Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. It is used to treat locally advanced or metastatic non-small cell lung cancer for people in whom at least one other type of chemotherapy treatment has been unsuccessful or in cases where the lung cancer activates epidermal growth factor. It may also be used by people who have EGFR-positive tumours for maintenance therapy after successful standard chemotherapy.

It should not be used by people with EGFR-negative tumours. Epidermal growth factor receptor is a protein that is involved in the growth and spread of cancer cells; erlotinib works by preventing the action of this protein.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

The recommended daily dose of erlotinib is 150 mg taken once daily with a glass of plain water. Take this medication at least 1 hour before you eat, or at least 2 hours after you eat.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

Your doctor may want you to drink extra fluids while taking this medication in order to help you pass more fluid and protect your kidneys.

It is important to take this medication exactly as prescribed by your doctor. If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

25 mg
Each white-to-off-white, round, film-coated tablet, engraved "93" on one side and "E2" on the other side, contains 25 mg of erlotinib. Nonmedicinal ingredients: colloidal silicon dioxide, hydroxypropyl methylcellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polydextrose, polyethylene glycol, sodium lauryl sulphate, sodium starch glycolate, titanium dioxide and triacetin.

100 mg
Each white-to-off-white, round, film-coated tablet, engraved "93" on one side and "7663" on the other side, contains 100 mg of erlotinib. Nonmedicinal ingredients: colloidal silicon dioxide, hydroxypropyl methylcellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polydextrose, polyethylene glycol, sodium lauryl sulphate, sodium starch glycolate, titanium dioxide and triacetin.

150 mg
Each white-to-off-white, round, film-coated tablet, engraved "93" on one side and "7664" on the other side, contains 150 mg of erlotinib. Nonmedicinal ingredients: colloidal silicon dioxide, hydroxypropyl methylcellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polydextrose, polyethylene glycol, sodium lauryl sulphate, sodium starch glycolate, titanium dioxide and triacetin.

Do not take erlotinib if you are allergic to erlotinib or any ingredients of the medication.

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

• acne
• dizziness
• dry eyes
• dry skin
• headaches
• itching
• mouth sores
• nausea
• tiredness
• vomiting

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

• cough
• diarrhea
• difficulty breathing
• hair and nail changes (e.g., inflammation around fingernails)
• loss of appetite
• rash
• red, pink, irritated, or itchy eyes
• severe nausea or vomiting
• signs of infection (symptoms may include fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, weight loss, or listlessness)
• signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
• stomach pain

Stop taking the medication and seek immediate medical attention if any of the following occur:

• bleeding from the stomach or intestine (symptoms may include dark, tarry stools, blood in the stool, or coughing or vomiting up blood or material that looks like coffee grounds)
• signs of corneal perforation (e.g., eye pain, worsening vision, or loss of vision)
• signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
• signs of a severe skin reaction (e.g., blistering, peeling, a rash covering a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort)
• signs of intestinal perforation (e.g., fever or chills with severe abdominal pain, nausea or vomiting)
• sudden difficulty breathing, combined with cough or fever

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Before you begin taking a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should take this medication.

Corneal perforation: Rarely, erlotinib has been linked to corneal perforation, a severe injury to the part of the eye that focuses light into the eye. If you experience persistent eye pain or changes in vision, contact your doctor as soon as possible.

Dehydration: Severe dehydration can occur with the use of erlotinib. This may be due to severe or persistent diarrhea, vomiting, or decreased fluid intake. Dehydration can lead to low potassium levels in the blood and kidney failure, if it is severe enough. During treatment with erlotinib, you may be encouraged to drink extra water. Your doctor will do blood tests to check the function of your kidneys.

Gastrointestinal perforation and bleeding: Erlotinib can cause a number of problems in the digestive system. Gastrointestinal perforation is a serious and sometimes fatal condition in which a hole develops somewhere along the digestive system, resulting in inflammation of the abdomen. If you experience fever or chills with severe abdominal pain, nausea or vomiting, seek immediate medical attention.

