Sunitinib Malate

Class: Antineoplastic Agents
VA Class: AN900
Chemical Name: N - [2 - (Diethylamino)ethyl] - 5 - [(Z) - (5 - fluoro - 2 - oxo - 1,2 - dihydro - 3H - indol - 3 - ylidene)methyl] - 2,4 - dimethyl - 1H - pyrrole - 3 - carboxamide
Molecular Formula: C₂₂H₂₇FN₄O₂
CAS Number: 557795-19-4
Brands: Sutent

Special Alerts:

[Posted 07/14/2008] Genentech, Inc. informed healthcare professionals of reports of several cases of microangiopathic hemolytic anemia (MAHA) in patients with solid tumors receiving bevacizumab (Avastin) in combination with sunitinib malate (Sutent). Bevacizumab is not approved for use in combination with sunitinib malate and this combination is not recommended. Twenty-five patients were enrolled in a Phase I dose-escalation study combining bevacizumab and sunitinib malate. The study consisted of 3 cohorts using a fixed dose of bevacizumab at 10mg/kg/IV every 2 weeks and escalating doses of sunitinib that included 25, 37.5, and 50 mg orally daily given in a 4 weeks on/ 2 weeks off schedule. Five of 12 patients at the highest sunitinib dose level exhibited laboratory findings consistent with MAHA. Two of these cases were considered severe with evidence of thrombocytopenia, anemia, reticulocytosis, reductions in serum haptoglobin, schistocytes on peripheral smear, modest increases in serum creatinine levels, and severe hypertension, reversible posterior leukoencephalopathy syndrome, and proteinuria. The findings in these two cases were reversible within three weeks upon discontinuation of both drugs without additional interventions. Healthcare professionals should report cases of MAHA or any serious adverse events suspected to be associated with the use of bevacizumab. For more information visit the FDA website at: and .

REMS:

FDA approved a REMS for sunitinib malate to ensure that the benefits of a drug outweigh the risks. However, FDA later rescinded REMS requirements. See the FDA REMS page () or the ASHP REMS Resource Center ().

Introduction

Antineoplastic agent; an inhibitor of multiple receptor tyrosine kinases.^{1 2 4 5 6 7 9 10 11 12 14 15}

Uses for Sunitinib Malate

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Gastrointestinal Stromal Tumor (GIST)

Treatment of GIST in adults who are intolerant of or whose disease has progressed during imatinib therapy.^{1 2 9}

Effects on overall survival remain to be established.^{1 9}

Renal Cell Carcinoma

Treatment of advanced renal cell carcinoma.^{1 2 7 14 15}

Sunitinib Malate Dosage and Administration

Administration

Oral Administration

Administer orally without regard to meals.^{1 11}

Dosage

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Available as sunitinib malate; dosage expressed in terms of sunitinib.^{1 2}

Adults

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

GIST

Oral

50 mg once daily for 4 consecutive weeks followed by a 2-week period without the drug.¹ May continue therapy (i.e., 6-week cycles) for as long as the patient derives clinical benefit or until unacceptable toxicity occurs; in principal efficacy study, therapy was continued for a median of 5–6 cycles.²

Renal Cell Carcinoma

Oral

50 mg once daily for 4 consecutive weeks followed by a 2-week period without the drug.^{1 6} May continue therapy (i.e., 6-week cycles) for as long as the patient derives clinical benefit or until unacceptable toxicity occurs.²

Dosage Modification for Toxicity

Oral

Adjust dosage in increments or decrements of 12.5 mg daily (i.e., 1 dose level), depending on individual patient safety and tolerability.^{1 2}

In clinical studies, dosages reduced following drug-related adverse effects generally were not re-escalated, even in absence of toxicity; however, re-escalation back to previous dosage was permitted based on clinical judgment.² Initiation of next treatment cycle could be delayed if additional time (i.e., >2 weeks) was required to recover from toxicities that developed during previous treatment cycle.²

