form. It is divided into three types: adenocarcinoma, squamous cell carcinoma and large cell carcinoma.

Ceritinib is usually given to patients who have already been given a medication called crizotinib, but have found that that medication was not tolerated by the body, or their condition has since worsened. It works by affecting the growth of cancerous cells, helping the body to destroy them. It is part of a family of drugs called the antineoplastic (cancer) agents.

The drug is also marketed and sold under its brand name Zykadia in the United States.

Condition(s) treated

  • metastatic non-small cell lung cancer

Type of medication

  • tablet, to be take orally

Side effects

Ceritinib is a form of chemotherapy and a a very strong type of medication. Therefore, patients are likely to experience various side effects. Most of these are considered a normal consequence of the treatment and are, therefore, nothing to worry about. They may, however, be particularly unpleasant to deal with, so other medications may be taken to help ease the symptoms.

Patients may not experience all of the side effects below; however, these are common, experienced by more than 30% of patients:

  • Diarrhea
  • Reduction in hemoglobin
  • Abdominal pain
  • Increase in liver enzymes
  • Nausea
  • Vomiting
  • Increase in creatinine
  • Fatigue or drowsiness
  • Increase in glucose levels
  • Decrease in phosphate
  • Poor appetite

Less common side effects include those listed below, which have been recorded in around 10% to 29% of patients. You should call your doctor for advice if any of these become persistent or severe:

  • Constipation
  • Increase in lipase levels in the body
  • Esophageal disorder (heart burn, dyspepsia, dysphagia)
  • Rash on any area of the skin, or spots, hives, or itchiness
  • Increase in bilirubin levels

Dosage

Ceritinib capsules come in a strength of 150 mg. The usual dosage for adults is 750 mg taken orally, once a day, on empty stomach. This should be taken as five capsules.

This dosage is a long term treatment that can continue until the disease had progressed or the drug has reached unacceptable toxicity levels. In either case, an alternative treatment may be available to the patient.

If the patient is found to be intolerant to the drug, the dosage can be reduced in the following increments:

  • First reduction: 600 mg, once a day
  • Second reduction: 450 mg, once a day
  • Third reduction: 300 mg, once a day

If the patient is unable to tolerate the minimum dosage of 300 mg per day, the treatment should be discontinued.

Major drug interactions

There are various drugs that you should not take while taking ceritinib. This is because some substances can cause a reaction when taken at the same time, known as a drug interaction. There are three levels of drug interactions - minor, moderate and major. Those that have a minor reaction may still be taken at the same time; however, the dosage given to you may be altered as a result. You may also need to monitor closely for any unusual side effects while taking the combination. Moderate interactions should be avoided in the vast majority of cases, unless your doctor sees no other viable alternative. Major drug interactions should be avoided at all times, as the consequences of taking these drugs together are potentially dangerous and can make your conditions worse.

There are a large number of drugs that have been found to have a reaction of some level with this ceritinib. You should, therefore, always tell your doctor your full medical history and any drugs that you are taking now or have taken in the past. Major interactions with ceritinib include:

