Presentation

Erlocent 100: Each tablet contains Erlotinib Hydrochloride INN equivalent to Erlotinib 100 mg.

Erlocent 150: Each tablet contains Erlotinib Hydrochloride INN equivalent to Erlotinib 150 mg.

Description

Erlotinib, a kinase inhibitor, is a quinazolinamine with the chemical name N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)4-quinazolinamine. Erlotinib reversibly inhibits the kinase activity of EGFR, preventing autophosphorylation of tyrosine residues associated with the receptor and thereby inhibiting further downstream signaling. Erlotinib binding affinity for EGFR exon 19 deletion or exon 21 (L858R) mutations is higher than its affinity for the wild type receptor. Erlotinib inhibition of other tyrosine kinase receptors has not been fully characterized.

Indications

Erlotinib is a kinase inhibitor indicated for:

Non-small cell lung cancer (NSCLC)

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 receiving first-line, maintenance or second or greater line treatment after progression following at least one prior chemotherapy regimen

Pancreatic cancer

First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with Gemcitabine

Limitations of Use

Erlotinib is not recommended for use in combination with platinum-based chemotherapy

Safety and efficacy of Erlotinib have not been evaluated as first-line treatment in patients with metastatic NSCLC whose tumors have EGFR mutations other than exon 19 deletions or exon 21 (L858R) substitution

Dosage & Administration

Non-small cell lung cancer (NSCLC): The recommended daily dose of Erlotinib for NSCLC is 150 mg.

Pancreatic cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine.

Erlotinib should be taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should be continued until disease progression or unacceptable toxicity occurs.

Side Effects

The most common adverse reactions were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting.

Precautions

Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Erlotinib should be withheld for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Erlotinib should be discontinued if ILD is diagnosed

Renal Failure: Renal function and electrolytes should be monitored, particularly in patients at risk of dehydration. Erlotinib should be withheld for severe renal toxicity

Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Periodic liver testing should be monitored. Erlotinib should be withheld or discontinued for severe or worsening liver tests

Gastrointestinal perforations: Erlotinib should be discontinued

Bullous and exfoliative skin disorders: Erlotinib should be discontinued

Myocardial infarction (MI)/ischemia: The risk of MI is increased in patients with pancreatic cancer

Cerebrovascular accident (CVA): The risk of CVA is increased in patients with pancreatic cancer

Microangiopathic hemolytic anemia (MAHA): The risk of MAHA is increased in patients with pancreatic cancer

Ocular disorders: Erlotinib should be discontinued for corneal perforation, ulceration or persistent severe keratitis

Hemorrhage in patients taking Warfarin: INR should be monitored in patients taking warfarin or other coumarin-derivative anticoagulants

Embryo-Fetal Toxicity: Can cause fetal harm. Females should be advised of reproductive potential of potential risk to the fetus and to use highly effective contraception

Use in Pregnancy & Lactation

Pregnancy

Pregnancy Category D. Erlotinib can cause fetal harm when administered to a pregnant woman. If Erlotinib is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to a fetus.

Nursing Mothers

It is not known whether Erlotinib 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 Erlotinib, 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 Erlotinib in pediatric patients have not been established.

Use in Females

Patients should be advised on pregnancy planning and prevention. Females patients should be advised of reproductive potential to use highly effective contraception during treatment with Erlotinib, and for at least 2 weeks after the last dose of Erlotinib. Females patients should be advised to contact their healthcare provider if they become pregnant, or if pregnancy is suspected, while taking Erlotinib.

Hepatic Impairment

Patients with hepatic impairment (total bilirubin > upper limit of normal (ULN) or Child-Pugh A, B and C) should be closely monitored during therapy with Erlotinib. Treatment with Erlotinib should be used with extra caution in patients with total bilirubin > 3 x ULN

Renal Impairment

Less than 9% of a single dose is excreted in the urine. No clinical studies have been conducted in patients with compromised renal function.

Drug Interaction

CYP3A4 inhibitors increase Erlotinib plasma concentrations

CYP3A4 inducers decrease Erlotinib plasma concentrations

Drugs affecting gastric pH decrease Erlotinib plasma concentrations

Cigarette smoking decreases Erlotinib plasma concentrations

Commercial Pack

Erlocent 100: Each box contains 1 blister strip of 10 tablets.

Erlocent 150: Each box contains 1 blister strip of 10 tablets.