Non-Small Cell Lung Cancer (NSCLC)

TARCEVA (erlotinib) monotherapy is indicated for the maintenance treatment of patients with locally advanced or metastatic non-small cell lung cancer whose disease has not progressed after four cycles of platinum-based first-line chemotherapy [see Clinical Studies].

TARCEVA (erlotinib) monotherapy is indicated for the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen [see Clinical Studies].

Results from two, multicenter, placebo-controlled, randomized, Phase 3 trials conducted in first-line patients with locally advanced or metastatic NSCLC showed no clinical benefit with the concurrent administration of TARCEVA (erlotinib) with platinum-based chemotherapy [carboplatin and paclitaxel or gemcitabine and cisplatin] and its use is not recommended in that setting [see Clinical Studies].

Pancreatic Cancer

TARCEVA (erlotinib) in combination with gemcitabine is indicated for the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer [see Clinical Studies].

NSCLC

The recommended daily dose of TARCEVA (erlotinib) for NSCLC is 150 mg taken on an empty stomach at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs. There is no evidence that treatment beyond progression is beneficial.

Pancreatic Cancer

The recommended daily dose of TARCEVA (erlotinib) for pancreatic cancer is 100 mg taken on an empty stomach at least one hour before or two hours after the ingestion of food, in combination with gemcitabine [see Clinical Studies or the gemcitabine package insert]. Treatment should continue until disease progression or unacceptable toxicity occurs.

Dose Modifications

In patients who develop an acute onset of new or progressive pulmonary symptoms, such as dyspnea, cough or fever, treatment with TARCEVA (erlotinib) should be interrupted pending diagnostic evaluation. If Interstitial Lung Disease (ILD) is diagnosed, TARCEVA (erlotinib) should be discontinued and appropriate treatment instituted as necessary [see WARNINGS AND PRECAUTIONS]. Discontinue TARCEVA (erlotinib) for hepatic failure or gastrointestinal perforation. Interrupt or discontinue TARCEVA (erlotinib) in patients with dehydration who are at risk for renal failure, in patients with severe bullous, blistering or exfoliative skin conditions, or in patients with acute /worsening ocular disorders [see WARNINGS AND PRECAUTIONS].

Diarrhea can usually be managed with loperamide. Patients with severe diarrhea who are unresponsive to loperamide or who become dehydrated may require dose reduction or temporary interruption of therapy. Patients with severe skin reactions may also require dose reduction or temporary interruption of therapy.

When dose reduction is necessary, the TARCEVA (erlotinib) dose should be reduced in 50 mg decrements.

In patients who are taking TARCEVA (erlotinib) with a strong CYP3A4 inhibitor such as, but not limited to, atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin (TAO), voriconazole, or grapefruit or grapefruit juice, a dose reduction should be considered if severe adverse reactions occur. Similarly, in patients who are taking TARCEVA (erlotinib) with an inhibitor of both CYP3A4 and CYP1A2 like ciprofloxacin, a dose reduction of TARCEVA (erlotinib) should be considered if severe adverse reactions occur [see DRUG INTERACTIONS].

Pre-treatment with the CYP3A4 inducer rifampicin decreased erlotinib AUC by about 2/3 to 4/5. Use of alternative treatments lacking CYP3A4 inducing activity is strongly recommended. If an alternative treatment is unavailable, an increase in the dose of TARCEVA (erlotinib) should be considered as tolerated at two week intervals while monitoring the patient's safety. The maximum dose of TARCEVA (erlotinib) studied in combination with rifampicin is 450 mg. If the TARCEVA (erlotinib) dose is adjusted upward, the dose will need to be reduced immediately to the indicated starting dose upon discontinuation of rifampicin or other inducers. Other CYP3A4 inducers include, but are not limited to rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital and St. John's Wort. These too should be avoided if possible [see DRUG INTERACTIONS].

Cigarette smoking has been shown to reduce erlotinib exposure. Patients should be advised to stop smoking. If a patient continues to smoke, a cautious increase in the dose of TARCEVA (erlotinib) , not exceeding 300 mg may be considered, while monitoring the patient's safety. However, efficacy and long-term safety ( > 14 days) of a dose higher than the recommended starting doses have not been established in patients who continue to smoke cigarettes. If the TARCEVA (erlotinib) dose is adjusted upward, the dose should be reduced immediately to the indicated starting dose upon cessation of smoking [see CLINICAL PHARMACOLOGY].

Erlotinib is eliminated by hepatic metabolism and biliary excretion. Although erlotinib exposure was similar in patients with moderately impaired hepatic function (Child-Pugh B), patients with hepatic impairment (total bilirubin > ULN or Child-Pugh A, B and C) should be closely monitored during therapy with TARCEVA [see WARNINGS AND PRECAUTIONS]. Treatment with TARCEVA (erlotinib) should be used with extra caution in patients with total bilirubin > 3 x ULN. TARCEVA (erlotinib) dosing should be interrupted or discontinued if changes in liver function are severe such as doubling of total bilirubin and/or tripling of transaminases in the setting of pretreatment values outside normal range. In the setting of worsening liver function tests, before they become severe, dose interruption and/or dose reduction with frequent liver function test monitoring should be considered. TARCEVA (erlotinib) dosing should be interrupted or discontinued if total bilirubin is > 3 x ULN and/or transaminases are > 5 x ULN in the setting of normal pretreatment values [see WARNINGS AND PRECAUTIONS, ADVERSE REACTIONS and Use in Specific Populations].

Dosage Forms And Strengths

25 mg tablets

White film-coated tablets for daily oral administration. Round, biconvex face and straight sides, white film-coated, printed in orange with a “T” and “25” on one side and plain on the other side.

100 mg tablets

White film-coated tablets for daily oral administration. Round, biconvex face and straight sides, white film-coated, printed in gray with “T” and “100” on one side and plain on the other side.

150 mg tablets

White film-coated tablets for daily oral administration. Round, biconvex face and straight sides, white film-coated, printed in maroon with “T” and “150” on one side and plain on the other side.

Storage And Handling

25 mg Tablets

Round, biconvex face and straight sides, white film-coated, printed in orange with a “T” and “25” on one side and plain on the other side; supplied in: Bottles of 30: NDC 50242-062-01

100 mg Tablets

Round, biconvex face and straight sides, white film-coated, printed in gray with “T” and “100” on one side and plain on the other side; supplied in: Bottles of 30: NDC 50242-063-01

150 mg Tablets

Round, biconvex face and straight sides, white film-coated, printed in maroon with “T” and “150” on one side and plain on the other side; supplied in: Bottles of 30: NDC 50242-064-01

Store at 25°C (77°F); excursions permitted to 15° – 30°C (59° – 86°F). See USP Controlled Room Temperature.

Manufactured for: OSI Pharmaceuticals Inc., Melville, NY 11747. Manufactured by: Schwarz Pharma Manufacturing, Seymour, IN 47274. Distributed by: Genentech USA, Inc. 1 DNA Way, South San Francisco, CA 94080-4990. For further information please call 1-877-TARCEVA (erlotinib) (1-877-827-2382).

Last reviewed on RxList: 5/7/2010
This monograph has been modified to include the generic and brand name in many instances.