Erlotinib

What is Erlotinib?

• Erlotinib (Tarceva) is a kinase inhibitor used to treat non-small cell lung cancer (NSCLC) and pancreatic cancer.

Erlotinib

Erlotinib-3D-sticks

What are the uses of this medicine?

Erlotinib (Tarceva) used for the treatment of:

• patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations.
• First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.

Limitations of Use:

• Safety and efficacy of Tarceva have not been established in patients with NSCLC whose tumors have other EGFR mutations.
• Tarceva is not recommended for use in combination with platinum-based chemotherapy.

How does this medicine work?

• Erlotinib (er loe' ti nib) is a selective inhibitor of several tyrosine kinase receptors which are associated with tumor growth and angiogenesis.
• The tyrosine kinase receptors are often mutated and over expressed in tumor tissue and cause unregulated cell growth and proliferation.
• Erlotinib is one of several tyrosine kinase inhibitors that have been introduced into cancer chemotherapy and are specially directed at molecular abnormalities that occur in cancer cells.
• Inhibition of the receptor can lead to reversal of progression of the cancer, although clinical responses are sometimes limited by the development of tumor resistance caused by further mutations in the receptor gene.

Who Should Not Use this medicine ?

Limitations of Use:

• Safety and efficacy of Tarceva have not been established in patients with NSCLC whose tumors have other EGFR mutations.
• Tarceva is not recommended for use in combination with platinum-based chemotherapy.

What drug interactions can this medicine cause?

• Avoid co-administering Tarceva with strong CYP3A4 inhibitors (e.g., boceprevir, clarithromycin, conivaptan, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telithromycin, voriconazole, grapefruit or grapefruit juice) or a combined CYP3A4 and CYP1A2 inhibitor (e.g., ciprofloxacin). Reduce the Tarceva dosage when co-administering with a strong CYP3A4 inhibitor or a combined CYP3A4 and CYP1A2 inhibitor if co-administration is unavoidable.
• Increase the Tarceva dosage if co-administration with CYP3A4 inducers (e.g., carbamazepine, phenytoin, rifampin, rifabutin, rifapentine, phenobarbital and St. John's wort) is unavoidable.
• Increase the Tarceva dosage in patients that smoke tobacco or when co-administration with moderate CYP1A2 inducers is unavoidable.
• Co-administration of Tarceva with proton pump inhibitors (e.g., omeprazole) and H-2 receptor antagonists (e.g., ranitidine) decreased erlotinib exposure.
• Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions, which in some cases were fatal, have been reported in patients receiving Tarceva.

Is this medicine FDA approved?

• Erlotinib has special activity against the human epidermal growth factor (EGF) tyrosine kinase receptors HER-1 and EGFR which are found in several forms of cancer. Erlotinib received approval for use in the United States in 2004.

How should this medicine be used?

• Select patients for the treatment of metastatic NSCLC with Tarceva based on the presence of EGFR exon 19 deletions or exon 21 (L858R) substitution mutations in tumor or plasma specimens.

Recommended dosage:

• Recommended Dose – NSCLC:

The recommended daily dose of Tarceva for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food.

• Recommended Dose – Pancreatic Cancer:

100 mg orally, on an empty stomach, once daily.

Administration:

• Take Tarceva on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 25 mg, 100 mg, and 150 mg

This medicine is available in fallowing brand namesː

• Tarceva

What side effects can this medication cause?

The most common side effects of this medicine include:

• rash
• diarrhea
• anorexia
• fatigue
• dyspnea
• cough
• nausea
• vomiting

What special precautions should I follow?

• Cases of serious ILD, including fatal cases, can occur with Tarceva treatment. Withhold Tarceva for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Tarceva if ILD is diagnosed.
• Hepatorenal syndrome, severe acute renal failure including fatal cases, and renal insufficiency can occur with Tarceva treatment. Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Tarceva for severe renal toxicity.
• Hepatic failure and hepatorenal syndrome, including fatal cases, can occur with Tarceva treatment in patients with normal hepatic function; the risk of hepatic toxicity is increased in patients with baseline hepatic impairment. Monitor periodic liver testing. Withhold or discontinue Tarceva for severe or worsening liver tests.
• Gastrointestinal perforation, including fatal cases, can occur with Tarceva treatment. Discontinue Tarceva.
• Bullous, blistering and exfoliative skin conditions, including cases suggestive of Stevens-Johnson syndrome/toxic epidermal necrolysis, which in some cases were fatal, can occur with Tarceva treatment. Discontinue Tarceva.
• In the pancreatic carcinoma trial, seven patients in the Tarceva/gemcitabine group developed cerebrovascular accidents. The risk of CVA is increased in patients with pancreatic cancer.
• Microangiopathic hemolytic anemia (MAHA) may occur. The risk of MAHA is increased in patients with pancreatic cancer. The risk of MAHA is increased in patients with pancreatic cancer.
• Decreased tear production, abnormal eyelash growth, keratoconjunctivitis sicca or keratitis can occur with Tarceva treatment and can lead to corneal perforation or ulceration. Discontinue Tarceva for corneal perforation, ulceration or persistent severe keratitis.
• Severe and fatal hemorrhage associated with International Normalized Ratio (INR) elevations can occur when Tarceva and warfarin are administered concurrently. Regularly monitor INR in patients taking warfarin or other coumarin-derivative anticoagulants.
• Based on animal data and its mechanism of action, Tarceva can cause fetal harm when administered to a pregnant woman. Advise females of reproductive potential of the potential risk to the fetus and to use effective contraception.

What to do in case of emergency/overdose?

Treatment of overdosage:

• Withhold Tarceva in patients with an overdose or suspected overdose and institute symptomatic treatment.

Can this medicine be used in pregnancy?

• Based on animal data and its mechanism of action, Tarceva can cause fetal harm when administered to a pregnant woman.
• Limited available data on use of Tarceva in pregnant women are not sufficient to inform a risk of major birth defects or miscarriage.

Can this medicine be used in children?

• The safety and effectiveness of Tarceva in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active Ingredient: erlotinib hydrochloride

Inactive Ingredients: none

Who manufactures and distributes this medicine?

Manufactured for: OSI Pharmaceuticals, LLC, Northbrook, IL 60062 an affiliate of Astellas Pharma US, Inc.

Product of Japan or Italy.

Distributed by: Genentech USA, Inc., A Member of the Roche Group, 1 DNA Way, South San Francisco, CA

What should I know about storage and disposal of this medication?

• Store at 25°C (77°F); excursions permitted to 15°C - 30°C (59°F - 86°F).

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• Dailymed label info on Erlotinib
• FDA Erlotinib