Cardiovascular Toxicities

If manifestations of CHF develop, discontinue sunitinib.¹ In patients without clinical evidence of CHF but in whom left ventricular ejection fraction (LVEF) is <50% and is reduced from baseline by >20%, interrupt therapy and/or reduce sunitinib dosage.¹

If severe hypertension occurs, temporarily interrupt therapy until BP is controlled.¹

In clinical studies, sunitinib was temporarily withheld following development of certain grade 2 (i.e., asymptomatic decrease in LVEF from baseline by 20% and to a level below the lower limit of normal [LVEF <50%], nonurgent ventricular paroxysmal dysrhythmia requiring intervention) or grade 3 cardiac toxicities.² When manifestations resolved or decreased in intensity to ≤grade 1, patients who originally experienced grade 2 cardiac toxicity could resume sunitinib therapy at same dosage (if toxicity resolved within 1 week) or at 1 dose level lower than previous dosage; patients who originally experienced grade 3 cardiac toxicity could resume therapy at 1 dose level lower than previous dosage.² Patients who developed grade 4 cardiac toxicity were required to permanently discontinue therapy.²

If thrombotic microangiopathy occurs, temporarily suspend drug.¹ After resolution, may resume treatment as appropriate.¹ (See Cardiovascular and Cerebrovascular Effects under Cautions.)

Other Nonhematologic Toxicities

If manifestations of pancreatitis or hepatic failure develop, discontinue sunitinib.¹ (See Pancreatic and Hepatic Effects under Cautions.)

In clinical studies, sunitinib was temporarily withheld following development of grade 3 or 4 nonhematologic toxicity.² When manifestations resolved or decreased in intensity to ≤grade 1, patients with GIST who originally experienced grade 3 nonhematologic toxicity could resume sunitinib therapy at same dosage, while those with advanced renal cell carcinoma could resume therapy at same dosage or at 1 dose level lower than previous dosage; patients who originally experienced grade 4 nonhematologic toxicity could resume therapy at 1 dose level lower than previous dosage or discontinue therapy based on clinical judgment.²

If manifestations of nephrotic syndrome develop, discontinue sunitinib.¹ (See Renal and Metabolic Effects under Cautions.)

If seizures or manifestations of reversible posterior leukoencephalopathy syndrome (RPLS) occur, discontinue sunitinib.¹ Institute medical management including control of hypertension.¹ Following recovery, may resume treatment as appropriate.¹ (See Reversible Posterior Leukoencephalopathy Syndrome under Cautions.)

Hematologic Toxicity

In clinical studies, sunitinib was temporarily withheld following development of grade 3 or 4 hematologic toxicity (excluding lymphopenia).² When manifestations resolved or decreased in intensity to ≤grade 2, patients who originally experienced grade 3 hematologic toxicity could resume sunitinib therapy at same dosage; patients who originally experienced grade 4 hematologic toxicity could resume therapy at 1 dose level lower than previous dosage.² Patients who experienced grade 3 or 4 lymphopenia could continue therapy without interruption.²

Concomitant Use with Drugs and Foods Affecting Hepatic Microsomal Enzymes

Concomitant use with potent inhibitors or inducers of CYP3A4 may alter the combined plasma concentrations of sunitinib and its primary active metabolite.¹ (See Drugs and Foods Affecting Hepatic Microsomal Enzymes under Interactions.)

If concomitant use with a potent CYP3A4 inhibitor cannot be avoided, consider reducing sunitinib dosage to no less than 37.5 mg daily.¹

If concomitant use with a CYP3A4 inducer cannot be avoided, consider increasing sunitinib dosage, up to maximum of 87.5 mg daily; monitor patient carefully for toxicity.¹

Special Populations

Hepatic Impairment

No dosage adjustment required in patients with Child-Pugh class A or B hepatic impairment; not studied in patients with severe (Child-Pugh class C) hepatic impairment.^{1 2 12} Discontinue drug if manifestations of hepatic failure develop.¹ (See Pancreatic and Hepatic Effects and also Hepatic Impairment under Cautions.)

