Crizotinib (Oral)

Used to treat metastatic non-small cell lung cancer, Crizotinib inhibits the growth of cancer cells.

Overview

Although non-small cell lung cancer can be caused in various ways, Crizotinib is used to treat this type of lung cancer when it has been caused by a defect in either the anaplastic lymphoma kinase (ALK) gene or the ROS1 gene. Normally used to treat cancer which has become metastatic, Crizotinib is offered to patients if their cancer has spread.

As a tyrosine kinase inhibitor, Crizotinib affects the way cancer cells grow. If patients have cancer cells which contain an overactive form of anaplastic lymphoma kinase, Crizotinib blocks the enzyme which causes the cells to grow, divide and replicate. By preventing this from happening, Crizotinib prevents further spread of the disease and enables the body to destroy the harmful cells which are already present.

Although Crizotinib is not suitable for all cancer patients, it can be effective for some patients with advanced forms of metastatic non-small cell lung cancer.

Conditions Treated:

  • Metastatic non-small cell lung cancer caused by the ALK or ROS1 genes.

Type of Medicine:

  • Oral tyrosine kinase inhibitor
  • Antineoplastic

Side Effects:

Similar to many antineoplastic drugs, Crizotinib can cause some side effects. The following effects have been noted in some patients who have been treated with this medication:

  • Stomach and abdominal pain or discomfort
  • Sour or acid feeling in stomach
  • Pain in back
  • Belching
  • Change or decrease in vision
  • Changes to taste
  • Stomach and abdominal tenderness
  • Reduced appetite
  • Diarrhea
  • Heartburn
  • Indigestion
  • Difficulty having a bowel movement (stool)
  • Increased sensitivity of the eyes to sunlight
  • Difficulty moving
  • Muscle stiffness and/or pain
  • Difficulty swallowing
  • Nausea
  • Burning and/or pain in the throat
  • Difficulty getting to sleep
  • Trouble staying asleep
  • Joint pain
  • Inflammation and/or swelling of the mouth
  • Discomfort or pain in the upper stomach, throat and/or chest
  • Problems with balance
  • Soreness, swelling and/or redness of the tongue
  • Seeing sparks of lights or flashes
  • Rash on the skin
  • Burning, scaling, pain, chapping, redness, inflammation and/or swelling of the lips

Although these side effects can be unpleasant, they do not necessarily mean that the treatment is failing. Anti-cancer medications, such as Crizotinib, are used to target cancer cells but they can temporarily affect healthy cells too. Although this is necessary in order for the medication to work, it can result in patients experiencing some side effects when they're taking the drug.

In most instances, the side effects listed above will diminish over time and may not need medical intervention. However, if patients are concerned about side effects when taking Crizotinib or if their side effects are severe and persistent, they should not hesitate to seek medical help.

If patients experience any of the following side effects when taking Crizotinib, they are normally advised to seek medical advice:

  • Tarry, black stools
  • Swelling and/or bloating of the arms, face, hands, feet and/or lower legs
  • Pain or body aches
  • Numbness, itching, crawling, tingling, Ĺ“pins and needle and/or prickling feelings
  • Pain or discomfort in the chest
  • Ear congestion
  • Trouble with breathing
  • Hoarseness
  • Labored or difficult breathing
  • Coughing
  • Sneezing
  • Chills and/or fever
  • Increased sensitivity to touch and/or pain
  • Headache
  • Fainting, dizziness or lightheadedness
  • Pale skin
  • Loss of voice
  • Pain in side or lower back
  • Difficulty urinating
  • Nerve pain
  • Rapid increase in weight
  • Painful urination
  • Stuffy and/or runny nose
  • Irregular or slow heartbeat
  • Sore throat
  • Unusual bruising or bleeding
  • White spots, sores and/or ulcers in the mouth
  • Awkwardness and/or unsteadiness
  • Weakness in the hands, arms, feet and/or legs
  • Tightness in chest
  • Bleeding gums
  • Unusual weakness or tiredness
  • Blood in the stools or urine
  • Unusual weight gain or loss
  • Pinpoint spots on the skin which may be red in color

Whilst the above symptoms may not prevent treatment with Crizotinib from continuing, they should be assessed by a medical professional. If necessary, doctors may be able to prescribe additional medications to minimize the patient's side effects.

Dosage:

When patients are taking Crizotinib, they should follow their doctor's instruction exactly. Their dose will depend on the strength of the medication they are prescribed, along with their clinical presentation, age, medical history, and weight.

