Tarceva

Tarceva is the brand name for erlotinib, an oral tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR). By binding to the ATP-binding site of the EGFR catalytic domain, erlotinib blocks receptor phosphorylation and downstream signaling, reducing tumor cell proliferation and promoting apoptosis in cancers with EGFR activation or overexpression.

Indications and use vary by country. In many regions, Tarceva is approved for metastatic pancreatic cancer in combination with gemcitabine. In non-small cell lung cancer (NSCLC), it is used for patients whose disease has progressed after prior chemotherapy and, in some settings, as first-line therapy for NSCLC in patients with activating EGFR mutations (such as exon 19 deletions or L858R). The choice of use often depends on EGFR mutation testing and clinical guidelines.

Administration and dosing are by mouth once daily. Dose and duration depend on the indication and tolerability. Caution is advised with certain drug interactions and conditions: erlotinib is metabolized by CYP3A4, so strong CYP3A4 inhibitors or inducers can alter exposure; avoidance of grapefruit juice is commonly recommended; proton pump inhibitors may reduce absorption in some patients. Dose adjustments may be needed for liver impairment or significant adverse effects.

Common adverse effects include rash and diarrhea, with other frequent symptoms such as nausea, reduced appetite, fatigue, and dry skin. Serious but less frequent risks include interstitial lung disease, hepatotoxicity, and ocular or ocular-surface toxicity. Rare severe cutaneous reactions can occur. Monitoring liver function, skin reactions, and overall tolerability is standard during therapy.

History notes: Tarceva was developed by Genentech/Roche and received FDA approval for NSCLC after chemotherapy failure (2004) and pancreatic cancer with gemcitabine (2005), with later expansion to EGFR-mutant NSCLC in some regimens. Generic erlotinib is available in many markets.