Erlotinib

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Generic Name of Erlotinib - Learn More

Erlotinib

Erlotinib Precaution - What You Need to Know

Erlotinib is an oral tyrosine kinase inhibitor primarily used for the treatment of non-small cell lung cancer (NSCLC) and pancreatic cancer. It specifically targets the epidermal growth factor receptor (EGFR) to inhibit tumor growth. Precautions should be taken in patients with pre-existing lung or gastrointestinal conditions such as interstitial lung disease (ILD), as erlotinib may exacerbate pulmonary toxicity, leading to life-threatening ILD. Baseline lung function should be assessed, and patients should be closely monitored for any signs of pulmonary distress, such as cough, dyspnea, or fever.

Erlotinib is contraindicated during pregnancy due to its teratogenic potential, and it should only be used during breastfeeding if the benefits outweigh the risks, as it is excreted in breast milk. Dose reduction or discontinuation is necessary for patients who experience significant liver toxicity, such as increased serum transaminase levels. It is important to monitor liver function tests before and during treatment. The drug should be used cautiously in patients with a history of gastrointestinal obstruction or perforation.

Patients should also be monitored for skin reactions, as erlotinib can cause severe rash, dry skin, and pruritus, which are common side effects. Additionally, erlotinib is metabolized by the liver enzyme CYP3A4, so interactions with other drugs that inhibit or induce this enzyme should be considered when co-administering medications.

Erlotinib Indication - Uses and Benefits

Erlotinib is primarily indicated for the treatment of non-small cell lung cancer (NSCLC), particularly in patients with EGFR mutations who have advanced or metastatic disease. It is also used in combination with gemcitabine for the treatment of pancreatic cancer. The drug works by inhibiting the EGFR, which plays a key role in the growth and spread of certain cancer cells.

Erlotinib is typically used in patients who have failed other therapies or those with metastatic disease who have not been candidates for chemotherapy. It is commonly administered as a first-line treatment for EGFR-mutant NSCLC, offering an alternative to chemotherapy with fewer systemic side effects. Off-label, erlotinib has been explored for use in other cancers, such as head and neck cancers, and occasionally in combination with other agents for metastatic colorectal cancer, but these uses are less common and not always supported by widespread clinical guidelines.

Erlotinib Contraindications - Important Warnings

Erlotinib is contraindicated in patients with a history of severe hypersensitivity or allergic reactions to the drug or any of its components. It should not be used in patients who are pregnant or planning to become pregnant due to its teratogenic effects, which could cause fetal harm. Additionally, it is contraindicated in patients with severe hepatic impairment, as erlotinib is extensively metabolized in the liver, and impaired liver function could lead to increased drug levels and an elevated risk of toxicity.

Erlotinib is also contraindicated in patients with significant gastrointestinal perforation, obstruction, or other severe gastrointestinal disorders due to the risk of exacerbating these conditions. Its use is not recommended for breastfeeding women, as the drug can pass into breast milk and may harm the infant. Due to its potential to cause serious side effects such as interstitial lung disease, erlotinib should be used with extreme caution in patients with pre-existing pulmonary conditions.

Erlotinib Side Effects - What to Expect

Common side effects of erlotinib include skin reactions, such as acneiform rash, dry skin, and pruritus, which occur in many patients and can be severe. The rash typically begins within the first two weeks of treatment and may worsen before improving. Other dermatologic reactions such as dermatitis, erythema, and skin peeling are also common. Managing these reactions includes topical treatments, oral antibiotics, or adjusting the dose of erlotinib if necessary.

Gastrointestinal side effects, including diarrhea, nausea, vomiting, and anorexia, are also frequently reported. These side effects may lead to dehydration and weight loss in some patients, requiring electrolyte monitoring and possible dose adjustments. Severe gastrointestinal symptoms such as gastrointestinal perforation, although rare, are serious and require immediate discontinuation of the drug.

More severe but less common side effects include interstitial lung disease (ILD), which can cause symptoms such as cough, dyspnea, fever, and fatigue. If ILD is suspected, erlotinib should be discontinued immediately. Hepatotoxicity is another serious concern, with elevated liver enzymes being a potential sign of liver damage. Regular monitoring of liver function tests is recommended during treatment.