Renal Impairment

Dosage adjustment based on Cl_cr not required.² However, discontinue drug if nephrotic syndrome develops.¹ (See Renal and Metabolic Effects under Cautions and also see Absorption: Special Populations under Pharmacokinetics.)

Cautions for Sunitinib Malate

Warnings/Precautions

Warnings

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm;¹ teratogenicity and embryolethality demonstrated in animals.¹ Avoid pregnancy during therapy.¹ If used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard.¹

Major Toxicities

Cardiovascular Effects

Decreases in LVEF to below the lower limit of normal reported; grade 3 reductions in left ventricular systolic function (i.e., LVEF <40%) reported rarely.¹ Fatal heart failure and fatal cardiac arrest reported rarely.¹

Unknown whether patients with recent (i.e., within 12 months) history of cardiovascular disease (e.g., MI, severe or unstable angina, coronary or peripheral artery bypass graft, symptomatic CHF, cerebrovascular accident or TIA, pulmonary embolism) may be at a higher risk of developing drug-related left ventricular dysfunction since such patients were excluded from clinical studies.¹ Weigh this risk against potential benefits of the drug.¹ Carefully monitor such patients for clinical signs and symptoms of CHF during sunitinib therapy and consider baseline and periodic evaluations of LVEF.¹ Also consider baseline evaluation of ejection fraction in patients without cardiac risk factors.¹ (See Cardiovascular Toxicities under Dosage and Administration.)

Venous thromboembolic events (including DVT and pulmonary embolism) reported.¹

Thrombotic microangiopathy reported rarely.¹ (See Cardiovascular Toxicities under Dosage and Administration.)

QT Interval Prolongation and Torsades de Pointes

Dose-dependent prolongation of the QT interval reported; may result in increased risk of ventricular arrhythmias, including torsades de pointes.¹ Torsades de pointes reported rarely.¹

Use with caution in patients with history of QT interval prolongation, patients receiving antiarrhythmic agents or potent CYP3A4 inhibitors, and patients with relevant preexisting cardiac disease, bradycardia, or electrolyte disturbances.¹ (See Specific Drugs under Interactions.)

Consider periodic monitoring of ECG and electrolytes (potassium, magnesium).¹

Hypertension

Hypertension, including severe hypertension (SBP >200 mm Hg or DBP >110 mm Hg) reported.^{1 9 10}

Monitor BP and treat hypertension with standard antihypertensive therapy as needed.¹ If severe hypertension develops, withhold sunitinib until BP is controlled.¹

Hemorrhage

Bleeding events (epistaxis or, less commonly, rectal/gingival/upper GI/genital/wound bleeding) reported.¹ Most events were grade 1–2; grade 3–5 events also reported.¹

Tumor-related hemorrhage (including fatal pulmonary hemorrhage) reported.¹ May occur suddenly and, in the case of pulmonary tumors, may present as severe and life-threatening hemoptysis or pulmonary hemorrhage.¹ Monitor patients carefully with periodic clinical and laboratory evaluations (e.g., serial CBCs, physical examinations) for development of tumor hemorrhage.¹

Serious, sometimes fatal GI complications, including GI perforation, reported rarely in patients with intra-abdominal malignancies.¹

Other Hematologic Effects

Possible hematologic laboratory abnormalities, including anemia, thrombocytopenia, leukopenia, neutropenia, and lymphopenia.¹

Serious infections, with or without neutropenia, may occur; sometimes fatal.^b

Hypothyroidism

Hypothyroidism reported.^{1 13 14}

Obtain baseline thyroid function tests and treat hypothyroidism before initiating sunitinib therapy.¹

During sunitinib therapy, observe all patients closely; if signs and symptoms of hypothyroidism develop, obtain thyroid function tests and provide treatment per standard medical practice.¹

Adrenal Toxicity

Adrenal toxicity (characterized histologically by hemorrhage, necrosis, congestion, hypertrophy, and inflammation) reported in animals; however, no evidence of adrenal hemorrhage or necrosis in humans.¹

