Erlotinib (Oral)

Erlotinib (Tarceva) is a cancer medicine used to treat metastatic non-small cell lung cancer (NSCLC), in patients who have certain types of abnormal epidermal growth factor receptor (EGFR) mutations, and pancreatic cancer.

Overview

Erlotinib functions as a first-line, monotherapy medicine that prevents further spreading of this type of cancer, in patients who have certain types of abnormal EGFR gene mutations. It is designed to be used before considering chemotherapy.

Another use of the medicine is for treating patients with cancer of the pancreas. It is used together with another drug, called Gemcitabine, for treating this type of cancer.

Erlotinib essentially works by blocking the activity of the epidermal growth factor receptor (EGRR). This is a protein found in cancer cells that causes the cells to divide, grow, and spread.

The drug is effective in patients with abnormal EGFR mutations, but can become resistant if used for long-term treatment.

The medicine is sold in the US under the brand name, Tarceva. It is supplied in the form of a tablet and is available to patients through a doctor's prescription only. It may be used to treat other types of cancers not discussed here.

Conditions Treated

  • Non-small cell lung cancer (NSCLC)
  • Pancreatic cancer

Type Of Medicine

  • Antineoplastic

The use of prescription medicines generally comes with potential risks and benefits. Since erlotinib can affect both the cancer cells and healthy cells of a patient and cause other unwanted adverse effects, your doctor may help you decide if it is right for you.

Tell your doctor if you have had an unusual or allergic reaction to this or other medicines; or allergic to inactive ingredients in this medicine. Also let your doctor know if you have any allergy to foods, preservatives, dyes or animals.

Give your doctor a list of all medications you are taking or plan to take. These include prescription and over-the-counter medicines (OTCs), vitamins, and nutritional supplements.

Certain medical conditions may affect the way the tablet works. It is important to let your doctor know if you are being or was recently treated with radiation therapy or chemotherapy, or had a recent medical or dental surgery.

Let your doctor know if you have (or have a history of) any other medical problems, especially lung infection or disease, kidney or liver disease, stomach ulcers or diverticular disease.

Pediatrics

The safety and efficacy of using this medicine in children have not been established.

Geriatrics

There are no specific problems found that would limit the use of the medicine in elderly patients.

  • Pregnancy

Tell your doctor if you are pregnant, may be pregnant or plan to become pregnant. Studies done in animals show a possible risk of harm to an unborn baby if erlotinib is used to treat a pregnant woman.

Breastfeeding

There is no specific information available that suggests the medicine can pass through breast milk and harm a breastfeeding infant.

If you are within any of the above risk groups, your doctor will determine treatment with erlotinib based on the potential benefits and risks involved and may take necessary precautions.

Side Effects

Side effects, hypersensitivity, or allergic reactions may occur from taking erlotinib. Some side effects are expected as the medicine begins to work in the body. Other effects are unwanted and may or may not require medical attention.

The following side effects may occur and need immediate medical attention. Call your doctor right away if you experience any of them.

More commonly occur

  • Diarrhea (severe)
  • Rash (severe)
  • Fever
  • Chills
  • Pain in the lower back or side
  • Chest pain with'a âœstabbing sensation
  • Prickling sensation that feels like pins and needles
  • Tightness in the chest
  • Numbness, tingling, burning or pain in the arms, hands, feet or legs
  • Hoarseness or change in the sound of your voice
  • Cough
  • Breathing problems (including labored breathing)
  • Difficult or painful urination

Rarely occur

  • Pain in the stomach (severe)
  • Sweating
  • Pain or discomfort in the chest (sometimes sudden and severe)
  • Constipation
  • Stool that is black or tarry
  • Blurred vision
  • Vomiting blood
  • Chest pain or discomfort
  • Redness or irritation of the eye
  • Vision changes
  • Unable to speak
  • Pain or discomfort in the jaw, back, arms or neck
  • Slurred speech
  • Headache (sudden and severe)
  • Weakness on one side of the body or of the arm or leg (sudden and severe)
  • Seizures
  • Vomit that looks like coffee grounds

Incidence unknown

  • Troubled breathing
  • Nausea
  • Nose bleeds
  • Upper abdominal or stomach pain with a burning sensation
  • Confusion
  • Darkening of the skin
  • Reduced amount of urine
  • Agitation
  • Feeling generally weak or tired
  • Burning sensation in the chest or stomach
  • Swelling of the face, hands or ankles
  • Headache
  • Sore throat
  • Lethargy
  • Peeling, blistering or loosening of the skin
  • Excessive thirst
  • Urine dark in color
  • Irregular heartbeat
  • Light-colored stools
  • Loss of appetite
  • Change in moods
  • Twitching, pain or stiffness of the muscle
  • Continuous stomach pain
  • Vomiting
  • Stupor
  • Rapid weight gain
  • Skin lesions that are red with a purple center
  • Tenderness of the stomach
  • Unusual weakness or tiredness
  • Yellow skin or eyes
  • White spots, sores or ulcers on the lips or in the mouth

Certain side effects which may occur tend to go away on their own as the body gets used to the medicine. They may require medical attention only if they become worse, bothersome or do not go away.

