Tarceva 100 mg Generic Tablet

(erlotinib) Tablets

DESCRIPTION

TARCEVA (erlotinib), a kinase inhibitor, is a quinazolinone with the chemical name N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)4-quinazolinamine. TARCEVA contains erlotinib as the hydrochloride salt that has the following structural formula:

 

Erlotinib hydrochloride has the molecular formula C₂₂H₂₃N₃O₄.HCl and a molecular weight of 429.90. The molecule has a pKa of 5.42 at 25°C. Erlotinib hydrochloride is very slightly soluble in water, slightly soluble in methanol and practically insoluble in acetonitrile, acetone, ethyl acetate and hexane.

Aqueous solubility of erlotinib hydrochloride is dependent on pH with increased solubility at a pH of less than 5 due to protonation of the secondary amine. Over the pH range of 1.4 to 9.6, maximal solubility of approximately 0.4 mg/mL occurs at a pH of approximately 2.

TARCEVA tablets for oral administration are available in three dosage strengths containing erlotinib hydrochloride (27.3 mg, 109.3 mg and 163.9 mg) equivalent to 25 mg, 100 mg and 150 mg erlotinib and the following inactive ingredients: lactose monohydrate, hypromellose, hydroxypropyl cellulose, magnesium stearate, microcrystalline cellulose, sodium starch glycolate, sodium lauryl sulfate and titanium dioxide. The tablets also contain trace amounts of color additives, including FD&C Yellow #6 (25 mg only) for product identification.

Non-Small Cell Lung Cancer (NSCLC)

TARCEVA® Is 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].

Limitations Of Use

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

Pancreatic Cancer

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