Abnormal response to rapid corticotropin (ACTH) stimulation tests (e.g., decreased plasma cortisol concentrations) observed in some patients; however, no clinical evidence of adrenal insufficiency.¹

Monitor for development of adrenal insufficiency in patients who experience stress (e.g., surgery, trauma, severe infection).¹

Reversible Posterior Leukoencephalopathy Syndrome (RPLS)

Seizures and radiologic evidence of RPLS reported rarely.¹

If seizures and manifestations of RPLS (e.g., hypertension, headache, decreased alertness, altered mental functioning, visual loss [including cortical blindness]) occur, temporarily withhold sunitinib and treat manifestations (including management of hypertension).¹ (See Other Nonhematologic Toxicities under Dosage and Administration.)

Pancreatic and Hepatic Effects

Pancreatitis and hepatic failure reported.¹ (See Other Nonhematologic Toxicities under Dosage and Administration.)

Possible hepatic laboratory abnormalities including elevated AST, ALT, bilirubin, and alkaline phosphatase.¹

Possible pancreatic laboratory abnormalities including elevated amylase and elevated serum lipase.¹

Renal and Metabolic Effects

Hypophosphatemia, hyperuricemia, elevated S_cr and elevated serum creatine kinase reported.^{1 15}

Proteinuria, and rarely, nephrotic syndrome reported.^b Perform baseline urinalysis and monitor for development or worsening of proteinuria.¹ Safety of continued treatment in moderate-to-severe proteinuria not yet evaluated.^b (See Other Nonhematologic Toxicities under Dosage and Administration.)

General Precautions

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Clinical and Laboratory Monitoring

Obtain CBCs (including platelet count) and serum chemistry tests (including phosphate) at beginning of each treatment cycle.¹

Perform clinical and/or laboratory assessments periodically to detect severe adverse effects (e.g., left ventricular dysfunction, hypertension, tumor hemorrhage, myelosuppression).^{1 2} (See Major Toxicities under Cautions.)

Musculoskeletal Effects

Myopathy and/or rhabdomyolysis, some with acute renal failure, reported rarely; most involved patients with pre-existing risk factors and/or taking concomitant drugs associated with myopathy and/or rhabdomyolysis.^b Manage signs and symptoms of muscle toxicity per standard medical protocol.^b

Specific Populations

Pregnancy

Category D.¹ (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Lactation

Distributed into milk in rats; drug concentration up to 12-fold higher in milk than in plasma.¹ Not known whether sunitinib or its primary active metabolite is distributed into human milk.¹ Discontinue nursing or the drug because of potential risk in nursing infants.¹

Pediatric Use

Safety and efficacy not established.¹

Geriatric Use

No substantial differences in safety and efficacy in patients ≥65 years of age relative to younger adults.¹

Hepatic Impairment

Clinical studies excluded patients with AST or ALT concentrations >2.5 times the ULN or, if due to liver metastases, >5 times the ULN.¹ (See Hepatic Impairment under Dosage and Administration.)

Renal Impairment

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Safety and efficacy not established in patients with renal impairment.^{1 2} Clinical studies excluded patients with S_cr >2 times the ULN.^{1 2}

Common Adverse Effects

Fatigue,¹ asthenia,¹ diarrhea,¹ nausea,¹ mucositis/stomatitis,¹ vomiting,¹ dyspepsia,¹ abdominal pain,¹ constipation,¹ hypertension,¹ rash,¹ hand-foot syndrome,¹ skin discoloration,¹ altered taste,¹ anorexia,¹ bleeding.¹

Interactions for Sunitinib Malate

Sunitinib and its primary active metabolite are metabolized principally by CYP3A4.^{1 5}

Sunitinib does not inhibit or induce major CYP isoenzymes.¹

Drugs and Foods Affecting Hepatic Microsomal Enzymes

Potent inhibitors of CYP3A4: Potential pharmacokinetic interaction (increased combined plasma concentrations of sunitinib and its primary active metabolite).¹ (See Specific Drugs and Foods under Interactions and also see QT Interval Prolongation and Torsades de Pointes under Cautions.)

