Oral Locally advanced, unresectable pancreatic cancer, Metastatic pancreatic cancer
Adult: In combination with gemcitabine for 1st-line treatment: 100 mg once daily. Continue therapy until disease progression or unacceptable toxicity occurs. Dose reduction, dosing interruption, or discontinuation may be required if adverse reactions or toxicities occur (refer to detailed product guidelines).
Adult: As a 1st-line or maintenance treatment in patients with epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations and in those with disease progression after at least 1 prior chemotherapy regimen: 150 mg once daily. Continue therapy until disease progression or unacceptable toxicity occurs. Dose reduction, dosing interruption, or discontinuation may be required if adverse reactions or toxicities occur. Treatment recommendations may vary among countries and between individual products (refer to local or detailed product guidelines).
What are the brands available for Erlotinib in Philippines?
Patients taking potent CYP3A4 inhibitors (e.g. ketoconazole, voriconazole, clarithromycin, ritonavir, saquinavir, grapefruit juice): Avoid concomitant use whenever possible. If concomitant use is necessary, reduce the dose of erlotinib in 50 mg decrements, particularly if severe adverse reactions or toxicity occur.
Patients taking moderate or potent CYP3A4 inducers (e.g. rifampicin, phenytoin, carbamazepine, phenobarbital, St. John's wort): Avoid concomitant use whenever possible. If concomitant use is necessary, increase the dose of erlotinib in 50 mg increments at 2-week intervals as tolerated up to a Max of 450 mg daily.
Active cigarette smokers: Avoid smoking. If unavoidable, increase the dose of erlotinib in 50 mg increments at 2-week intervals up to a Max of 300 mg daily. Immediately decrease the erlotinib dose to the recommended initial dose upon smoking cessation.
Renal Impairment
Severe: Not recommended.
Hepatic Impairment
Severe: Not recommended.
Administration
Erlotinib Should be taken on an empty stomach.
Special Precautions
Patient with history of peptic ulceration or diverticular disease; history of keratitis, ulcerative keratitis or severe dry eye; genetic glucuronidation disorders (e.g. Gilbert's disease). Patients concomitantly receiving moderate or potent CYP3A4 inducers or potent CYP3A4 inhibitors. Cigarette smokers. Renal and hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Abnormal eyelash growth, decreased tear production, keratoconjunctivitis sicca or keratitis; diarrhoea (may lead to dehydration). Rarely, corneal perforation or ulceration, hypokalaemia; microangiopathic haemolytic anaemia with thrombocytopenia (in combination with gemcitabine). Cardiac disorders: Chest pain. Gastrointestinal disorders: Nausea, vomiting, abdominal pain, dyspepsia, flatulence, stomatitis, mucosal swelling. General disorders and administration site conditions: Fatigue, asthenia, pyrexia, rigors. Infections and infestations: Infections (including pneumonia, sepsis, and cellulitis). Investigations: Decreased weight, abnormal LFTs (including increased ALT, AST, and bilirubin). Metabolism and nutrition disorders: Anorexia. Musculoskeletal and connective tissue disorders: Arthralgia, back pain, musculoskeletal pain. Nervous system disorders: Headache, neuropathy. Psychiatric disorders: Depression. Respiratory, thoracic and mediastinal disorders: Dyspnoea, cough, epistaxis. Skin and subcutaneous tissue disorders: Rash, pruritus, dry skin, alopecia, paronychia, folliculitis, acne, dermatitis acneiform, skin fissures. Potentially Fatal: Interstitial lung disease, gastrointestinal perforation, CVA, MI, myocardial ischaemia. Rarely, acute renal failure; hepatic failure, hepatorenal syndrome; bullous, blistering and exfoliative skin reactions (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis).
Women of childbearing potential must use proven birth control methods during and for at least 2 weeks after treatment. Avoid breastfeeding during therapy and for at least 2 weeks after the last dose.
