Generic name: erlotinib
Brand name: Tarceva
Dosage form: oral tablet
Drug class: EGFR inhibitors
Medically reviewed by A Ras MD.
What is erlotinib?
Erlotinib is a prescription medicine that is used to treat lung cancer. It is used to treat pancreatic cancer.
Before taking erlotinib, tell your doctor if you are allergic to erlotinib; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had, If you are being treated with a platinum-based chemo drug like cisplatin or carboplatin, If you take any other drugs (prescription or OTC, natural products, vitamins). There are many drugs that interact with erlotinib, like certain drugs that are used for infections, seizures, or stomach or bowel problems, If you are breast-feeding. Do not breast-feed while you take erlotinib and for 2 weeks after your last dose.
Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take erlotinib with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.
Erlotinib a kinase inhibitor, is a quinazolinamine with the chemical name N-(3-ethynylphenyl)-6,7bis(2-methoxyethoxy)-4-quinazolinamine Hydrochloride. Erlotinib contains erlotinib as the hydrochloride salt that has the following structural formula:
Erlotinib hydrochloride has the molecular formula C22H23N3O4•HCl and a molecular weight of 429.90. The molecule has a pKa of 5.4. Erlotinib hydrochloride is slightly soluble in Dimethyl sulfoxide, Dimethyl formamide and Methanol.
Aqueous solubility of erlotinib hydrochloride is dependent on pH with increased solubility at a pH of less than 5 due to protonation of the secondary amine. Over the pH range of 1.4 to 9.6, maximal solubility of approximately 1.69 mg/mL occurs at a pH of approximately 2.
Erlotinib tablets for oral administration are available in three dosage strengths containing erlotinib hydrochloride (27.3 mg, 109.3 mg and 163.9 mg) equivalent to 25 mg, 100 mg and 150 mg erlotinib and the following inactive ingredients: micro crystalline cellulose, lactose monohydrate, sodium starch glycolate, sodium lauryl sulfate, magnesium stearate, and ﬁnished tablets are coated with opadry white[Y-5-7068] contains following ingredients hypromellose, hydroxypropyl cellulose, titanium dioxide, polyethylene glycol
Mechanism of Action
Epidermal growth factor receptor (EGFR) is expressed on the cell surface of both normal and cancer cells. In some tumor cells signaling through this receptor plays a role in tumor cell survival and proliferation irrespective of EGFR mutation status. Erlotinib reversibly inhibits the kinase activity of EGFR, preventing autophosphorylation of tyrosine residues associated with the receptor and thereby inhibiting further downstream signaling. Erlotinib binding afﬁnity for EGFR exon 19 deletion or exon 21 (L858R) mutations is higher than its afﬁnity for the wild type receptor. Erlotinib inhibition of other tyrosine kinase receptors has not been fully characterized.
What are some things I need to know or do while I take erlotinib?
- Tell all of your health care providers that you take erlotinib. This includes your doctors, nurses, pharmacists, and dentists.
- If you have upset stomach, throwing up, diarrhea, or are not hungry, talk with your doctor. There may be ways to lower these side effects.
- Have blood work checked as you have been told by the doctor. Talk with the doctor.
- Very bad and sometimes deadly bleeding can happen when warfarin is taken with erlotinib. If you are taking warfarin or another drug like warfarin, you may need to have your blood work checked more closely. Talk with your doctor.
- If you smoke, talk with your doctor.
- If you start or stop smoking, talk with your doctor. How much drug you take may need to be changed.
- If you drink grapefruit juice or eat grapefruit often, talk with your doctor.
- It is common to get a rash with erlotinib but other skin reactions may also happen. Sometimes, these rashes and skin reactions can be very bad and may need treatment in the hospital. Call your doctor right away if you have acne, skin redness, or a skin rash that bothers you or does not go away. Call your doctor right away if you have redness or irritation of the palms of hands or soles of feet.
- You may get sunburned more easily. Avoid sun, sunlamps, and tanning beds. Use sunscreen and wear clothing and eyewear that protects you from the sun.
- Use an alcohol-free lotion or cream to help with pimple-like skin effects or dry skin.
- Very bad and sometimes deadly lung, liver, or kidney problems have happened with erlotinib. Talk with your doctor.
- Very bad and sometimes deadly holes in the GI (gastrointestinal) tract have happened with erlotinib. Talk with the doctor.
- This medicine may cause harm to the unborn baby if you take it while you are pregnant.
- Women must use birth control while taking erlotinib and for some time after the last dose. Ask your doctor how long to use birth control. If you get pregnant, call your doctor right away.
How is erlotinib best taken?
Use erlotinib as ordered by your doctor. Read all information given to you. Follow all instructions closely.
- Take on an empty stomach. Take 1 hour before or 2 hours after meals.
- Keep taking erlotinib as you have been told by your doctor or other health care provider, even if you feel well.
- If you need to take an antacid or a drug like famotidine or ranitidine, talk with your doctor about how to take it while taking erlotinib.
What do I do if I miss a dose?
- Take a missed dose as soon as you think about it.
- If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
- Do not take 2 doses at the same time or extra doses.
What are the side effects of erlotinib that I need to call my doctor about immediately?
WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:
- Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
- Signs of infection like fever, chills, very bad sore throat, ear or sinus pain, cough, more sputum or change in color of sputum, pain with passing urine, mouth sores, or wound that will not heal.
- Signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.
- Signs of kidney problems like unable to pass urine, change in how much urine is passed, blood in the urine, or a big weight gain.
- Signs of lung or breathing problems like shortness of breath or other trouble breathing, cough, or fever.
- Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight.
- Chest pain or pressure.
- Any unexplained bruising or bleeding.
- Feeling very tired or weak.
- Change in eyesight, eye pain, or very bad eye irritation.
- If bright lights bother your eyes.
- Low mood (depression).
- Very bad belly pain.
- Throwing up blood or throw up that looks like coffee grounds.
- Black, tarry, or bloody stools.
- A very bad skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis) may happen. It can cause very bad health problems that may not go away, and sometimes death. Get medical help right away if you have signs like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in your mouth, throat, nose, or eyes.
What are some other side effects of erlotinib?
All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
- Feeling tired or weak.
- Upset stomach.
- Not hungry.
- Mouth irritation or mouth sores.
- Back, muscle, or joint pain.
- Change in hair or nails.
- Dry skin.
- Weight loss.
These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.
You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.
If overdose is suspected:
If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.
How do I store and/or throw out erlotinib?
- Store at room temperature.
- Store in a dry place. Do not store in a bathroom.
Keep all in a safe place. Keep all drugs out of the reach of children and pets.
- Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.
SRC: NLM .