Tell your doctor if you experience any of them, as follows:

More commonly occur

  • Feeling full or bloated
  • Dryness, itchiness or burning sensation of the eyes
  • Sour or acidic stomach
  • Dizziness
  • Pain or swelling of the joint
  • Bone pain
  • Excessive tearing
  • Feeling sad, empty or afraid
  • Diarrhea (mild)
  • Skin blemishes
  • Feeling unusually cold
  • Dry skin
  • Thinning or loss of hair
  • Nervousness
  • Difficulty moving
  • Headache
  • Indigestion
  • Loss of interest or pleasure
  • Excessive gas or air in the stomach or intestines
  • Inflamed or swollen mouth
  • Passing gas
  • Belching
  • Pimples
  • Rash (mild)
  • Itchy skin
  • Heartburn
  • Redness, swelling or pain of the eye or areas around the eye
  • Shivering
  • Dry eyes
  • Irritability
  • Pain or discomfort in the stomach
  • Unable to sleep or trouble sleeping
  • Swelling
  • Tiredness
  • Trouble concentrating
  • Weight loss
  • Upset stomach

Less commonly occur

  • Fingernails that are loose
  • Soreness or redness around the fingernails

Incidence unknown

  • Nails that are brittle or loose
  • Increased hair growth (especially facial hair)
  • Excessive tearing or eye discharge

One or more of these side effects may occur, but not all of them may occur at once in one single patient. Some patients may experience other side effects not listed here.

Check with your doctor if you notice any unusual symptom that becomes bothersome or does not go away. You can ask your doctor or health care professional about ways to prevent or reduce side effects.

You may also call the FDA at 1-800-FDA-1088 to report side effects.

Dosage

This drug is supplied as a tablet which should be taken only by mouth.

Since food tends to interfere with the absorption of the medicine in the body, you may be told to take your dose on an empty stomach (at least 1 hour before or 2 hours after a meal). Meals of grapefruit or grapefruit juice should be avoided.

Your dose will be set based on the condition you are being treated for. Your doctor will also decide the strength of the dose, time between each dose, and the duration of your treatment.

Take your dose exactly as you are told to and follow all other directions given to you by your doctor, pharmacist, and prescription label. Also read the patient information leaflet that comes with the medicine.

The recommended dosage is as follows.

For treating non-small cell lung cancer

Adults: Take 150 milligrams (mg) of the tablet, once a day by mouth. If necessary, your doctor may adjust your dose.

For treating cancer of the pancreas

Adults: Take 100 milligrams (mg) of the tablet, once a day by mouth. Take it together with Gemcitabine, as prescribed. If necessary, your doctor may adjust your dose.

Missed dose

If you missed a dose of your medicine, take it as soon as possible. However, if it is time to take the next dose, skip the missed dose and take the next dose as scheduled. Continue with the regular dosing schedule.

An extra dose should not be taken to make up for the missed dose. Also, remember to take your tablet on an empty stomach.

Overdose

Call your doctor, 911 or the local poison control center at 1-800-222-1222, if you overdose on this drug. If the patient collapses or is not breathing, call 911.

Emergency medical attention is needed if you experience any of the following symptoms of overdose:

Interactions

Food, alcohol, tobacco, and other medicines or medical problems may cause adverse interaction with erlotinib. Your doctor will use the information disclosed in your medical history to decide how to treat you.

The following interactions have been included in this guide due to their significance.

Food, alcohol, and tobacco

The medicine should not be used with the following foods:

  • Grapefruit
  • Grapefruit juice

The following substance should not be used during treatment because it can significantly reduce the effect of the medicine:

  • Tobacco

If the use of these foods or tobacco cannot be avoided, your doctor may need to change the dose of your medicine or how often take it. Your doctor may also give you special instructions on the use of other foods, or substances such as alcohol.

Other medicines

None of the medicines on the following list should be taken with erlotinib. They may interact and increase or reduce the effects of the cancer medication. Other medicines may cause an adverse interaction, but are not mentioned here.

