Erlotinib

CLINICAL USE

Antineoplastic agent:Treatment of locally advanced or metastatic non-small cell lung cancer after failure of at least 1 other regime

DOSE IN NORMAL RENAL FUNCTION

150 mg daily at least 1 hour before or 2 hours after foodOr see local protocol

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :429.9 (as hydrochloride)

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :93–95

%Excreted unchanged in urine &nbsp &nbsp : 9 (<2% as unchanged drug)

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :232 litres

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :36

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function 15–20 Dose as in normal renal function<15 Use with caution

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unlikely to be dialysed. Dose as in GFR<15 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unlikely to be dialysed. Dose as in GFR<15 mL/min

HDF/high flux &nbsp :Unlikely to be dialysed. Dose as in GFR<15 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Unlikely to be dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Analgesics: increased risk of bleeding with NSAIDs

Anticoagulants: increased risk of bleeding with coumarins

Antipsychotics: avoid concomitant use with clozapine, increased risk of agranulocytosis

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Has not been tried in patients with a GFR<15 mL/min; therefore use with caution, but drug has limited renal excretionMajor side effects are rash and diarrhoea Can cause interstitial lung disease and abnormal liver function testsSmoking may reduce erlotinib concentration by increasing clearance.

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