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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Kinase Inhibitor [EPC]
Erlotinib is a potent tyrosine kinase inhibitor primarily used for EGFR-mutated non-small cell lung cancer and pancreatic cancer. It works by blocking specific proteins that signal cancer cells to multiply.
Name
Erlotinib
Raw Name
ERLOTINIB HYDROCHLORIDE
Category
Kinase Inhibitor [EPC]
Salt Form
Hydrochloride
Drug Count
3
Variant Count
30
Last Verified
February 17, 2026
RxCUI
603203, 603206, 603208
UNII
DA87705X9K, J4T82NDH7E
About Erlotinib
Erlotinib is a potent tyrosine kinase inhibitor primarily used for EGFR-mutated non-small cell lung cancer and pancreatic cancer. It works by blocking specific proteins that signal cancer cells to multiply.
Detailed information about Erlotinib
This page is for informational purposes only and does not replace medical advice. Consult a qualified healthcare professional before using any medication containing Erlotinib.
Erlotinib was first approved by the U.S. Food and Drug Administration (FDA) in 2004. Over the last two decades, its role has evolved from a late-line salvage therapy to a primary first-line treatment for patients whose tumors harbor specific genetic mutations. Specifically, it targets the intracellular phosphorylation of the EGFR, a protein found on the surface of both normal and cancer cells. In certain cancers, this receptor is overactive or mutated, sending constant signals to the cell nucleus to grow, divide, and resist programmed cell death (apoptosis). By binding to this receptor, Erlotinib effectively 'turns off' the growth signal.
At the molecular level, Erlotinib functions by competitively inhibiting the adenosine triphosphate (ATP) binding site of the intracellular tyrosine kinase domain of the Epidermal Growth Factor Receptor (EGFR), also known as HER1 or ErbB1. In a healthy cell, the binding of a ligand (like epidermal growth factor) to the external portion of the receptor triggers the internal tyrosine kinase to bind ATP, leading to autophosphorylation. This phosphorylation initiates a cascade of downstream signaling pathways, including the Ras/Raf/MAPK, PI3K/Akt, and STAT pathways, which collectively promote cell cycle progression and survival.
In many cases of non-small cell lung cancer (NSCLC), mutations in the EGFR gene (most commonly Exon 19 deletions or Exon 21 L858R substitutions) cause the receptor to remain in a 'constantly on' state. Erlotinib has a much higher affinity for these mutated receptors than for wild-type (normal) receptors. By occupying the ATP-binding pocket, Erlotinib prevents the phosphorylation event, thereby halting the signal transduction cascade. This leads to cell cycle arrest and, ultimately, the death of the cancer cell. Because this mechanism is specific to the EGFR pathway, it allows for a more focused attack on the tumor while sparing many types of healthy cells, though side effects still occur due to the presence of EGFR in normal tissues like the skin and gastrointestinal tract.
Understanding how the body processes Erlotinib is vital for optimizing its efficacy and minimizing toxicity. The pharmacokinetics of Erlotinib are characterized by significant inter-patient variability, influenced by factors such as genetics, smoking status, and concurrent medications.
Erlotinib is FDA-approved for several specific oncological indications, typically requiring molecular confirmation of the tumor's genetic profile before initiation.
Erlotinib is available exclusively as an oral tablet. It is commonly supplied in three strengths to allow for precise dose titration and management of side effects:
The tablets are typically round, film-coated, and white to yellowish in color. They should be stored at room temperature (20°C to 25°C or 68°F to 77°F).
> Important: Only your healthcare provider can determine if Erlotinib is right for your specific condition. Treatment decisions are based on genetic testing of the tumor and a comprehensive assessment of your overall health.
The dosage of Erlotinib is strictly individualized based on the specific type of cancer being treated and the patient's tolerance to the medication. Healthcare providers follow evidence-based protocols to ensure the maximum therapeutic effect with manageable toxicity.
Erlotinib is not currently FDA-approved for use in pediatric patients. The safety and effectiveness of this medication in children and adolescents under the age of 18 have not been established. Clinical trials in pediatric brain tumors have generally not shown the same level of efficacy seen in adult lung cancer populations. If a healthcare provider considers Erlotinib for a minor, it is typically done under a compassionate use protocol or a specific clinical trial.
Adjustments to the standard dose are frequently necessary to manage side effects or account for physiological changes in the patient.
Specific studies in patients with severe renal impairment have not been conducted. However, since less than 9% of the dose is excreted via the kidneys, dose adjustments are generally not required for patients with mild to moderate kidney dysfunction. Patients with a creatinine clearance of less than 30 mL/min should be monitored with extreme caution.