Inducers of CYP3A4: Potential pharmacokinetic interaction (decreased combined plasma concentrations of sunitinib and its primary active metabolite).¹ (See Specific Drugs and Foods under Interactions.)

Drugs Metabolized by Hepatic Microsomal Enzymes

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Substrates of CYP isoenzymes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4/5, or 4A9/11: Pharmacokinetic interaction unlikely.¹

Drugs that Prolong QT Interval

Risk of prolonged QT interval and potentially serious or life-threatening arrhythmias.¹ Use with caution in patients taking antiarrhythmics.¹ (See QT Interval Prolongation and Torsades de Pointes under Cautions.)

Specific Drugs and Foods

Drug or Food	Interaction	Comments
Antiarrhythmic agents		Use concomitantly with caution1 (see QT Interval Prolongation and Torsades de Pointes under Cautions)
Anticonvulsants (carbamazepine, phenobarbital, phenytoin)	Possible decreased combined plasma concentrations of sunitinib and its primary active metabolite1	Select an alternative agent with minimal or no enzyme induction potential; if concomitant use cannot be avoided, consider increasing sunitinib dosage to no more than 87.5 mg daily and carefully monitor patient for toxicity1
Antifungals, azoles (itraconazole, ketoconazole, voriconazole)	Ketoconazole: Increased combined plasma concentrations of sunitinib and its primary active metabolite1	Select an alternative agent with minimal or no enzyme inhibition potential; if concomitant use cannot be avoided, consider reducing sunitinib dosage to no less than 37.5 mg daily1
Antimycobacterials (rifabutin, rifampin, rifapentine)	Rifampin: Decreased combined plasma concentrations of sunitinib and its primary active metabolite1	Select an alternative agent with minimal or no enzyme induction potential; if concomitant use cannot be avoided, consider increasing sunitinib dosage to no more than 87.5 mg daily and carefully monitor patient for toxicity1
Dexamethasone	Possible decreased combined plasma concentrations of sunitinib and its primary active metabolite1	Select an alternative agent with minimal or no enzyme induction potential; if concomitant use cannot be avoided, consider increasing sunitinib dosage to no more than 87.5 mg daily and carefully monitor patient for toxicity1
Grapefruit	Possible increased combined plasma concentrations of sunitinib and its primary active metabolite1	Select alternative product with minimal or no enzyme inhibition potential; if concomitant use cannot be avoided, consider decreasing sunitinib dosage to no less than 37.5 mg daily1
HIV protease inhibitors (e.g., atazanavir, indinavir, nelfinavir, ritonavir, saquinavir)	Possible increased combined plasma concentrations of sunitinib and its primary active metabolite1	Select an alternative agent with minimal or no enzyme inhibition potential; if concomitant use cannot be avoided, consider reducing sunitinib dosage to no less than 37.5 mg daily1
Macrolides (e.g., clarithromycin, telithromycin)	Possible increased combined plasma concentrations of sunitinib and its primary active metabolite1	Select an alternative agent with minimal or no enzyme inhibition potential; if concomitant use cannot be avoided, consider reducing sunitinib dosage to no less than 37.5 mg daily1
Nefazodone	Possible increased combined plasma concentrations of sunitinib and its primary active metabolite1	Select an alternative agent with minimal or no enzyme inhibition potential; if concomitant use cannot be avoided, consider reducing sunitinib dosage to no less than 37.5 mg daily1
St. John's wort (Hypericum perforatum)	Possible unpredictable decreases in plasma sunitinib concentrations1	Avoid concomitant use1

Sunitinib Malate Pharmacokinetics

Absorption

Bioavailability

Following oral administration, peak plasma concentrations are attained within 6–12 hours.¹

