ERLOTINIB HYDROCHLORIDE

ERLOTINIB HYDROCHLORIDE — erlotinib hydrochloride tablet, film coated
Alembic Pharmaceuticals Limited

1 INDICATIONS AND USAGE

1.1 Non-Small Cell Lung Cancer (NSCLC)

Erlotinib tablets are indicated 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 as detected by an FDA-approved test receiving first-line, maintenance, or second or greater line treatment after progression following at least one prior chemotherapy regimen [see Clinical Studies (14.1, 14.3)].

Limitations of use:

  • Safety and efficacy of erlotinib tablets have not been established in patients with NSCLC whose tumors have other EGFR mutations [see Clinical Studies (14.1, 14.2)].
  • Erlotinib tablets are not recommended for use in combination with platinum-based chemotherapy [see Clinical Studies (14.4)].

1.2 Pancreatic Cancer

Erlotinib tablet in combination with gemcitabine is indicated for the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer [see Clinical Studies (14.5)].

2 DOSAGE AND ADMINISTRATION

2.1 Selection of Patients with Metastatic NSCLC

Select patients for the treatment of metastatic NSCLC with erlotinib tablets based on the presence of EGFR exon 19 deletions or exon 21 (L858R) substitution mutations in tumor or plasma specimens [See Clinical Studies (14.1, 14.2)]. If these mutations are not detected in a plasma specimen, test tumor tissue if available. Information on FDA-approved tests for the detection of EGFR mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics.

2.2 Recommended Dose – NSCLC

The recommended daily dose of erlotinib tablets 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. Treatment should continue until disease progression or unacceptable toxicity occurs.

2.3 Recommended Dose – Pancreatic Cancer

The recommended daily dose of erlotinib tablets for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take erlotinib tablets on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs [see Clinical Studies (14.5)].

2.4 Dose Modifications

Adverse Reactions
Pulmonary Interstitial Lung Disease (ILD) Discontinue erlotinib tablets
During diagnostic evaluation for possible ILD Withhold erlotinib tablets*
Hepatic Severe hepatic toxicity that does not improve significantly or resolve within three weeks Discontinue erlotinib tablets
In patients with pre-existing hepatic impairment or biliary obstruction for doubling of bilirubin or tripling of transaminases values over baseline Withhold erlotinib tablets* and consider discontinuation
In patients without pre-existing hepatic impairment for total bilirubin levels greater than 3 times the upper limit of normal or transaminases greater than 5 times the upper limit of normal Withhold erlotinib tablets* and consider discontinuation
Renal For severe (CTCAE grade 3 to 4) renal toxicity Withhold erlotinib tablets* and consider discontinuation
Gastrointestinal Gastrointestinal perforation Discontinue erlotinib tablets
For persistent severe diarrhea not responsive to medical management (e.g., loperamide) Withhold erlotinib tablets*
Skin Severe bullous, blistering or exfoliating skin conditions Discontinue erlotinib tablets
For severe rash not responsive to medical management Withhold erlotinib tablets*
Ocular Corneal perforation or severe ulceration Discontinue erlotinib tablets
For keratitis of (NCI-CTC version 4.0) grade 3 to 4 or for grade 2 lasting more than 2 weeks Withhold erlotinib tablets*
For acute/worsening ocular disorders such as eye pain Withhold erlotinib tablets* and consider discontinuation
Drug Interactions
CYP3A4 inhibitors If severe reactions occur with concomitant use of strong CYP3A4 inhibitors [such as atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin (TAO), voriconazole, or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., ciprofloxacin) Reduce erlotinib tablets by 50 mg decrements; avoid concomitant use if possible
CYP3A4 inducers Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John’s Wort Increase erlotinib tablets by 50 mg increments at 2-week intervals to a maximum of 450 mg as tolerated. Avoid concomitant use if possible
Concurrent Cigarette Smoking ठConcurrent cigarette smoking Increase erlotinib tablets by 50 mg increments at 2-week intervals to a maximum of 300 mg. Immediately reduce the dose of erlotinib tablets to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking
Proton Pump inhibitors Separation of doses may not eliminate the interaction since proton pump inhibitors affect the pH of the upper GI tract for an extended period Avoid concomitant use if possible
H2 -receptor antagonists If treatment with an H2 -receptor antagonist such as ranitidine is required, separate dosing. Erlotinib tablets must be taken 10 hours after the H2 -receptor antagonist dosing and at least 2 hours before the next dose of the H2 ­ receptor antagonist
Antacids The effect of antacids on erlotinib pharmacokinetics has not been evaluated. The antacid dose and the erlotinib tablets dose should be separated by several hours, if an antacid is necessary

For additional information see Warnings and Precautions (5).

* Reduce erlotinib tablets by 50 mg decrements when restarting therapy following withholding treatment for a dose-limiting toxicity that has resolved to baseline or grade ≤ 1.

For additional information see Drug Interactions (7).

§ For additional information see Clinical Pharmacology (12.3).

3 DOSAGE FORMS AND STRENGTHS

Erlotinib tablets are available in the following strengths:

Erlotinib tablets 25 mg are round, biconvex, white film-coated tablet debossed with “L55” on one side and plain on other side.

Erlotinib tablets 100 mg are round, biconvex, white film-coated tablet debossed with “L630” on one side and plain on other side.

Erlotinib tablets 150 mg are round, biconvex, white film-coated tablet debossed with “L631” on one side and plain on other side.

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