sorafenib

CLINICAL USE

Treatment of advanced renal cell carcinoma

DOSE IN NORMAL RENAL FUNCTION

400 mg twice daily

PHARMACOKINETICS

Molecular weight :464.8 (637 as tosylate)

%Protein binding :99.5

%Excreted unchanged in urine : 0

Volume of distribution (L/kg) :No data

half-life – normal/ESRD (hrs) :25–48

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

30–50 Dose as in normal renal function10–30 Dose as in normal renal function

<10 : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Unlikely to be dialysed. Dose as in GFR <10 mL/min

HD :Unlikely to be dialysed. Dose as in GFR <10 mL/min

HDF/high flux :Unlikely to be dialysed. Dose as in GFR <10 mL/min

CAV/VVHD :Unlikely to be dialysed. Dose as in GFR=10–30 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anticoagulants: may enhance effect of coumarins

Antipsychotics: avoid concomitant use with clozapine (increased risk of agranulocytosis)

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

–

Comments

Administer preferably without food

OTHER INFORMATION

Increased amylase and lipase and hypophosphataemia are commonMost common side effects are diarrhoea and dermatological effectsSorafenib is metabolised primarily in the liver and undergoes oxidative metabolism mediated by CYP3A4, as well as glucuronidation mediated by UGT1A9Following oral administration of a 100 mg dose of a solution formulation of sorafenib, 96% of the dose was recovered within 14 days, with 77% of the dose excreted in faeces, and 19% of the dose excreted in urine as glucuronidated metabolites. Unchanged sorafenib, accounting for 51% of the dose, was found in faeces but not in urine, indicating that biliary excretion of unchanged drug might contribute to the elimination of sorafenibA case report of interstitial nephritis has been reported in a patient with CRF due to FSGS.

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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