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Erlotinib

Pronouncation: (er-LOE-tye-nib)
Class: Epidermal growth factor receptor inhibitor

Trade Names:
Tarceva
- Tablets 25 mg
- Tablets 100 mg
- Tablets 150 mg

Pharmacology

Feedback for Erlotinib

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Inhibits intracellular phosphorylation of tyrosine kinase associated with epidermal growth factor receptor.

Pharmacokinetics

Absorption

Approximately 60% after oral administration; increased to almost 100% by food.

Distribution

Approximately 93% protein bound to albumin and alpha-1 acid glycoprotein. Apparent Vd is 232 L.

Metabolism

Metabolized primarily by CYP3A4 and, to a lesser degree, by CYP1A2 and the extrahepatic isoform CYP1A1.

Elimination

About 83% excreted in feces and 8% in urine. The t _½ is about 36 h. Smokers had a 24% higher rate of Cl.

Indications and Usage

Treatment of locally advanced or metastatic nonsmall cell lung cancer (NSCLC) after failure of at least 1 prior chemotherapy regimen; first-line treatment of locally advanced, unresectable, or metastatic pancreatic cancer.

Unlabeled Uses

Treatment of squamous cell head and neck cancer.

Contraindications

Standard considerations.

Dosage and Administration

NSCLC
Adults

PO 150 mg at least 1 h before or 2 h after food. Continue treatment until disease progression or unacceptable toxicity occurs.

Pancreatic Cancer
Adults

PO 100 mg 1 h before or 2 h after food. Continue treatment until disease progression or unacceptable toxicity occurs.

Dose Modification
Adults

PO When dose reduction is necessary, decrease the dose in 50 mg decrements.

General Advice

May be used alone or in combination with other chemotherapy agents (except platinum-based chemotherapy).

Storage/Stability

Store tablets in at controlled room temperature (59° to 86°F).

Drug Interactions

CYP inducers (eg, carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine, St. John's wort)

May reduce erlotinib plasma concentrations, decreasing the therapeutic effect and necessitating dosage adjustments or changes in therapy.

Strong CYP3A4 inhibitors (eg, atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin, voriconazole)

May elevate erlotinib plasma concentrations, increasing the risk of adverse reactions and necessitating dosage reduction.

Warfarin

INR elevations and bleeding have been reported with erlotinib coadministration.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Pancreatic cancer treatment (erlotinib plus gemcitabine)

Arrhythmias, cerebrovascular accidents including cerebral hemorrhage, MI/ischemia, syncope (less than 5%).

CNS

NSCLS treatment (erlotinib alone)

Fatigue (52%).

Pancreatic cancer treatment (erlotinib plus gemcitabine)

Fatigue (73%); pyrexia (36%); depression (19%); dizziness, headache, insomnia (15%); anxiety, neuropathy (13%).

Dermatologic

NSCLS treatment (erlotinib alone)

Rash (75%); pruritus (13%); dry skin (12%).

Pancreatic cancer treatment (erlotinib plus gemcitabine)

Rash (69%); alopecia (14%).

EENT

NSCLS treatment (erlotinib alone)

Conjunctivitis, keratoconjunctivitis (12%); corneal ulcerations.

GI

NSCLS treatment (erlotinib alone)

Diarrhea (54%); anorexia (52%); nausea (33%); vomiting (23%); stomatitis (17%); abdominal pain (11%).

Pancreatic cancer treatment (erlotinib plus gemcitabine)

Nausea (60%); anorexia (52%); diarrhea (48%); abdominal pain (46%); vomiting (42%); constipation (31%); stomatitis (22%); dyspepsia (17%); flatulence (13%); ileus, pancreatitis (less than 5%).

Genitourinary

Pancreatic cancer treatment (erlotinib plus gemcitabine)

Renal insufficiency (less than 5%).

Hematologic-Lymphatic

Pancreatic cancer treatment (erlotinib plus gemcitabine)

Hemolytic anemia (less than 5%).

Lab Tests

NSCLS treatment (erlotinib alone)

Abnormal LFTs.

Metabolic-Nutritional

Pancreatic cancer treatment (erlotinib plus gemcitabine)

Weight decrease (39%).

Musculoskeletal

Pancreatic cancer treatment (erlotinib plus gemcitabine)

Bone pain (25%); myalgia (21%); rigors (12%).

Respiratory

NSCLS treatment (erlotinib alone)

Dyspnea (41%); cough (33%).

Pancreatic cancer treatment (erlotinib plus gemcitabine)

Cough (28%); dyspnea (25%).

Miscellaneous

NSCLS treatment (erlotinib alone)

Infection (24%).

Pancreatic cancer treatment (erlotinib plus gemcitabine)

Infection (39%); edema (37%).

Precautions

Monitor

Monitor patient for DERM, GI, OPHTH, RESP, and general body adverse reactions. Be prepared to reduce the dose or temporarily interrupt therapy if diarrhea unresponsive to loperamide develops, the patient becomes dehydrated, or if severe skin reactions are noted.

Pregnancy

Category D .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hepatic function impairment

Use with caution. Consider periodically evaluating liver function (eg, alkaline phosphatase, bilirubin, transaminases) during treatment with erlotinib. Consider erlotinib dose reduction (in 50 mg increments) or interruption of therapy if severe changes in liver function develop.

Pulmonary toxicity

Serious, sometimes fatal, interstitial lung disease has been reported. Monitor patient for acute onset or progression of pulmonary symptoms (eg, cough, dyspnea, fever). Interrupt therapy and notify health care provider. If diagnostic evaluation indicates interstitial lung disease, discontinue erlotinib and be prepared to institute appropriate treatment.

Overdosage

Symptoms

Diarrhea, liver transaminase elevations, rash.

Patient Information

Explain name, action, and potential side effects of the treatment regimen. Review the treatment regimen, including dosing schedule, duration of treatment, and monitoring that will be required.
Advise patient to take prescribed dose once daily, at least 1 h before or 2 h after meals or snacks.
Advise patient or caregiver to immediately report noted or significant side effects, including any of the following, to health care provider: severe or persistent diarrhea, nausea, appetite loss, or vomiting; eye irritation; new onset or worsening of unexplained shortness of breath or cough.
Caution woman of childbearing potential to avoid becoming pregnant during therapy. Advise patient to use effective contraceptive methods during and for 2 wk following completion of therapy.