sunitinib malate

sunitinib malate


Pharmacologic class: Receptor tyrosine kinase inhibitor

Therapeutic class: Antineoplastic

Pregnancy risk category D

FDA Box Warning

• Hepatotoxicity, which has been observed in clinical trials and postmarketing experience, may be severe, and deaths have occurred.


Inhibits multiple receptor tyrosine kinases, some of which are implicated in tumor growth, pathologic angio-genesis, and metastatic cancer progression


Capsules: 12.5 mg, 25 mg, 50 mg

Indications and dosages

GI stromal tumor after disease progression with or intolerance to imatinib mesylate; advanced renal cell carcinoma

Adults: 50 mg P.O. daily on cycle of 4 weeks on and 2 weeks off treatment; may increase or decrease dosage in 12.5-mg increments based on safety and tolerance

Dosage adjustment

• Concurrent use of strong CYP3A4 inducers or inhibitors


• Hypersensitivity to drug or its components


Use cautiously in:

• left ventricular dysfunction, hypertension, history of prolonged QT interval, concurrent use of antiarrhythmics, patients with relevant preexisting cardiac disease, bradycardia, or electrolyte disturbances

• patients who have experienced cardiac events within previous 12 months

• hepatotoxicity

• concurrent use of strong CYP3A4 inhibitors

• pregnant or breastfeeding patients

• children (safety and efficacy not established).


Monitor liver function tests before start of treatment.

• Administer with or without food.

• Interrupt therapy or reduce dosage, as prescribed, in patients who lack clinical evidence of heart failure but have ejection fractions (EFs) below 50% and above 20% below baseline.

Adverse reactions

CNS: headache, asthenia

CV: hypertension, left ventricular dysfunction

EENT: epistaxis, oral pain

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, mucositis, stomatitis, anorexia

Hematologic: bleeding, anemia, thrombocytopenia, neutropenia, lymphopenia, hemorrhage

Hepatic: hepatotoxicity

Metabolic: acquired hypothyroidism, adrenal toxicity

Musculoskeletal: arthralgia, back pain, limb pain, myalgia

Respiratory: dyspnea, cough, pulmonary embolism

Skin: skin abnormalities, skin discoloration, rash, palmar-plantar erythrodysesthesia, alopecia, hair color changes

Other: altered taste, fatigue, fever


Drug-drug. Atazanavir, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole: increased sunitinib blood level

Carbamazepine, dexamethasone, phenobarbital, phenytoin, rifabutin, rifampin, rifapentin: decreased sunitinib blood level

Drug-diagnostic tests. Amylase, creatinine, lipase, uric acid: increased

Liver function tests: abnormal

Serum phosphorus, potassium, sodium: decreased

Drug-food. Grapefruit juice, pomegranate: increased sunitinib blood level

Drug-herbs. Alpha-lipoic acid: decreased chemotherapeutic efficacy

American elder, bishop's weed, cat's claw, devil's claw, eucalyptus, feverfew, Siberian ginseng, valerian: increased sunitinib blood level

St. John's wort: unpredictable decrease in sunitinib blood level

Patient monitoring

• Obtain CBC with platelet count and blood chemistries (including phosphate) at start of each treatment cycle and frequently thereafter.

• Know that physician may order baseline and periodic evaluation of left ventricular EF in patients who experienced cardiac events within 12 months before starting drug. Watch closely for signs and symptoms of left ventricular dysfunction (especially heart failure).

• Be aware that physician may order baseline EF testing for patients without cardiac risk factors.

• Monitor for hypertension; administer standard antihypertensive therapy as ordered and needed.

• Monitor for adrenal insufficiency if patient experiences stress (as from surgery, trauma, or severe infection).

Monitor liver function tests during each cycle of treatment and as clinically indicated. Interrupt therapy for Grade 3 or 4 drug-related hepatic adverse events; discontinue drug if no resolution. Don't restart drug if severe changes in liver function tests subsequently occur or if patient has other signs and symptoms of liver failure.

Patient teaching

• Instruct patient to take drug with or without food.

Urge patient to immediately report sudden signs and symptoms of liver problems (such as yellowing of skin or eyes, unusual tiredness, loss of appetite), chest pain, swelling, or difficulty breathing.

• Tell patient drug may cause skin changes (drying, cracking, or rashes on hands or feet) and hair color changes.

• Advise patient to consult prescriber before taking other drugs, including over-the-counter drugs and herbs.

• Caution patient not to take St. John's wort during therapy.

• Advise female with childbearing potential to avoid pregnancy and breastfeeding during therapy.

•As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.


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References in periodicals archive ?
Sunitinib Malate Market Forecast for Pancreatic Cancer, 2016-2017, G7 Countries, (U.
The Sunitinib Malate or Sorafenib Tosylate in Treating Patients With Kidney Cancer That Was Removed By Surgery (ASSURE) study was a Phase 3 study involving 1943 patients with resected RCC (pT1b high-grade to pT4 any grade) at intermediate-high to very high risk.
Stivarga is a kinase inhibitor approved for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy; and locally advanced, unresectable or metastatic gastrointestinal stromal tumors (GIST) that have been previously treated with imatinib mesylate and sunitinib malate, concluded the company.
53,55,56) Sunitinib malate has been approved by the FDA for the treatment of patients who progressed on or are intolerant of imatinib, after the results of a randomized placebo-controlled phase III study.
The results could breathe new life into the use of interferon and provide an alternative to current treatment options, including the recently approved antiangiogenic agent, sunitinib malate (Sutent).
The response to therapy (imatinib mesylate [Gleevec, Novartis Pharmaceuticals, East Hanover, New Jersey] or sunitinib malate [Sutent, Pfizer Pharmaceuticals, New York, New York]) appears to correlate with specific KIT or PDGFRA mutations (discussed later in the section on "Therapeutic Implications of Activating KIT Mutations").
ATLANTA -- Sunitinib malate is more effective than the current standard therapy, interferon-[alpha], as first-line treatment for metastatic renal cell carcinoma, according to the results of an international phase III trial presented at the annual meeting of the American Society of Clinical Oncology.
The approval of Stivarga is based on the positive results from the pivotal Phase III GRID (GIST a Regorafenib In Progressive Disease) trial that demonstrated a statistically significant improvement in progression-free survival (PFS) compared to placebo in patients with GIST whose disease had progressed after treatment with imatinib mesylate and sunitinib malate.
FDA for the treatment of patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate and sunitinib malate in February 2013.