When telling your doctor about all the medicines you use, remember to mention if you are using any of the following. Your doctor may decide that it is best to still treat you with the cancer medicine but may adjust your dose or how often you take one or more of your medicines.

  • Rabeprazole
  • Ketoconazole
  • Phenobarbital
  • Acenocoumarol
  • Ritonavir
  • Famotidine
  • Voriconazole
  • Posaconazole
  • Boceprevir
  • Idelalisib
  • Ciprofloxacin
  • Rifampin
  • Clarithromycin
  • Pantoprazole
  • Conivaptan
  • Enzalutamide
  • Rifapentine
  • Fosphenytoin
  • Phenytoin
  • Indinavir
  • Cimetidine
  • St John's Wort
  • Cobicistat
  • Itraconazole
  • Ranitidine
  • Lansoprazole
  • Carbamazepine
  • Mitotane
  • Warfarin
  • Dexlansoprazole
  • Nelfinavir
  • Omeprazole
  • Rifabutin
  • Lopinavir
  • Saquinavir
  • Nefazodone
  • Telaprevir
  • Esomeprazole
  • Lumacaftor
  • Telithromycin
  • Phenprocoumon
  • Nizatidine

If you must take any stomach ulcer or heartburn medicine such famotidine, cimetidine or ranitidine, take it at least 10 hours before or two hours after taking this cancer drug. Take antacids, such as Maalox, several hours before or after taking erlotinib.

Other medical problems

Erlotinib should be used with caution in patients with the following medical conditions. Tell your doctor if you have (or have a history of) any of them, as the cancer drug can make these conditions worse.

To protect your health, your doctor may adjust the dose of your medicine and how often you take it.

The medicine should also be used with caution in patients who have the following condition. This condition slows down the removal of the drug from the body. The result may be a toxic level of the medicine in the body.

  • Liver disease

Your doctor may adjust the dose of your medicine and how often you take it to reduce the risk posed due to the liver disease.

Warnings

  • Do not use erlotinib if you are allergic to it or hypersensitive to any of its ingredients.
  • Do not start, stop or change the dose of the drug, unless approved by your doctor.
  • Do not use the medicine together with chemotherapy that is platinum-based.
  • Avoid smoking tobacco. It can significantly reduce the effect of the medication. Your doctor may need to change your dose if you start using tobacco or increase your use of it.
  • Do not use antacids or medicines for stomach ulcers or other stomach problems, unless you took them at least several hours before or after using erlotinib.
  • Avoid unnecessary exposure to sunlight, or artificial tanning lights such as tanning beds. Use sunscreen and protective clothing to avoid skin irritation, dryness or rash.
  • Avoid using skin products that may cause dryness or irritation of the skin. Instead, use alcohol-free products and products that are mild on the skin, such as a mild soap or skin cleanser.
  • You should not eat grapefruit or drink grapefruit juice during your treatment with the medicine.
  • To reduce the risk of diarrhea while taking the medicine, you should take small sips of a sugar-free drink (such as a sports drink) throughout the day.
  • Avoid eating spicy foods during treatment.
  • Ensure you tell your doctor if your condition gets worse or you experience side effects that bother you.
  • During treatment, do not start taking any other medicine unless your doctor approves it.

Storage

Store the medicine in a closed container and at room temperature of about 20° to 25°C (68° to 77°F).

Keep away from heat, moisture, and direct light. Keep from extremely cold temperatures and freezing.

Keep out of the reach of children.

Throw away medicine that is expired or no longer needed.

Ask your healthcare professional or local waste disposal agency how to safely dispose of it.

Summary

Prior to 2013, erlotinib was used as an alternative treatment in patients with NSCLC who have certain types of abnormal epidermal growth factor receptor (EGFR) mutations. This was after other treatments had failed.

The US Food and Drug Administration (FDA) finally approved erlotinib as a first-line, monotherapy medicine for treating this condition. One of its primary values is that it helps to postpone the need for chemotherapy in these patients.

Erlotinib's secondary use is for the treatment of pancreatic cancer, when used along with another cancer medicine called Gemcitabine.

Despite its efficacy, the medicine can affect both the healthy cells and cancer cells of a patient. It may also worsen certain medical conditions present in patients undergoing treatment.

Additionally, long-term treatment may cause the body to become resistant to the medicine. This tends to occur after about 12 months of treatment, following another abnormal EGFR protein mutation.

Once the body stops responding to erlotinib, an alternative treatment is needed to prevent the cancer cells from spreading further.