Food

Food has no effect on bioavailability of sunitinib.^{1 11}

Special Populations

Systemic exposures after a single dose were similar in individuals with mild (Child-Pugh class A) or moderate (Child-Pugh class B) hepatic impairment compared with those with normal hepatic function.¹

Pharmacokinetics of sunitinib and its primary active metabolite are not substantially affected by age, body weight, Cl_cr (i.e., in the range of 42–347 mL/minute), race, gender, or ECOG performance status.¹

Distribution

Extent

Sunitinib and metabolites are distributed into milk in animals; not known whether the drug or its primary active metabolite is distributed into human milk.¹

Plasma Protein Binding

Approximately 95% (for sunitinib) and 90% (for primary active metabolite).¹

Elimination

Metabolism

Metabolized in the liver, principally by CYP3A4 to several metabolites.^{1 5 11 12}

Primary active metabolite appears to be equipotent to sunitinib;^{1 5} this metabolite accounts for approximately 23–37% of total plasma concentrations of the drug and also is metabolized by CYP3A4.¹

Elimination Route

Excreted in feces (61%) and urine (16%), mainly as sunitinib and primary active metabolite.^{1 2} Minor metabolites recovered in feces and urine but generally not found in plasma.^{1 2}

Half-life

Approximately 40–60 hours (for sunitinib) or 80–110 hours (for primary active metabolite).^{1 12}

Special Populations

Results of one pharmacokinetic study indicated a slightly longer sunitinib half-life in individuals with mild (Child-Pugh score of 5–6) or moderate (Child-Pugh score of 7–9) hepatic impairment; however, clearance of sunitinib not significantly different from that in individuals with normal hepatic function.¹²

Stability

Storage

Oral

Capsules

25°C (may be exposed to 15–30°C).¹

Actions

• 
  

  Inhibits multiple receptor tyrosine kinases (RTKs), ^{1 2 4 5 6 7 9 10 11 12} which are involved in the initiation of various cascades of intracellular signaling events that lead to cell proliferation and/or influence processes critical to cell survival and tumor progression (e.g., angiogenesis, metastasis, inhibition of apoptosis), based on the respective kinase.^{1 2 4 6 7 11}

  
  


• 
  

  May inhibit signal transduction pathways involving multiple receptor (i.e., cell surface) tyrosine kinases, including platelet-derived growth factor receptors (i.e., PDGFR-α, PDGFR-β), vascular endothelial growth factor receptors (i.e., VEGFR-1, VEGFR-2, VEGFR-3), stem cell factor receptor (i.e., c-Kit), fms-like tyrosine kinase 3 (Flt-3), colony stimulating factor receptor type 1 (CSF-1R), and the glial cell line-derived neurotrophic factor receptor (RET).^{1 2 4 5 9 10 11 12}

  
  


• 
  

  Shown to inhibit growth of tumor cells expressing dysregulated target RTKs (i.e., PDGFR, RET, c-Kit) in vitro; also shown to inhibit PDGFR-β- and VEGFR-2-dependent tumor angiogenesis in vivo.¹

  
  

Advice to Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

• 
  

  Risk of adverse GI effects (e.g., diarrhea, nausea, vomiting, dyspepsia, mouth pain/irritation/stomatitis, taste disturbance).¹ Supportive care for adverse GI effects requiring treatment may include antiemetic or antidiarrheal therapy.¹

  
  


• 
  

  Risk of adverse dermatologic effects (e.g., skin discoloration due to the drug color [yellow]; hair or skin depigmentation; skin dryness, thickness, or cracking; blisters or rash on the hands and soles of the feet).¹

  
  


• 
  

  Risk of fatigue, hypertension, bleeding, and edema.¹

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹ Advise pregnant women of risk to the fetus and/or of potential risk for loss of pregnancy.¹

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal supplements (e.g., St. John’s wort), as well as any concomitant illnesses.¹

  
  


• 
  

  Importance of informing patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Sunitinib Malate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules	12.5 mg (of sunitinib)	Sutent	Pfizer
		25 mg (of sunitinib)	Sutent	Pfizer
		50 mg (of sunitinib)	Sutent	Pfizer

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 10/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Sutent 12.5MG Capsules (PFIZER U.S.): 28/$2,596.10 or 84/$7,396.68

Sutent 25MG Capsules (PFIZER U.S.): 28/$5,214.86 or 84/$14,954.77

Sutent 50MG Capsules (PFIZER U.S.): 28/$10,465.92 or 84/$30,651.87

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions October 27, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Pfizer Labs. Sutent (sunitinib malate) capsules prescribing information. New York, NY; 2007 Feb .

