Erlotinib

Indications
 Oral
Locally advanced or metastatic non small cell lung carcinoma
Adult: In patients who have failed at least one prior chemotherapy regimen: 150 mg once daily. Maintenance: 150 mg once daily. Reduce in steps of 50 mg when necessary. Continue treatment until disease progression or unacceptable toxicity occurs. May require dose modifications when coadministered with strong CYP3A4 inhibitors or inducers; or in cigarette smoking patients.
Oral
Locally advanced, unresectable or metastatic pancreatic cancer
Adult: As 1st-line treatment with gemcitabine: 100 mg once daily, reduce dose in steps of 50 mg when necessary. May require dose modifications when coadministered with strong CYP3A4 inhibitors or inducers; or in cigarette-smoking patients.
Warnings / Precautions
 Pregnancy and lactation. Interrupt Erlotinib therapy if patient develops unexplained pulmonary symptoms e.g. dyspnoea, cough, fever; discontinue therapy if interstitial lung disease is diagnosed. Monitor liver functions periodically; extreme caution is needed if total bilirubin is 3x >ULN; close monitoring is required in patients with hepatic impairment. Interrupt/discontinue therapy if severe changes in liver functions (doubling of total bilirubin and/or tripling of transaminases) occur. Interrupt therapy in the event of dehydration especially in patients with predisposing factors to renal failure. Monitor renal function and serum electrolytes in patients at risk of dehydration. Interrupt or discontinue therapy if patient develops severe bullous and exfoliative skin disorders; eye pain or other acute/worsening ocular disorders. If patient develops GI perforation, discontinue therapy permanently. Patients with CV disorders. Monitor prothrombin time/INR in patients taking warfarin or other coumarin-derivative anticoagulants.
Adverse Reactions
 Adverse reactions reported with monotherapy: Fatigue, diarrhoea, anorexia, nausea, abdominal pain, stomatitis, weight loss, rash, pruritus, acne, dermatitis acneiform, dry skin, cough, dyspnoea, infection, conjunctivitis, conjunctivitis sicca, liver function test abnormalities. Adverse reactions reported when used with gemcitabine: Fatigue, rash, nausea, anorexia, diarrhoea, abdominal pain, vomiting, weight decreased, infection, oedema, pyrexia, constipation, bone pain, dyspnoea, stomatitis, myalgia, depression, dyspepsia, cough, dizziness, headache, insomnia, alopecia, anxiety, neuropathy, flatulence, rigors.
Overdose Reactions
 Incidence of severe adverse reactions e.g. diarrhoea, rash, liver transaminases elevation may occur above the recommended dose.
Drug Interactions
 Increased exposure (AUC) when used with ketoconazole, or other strong CYP3A4 inhibitors e.g. atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin, voriconazole, grapefruit or grapefruit juice. Increased exposure and Cmax when coadministered with ciprofloxacin (CYP3A4 and CYP1A2 inhibitor). CYP3A4 inducers e.g. rifampicin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital and St. John's Wort may reduce exposure of Erlotinib. Pretreatment and concurrent use of Erlotinib may decrease AUC of midazolam. Concurrent use with drugs that alter pH of the upper GI tract e.g. omeprazole, ranitidine may alter solubility and reduce Erlotinib bioavailability. Reduced exposure in cigarette-smoking patients.
Potentially Fatal: Immunosuppressants may enhance the adverse effects of live vaccines or diminish the therapeutic effect of live vaccines.
See Below for More erlotinib Drug Interactions
Food Interactions
 Bioavailability is increased with food. Avoid grapefruit/grapefruit juice.
Mechanism of Actions
 Exact mechanism of antitumour action is not fully understood. Erlotinib inhibits intracellular phosphorylation of tyrosine kinase associated with epidermal growth factor receptor.
Absorption: Solubility decreases as pH increases. Bioavailability: About 60%; increased to almost 100% by food. Tmax: 4 hr. Time to reach steady-state: 7-8 days.
Distribution: Apparent Vd: 232 L. Protein binding: About 93% to plasma albumin and α-1 acid glycoprotein.
Metabolism: Metabolised predominantly by CYP3A4, to a lesser extent by CYP1A2 and extrahepatic isoform CYP1A1. Metabolic pathways include demethylation, oxidation and aromatic hydroxylation.
Excretion: Median half-life: Approximately 36.2 hr. Eliminated primarily by hepatic metabolism and biliary excretion. About 83% excreted in faeces (1% as unchanged drug); 8% in urine.
Administration
 Should be taken on an empty stomach. (Take on an empty stomach at least 1 hr before or 2 hr after meals.)
Storage Conditions
 Oral: Store at 25°C (77°F); excursions permitted to 15-30°C (59- 86°F).
ATC Classification
 L01XE03 - erlotinib ; Belongs to the class of protein kinase inhibitors, other antineoplastic agents. Used in the treatment of cancer.
Storage
 Oral: Store at 25°C (77°F); excursions permitted to 15-30°C (59- 86°F).
Available As
  • Erlotinib 150 mg

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