Ertinib100 mg

First-line 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 substitution mutations as detected.Maintenance treatment of patients with locally advanced or metastatic NSCLC whose ... Read moreFirst-line 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 substitution mutations as detected.Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.

Targeted Cancer Therapy

Ertinib 100 mg is an epidermal growth factor receptor/human epidermal growth factor receptor type 1 (EGFR/HER1) tyrosine kinase inhibitor. It reversibly inhibits the kinase activity of EGFR, preventing autophosphorylation of tyrosine residues associated w/ the receptor, thereby inhibiting further downstream signaling and resulting in cell death.

NSCLC: The recommended daily dose of Ertinib 100 mg 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.Pancreatic Cancer: The recommended daily dose of Ertinib 100 mg for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Ertinib 100 mg 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.Reduce Ertinib 100 mg by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).Increase Ertinib 100 mg by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Ertinib 100 mg to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.

Should be taken on an empty stomach. Take at least 1 hr before or 2 hr after meals.

Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.CYP3A4 inhibitors: Ertinib 100 mg is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Ertinib 100 mg AUC by 67%. When Ertinib 100 mg was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Ertinib 100 mg exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Ertinib 100 mg decreased Ertinib 100 mg AUC by 58% to 80%. Dose modifications are recommended.Drugs affecting gastric pH: Co-administration of Ertinib 100 mg with omeprazole decreased Ertinib 100 mg AUC by 46% and co-administration of Ertinib 100 mg with Ranitidine 300 mg decreased Ertinib 100 mg AUC by 33%.

Contraindicated in pregnancy, hypersensitivity

The most common adverse reactions (20%) with Ertinib 100 mg from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities. Interstitial Lung Disease (ILD) Renal Failure Hepatotoxicity with or without Hepatic Impairment Gastrointestinal Perforation Bullous and Exfoliative Skin Disorders Myocardial Infarction/Ischemia Cerebrovascular Accident Microangiopathic Hemolytic Anemia with Thrombocytopenia Ocular Disorders Hemorrhage in Patients Taking Warfarin

Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Ertinib 100 mg for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Ertinib 100 mg if ILD is diagnosed. Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Ertinib 100 mg for severe renal toxicity. Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Ertinib 100 mg for severe or worsening liver tests. Gastrointestinal perforations-discontinue Ertinib 100 mg. Bullous and exfoliative skin disorders-discontinue Ertinib 100 mg. Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.

Single oral doses of Ertinib 100 mg up to 1,000 mg in healthy subjects and weekly doses up to 1,600 mg in cancer patients have been tolerated. Repeated twice-daily doses of 200 mg single-agent Ertinib 100 mg in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, an unacceptable incidence of severe adverse reactions, such as diarrhea, rash, and liver transaminase elevation, may occur above the recommended dose. In case of suspected overdose, Ertinib 100 mg should be withheld and symptomatic treatment instituted.

Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.

Targeted Cancer Therapy

Pregnancy category D. Based on its mechanism of action, Ertinib 100 mg can cause fetal harm when administered to a pregnant woman. It is not known whether Ertinib 100 mg is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Ertinib 100 mg, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric use: The safety and effectiveness of Ertinib 100 mg in pediatric patients have not been established.Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.