2. Pfizer Inc., Parsippany, NJ: Personal communication.

4. Arora A, Scholar EM. Role of tyrosine kinase inhibitors in cancer therapy. J Pharmacol Exp Ther. 2005; 315:971-9. [PubMed 16002463]

5. Faivre S, Delbaldo C, Vera K et al. Safety, pharmacokinetic, and antitumor activity of SU11248, a novel oral multitarget tyrosine kinase inhibitor, in patients with cancer. J Clin Oncol. 2006; 24:25-35. [PubMed 16314617]

6. Schöffski P, Dumez H, Clement P et al. Emerging role of tyrosine kinase inhibitors in the treatment of advanced renal cell cancer: a review. Ann Oncol. 2006 (Advance access [doi:]).

7. Motzer RJ, Michaelson MD, Redman BG et al. Activity of SU11248, a multitargeted inhibitor of vascular endothelial growth factor receptor and platelet-derived growth factor receptor, in patients with metastatic renal cell carcinoma. J Clin Oncol. 2006; 24:16-24. [PubMed 16330672]

8. Robert C, Soria CJ, Spatz A. Cutaneous side-effects of kinase inhibitors and blocking antibodies. Lancet Oncol. 2005; 6:491-500. [PubMed 15992698]

9. Demetri GD, van Oosterom AT, Garrett CR et al. Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial. Lancet. 2006; 368:1329-38. [PubMed 17046465]

10. Motzer RJ, Rini BI, Bukowski RM et al. Sunitinib in patients with metastatic renal cell carcinoma. JAMA. 2006; 295:2516-24. [PubMed 16757724]

11. Bello CL, Sherman L, Zhou J et al. Effect of food on the pharmacokinetics of sunitinib malate (SU11248), a multi-targeted receptor tyrosine kinase inhibitor: results from a phase I study in healthy subjects. Anticancer Drugs. 2006; 17:353-8. [PubMed 16520665]

12. Bello CL, Garrett M, Smeraglia J et al. Pharmacokinetics (PK) of sunitinib malate (SU11248) in subjects with hepatic impairment. Poster presented at the European Society of Medical Oncology (ESMO). Istanbul, Turkey: 2006 Sep 29–Oct 3.

13. Desai J, Yassa L, Marqusee E et al. Hypothyroidism after sunitinib treatment for patients with gastrointestinal stromal tumors. Ann Intern Med. 2006; 145:660-4. [PubMed 17088579]

14. Rini BI, Tamaskar I, Shaheen P et al. Hypothyroidism in patients with metastatic renal cell carcinoma treated with sunitinib. J Natl Cancer Inst. 2007; 99:81-3. [PubMed 17202116]

15. Motzer RJ, Hutson TE, Tomczak P et al. Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N Engl J Med. 2007; 356:115-24. [PubMed 17215529]

b. Pfizer Labs. Sutent (sunitinib malate) capsules prescribing information. New York, NY; 2008 May.

More Sunitinib Malate resources

• Sunitinib Malate Side Effects (in more detail)
• Sunitinib Malate Dosage
• Sunitinib Malate Use in Pregnancy & Breastfeeding
• Sunitinib Malate Drug Interactions
• Sunitinib Malate Support Group
• 7 Reviews for Sunitinib Malate - Add your own review/rating

Compare Sunitinib Malate with other medications

• Gastrointestinal Stromal Tumor
• Pancreatic Cancer
• Renal Cell Carcinoma