Alvoceva

Erlotinib HCl

1st-line treatment of locally advanced or metastatic NSCLC w/ epidermal growth factor receptor (EGFR) activating mutations. Switch maintenance treatment of locally advanced or NSCLC w/ EGFR activating mutations & stable disease after 1st-line chemotherapy. Locally advanced or metastatic NSCLC after failure of at least 1 prior chemotherapy regimen. In combination w/ gemcitabine for metastatic pancreatic cancer.

NSCLC 150 mg once daily. Smokers Max dose: 300 mg. Pancreatic cancer Combination w/ gemcitabine: 100 mg once daily. Dose adjustment: Reduce dose in 50 mg steps.

Should be taken on an empty stomach.

Hypersensitivity.

Discontinue in patients experiencing pulmonary toxicity; if ILD is diagnosed; if perforation & severe bullous, blistering or exfoliative disorders occur; confirmed ulcerative keratitis. Interrupt therapy in patients who develop acute onset of new &/or progressive unexplained pulmonary symptoms eg, dyspnoea, cough & fever; severe or persistent diarrhoea, nausea, anorexia, or vomiting associated w/ dehydration; severe changes in liver function. Increased risk of perforation in patients w/ history of PUD or diverticulitis & receiving concomitant therapy w/ anti-angiogenesis drugs, corticosteroids, NSAIDs &/or taxane-based chemotherapy. History of ulcerative keratitis or severe dry eye. Perform EGFR mutation testing prior to initiation of therapy in chemo-naïve patients w/ advanced or metastatic NSCLC. Advise current smokers to stop smoking. Treat moderate or severe diarrhoea w/ loperamide. Monitor renal function & serum electrolytes including K in patients at risk of dehydration. Consider periodic LFT. Galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. Concomitant use w/ gemcitabine; hepatotoxic medications. Avoid concomitant use w/ potent CYP3A4 inducers & inhibitors; PPIs, H₂ antagonists & antacids. Antacids should be taken at least 4 hr before or 2 hr after daily treatment dose. Not recommended in patients w/ severe hepatic & renal dysfunction. Women of childbearing potential should avoid pregnancy during therapy & use adequate contraceptive methods during & at least 2 wk after completing therapy. Pregnancy & lactation. Childn <18 yr.

Infection; anorexia, decreased wt; keratoconjunctivitis sicca, conjunctivitis; dyspnoea, cough; diarrhoea, nausea, vomiting, stomatitis, abdominal pain, dyspepsia, flatulence; rash, pruritus, dry skin, alopecia; fatigue, pyrexia, rigors; depression; neuropathy, headache; LFT abnormalities. Epistaxis; GI bleeding; paronychia, folliculitis, acne/dermatitis acneiform, skin fissures; renal insufficiency. SJS/TEN.

Increased exposure w/ moderate CYP1A2 inhibitor eg, ciprofloxacin. Concomitant use w/ potent CYP1A2 inhibitors (eg, fluvoxamine) & proteasome inhibitors (eg, bortezomib). Decreased oral bioavailability of midazolam. Increased serum bilirubin conc w/ UGT1A1 substrates. Decreased metabolism & increased plasma conc w/ potent CYP3A4 inhibitors eg, ketoconazole, itraconazole, voriconazole, PIs, erythromycin or clarithromycin. Increased metabolism & decreased plasma conc w/ potent CYP3A4 inducers eg, rifampicin. Reduced exposure w/ phenytoin, carbamazepine, barbiturates or St. John's wort (Hypericum perforatum). Increased INR & bleeding events w/ coumarin-derived anticoagulants including warfarin. Increased potential statin-induced myopathy including rhabdomyolysis. Altered distribution &/or elimination w/ P-gp inhibitors eg, cyclosporine & verapamil. Altered bioavailability w/ drugs that alter pH of upper GI tract. Decreased exposure & C_max w/ omeprazole & ranitidine. Increased total platinum AUC_0-48 w/ carboplatin & paclitaxel. Increased conc w/ capecitabine.

Targeted Cancer Therapy

L01EB02 - erlotinib ; Belongs to the class of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Used in the treatment of cancer.

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