  • abarelix
  • acetaminophen, propoxyphene
  • adenosine
  • alfuzosin
  • aminophylline, ephedrine, guaifenesin, phenobarbital
  • aminophylline, ephedrine, phenobarbital, potassium iodide
  • amiodarone
  • amitriptyline
  • amitriptyline, chlordiazepoxide
  • amitriptyline, perphenazine
  • amoxapine
  • amoxicillin, clarithromycin, lansoprazole
  • amoxicillin, clarithromycin, omeprazole
  • amprenavir
  • anagrelide
  • anhydrous calcium iodide, isoproterenol
  • apomorphine
  • arsenic trioxide
  • artemether, lumefantrine
  • asenapine
  • aspirin, caffeine, propoxyphene
  • astemizole
  • atazanavir
  • atazanavir, cobicistat
  • atomoxetine
  • atropine, hyoscyamine, phenobarbital, scopolamine
  • atropine, phenobarbital
  • azithromycin
  • azithromycin, trovafloxacin
  • bedaquiline
  • belladonna, ergotamine, phenobarbital
  • bepridil
  • boceprevir
  • bosutinib
  • bupivacaine, fentanyl
  • buprenorphine
  • buprenorphine, naloxone
  • carbamazepine
  • chloroquine
  • chlorpromazine
  • ciprofloxacin
  • cisapride
  • citalopram
  • clarithromycin
  • clofazimine
  • clomipramine
  • clozapine
  • cobicistat
  • cobicistat, darunavir
  • codeine, phenylephrine, promethazine
  • codeine, promethazine
  • colchicine
  • colchicine, probenecid
  • conivaptan
  • crizotinib
  • cytarabine liposomal, daunorubicin liposomal
  • dasabuvir, ombitasvir, paritaprevir, ritonavir
  • dasatinib
  • daunorubicin
  • daunorubicin liposomal
  • degarelix
  • delavirdine
  • desipramine
  • deutetrabenazine
  • dextromethorphan, promethazine
  • dextromethorphan, quinidine
  • disopyramide
  • dofetilide
  • dolasetron
  • doxepin
  • doxepin topical
  • doxorubicin
  • doxorubicin liposomal
  • dronedarone
  • droperidol
  • droperidol, fentanyl
  • dyphylline, ephedrine, guaifenesin, phenobarbital
  • efavirenz
  • efavirenz, emtricitabine, tenofovir
  • emtricitabine, lopinavir, ritonavir, tenofovir
  • emtricitabine, nelfinavir, tenofovir
  • enzalutamide
  • ephedrine, hydroxyzine, theophylline
  • ephedrine, phenobarbital, potassium iodide, theophylline
  • ephedrine, phenobarbital, theophylline
  • epirubicin
  • eribulin
  • erythromycin
  • erythromycin, sulfisoxazole
  • escitalopram
  • ezogabine
  • fentanyl
  • fentanyl, ropivacaine
  • fingolimod
  • flecainide
  • fluconazole
  • fluoxetine
  • fluoxetine, olanzapine
  • fluphenazine
  • fosamprenavir
  • fosphenytoin
  • gatifloxacin
  • gemifloxacin
  • goserelin
  • granisetron
  • grepafloxacin
  • halofantrine
  • haloperidol
  • halothane
  • histrelin
  • hydroxychloroquine
  • telaprevir
  • hydroxyzine
  • hyoscyamine, phenobarbital
  • ibutilide
  • idarubicin
  • idelalisib
  • iloperidone
  • imipramine
  • indinavir
  • inotuzumab ozogamicin
  • isoniazid, pyrazinamide, rifampin
  • isoniazid, rifampin
  • isoproterenol
  • isoproterenol, phenylephrine
  • itraconazole
  • ivabradine
  • ivacaftor, lumacaftor
  • ketoconazole
  • lapatinib
  • leflunomide
  • lenvatinib
  • letrozole, ribociclib
  • leuprolide
  • leuprolide, norethindrone
  • levofloxacin
  • levomethadyl acetate
  • lithium
  • lomefloxacin
  • lomitapide
  • lopinavir, ritonavir
  • maprotiline
  • mefloquine
  • meperidine, promethazine
  • mesoridazine
  • metaproterenol
  • methadone
  • methotrimeprazine
  • mibefradil
  • midostaurin
  • trifluoperazine
  • mifepristone
  • mipomersen
  • mirtazapine
  • mitotane
  • moxifloxacin
  • nefazodone
  • terbutaline
  • nelfinavir
  • netupitant, palonosetron
  • nilotinib
  • norfloxacin
  • nortriptyline
  • ofloxacin
  • ombitasvir, paritaprevir, ritonavir
  • ondansetron
  • osimertinib
  • oxaliplatin
  • paliperidone
  • palonosetron
  • panobinostat
  • papaverine
  • pasireotide
  • pazopanib
  • pentamidine
  • perflutren
  • perphenazine
  • phenobarbital
  • phenylephrine, promethazine
  • phenytoin
  • pimavanserin
  • pimozide
  • posaconazole
  • telavancin
  • primidone
  • probucol
  • procainamide
  • tamoxifen
  • prochlorperazine
  • sparfloxacin
  • promazine
  • promethazine
  • propafenone
  • propoxyphene
  • protriptyline
  • pseudoephedrine, terfenadine
  • quetiapine
  • quinidine
  • quinine
  • terfenadine
  • tizanidine
  • ranolazine
  • ribociclib
  • teriflunomide
  • rifampin
  • rilpivirine
  • risperidone
  • sevoflurane
  • st. john's wort
  • sotalol
  • ritodrine
  • tacrolimus
  • ritonavir
  • romidepsin
  • saquinavir
  • sertraline
  • sunitinib
  • solifenacin
  • telithromycin
  • trazodone
  • triflupromazine
  • toremifene
  • tetrabenazine
  • thioridazine
  • trimipramine
  • triptorelin
  • troleandomycin
  • valbenazine
  • vandetanib
  • vardenafil
  • vasopressin
  • vemurafenib
  • venlafaxine
  • voriconazole
  • sorafenib
  • ziprasidone

Warnings

Food interactions

If you are taking ceritinib, you should avoid consuming grapefruit throughout your treatment. Eating grapefruit can increase the levels of ceritinib in the blood, leading to symptoms that are similar to those of overdosing. Levels can become dangerous, so if you think you may be experiencing unpleasant side effects as a result of eating grapefruit while taking ceritinib, you should contact your doctor for advice immediately. Particularly dangerous side effects include an irregular heartbeat. Other side effects include nausea, vomiting, diarrhea, pain in the stomach and high blood sugar levels. Rarer symptoms, such as faintness, lightheadedness, heart palpitations or a difficulty catching a breath, should be reported immediately.