Erlotinib is cleared primarily by the liver. Patients with hepatic impairment (Child-Pugh Class B or C) or those with biliary obstruction are at an increased risk of severe toxicity. Healthcare providers may reduce the starting dose or suspend treatment if liver function tests (bilirubin, ALT, AST) become significantly elevated.
In clinical trials, no overall differences in safety or efficacy were observed between patients over 65 and younger patients. However, because older adults may have a higher prevalence of comorbid conditions and decreased organ function, they should be monitored closely for dehydration and electrolyte imbalances, especially if diarrhea occurs.
Proper administration is critical to ensure the drug is absorbed correctly and to prevent unnecessary side effects.
If you miss a dose of Erlotinib, do not try to 'double up' to make up for the missed one. If it is within a few hours of your scheduled time, you may take the dose. However, if it is almost time for your next dose, skip the missed dose and resume your regular schedule. If you miss multiple doses, contact your oncology team for guidance.
An overdose of Erlotinib can lead to severe side effects, particularly an intense skin rash, severe diarrhea, and potential liver toxicity. If an overdose is suspected, seek emergency medical attention immediately or contact a poison control center. Treatment is generally supportive, focusing on hydration and managing symptoms.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop taking the medication without medical guidance, as this could allow the cancer to grow more rapidly.
Because EGFR is expressed in normal skin and gastrointestinal tissues, side effects are very common with Erlotinib. Most patients will experience at least one of the following:
> Warning: Stop taking Erlotinib and call your doctor immediately if you experience any of these symptoms.
Patients who remain on Erlotinib for several years may experience chronic skin changes, such as thinning of the skin, persistent dryness, or changes in hair texture (hair may become curly, brittle, or fine). There is also a risk of chronic paronychia (infection/inflammation around the nails) which may require specialized dermatological care. Long-term monitoring of liver and kidney function is essential to ensure no cumulative damage is occurring.
While Erlotinib does not currently carry a formal FDA 'Black Box Warning' in the same way some other drugs do, it contains 'Warnings and Precautions' that are of equivalent clinical significance, particularly regarding Interstitial Lung Disease (ILD) and Hepatotoxicity. Healthcare providers treat these risks with the highest level of vigilance. The labeling emphasizes that Erlotinib should be permanently discontinued if ILD is diagnosed or if severe hepatic impairment develops.
Report any unusual symptoms to your healthcare provider. Early intervention, such as the use of prophylactic moisturizers or early anti-diarrheal medication, can often prevent side effects from becoming severe.
Erlotinib is a potent medication that requires careful supervision by an oncologist. Patients must be aware that while it targets cancer cells, it can affect various organ systems. The most critical safety point is the immediate reporting of respiratory symptoms, as lung inflammation can progress rapidly. Additionally, patients must adhere to the fasting requirements (taking the drug on an empty stomach) to prevent unpredictable fluctuations in drug levels.
No FDA black box warnings for Erlotinib are currently mandated. However, the FDA-approved labeling includes prominent warnings for Interstitial Lung Disease-like events, Hepatotoxicity, and Gastrointestinal Perforation. These are considered 'major' warnings that dictate the monitoring and discontinuation protocols used by clinicians.
To ensure safety, your healthcare provider will order regular laboratory tests:
Erlotinib generally does not cause sedation or cognitive impairment. However, if a patient experiences side effects like extreme fatigue, blurred vision (from dry eyes), or dizziness, they should avoid driving or operating heavy machinery until they know how the medication affects them.
There is no direct contraindication between Erlotinib and alcohol. However, alcohol can irritate the gastrointestinal tract and may worsen diarrhea or nausea. Furthermore, heavy alcohol use can stress the liver, which is already processing the Erlotinib. Moderate consumption should be discussed with your oncologist.
Erlotinib does not cause a physical withdrawal syndrome, so it does not typically require a tapering schedule. However, stopping the drug suddenly can allow the cancer to begin growing again ('rebound growth'). You should never stop taking Erlotinib without a direct order from your oncologist. If the drug is stopped due to toxicity, the doctor will decide when or if it is safe to restart at a lower dose.
> Important: Discuss all your medical conditions, especially lung, liver, or kidney disease, with your healthcare provider before starting Erlotinib.
Erlotinib does not typically interfere with the chemical assays used in standard lab tests. However, it can cause physiological changes that are reflected in lab results, such as elevated liver enzymes (ALT/AST), increased bilirubin, or increased INR in patients taking warfarin.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter antacids.