A standard dose of Crizotinib for the treatment of non-small cell lung cancer may be 250mg twice per day, but this could change depending on the patient's needs.

Generally, patients can take their dose of Crizotinib with or without food, unless they are advised otherwise. Patients should not crush, open or break the capsule when taking Crizotinib. Instead, the capsule should be swallowed whole with water.

If patients accidentally miss a dose of Crizotinib, they should take it once they remember. However, if patients have missed a dose and their next dose of Crizotinib is due within 6 hours, they should skip the missed dose and continue with their normal dosing schedule.

If patients vomit after taking Crizotinib, they should take their next dose at the regular time. They should notify their physician if this is a common occurrence.

Patients should not attempt to take double doses of Crizotinib, even if they have missed a dose of their medication. If patients are unsure how to take Crizotinib or how to proceed after missing a dose, they should seek medical advice from their pharmacist or doctor.

Potential Drug Interactions:

When patients are taking numerous medications, there is a chance that the active ingredients could interact with each other. In some cases, this could be dangerous, so certain drugs are not usually prescribed in conjunction with one another.

If patients are taking any of the following medications, physicians may choose not to treat them with Crizotinib or to change their existing treatment:

  • Amifampridine
  • Cobicistat
  • Amisulpride
  • Bepridil
  • Atazanavir
  • Ketoconazole
  • Boceprevir
  • Pimozide
  • Cisapride
  • Ziprasidone
  • Dronedarone
  • Thioridazine
  • Fluconazole
  • Terfenadine
  • Lopinavir
  • Saquinavir
  • Mesoridazine
  • Sparfloxacin
  • Nelfinavir
  • Posaconazole
  • Piperaquine
  • Ritonavir

Although Crizotinib should not usually be prescribed at the same time as the following medications, it may be necessary in some cases. If Crizotinib is given to the patient alongside any of the following medications, doctors may alter their dose or advise them to take their medications at specific times to lower the risk of them interacting:

  • Acebutolol
  • Bedaquiline
  • Alfentanil
  • Bisoprolol
  • Alfuzosin
  • Betaxolol
  • Amiodarone
  • Buserelin
  • Amitriptyline
  • Carbamazepine
  • Amprenavir
  • Carvedilol
  • Anagrelide
  • Carteolol
  • Apomorphine
  • Celiprolol
  • Aripiprazole
  • Chlorpromazine
  • Arsenic Trioxide
  • Ceritinib
  • Artemether
  • Chloroquine
  • Asenapine
  • Cilostazol
  • Astemizole
  • Clarithromycin
  • Atenolol
  • Citalopram
  • Azithromycin
  • Ciprofloxacin
  • Ebastine
  • Clomipramine
  • Droperidol
  • Clonidine
  • Eletriptan
  • Clozapine
  • Dabrafenib
  • Conivaptan
  • Digoxin
  • Cyclobenzaprine
  • Delamanid
  • Cyclosporine
  • Dasatinib
  • Efavirenz
  • Degarelix
  • Eliglustat
  • Delavirdine
  • Erythromycin
  • Desipramine
  • Escitalopram
  • Deslorelin
  • Famotidine
  • Dihydroergotamine
  • Flecainide
  • Diltiazem
  • Fingolimod
  • Disopyramide
  • Fluoxetine
  • Dofetilide
  • Fosamprenavir
  • Dolasetron
  • Esmolol
  • Domperidone
  • Foscarnet
  • Donepezil
  • Felbamate
  • Doxepin
  • Ergotamine
  • Doxorubicin
  • Fosphenytoin
  • Doxorubicin Hydrochloride Liposome
  • Enzalutamide
  • Eribulin
  • Galantamine
  • Lapatinib
  • Gatifloxacin
  • Halofantrine
  • Gemifloxacin
  • Histrelin
  • Gonadorelin
  • Hydroxychloroquine
  • Goserelin
  • Ibutilide
  • Granisetron
  • Haloperidol
  • Hydroquinidine
  • Hydroxyzine
  • Idelalisib
  • Labetalol
  • Ifosfamide
  • Levobunolol
  • Iloperidone
  • Mefloquine
  • Imipramine
  • Lumefantrine
  • Indinavir
  • Lurasidone
  • Itraconazole
  • Levofloxacin
  • Ivabradine
  • Nadolol
  • Ivacaftor
  • Leuprolide
  • Metipranolol
  • Methadone
  • Nafarelin
  • Metoprolol
  • Nebivolol
  • Metronidazole
  • Nilotinib
  • Mifepristone
  • Norfloxacin
  • Mizolastine
  • Octreotide
  • Moxifloxacin
  • Olanzapine
  • Naloxegol
  • Ofloxacin
  • Nefazodone
  • Ondansetron
  • Nortriptyline
  • Olaparib
  • Oxprenolol
  • Quinidine
  • Paclitaxel
  • Quetiapine
  • Paliperidone
  • Quinine
  • Panobinostat
  • Sirolimus
  • Paroxetine
  • Simeprevir
  • Pasireotide
  • Sertindole
  • Pazopanib
  • Ranolazine
  • Penbutolol
  • Rilpivirine
  • Pentamidine
  • Rifampin
  • Perflutren Lipid Microsphere
  • Sevoflurane
  • Rifabutin
  • Perhexiline
  • Risperidone
  • Perphenazine
  • Sodium Phosphate, Monobasic
  • Phenytoin
  • Sodium Phosphate
  • Pimavanserin
  • Sodium Phosphate, Dibasic
  • Pindolol
  • Solifenacin
  • Pitolisant
  • Sunitinib
  • Practolol
  • St John's Wort
  • Triptorelin
  • Probucol
  • Sulpiride
  • Procainamide
  • Telithromycin
  • Prochlorperazine
  • Telavancin
  • Promethazine
  • Tamoxifen
  • Propafenone
  • Sorafenib
  • Propranolol
  • Terodiline
  • Protriptyline
  • Sotalol
  • Tacrolimus
  • Vemurafenib
  • Troleandomycin
  • Tetrabenazine
  • Venlafaxine
  • Timolol
  • Vilanterol
  • Verapamil
  • Tizanidine
  • Vardenafil
  • Tolterodine
  • Vandetanib
  • Tolvaptan
  • Vinflunine
  • Toremifene
  • Voriconazole
  • Trazodone
  • Vorinostat
  • Trifluoperazine
  • Zuclopenthixol
  • Trimipramine