Doses and food

You should always take ceritinib on an empty stomach. This is because food in general can also increase the levels of ceritinib in the body, sometimes increasing then to dangerous levels. Always leave at least two hours either side of taking your daily dose of ceritinib.

Vitamins and herbs

Always tell your doctor if you are taking any vitamin or herb supplements. This is because vitamins and herbs can, in some cases, interfere with the drug in your system or increase the levels of ceritinib in your body.

Disease interactions

Just as there are other drugs or foods that can cause a reaction with ceritinib, there are other diseases and conditions that can interfere with your medication. You should always consult your doctor about your medical history, including telling them about any other conditions or diseases that you may suffer from. Some conditions can actually interfere with the impact of ceritinib on the body, making it less effective. Equally, certinib may aggravate any other conditions you have, in some cases making them worse. There are eight serious disease interactions with ceritinib. These are:

  • Qt prolongation
  • Bradycardia
  • Gi complications
  • Hepatic impairment
  • Hyperglycemia
  • Pancreatitis
  • Renal impairment
  • Lung toxicity

Do not take ceritinib if you suffer from any of these conditions.

Pneumonitis

Pneumonitis (swelling of the lungs) is a very uncommon but serious side effect that patients can experience as a result of taking ceritinib. Symptoms of this condition include difficulty breathing, cough and fever. Symptoms can also be similar to those that have been suffered as a result of the original lung cancer.

Storage

Ceritinib is a very strong medication that is strictly intended for the recipient only. Therefore, patients should take all necessary precautions to ensure that the drugs do not get into the wrong hands - particularly those of children. Ceritinib should be kept in its original packaging at all times, where it will remain clearly labelled. This will prevent it from becoming mixed up with other drugs and being wrongfully consumed.

You should also ensure that your drugs are kept at room temperature - meaning around 20 to 25 degrees Celcius at all times. Do not refrigerate or freeze your drugs at any time. Doing so may impact their effectiveness. You must also not store your ceritinib prescription in direct heat or light.

Also, make sure you keep your prescription in a dry area, away from damp conditions, such as those often found in bathrooms.

Disposal

You should not consume ceritinib once it goes of date. If you discover that your drugs have exceeded their expiry date, you should throw them away. Medication needs to be disposed of in a safe and responsible way; do not attempt to just flush your medication down the toilet or a drain, unless your doctor has specifically told you to do so. Instead, take your capsules out of their wrapping and place them in a waterproof sealable plastic bag. Then mix the tablets with some inedible substance, such as cat litter, soil, dirt or used coffee beans. This will reduce the risk of the mixture being consumed. Then, you should seal the bag fully and place it in the regular trash can for collection.

An even better and more effective way to dispose of unwanted or unused medication safely is to use one of your local take back schemes. These schemes are organized by the FDA and are designed to offer a safe way to get rid of and recycle old medicines. You can find out where your nearest take back schemes are by visiting the FDA's website. If there are no schemes available, you should follow the instructions on the FDA website regarding medicine disposal.

Summary

Ceritinib has been found to be a very effective drug at treating non small cell lung cancer, which is by far the most common type of lung cancer. It can become a long term treatment for the disease, with patients able to take it until it stops working and their condition becomes worse or their bodies become unable to tolerate the drug any longer.

This medication offers a significant improvement in prognosis for those that are suffering with non-small cell lung cancer when it has spread to other parts of the body. Unfortunately, there is no cure for the disease at this stage; however, if the patient responds well, then ceritinib can help to manage the condition, preventing it from spreading further.

Patients must tell their doctors about any other medication that they are taking, due to the large number of drugs that have been reported to have a major interaction with this one. Some drugs can cause a very serious reaction when taken with ceritinib, and, therefore, need to be avoided.

As lung cancer is mainly caused by exposure to certain harmful substances, patients taking ceritinib will need to also make various lifestyle changes to help lessen the chances of their conditions worsening. This includes avoiding smoking; smoking cigarettes may rescue the time that a course of ceritinib will be effective for.

Instructions for taking ceritinib should be carefully followed at all times and it is important that patients only take the amount of the drug that is prescribed by a qualified doctor. Patients will be periodically monitored while taking this prescription. However, patients should also be mindful of side effects and report anything unusual or persistent to their doctors. There are other forms of treatment available for managing lung cancer that has spread to other parts of the body, so patients should not continue taking this if they think their bodies may have become intolerant of the medication.