Erlotinib, sold under the brand name Tarceva among others, is a medication used to treat non-small cell lung cancer (NSCLC) and pancreatic cancer.
Molar mass: | 393.436 g/mol |
CAS ID: | 183321-74-6 |
Formula: | C22H23N3O4 |
Other names: | Erlotinib hydrochloride |
US Brand: | Tarceva |
IN Brands (Generic): | Erlonat, Erlocip, Erlotib, Zyceva |
Manufacturers: | Roche, Natco, Cipla, Intas, Zydus |
Dosage Forms & Strengths: | 25mg, 100mg, 150mg |
Indicated for 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 as detected by an FDA-approved test receiving first-line, maintenance, or ≥second-line treatment after progression following at least 1 prior chemotherapy regimen
150 mg PO qDay 1 hr before or 2 hrs after meals
Continue until disease progression or unacceptable toxicity
NSCLC limitations of use
- Not recommended for use in combination with platinum-based chemotherapy
- Safety and efficacy has 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
Indicated for first-line treatment in patients with locally advanced, unresectable, or metastatic pancreatic cancer
100 mg/day PO with gemcitabine
Continue until disease progression or unacceptable toxicity
Decrease dose by 50 mg decrements
- Strong CYP3A4 inhibitors: Reduce by 50 mg decrements if severe reactions occur when coadministered with strong CYP3A4 inhibitors (eg, atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin, voriconazole, or grapefruit or grapefruit juice)
- CYP3A4 and CYP1A2 inhibitors: Avoid concomitant use if possible when coadministered with an inhibitor of both CYP3A4 and CYP1A2 (eg, ciprofloxacin)
- When restarting therapy following withholding treatment for a dose-limiting toxicity that has resolved to baseline or grade ≤1
Increase dose by 50 mg increments
- CYP3A4 inducers: Increase by 50 mg increments at 2 week intervals as tolerated to a maximum of 450 mg for concomitant use with CYP3A4 inducers (eg, rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, St. John’s Wort); if possible, avoid concomitant use
- Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg; immediately reduce dose to recommended dose (ie, 100 mg or 150 mg daily) upon smoking cessation
Drugs affecting gastric pH
- Proton pump inhibitors: Avoid coadministration if possible
- H2-antagonists: Take erlotinib 10 hr after or at least 2 hr before H2-anagonist
- Antacids: Separate erlotinib and antacid doses by several hours
Discontinue erlotinib for
- Interstitial lung disease (ILD) Severe hepatic toxicity that is unimproved or does not resolve
- GI perforation
- Severe bullous, blistering, or exfoliating skin conditions
- Corneal perforation or severe ulceration
Withhold erlotinib
- During diagnostic evaluation for ILD
- Severe renal toxicity (grades 3-4)
- Total bilirubin levels >3 xULN or transaminases >5 xULN in patients without pre-existing hepatic impairment
- In patients with pre-existing hepatic impairment for bilirubin 2 xULN or transaminases 3 xULN
- Persistent severe diarrhea or rash unresponsive to medical management
- Keratitis (grades 3-4, or grade 2 for >2 wk)
- Acute/worsening ocular disorders