Similarly, taking Crizotinib at the same time as Midazolam may increase the chance of side effects occurring. If the two medicines need to be prescribed together, doctors may prescribe specific instructions to reduce the risk of the patient suffering adverse effects. Alternatively, they may prescribe extra medication to treat any side-effects which happen to occur.

As well as interacting with prescribed medicines, Crizotinib could interact with over-the-counter medicines and/or vitamins and supplements. Patients should inform their physician if they regularly take these substances. In addition to this, patients should seek medical advice before using any other substances when also taking Crizotinib.

As Crizotinib can also interact with grapefruit juice, patients should not consume grapefruits, grapefruit juice or any grapefruit derivatives when taking this medication. Grapefruit can affect the way that Crizotinib is metabolized and may result in the patient absorbing the incorrect amount of medication or it may lead to an increase of side-effects occurring.

Warnings:

Before beginning treatment with Crizotinib, patients should disclose their medical history to their physician. Certain conditions may affect the use of Crizotinib when treating metastatic non-small cell lung cancer. These may include:

  • Liver Disease
  • Bradycardia (Slow heartbeat)
  • Kidney Disease
  • Congenital long QT syndrome
  • QT prolongation
  • Mineral or electrolyte imbalance
  • Congestive heart failure

Taking Crizotinib when pregnant can cause harm to the unborn baby. Due to this, patients will not normally be treated with Crizotinib if they are pregnant. Similarly, fathering a child while taking Crizotinib may cause the infant to develop birth defects. Male patients should advise their sexual partner of these risks and ensure that appropriate and effective birth control is used during and after treatment.

Crizotinib may remain in the patient's system for some time after their last dose of medicine. Patients should, therefore, use an effective form of contraceptive whilst taking Crizotinib and for at least 45-90 days after their last dose of medication.

If a patient becomes pregnant whilst taking Crizotinib, they should seek immediate medical advice. Similarly, if a patient impregnates their sexual partner whilst taking Crizotinib, they should contact their doctor for medical advice immediately.

Crizotinib can affect the fertility of both male and female patients. In some instances, patients may become infertile after receiving treatment with Crizotinib. If patients are planning to have children in the future, this is something they should discuss with their physician before taking Crizotinib.