Erlotinib Pregnancy Category ID - Safety Information

4

Erlotinib Mode of Action - How It Works

Erlotinib acts by selectively inhibiting the epidermal growth factor receptor (EGFR) tyrosine kinase activity. EGFR is a receptor involved in regulating cell growth, survival, and proliferation, and its activation is associated with the development and progression of various cancers, including NSCLC. Erlotinib binds to the ATP-binding site of the EGFR tyrosine kinase, preventing the activation of downstream signaling pathways that promote tumor cell growth and survival.

By inhibiting EGFR, erlotinib prevents the phosphorylation of downstream proteins involved in cell division and survival, such as MAPK and PI3K/Akt pathways, thereby inhibiting tumor growth. This mechanism is particularly effective in patients with EGFR mutations, as these mutations often lead to constitutive activation of EGFR signaling. Erlotinib’s specificity for EGFR helps to minimize effects on other tyrosine kinases, contributing to its selective action against EGFR-driven cancers.

Erlotinib Drug Interactions - What to Avoid

Erlotinib interacts with several drugs that affect its absorption, metabolism, and clearance. It is primarily metabolized by the liver enzyme CYP3A4, so drugs that inhibit or induce CYP3A4 can affect the plasma concentration of erlotinib. Strong CYP3A4 inducers (such as rifampin, phenytoin, and carbamazepine) can decrease erlotinib plasma levels, reducing its efficacy. On the other hand, strong CYP3A4 inhibitors (such as ketoconazole, itraconazole, and grapefruit juice) can increase erlotinib concentrations, increasing the risk of adverse effects.

Additionally, erlotinib may increase the plasma concentration of warfarin, leading to an enhanced anticoagulant effect, so monitoring of the INR (International Normalized Ratio) is recommended when co-administering these drugs. Antacids, proton pump inhibitors (PPIs), and H2 blockers may reduce the absorption of erlotinib by altering gastric pH, so it is recommended that erlotinib be taken on an empty stomach to maximize its bioavailability.

Patients should avoid taking erlotinib concurrently with drugs that can cause QT prolongation, as the combination may increase the risk of life-threatening arrhythmias. Additionally, since erlotinib can cause significant skin reactions, concurrent use with other drugs that affect the skin or immune system, such as immunosuppressive agents, should be carefully monitored.

Erlotinib Adult Dose - Recommended Dosage

The recommended dose of erlotinib for non-small cell lung cancer (NSCLC) is 150 mg orally once daily. This dose should be taken on an empty stomach, at least one hour before or two hours after food, to maximize bioavailability. If the patient experiences intolerable side effects, particularly dermatologic or gastrointestinal symptoms, the dose may be reduced to 100 mg or 50 mg daily.

In the case of pancreatic cancer, erlotinib is typically administered in combination with gemcitabine. The standard dose in this context is 100 mg orally once daily, taken one hour before or two hours after a meal, as part of a combination therapy regimen.

It is important to monitor patients for adverse effects during treatment, and if significant toxicities occur, dose reduction or discontinuation may be necessary.

Erlotinib Child Dose - Dosage for Children

Erlotinib is not approved for use in pediatric patients, as there is insufficient data to establish safety and efficacy in children. The use of erlotinib in children is generally not recommended, except in clinical trials or special circumstances where potential benefits may outweigh the risks. If used in a pediatric setting, dosing should be highly individualized, and the patient should be closely monitored for any adverse effects, particularly those related to skin and gastrointestinal function.

In general, erlotinib's role in pediatric oncology is limited, and alternative treatments with more established safety profiles are preferred in children.

Erlotinib Renal Dose - Dosage for Kidney Conditions

Erlotinib is primarily metabolized by the liver and excreted via bile and feces, with minimal renal excretion. Therefore, no dose adjustments are required for patients with renal impairment. However, for patients with severe renal dysfunction, careful monitoring is still recommended, particularly for potential side effects such as diarrhea or hepatotoxicity, as these may exacerbate underlying renal issues.

Patients with mild to moderate renal impairment can generally receive the standard dose of erlotinib, but dose adjustments should be considered in the context of the patient’s overall clinical status and comorbidities.