Erlotinib  

Brand name: Tarceva®  

Generic name: Erlotinib 

Therapeutic Class: kinase inhibitor 

Manufacturer / Distributor: Roche, Genentech and OSI Pharmaceuticals 

Availability: Tarceva is available by prescription only  

FDA Approval: Tarceva (Erlotinib) was approved by the U.S. Food and Drug Administration (FDA) in November 2005 for the treatment of metastatic pancreatic cancer (see indications below) in combination with Gemcitabin.   

Indications: Erlotinib is used to treat:    

• locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy  
• Locally advanced, unresectable or metastatic pancreatic cancer in combination with gemcitabine (Gemzar). 

Erlotinib can be used to treat other medical conditions; talk to your doctor or pharmacist for more information.  

Dosage form: Erlotinib comes as a tablet to take by mouth 

Dosage: Each tablet of Erlotinib is white turning to yellow, round, biconvex and film coated; tablets are available in 25mg, 100mg and 150mg. To determine a dose capable of fighting your cancer, your oncologist will consider your age, health status, and body surface area (BSA). If you are taking other chemotherapy drugs or undergoing radiotherapy, you may receive a lower dosage. 

Usually, the daily dose of Erlotinib is 150 mg, taken once per day with a glass of water. Take the medication at least 1 hour before meals or at least 2 hours after a meal. It is very important that you take Erlotinib at around the same time every day. Depending on the reaction of your body to the drug, your doctor may recommend you to take Erlotinib otherwise. Do not change the way you are told to take the medication without first consulting your doctor.   

Storage:  Erlotinib should be kept tightly closed in the container it came, out of the reach of children. The drug must be stored at room temperature, away from heat, light and moisture. Erlotinib and all other medications should not be used beyond the expiration date printed on the container.    

Overdose:  overdosing any chemotherapy drug can cost you your life. The risk of complication increases considerably when the drug is overdosed for a long period of time. Even in the absence of overdose, Erlotinib tends to damage the bone marrow, and lead to serious decreased blood cells count.  It is extremely important that you take Erlotinib as indicated by your physician or pharmacist; don’t ever take it more or more often.   

Missing dose: misusing Erlotinib is a serious matter. Taking less can decrease the therapeutic effects of the drug; taking more can lead to serious health problems and even death. Do your best to take it around the same time every day; do not miss or take less of it. In case you forget to take a dose, take the missed one as soon as you remember it. However, if it is time for your next dose, do not double it to recover the missed one. Contact your doctor or wait to go back to your regular schedule.    

Mechanism of action (MOA): Erlotinib is a kinase inhibitor; it prevents the development and selectively induces death of cancer cells by blocking the action of protein-tyrosine kinase, an abnormal protein that signals cancer cells to multiply.  

Contraindications: Erlotinib is contraindicated or should use with precaution in the following conditions: 

• allergy to the drug or any of the constituents 
• smoking  
• pregnancy  
• breast-feeding 
• lactase deficiency 
• prolonged exposure to sunlight  
• consummation of grape fruit  
• allergy to lactose or in case of galactosemia 
• Glucose-galactose malabsorption.   

Interactions:  if you are taking Erlotinib , it is safe to first contact your physician before consuming grapefruit, aspirin, vitamins, nutritional supplements, or St. John's wort. Certain substances can interact with Erlotinib, and increase the risk of the development of side effects. Tell your doctor or pharmacist if you are taking any of these medications:   

• Omeprazole 
• Pioglitazone 
• Rifampin 
• Warfarin 
• glucocorticoids (Prednisone, and others)  
• calcium antagonists (Diltiazem, verapamil, and others) 
• macrolide antibiotics (Erythromycin, clarithromycin, and others)  
• anticonvulsants (Phenytoin, carbamazepine, and others)  
• antifungals (Ketoconazole, fluconazole, and others)  
• HIV drugs ( Ritonavir, indinavir, efavirenz, and others)  
• barbiturates (Phenobarbital)  
• Fluoroquinolones (Ciprofloxacin, norfloxacin, and others).  

Side effects: i n addition to attacking cancer cells, Erlotinib may interfere with certain normal cells, and cause a number of adverse effects in most patients; common Erlotinib side effects include:     

• weight loss 
• hair loss 
• tiredness 
• weakness 
• diarrhea 
• dry mouth  
• constipation 
• nausea and vomiting 
• sores on your lips or mouth
• dry mouth 
• change in taste 
• decreased appetite 
• darkening of skin 
• skin rash 
• muscle or limb pain 
• white horizontal discoloration of the nail plate
• pain, burning, numbness, or tingling in the hands or feet 
• Swelling of the arms, hands, feet, ankles, or lower legs.  

If the side effects above persist for weeks, contact your oncologist. In addition, contact your doctor if you experience any of these symptoms:   

• blurred vision 
• chest pain  
• fainting  
• sunken eyes, scarring or abnormal eyelash growth
• painful or decreased urination 
• blood in urine or stool  
• difficulty breathing or shortness of breath
• blistering, peeling, dry, or cracked skin 
• itching and/or burning of the skin 
• skin rash on the face, upper chest, or back 
• Signs of infections: persistent cough, fever, chills, etc. 
• dry, red, painful, or irritated eyes 
• pain in the arms, neck, or upper back  
• rapid, irregular, or pounding heartbeat 
• weakness or numbness of an arm or leg  
• unusual bruising or bleeding 
• black and tarry or bloody stools 
• bloody or coffee-like vomit  
• Redness, warmth, pain, tenderness, or swelling in one leg.