Due to the risks posed to the infant, patients should not breastfeed whilst taking Crizotinib. In addition to this, patients should refrain from breastfeeding for at least 45-90 days after their last dose of medication. Patients should discuss the risks with their doctor and seek advice before starting to breastfeed after receiving treatment with Crizotinib.

In some cases, Crizotinib may cause patients to suffer from swelling of the lungs. Also known as pneumonitis, this condition can be life-threatening. Symptoms may include trouble breathing, shortness of breath, cough with or without mucous and/or a fever. If patients experience any of these symptoms or suspect they are suffering from pneumonitis, they must seek immediate medical help.

If patients are unable to process medication normally, they may develop liver problems. If patients experience tenderness or pain in the upper stomach, nausea, loss of appetite, dark urine, pale stools, weakness, tiredness and/or yellowing of the skin or eyes, they may be developing liver problems. If so, patients should seek immediate medical advice. If patients are unable to process Crizotinib normally, the drug is likely to build up in their system. As well as causing increased side-effects, this could be harmful to the patient if it is left untreated.

When using Crizotinib, patients may be at risk of developing heart problems. If the patient notices any changes to their heart rhythm, they should notify their doctor immediately. In addition to this, patients should seek medical help if they suffer from faintness, dizziness, pounding heart, fast or slow heart rate and/or an uneven heartbeat. If patients have a family history of heart problems, they should inform their doctor before taking Crizotinib capsules.

Antineoplastic drugs, such as Crizotinib, can cause diarrhea, vomiting, nausea and/or constipation. If patients are taking additional medicines to combat these side effects but they are not working, they should contact their physician. Often, medications can be changed and doctors should be able to provide advice regarding the management of these side effects.

When taking Crizotinib, patients can experience excessive tiredness and blurred vision, in addition to other side effects. Patients should not drive, operate heavy machinery or carry out tasks which require their full attention if they are suffering from these side effects when taking Crizotinib.

If patients notice changes to their vision when taking Crizotinib, they should notify their physician. Patients may be advised to consult their ophthalmologist if they experience eye problems or changes to their vision when taking this medicine.

Patients should ensure their doctor is aware of any allergies they have before beginning treatment. If patients begin to develop a reaction to Crizotinib, they should seek urgent medical attention. Symptoms, such as itching, swelling of the face, throat and/or lips, difficulty breathing and/or wheezing, may indicate that the patient is allergic to this medication or one of its ingredients. As allergic reactions can be life-threatening, patients will need to access emergency assistance if a reaction occurs.

Storage

When patients are prescribed Crizotinib, they are normally instructed to take the medicine on a daily basis. This means that they will need to store their medication at home. When keeping medicine in the home, it's important that the patient identifies a secure and appropriate storage location. In addition to this, medicines should be kept out of reach of pets and/or children.

When storing Crizotinib, patients should follow the storage instructions on the medication's labelling or guide. In most instances, patients should keep Crizotinib capsules at room temperature and in a closed container. If Crizotinib capsules are packaged in blister packs, they should not be opened until the patient is ready to take them. Patients should also keep Crizotinib away from direct light, moisture and/or heat.

If patients are advised to stop taking Crizotinib, they will need to dispose of any excess medication carefully. In addition to this, patients should check the use-by date on their medicine and dispose of any capsules which are out-of-date.

When throwing medication out, patients should not use regular household waste facilities. Most clinics and pharmacists will take back unused medication so that it can be disposed of safely. Patients should liaise with their pharmacist or doctor's office to arrange for the safe disposal of any Crizotinib capsules which are no longer needed.

Summary

When non-small cell lung cancer has become metastatic, it means that the cancer cells have spread to other areas. This often means that patients require different treatment or a range of alternative medications.

If patients have developed non-small lung cancer because of a defect in the anaplastic lymphoma kinase (ALK) or ROS1 gene, Crizotinib may be a suitable treatment for them. Like most anti-cancer medications, Crizotinib is associated with a number of side effects but it does effectively target cancer cells.

Crizotinib will block the ALK enzyme and prevent cancer cells from spreading further. Once Crizotinib has damaged the cancer cells, the patient's body should have the opportunity to destroy them fully. Whilst patients may experience adverse effects during treatment, most individuals are prepared for this and accept that the risks associated with taking Crizotinib are often outweighed by the benefits.

When treatment is successful, Crizotinib can prevent metastatic non-small cell lung cancer from spreading further, enabling the body to destroy existing cells and halt the symptoms caused by the disease.