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Erlotinib information from DrugsUpdate  

See Available Brands of Erlotinib in India

Erlotinib is a first-line drug for the treatment of metastatic non-small cell lung cancer (NSCLC) which is either locally advanced or metastatic in nature. Erlotinib is indicated for patients who did not respond to at least one chemotherapy regimen. Erlotinib is also used as combined therapy with Gemcitabine as a first-line therapy for the treatment of locally-advanced, inoperable or metastatic pancreatic cancer.

Pharmacodynamics

Erlotinib reversibly inhibits the enzymatic activity of kinase in Epidermal growth factor receptor (EGFR) and thereby prevents autophosphorylation of receptor tyrosine residues and downstream signalling. The binding activity of Erlotinib against mutated (Exon 19 deletions or Exon 21 L858R) receptor is higher than the wild type receptors.

Pharmacokinetics

The oral bioavailability of Erlotinib is about 60% with an increase to 100% if taken with food. The peak plasma level is achieved after 4 hours, and solubility of the drug is pH-dependent. About 93% of Erlotinib is bound to plasma protein and alpha-1 acid glycoprotein. The Vss of Erlotinib is 232 litres. The time required to reach plasma steady state concentration is 7-8 days with a half-life of 36.2 hours. Erlotinib is believed to be metabolized via CYP3A4, CYP1A2 and CYP1A1. Erlotinib is mostly eliminated via feces and by urine to some extent. 

Erlotinib Indications / Erlotinib Uses

Information not available

Erlotinib Adverse Reactions / Erlotinib Side Effects

Erlotinib can cause chest pain, rapid breathing, shortness of breath, fatigue, rapid weight gain, jaundice-like symptoms, malena, mood changes, profuse sweating, mood changes, anuria, diarrhoea, anorexia, acne, fatigue, GI upset, dry skin and nausea.

Precautions

Erlotinib is contraindicated in patients with lung cancer, liver diseases, renal disorders, dehydration and in individuals with smoking habits.

Special Precautions

Information not available

Other Drug Interactions

Erlotinib may interact with isoniazid, imatinib, corticosteroids, St. John’s wort, ciprofloxacin, erythromycin, anti-fungal drugs, barbiturates, bosentan, boceprevir, nicardipine, warfarin, nefazodone, quinidine, armodafinil, atazanavir, NSAIDs, phenytoin and carbamazepine.

Other Interactions

Information not available

Dosage

Non-Small Cell Lung Cancer (Adults):
Start with an initial dose of 150 mg, once daily. Erlotinib treatment should be continued until the progression of disease or tolerance.
Pancreatic Cancer (Adults):
Start with an initial dose of 150 mg, once daily. Erlotinib treatment should be continued until the progression of disease or tolerance.

Food(before/after)

Erlotinib should be preferably taken at least one or two hours before food intake

List of Contraindications

Erlotinib and Pregnancy

Contraindicated in pregnancy
USFDA pregnancy category D. Erlotinib can harm the unborn fetus. Perform pregnancy tests before using Erlotinib. Use effective contraceptive modes to prevent unintended pregnancies while taking Erlotinib.

Erlotinib and Lactation

Nursing mothers should consult the healthcare provider before Erlotinib treatment.

Erlotinib and Children

Information not available

Erlotinib and Geriatic

Information not available

Erlotinib and Other Contraindications

Information not available

Storage

Store at 20-25°C.

Lab interference

Store at 20-25°C.

Erlotinib brands in India:

Erleva Erlocip Erlotec Lortinib Tarceva

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