Classifications: antineoplastic agent; growth factor receptor inhibitor; tyrosine kinase inhibitor; Therapeutic:antineoplastic; growth factor receptor inhibitor; tyrosine kinase inhibitor
Pregnancy Category: D
12.5 mg, 25 mg, 50 mg capsules
An antineoplastic agent that is a selective inhibitor of receptor tyrosine kinases (RTKs) in solid tumors. Carcinogenic
activity within these tumors is a result of tumor angiogenesis and proliferation.
Sunitinib causes tumor regression and decreased tumor growth.
Treatment of advanced renal cell cancer; treatment of gastrointestinal stromal tumors (GIST) after disease progression on
or intolerance to imatinib.
Hypersensitivity to sunitinib; uncontrolled hypertension, acute MI; fever, abnormal bleeding, sore throat; children, pregnancy
(category D), lactation.
Cardiac disease, CHF, history of hypertension, history of MI; CVA; females of childbearing age.
Route & Dosage
|Advanced Renal Cell Cancer
Adult: PO 50 mg/d for 4 wk, followed by 2 wk off treatment; repeat 6-wk cycle as needed.
Dosage Adjustments with Concurrent Hepatic CYP3A4 Modifiers
CYP3A4 Inducers: increase to maximum of 87.5 mg/d
CYP3A4 Inhibitors: decrease to minimum of 37.5 mg/d
- Note that this drug is given on a 6-wk cycle: 4 wk on therapy and 2 wk off.
- Incremental dosage changes of 12.5 mg are recommended.
- Store at 15°30° C (59°86° F).
Adverse Effects (≥1%)Body as a Whole: Alopecia, asthenia, dizziness, fatigue, fever,
hair color change, headache, peripheral edema. CV: Hypertension, myocardial ischemia. GI: Abdominal pain, altered taste, anorexia, constipation, diarrhea, dyspepsia, flatulence, glossodynia, nausea, mucositis,
stomatitis, vomiting. Hematologic: Anemia, bleeding, neutropenia, lymphopenia, thrombocytopenia. Metabolic: Dehydration, elevated hepatic enzymes (AST/ALT, alkaline phosphatase, pancreatic enzymes, amylasemia, lipasemia),
hypothyroidism, hyperbilirubinemia. Musculoskeletal: Arthralgia, back pain, myalgia/limb pain. Respiratory: Cough, dyspnea. Skin: Dry skin, hand-foot syndrome, rash, skin discoloration.
Coadministration of CYP3A4 inducers (e.g., carbamazepine, dexamethasone, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine
) may decrease plasma
levels of sunitinib. Coadministration of CYP3A4 inhibitors (e.g., atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir,
) may increase plasma
levels of sunitinib. Food: Grapefruit
and grapefruit juice
may increase the plasma
levels of sunitinib. Herbal: St. John's wort
may decrease the plasma
levels of sunitinib.
612 h. Distribution:
9598% protein bound. Metabolism:
Extensive hepatic metabolism
Primarily fecal elimination (61%) with minor renal
Assessment & Drug Effects
- Monitor for and report S&S of bleeding (e.g., GI, GU, gingival, etc.).
- Monitor BP regularly and assess regularly for S&S of congestive heart failure. Withhold drug and notify physician if severe
hypertension or signs of heart failure develop.
- Lab tests: At the beginning of each treatment cycle, CBC with differential and platelet count; periodic serum electrolytes;
thyroid function tests with symptoms suggestive of hypothyroidism.
Patient & Family Education
- Follow directions for taking the drug (see Administration).
- Do not use any prescription or nonprescription drugs without consulting a physician.
- Skin discoloration (yellow color) and/or loss of skin and hair pigmentation may occur with this drug.
- Report any of the following to a health care provider: painful redness of palms and soles of feet; severe abdominal pain,
vomiting, and diarrhea; signs of bleeding; chest pain or discomfort; shortness of breath; swelling of feet, legs, or hands;
rapid weight gain.
- Women of childbearing age are advised not be become pregnant while taking sunitinib.