Erlotinib

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

Pharmacology

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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 half-life is about 36 h. Smokers had a 24% higher rate of Cl.

Special Populations

Less than 9% is excreted in the urine.

Primarily cleared by the liver. Use with caution in patients with bilirubin levels 3 times ULN.

Indications and Usage

As monotherapy for the treatment of locally advanced or metastatic non–small cell lung cancer (NSCLC) after failure of at least 1 prior chemotherapy regimen. In combination with gemcitabine as 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

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

PO 100 mg 1 h before or 2 h after food, in combination with gemcitabine. Continue treatment until disease progression or unacceptable toxicity occurs.

PO When dose reduction is necessary, reduce the dose in 50 mg increments. In patients who develop an acute onset of new or progressive pulmonary symptoms (eg, cough, dyspnea, fever), interrupt treatment pending diagnostic evaluation. If interstitial lung disease is diagnosed, discontinue erlotinib and institute appropriate treatment. Patients who become dehydrated or who develop severe skin reactions may require dose reduction or temporary interruption of therapy. In patients receiving a strong CYP3A4 inhibitor, consider a dose reduction. In patients receiving CYP3A4 inducers, alternative treatment lacking CYP3A4 inducing activity is strongly recommended. If an alternative is unavailable, consider increasing the dose of erlotinib, as tolerated, at 2-wk intervals. Reduce the erlotinib dose immediately after discontinuing the CYP3A4 inducer.

Storage/Stability

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

Drug Interactions

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

Avoid coadministration of erlotinib and proton pump inhibitors. Separate erlotinib and antacid dosing by several hours.

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

INR elevations and bleeding have been reported with erlotinib coadministration.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

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

CNS

Fatigue (52%).

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

Dermatologic

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

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

EENT

Conjunctivitis, keratoconjunctivitis (12%); corneal ulcerations; epistaxis, hair and nail disorders including alopecia, brittle and loose nails, eyebrow/eyelash changes, hirsutism, inflammation of the nail fold with separation from the skin (postmarketing).

GI

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

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

Genitourinary

Renal insufficiency (less than 5%); acute renal failure, renal insufficiency including death (postmarketing).

Hematologic-Lymphatic

Hemolytic anemia (less than 5%); deep vein thrombosis (4%).

Hepatic

Hepatic failure (postmarketing).

Lab Tests

Abnormal LFTs.

Elevated ALT (31%); elevated AST (24%); elevated bilirubin (17%).

Metabolic-Nutritional

Weight decrease (39%).

Musculoskeletal

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

Respiratory

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

Dyspnea (24%); cough (16%).

Miscellaneous

Infection (24%).

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

Precautions

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.

Hepatotoxicity

Hepatic failure and hepatorenal syndrome (including fatalities) have been reported, particularly in patients with baseline hepatic impairment.

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). If diagnostic evaluation indicates interstitial lung disease, discontinue erlotinib and be prepared to institute appropriate treatment.

Renal failure

Hepatorenal syndrome, acute renal failure, and renal insufficiency have been reported, in some cases associated with severe dehydration due to diarrhea, vomiting, and/or anorexia or concomitant chemotherapy.

Overdosage

Symptoms

Diarrhea, liver transaminase elevations, rash.

Patient Information

• Explain name, action, and potential adverse reactions 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 adverse reactions to health care provider, including any of the following: eye irritation; new onset or worsening of unexplained shortness of breath or cough; severe or persistent diarrhea, nausea, appetite loss, or vomiting.
• 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.

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