There are very few absolute contraindications for Erlotinib, as it is often a life-prolonging treatment for advanced cancer. However, the following represent situations where the drug must not be used:
In these situations, the healthcare provider must carefully weigh the potential benefits of Erlotinib against the significant risks:
There is no documented cross-sensitivity between Erlotinib and other classes of chemotherapy (like platinum agents or taxanes). However, patients who have had a severe allergic reaction to other EGFR inhibitors (such as gefitinib or afatinib) should be treated with extreme caution, as the chemical structures are similar. There is no known cross-reactivity with common antibiotics or non-cancer medications.
> Important: Your healthcare provider will evaluate your complete medical history, including any previous lung or liver issues, before prescribing Erlotinib.
Erlotinib is classified as a drug that carries significant risks to a developing fetus. Based on its mechanism of action and animal studies, Erlotinib can cause fetal harm. In animal reproductive studies, erlotinib caused increased embryofetal toxicity and abortion.
It is not known whether Erlotinib is excreted in human milk. However, because many drugs are excreted in breast milk and because of the potential for serious adverse reactions in nursing infants, women should not breastfeed while taking Erlotinib and for at least two weeks after the final dose. The potential for the drug to interfere with the infant's growth and development is a significant concern.
As previously noted, Erlotinib is not approved for use in children. The safety and effectiveness have not been established in patients under 18. Clinical trials in pediatric populations (specifically for brain tumors like DIPG) have generally failed to show a survival benefit, and the side effect profile in children can be more difficult to manage.
In clinical studies of Erlotinib, approximately 40-50% of patients were 65 years of age or older. No overall differences in efficacy were observed between these patients and younger patients. However, elderly patients may be more susceptible to the dehydrating effects of diarrhea and should be monitored closely for electrolyte imbalances and renal strain. There is no specific age-based dose adjustment required, provided organ function is adequate.
Erlotinib exposure is increased in patients with hepatic impairment.
> Important: Special populations require individualized medical assessment. Always inform your oncology team if you are planning to become pregnant or have a history of liver or kidney disease.
Erlotinib is a small-molecule, quinazolinamine derivative. Its primary action is the potent inhibition of the tyrosine kinase activity associated with the Epidermal Growth Factor Receptor (EGFR/HER1/ErbB1). EGFR is a transmembrane glycoprotein that is a member of the erbB family of receptor tyrosine kinases.
Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. By preventing ATP from binding, Erlotinib inhibits the autophosphorylation of the tyrosine residues on the intracellular domain of the receptor. This effectively blocks the downstream signaling of pathways such as the mitogen-activated protein kinase (MAPK) and the AKT pathway. In tumors that are 'addicted' to EGFR signaling (those with activating mutations), this inhibition leads to a cessation of the cell cycle in the G1 phase and triggers apoptosis (programmed cell death).
| Parameter | Value |
|---|---|
| Bioavailability | ~60% (Fasting); ~100% (With Food) |
| Protein Binding | ~93% (Primarily to Albumin and AAG) |
| Half-life | ~36.2 Hours |
| Tmax | ~4 Hours |
| Metabolism | Primarily CYP3A4, CYP3A5; minor CYP1A2 |
| Excretion | Fecal 83%, Renal 8% |
Erlotinib is classified as a First-Generation EGFR Tyrosine Kinase Inhibitor (TKI). It is part of a broader class of targeted therapies that include other TKIs like Gefitinib (1st gen), Afatinib (2nd gen), and Osimertinib (3rd gen). Within the ATC (Anatomical Therapeutic Chemical) classification system, it is coded as L01EB02.
Medications containing this ingredient
Common questions about Erlotinib
Erlotinib is primarily used to treat non-small cell lung cancer (NSCLC) that has spread to other parts of the body and possesses specific mutations in the EGFR gene. It is also used as a first-line treatment for advanced or metastatic pancreatic cancer when given in combination with the chemotherapy drug gemcitabine. In lung cancer, it can be used as an initial treatment, a maintenance therapy, or a second-line treatment after other therapies have failed. Because it is a targeted therapy, it is only effective in patients whose tumors have specific genetic markers, which are identified through a biopsy and molecular testing. Your doctor will determine if your specific cancer type is likely to respond to this medication.