Erlotinib can also cause bleeding in the digestive system. This is also very serious and sometimes fatal. Get immediate medical attention if you experience signs of bleeding in the stomach or intestines, such as vomiting blood or material that looks like coffee grounds, or stools that are black and tarry.

Grapefruit juice: Grapefruit juice can interfere with how the liver removes erlotinib from the body, resulting in increased side effects. People should not drink grapefruit juice while taking this medication.

Interstitial lung disease (ILD): This is a rare but serious complication. People with other lung conditions (e.g., inflammation of the lung) have an increased risk of death from ILD. If you develop symptoms of ILD such as shortness of breath with cough or fever, seek immediate medical attention.

Kidney function: There have been rare reports of kidney failure occurring with the use of erlotinib. If you have reduced kidney function, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Lactose: This medication contains lactose. Discuss with your doctor if you have rare hereditary problems of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption.

Liver function: Liver disease or reduced liver function may cause this medication to build up in the body, which may cause side effects. If you have reduced liver function or liver disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Erlotinib has been reported to cause liver failure, which can cause death. If you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin, contact your doctor immediately.

Skin reactions: Severe skin reactions have been linked to erlotinib use. Although rare, they are considered medical emergencies and require immediate medical attention.

If you experience skin blistering or peeling, a rash that covers a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort, seek medical attention immediately.

Smoking: Smoking may cause your body to eliminate this medication more quickly. This results in less medication being available to treat the disease. If you smoke, speak to your doctor.

Pregnancy: There are no adequate studies of use of this medication by pregnant women. This medication should not be taken during pregnancy. If you are a woman who could become pregnant, use a reliable method of birth control (e.g., condoms, birth control pill) during treatment and for at least 2 weeks after treatment is finished. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: It is not known if erlotinib passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Due to the potential for serious harm to a baby if they are exposed to this medication, breast-feeding mothers should not use this medication.

Children: The safety and effectiveness of this medication have not been established for children.

There may be an interaction between erlotinib and any of the following:

• amiodarone
• antacids (e.g., aluminum hydroxide, calcium carbonate, magnesium hydroxide, sodium bicarbonate)
• aprepitant
• "azole" antifungals (e.g., fluconazole, itraconazole, ketoconazole, posaconazole)
• bicalutamide
• bosentan
• cannabis
• ciprofloxacin
• clozapine
• cobicistat
• conivaptan
• deferasirox
• diltiazem
• dronedarone
• echinacea
• enzalutamide
• estrogens (e.g., conjugated estrogen, estradiol, ethinyl estradiol)
• fenofibrate
• fluvoxamine
• grapefruit juice
• H2 antagonists (e.g., cimetidine, famotidine, nizatidine)
• HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs; e.g., efavirenz, etravirine, nevirapine)
• HIV protease inhibitors (e.g., atazanavir, indinavir, ritonavir, saquinavir)
• hormonal birth control (e.g., birth control pills, inserts, IUDs)
• leflunomide
• letermovir
• macrolide antibiotics (e.g., clarithromycin, erythromycin)
• mifepristone
• mitotane
• modafinil
• norfloxacin
• other protein kinase inhibitors (e.g., ceritinib, crizotinib, dabrafenib, dasatinib, imatinib, nilotinib)
• progestins (e.g., dienogest, levonorgestrel, medroxyprogesterone, norethindrone)
• proton pump inhibitors (e.g., esomeprazole, lansoprazole, omeprazole, pantoprazole)
• rifabutin
• rifampin
• St. John's wort
• seizure medications (e.g., carbamazepine, phenytoin, phenobarbital, primidone)
• "statin" anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
• sirolimus
• tacrolimus
• teriflunomide
• tobacco (smoked)
• verapamil
• warfarin

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

• stop taking one of the medications,
• change one of the medications to another,
• change how you are taking one or both of the medications, or
• leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.