Classifications: antineoplastic agent; tyrosine kinase inhibitor; multi-kinase inhibitor; Therapeutic:antineoplastic; multi-kinase inhibitor
Pregnancy Category: D
200 mg tablets
Sorafenib is a multi-kinase inhibitor targeting enzyme systems in both tumor cells and tumor vasculature. The anticancer
activity of sorafenib appears to be cytostatic, requiring continued drug exposure for tumor growth inhibition.
Sorafenib inhibits enzymes responsible for uncontrolled tumor cellular proliferation and angiogenesis. Antineoplastic activity
of sorafenib inhibits the growth of renal cell cancers.
Treatment of advanced renal cell cancer.
Treatment of advanced malignant melanoma. Treatment of metastatic hepatocellular cancer.
Active infection; severe renal impairment (<30 mL/min), or hemodialysis; pregnancy (category D), lactation. Safe use in
children <18 y is not established.
Previous myelosuppressive therapy, either radiation or chemotherapy; mild or moderate renal disease; hepatic disease; heart
failure, ventricular dysfunction, cardiac disease, peripheral edema; females of childbearing age.
Route & Dosage
|Renal Cell Cancer
Adult: PO 400 mg b.i.d.
Dosage Adjustments for Skin Toxicity
Grade 2 (1st episode): Continue therapy and treat symptoms. If no improvement in 7 d, DC until toxicity resolves to at least grade 1, then resume
with 400 mg/d or 400 mg q.o.d.
Grade 2 (2nd or 3rd episode): DC until toxicity resolves to at least grade 1, then resume with 400 mg/d or 400 mg q.o.d.
Grade 2 (4th episode): DC therapy.
Grade 3 (1st or 2nd episode): DC until toxicity resolves to at least grade 1, then resume with 400 mg/d or 400 mg q.o.d.
Grade 3 (3rd episode): DC therapy.
- Tablets must be swallowed whole. They should not be crushed, broken, or chewed.
- Give on an empty stomach 1 h before or 2 h after eating.
- Store at 15°30° C (59°86° F). Protect from moisture.
Adverse Effects (≥1%)Body as a Whole:
Asthenia, bone pain, decreased appetite, fatigue,
influenza-like illness, joint pain,
mouth pain, muscle pain, pyrexia. CNS: Depression
, headache, sensory neuropathy. CV: Hypertension. GI: Abdominal pain, anorexia, constipation, diarrhea,
dyspepsia, dysphagia, mucositis, nausea,
stomatitis, vomiting. Hematologic: Anemia, hemorrhage, leukopenia, lymphopenia, neutropenia, thrombocytopenia. Metabolic: Amylase elevation, hypophosphatemia, lipase elevation, weight loss. Musculoskeletal:
Arthralgia, myalgia. Respiratory: Cough, dyspnea,
hoarseness. Skin: Acne
, alopecia, desquamation, dry skin,
erythema, exfoliative dermatitis, flushing, hand-foot skin reaction, rash. Urogenital:
Sorafenib may increase levels of drugs requiring glucuronidation by the UGT1A1 and UGT1A9 pathways (e.g., irinotecan
). Due to thrombocytopenic effects, sorafenib can contribute to increased bleeding from nonsteroidal antiinflammatory drugs
, platelet inhibitors
(e.g., aspirin, clopidogrel
), thrombolytic agents
, and warfarin.
Inducers of CYP3A4 (e.g., carbamazepine, phenobarbital, phenytoin, rifampin
) may decrease the levels of sorafenib. Food:
Food decreases the absorption of sorafenib. Herbal: St. John's wort
may decrease the levels of sorafenib.
3849% absorbed. Peak:
3 h. Distribution:
99.5% protein bound. Metabolism:
In the liver. Elimination:
Primarily fecal (77%) with minor elimination in the urine (19%). Half-Life:
Assessment & Drug Effects
- Monitor for and report S&S of skin toxicity (e.g., rash, erythema, dermatitis, paresthesia, swelling, or pain in hands or
feet). Severe reactions may require temporary suspension of therapy or dose reduction.
- Monitor for S&S of bleeding, especially in those on anticoagulation therapy.
- Monitor BP weekly for the first 6 wk of therapy and periodically thereafter. New-onset hypertension has been associated with
- Lab tests: Periodic CBC with differential and platelet count, serum electrolytes, LFTs, lipase, amylase, and alkaline phosphatase.
- Monitor blood levels of warfarin with concurrent therapy
Patient & Family Education
- Follow directions for taking the drug (see Administration).
- Report any of the following to a health care provider: skin rash; redness, blisters, pain or swelling of the palms or hands
or soles of feet; signs of bleeding; unexplained chest, shoulder, neck and jaw, or back pain.
- Do not take any prescription or nonprescription drugs without consulting the physician.
- Male and female patients should use effective birth control during treatment and for at least 2 wk following completion of