Extrahepatic metabolism by CYP3A4 in intestine, CYP1A1 in lung, and 1B1 in tumour tissue potentially contribute to the metabolic clearance of erlotinib.There are three main metabolic pathways identified: 1) O-demethylation of either side chain or both, followed by oxidation to the carboxylic acids; 2) oxidation of the acetylene moiety followed by hydrolysis to the aryl carboxylic acid; and 3) aromatic hydroxylation of the phenyl-acetylene moiety.

However the largest benefit was observed in a predefined exploratory analysis in patients with EGFR activating mutations (n= 49) demonstrating a substantial PFS benefit (HR=0.10, 95% CI, 0.04 to 0.25; p<0.0001 and an overall survival HR of 0.83 (95% CI, 0.34 to 2.02).

No new covariate effects were identified. The effect of erlotinib on overall survival was similar in patients with a baseline performance status (ECOG) of 2-3 (HR = 0.77, 95% CI 0.6-1.0) or 0-1 (HR = 0.73, 95% CI 0.6-0.9), male (HR = 0.76, 95% CI 0.6-0.9) or female patients (HR = 0.80, 95% CI 0.6-1.1), patients < 65 years of age (HR = 0.75, 95% CI 0.6-0.9) or older patients (HR = 0.79, 95% CI 0.6-1.0), patients with one prior regimen (HR = 0.76, 95% CI 0.6-1.0) or more than one prior regimen (HR = 0.75, 95% CI 0.6-1.0), Caucasian (HR = 0.79, 95% CI 0.6-1.0) or Asian patients (HR = 0.61, 95% CI 0.4-1.0), patients with adenocarcinoma (HR = 0.71, 95% CI 0.6-0.9) or squamous cell carcinoma (HR = 0.67, 95% CI 0.5-0.9), but not in patients with other histologies (HR 1.04, 95% CI 0.7-1.5), patients with stage IV disease at diagnosis (HR = 0.92, 95% CI 0.7-1.2) or < stage IV disease at diagnosis (HR = 0.65, 95% CI 0.5-0.8). However, an adverse effect on the fertility cannot be excluded as animal studies have shown effects on reproductive parameters (see section 5.3). Visit the MedicineNet does not provide medical advice, diagnosis or treatment.

The mechanism of action of erlotinib in terms of the exact effects on downstream receptor signaling or activation and mechanisms of resistance to the drug are still being elucidated.
Erlotinib hydrochloride (trade name Tarceva, Genentech/OSIP, originally coded as OSI-774) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer.Similar to gefitinib, erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase. In erlotinib-treated patients the median time to onset of rash was 10 days, and the median time to onset of diarrhea was 15 days.Liver test abnormalities including ALT elevations were observed at Grade 2 or greater severity in 3% of erlotinib-treated patients and 1% of placebo-treated patients. There have been rare reports of serious lung disease, including deaths, in patients receiving erlotinib for treatment of NSCLC or other tumors.The usual dose of erlotinib is 150 mg daily for NSCLC and 100 mg daily for CYP3A4 is an enzyme in the liver that breaks-down and helps to eliminate erlotinib from the body. Withhold erlotinib in patients with pre-existing hepatic impairment or biliary obstruction for doubling of bilirubin or tripling of transaminases values over baseline. The studies were negative for carcinogenic findings. While the complete mechanism of action is not entirely understood, the HER1 and EGFR receptors are directly involved in inter-cellular signalling in systems governing cell division and prolifferation. Patients with bullous and exfoliative skin disorders should be tested for skin infection and treated according to local management guidelines.Patients presenting with signs and symptoms suggestive of keratitis such as acute or worsening: eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain and/or red eye should be referred promptly to an ophthalmology specialist. Metastatic 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 … As the potential for harm to the nursing infant is unknown, mothers should be advised against breast-feeding while receiving erlotinib and for at least 2 weeks after the final dose.Studies in animals have shown no evidence of impaired fertility.


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