Monitoring Parameters
Confirm EGFR mutation status (presence of exon 19 deletions or exon 21 [L858R] substitution mutations) before treatment initiation in patients with non-small cell lung carcinoma. Monitor renal function, serum electrolytes (periodically); LFTs (periodically; more frequently if with preexisting hepatic impairment or biliary obstruction); prothrombin time and INR (when given concomitantly with warfarin). Assess for signs and symptoms of dermatologic, ocular and pulmonary toxicity.
Overdosage
Symptoms: Severe adverse reactions including diarrhoea, rash, and increased activity of liver aminotransferases. Management: Symptomatic treatment.
Drug Interactions
Increased risk of gastrointestinal perforation with corticosteroids, NSAIDs, anti-angiogenic agents, and taxane-based chemotherapy. Decreased plasma concentration with CYP3A4 inducers (e.g. rifampicin, phenytoin, carbamazepine, phenobarbital). Increased exposure with potent CYP3A4 inhibitors (e.g. ketoconazole, voriconazole, clarithromycin, ritonavir, saquinavir), moderate or potent inhibitors of CYP1A2 (e.g. ciprofloxacin, fluvoxamine), and capecitabine. Agents that alter the pH of gastrointestinal tract, including antacids, PPI (e.g. omeprazole), and H2-receptor antagonists (e.g. ranitidine), may decrease the solubility and bioavailability of erlotinib, resulting in reduced exposure. Increased risk of rhabdomyolysis with statins. Concomitant use with P-gp inhibitors (e.g. ciclosporin, verapamil) may cause alteration in distribution and/or elimination of erlotinib. Potentially Fatal: Increased INR and risk of bleeding events with coumarin-derived anticoagulants (e.g. warfarin).
Food Interaction
Increased bioavailability with food. Decreased plasma concentration with St. John's wort. May increase plasma concentration with grapefruit or grapefruit juice.
Action
Description: Mechanism of Action: Erlotinib, an antineoplastic agent, is a reversible human epidermal growth factor receptor type 1 (HER1)/epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. It potently inhibits the intracellular phosphorylation of tyrosine kinase associated with EGFR, preventing further downstream signalling and resulting in cell death. Pharmacokinetics: Absorption: Absorbed from the gastrointestinal tract. Bioavailability: Approx 100% (with food); approx 60% (without food). Time to peak plasma concentration: Approx 4 hours. Distribution: Crosses the placenta. Volume of distribution: 232 L. Plasma protein binding: Approx 93% to albumin and α1-acid glycoprotein. Metabolism: Metabolised in the liver mainly by CYP3A4 and to a lesser extent by CYP1A2; metabolic pathways include O-demethylation forming OSI-420 and OSI-413 (primary metabolites), oxidation and aromatic hydroxylation. Excretion: Via faeces (83%; 1% as unchanged drug), urine (8%; <1% as unchanged drug). Elimination half-life: 36.2 hours.
Chemical Structure
Erlotinib Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 176870, Erlotinib. https://pubchem.ncbi.nlm.nih.gov/compound/Erlotinib. Accessed June 26, 2025.
Storage
Store below 30°C. Follow applicable procedures for receiving, handling, administration and disposal.
L01EB02 - erlotinib ; Belongs to the class of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Used in the treatment of cancer.
References
Alchemy Health Limited. Erlotinib 25 mg, 50 mg, 100 mg and 150 mg Film Coated Tablets data sheet 26 April 2024. Medsafe. http://www.medsafe.govt.nz. Accessed 02/04/2025.Brayfield A, Cadart C (eds). Erlotinib Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/04/2025.Erlotinib Sandoz 150 mg Film-coated Tablets (Sandoz Limited). MHRA. https://products.mhra.gov.uk. Accessed 02/04/2025.Erlotinib Tablet, Film Coated (Camber Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/04/2025.Erlotinib. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 02/04/2025.Erlotinib. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 02/04/2025.Joint Formulary Committee. Erlotinib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/04/2025.Riltared 25 mg, 100 mg, and 150 mg Film-coated Tablets (Dr. Reddy's Laboratories Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/04/2025.
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