The most frequent side effects of Erlotinib are an acne-like skin rash and diarrhea, which affect more than half of all patients. The rash usually appears on the face, scalp, and chest and is often a sign that the drug is working effectively against the cancer. Other common issues include fatigue, loss of appetite, dry skin, and mouth sores. While most of these are manageable with supportive care, some patients may also experience nausea or changes in their fingernails. It is important to communicate with your oncology team at the first sign of these symptoms so they can provide treatments to keep you comfortable. Severe side effects, like lung inflammation or liver problems, are rare but require immediate medical attention.
There is no known direct chemical interaction between Erlotinib and alcohol that makes the combination strictly forbidden. However, most oncologists recommend limiting alcohol consumption because it can worsen certain side effects like diarrhea, nausea, and dehydration. Additionally, both Erlotinib and alcohol are processed by the liver; excessive drinking could put unnecessary strain on liver function, which needs to be monitored closely during cancer treatment. If you do choose to drink, it is best to do so in moderation and only after discussing it with your healthcare provider. Always stay hydrated, as Erlotinib can already cause dry skin and thirst.
No, Erlotinib is not considered safe for use during pregnancy and is classified as potentially harmful to a developing fetus. The drug works by blocking growth signals that are also essential for normal fetal development, and animal studies have shown it can cause miscarriage and birth defects. Women who could become pregnant must use highly effective birth control while taking Erlotinib and for at least one month after the final dose. If you discover you are pregnant while taking this medication, you must notify your doctor immediately. Men taking Erlotinib should also use contraception if their partner could become pregnant to avoid any potential risks.
While Erlotinib begins working at the molecular level within hours of the first dose, it usually takes several weeks to see a measurable change in the tumor. Most healthcare providers will perform the first follow-up imaging scan (like a CT or PET scan) about 6 to 12 weeks after starting the medication to assess the response. Some patients may notice an improvement in their symptoms, such as reduced coughing or better breathing, within the first few weeks of treatment. However, the skin rash often appears within the first 10 to 14 days, which can be an early clinical indicator that the drug is active in the body. Consistency in taking the daily dose is key to achieving the best results.
You should never stop taking Erlotinib or change your dose without first consulting your oncologist. Stopping the medication suddenly can cause the cancer cells to begin growing and spreading again, a phenomenon sometimes called 'disease flare.' If you are experiencing severe side effects, your doctor may tell you to take a 'drug holiday' or reduce your dose, but this must be done under medical supervision. If the drug is stopped, your doctor will monitor you closely for any worsening of your cancer symptoms. Always ensure you have enough of a supply so that you do not accidentally run out and miss doses.
If you miss a dose of Erlotinib, you should take it as soon as you remember, provided it is still the same day. However, if you do not realize you missed the dose until the following day, you should skip the missed dose entirely and simply take your next scheduled dose at the regular time. Never take two doses at once to make up for a missed one, as this can significantly increase the risk of toxic side effects. If you find yourself frequently forgetting doses, consider using a pill organizer or a smartphone alarm to stay on track. If you miss more than two doses in a row, contact your healthcare provider for specific instructions.
Weight gain is not a typical side effect of Erlotinib; in fact, weight loss is much more common. Because the drug can cause diarrhea, a loss of appetite (anorexia), and occasional nausea, many patients find it difficult to maintain their weight during treatment. If you notice sudden or significant weight gain, it could be a sign of fluid retention, which might indicate a problem with your kidneys or heart, and you should report this to your doctor. To manage weight loss, your oncology team might recommend high-calorie supplements or a consultation with a dietitian. Maintaining adequate nutrition is an important part of your overall cancer treatment plan.
Erlotinib has several significant drug interactions, so it must be used cautiously with other medications. It is particularly important to avoid proton pump inhibitors (PPIs) like omeprazole, as they prevent Erlotinib from being absorbed by the body. Other interactions include certain antibiotics, anti-seizure medications, and blood thinners like warfarin. Even herbal supplements like St. John's Wort can interfere with how Erlotinib works. Always provide your doctor and pharmacist with a complete list of all prescriptions, over-the-counter drugs, and vitamins you are taking. Your doctor may need to adjust your doses or switch you to alternative medications to ensure Erlotinib remains effective.
Yes, Erlotinib is available as a generic medication, which can be significantly less expensive than the original brand-name version, Tarceva. The FDA approved the first generic versions of Erlotinib in 2016, and they are required to meet the same strict standards for safety, strength, and quality as the brand-name drug. Both the brand and the generic versions are available in 25 mg, 100 mg, and 150 mg tablets. Most insurance plans now cover the generic version of Erlotinib. If you have concerns about switching between the brand and generic, discuss them with your pharmacist or oncologist, though they are considered therapeutically equivalent.