Sunitinib

Sunitinib is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs), some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Sunitinib was evaluated for its inhibitory activity against a variety of kinases (>80 kinases) and was identified as an inhibitor of platelet-derived growth factor receptors (PDGFRα and PDGFRβ), vascular endothelial growth factor receptors (VEGFR1, VEGFR2, and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor Type 1 (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET).

• Sunitinib malate is a kinase inhibitor indicated for: treatment of adult patients with gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib mesylate. ( 1.1 ) treatment of adult patients with advanced renal cell carcinoma (RCC).

• None.contraindicated

GIST and Advanced RCC : The recommended dosage is 50 mg orally once daily for the first 4 weeks of each 6-week cycle (Schedule 4/2). ( 2.1 ) Adjuvant Treatment of RCC : The recommended dosage is 50 mg orally once daily for the first 4 weeks of a 6-week cycle (Schedule 4/2) for a maximum of 9 cycles. ( 2.2 ) pNET : The recommended dosage is 37.5 mg orally once daily. ( 2.3 ) 2.1 Recommended Dosage for GIST and Advanced RCC The recommended dosage of sunitinib malate capsules for gastrointestinal stromal tumor (GIST) and advanced renal cell carcinoma (RCC) is 50 mg taken orally once daily, on a schedule of 4 weeks on treatment followed by 2 weeks off (Schedule 4/2) until disease progression or unacceptable toxicity. Sunitinib malate capsules may be taken with or without food. 2.2 Recommended Dosage for Adjuvant Treatment of RCC The recommended dosage of sunitinib malate capsules for the adjuvant treatment of RCC is 50 mg taken orally once daily, on a schedule of 4 weeks on treatment followed by 2 weeks off (Schedule 4/2), for nine 6-week cycles. Sunitinib malate capsules may be taken with or without food. 2.3 Recommended Dosage for pNET The recommended dosage of sunitinib malate capsules for pancreatic neuroendocrine tumors (pNET) is 37.5 mg taken orally once daily until disease progression or unacceptable toxicity. Sunitinib malate capsules may be taken with or without food. 2.4 Dosage Modifications for Adverse Reactions To manage adverse reactions, the recommended dosage modifications are provided in Table 1.

Hepatotoxicity : Fatal liver failure has been observed. Monitor liver function tests at baseline, during each cycle, and as clinically indicated. Interrupt sunitinib malate for Grade 3 hepatotoxicity until resolution to Grade ≤1 or baseline and resume sunitinib malate at a reduced dose; discontinue if no resolution. Discontinue sunitinib malate in patients with Grade 4 hepatoxicity, in patients who have subsequent severe changes in liver function tests or other signs and symptoms of liver failure. ( 2.4 , 5.1 ) Cardiovascular Events : Myocardial ischemia, myocardial infarction, heart failure, cardiomyopathy, and decreased left ventricular ejection fraction (LVEF) to below the lower limit of normal including death have occurred. Monitor for signs and symptoms of congestive heart failure and consider monitoring LVEF at baseline and periodically during treatment. Discontinue sunitinib malate for clinical manifestations of congestive heart failure. Interrupt and/or dose reduce for decreased LVEF. ( 5.2 ) QT Interval Prolongation and Torsade de Pointes : Monitor patients at higher risk for developing QT interval prolongation. Consider monitoring of electrocardiograms and electrolytes. ( 5.3 ) Hypertension : Monitor blood pressure at baseline and as clinically indicated. Initiate and/or adjust antihypertensive therapy as appropriate. Interrupt sunitinib malate for Grade 3 hypertension until resolution to Grade ≤1 or baseline, then resume sunitinib malate at a reduced dose. Discontinue sunitinib malate in patients who develop Grade 4 hypertension.

The following clinically significant adverse reactions are described elsewhere in the labeling. Hepatotoxicity [see Warnings and Precautions ( 5.1 )] Cardiovascular Events [see Warnings and Precautions ( 5.2 )] QT Interval Prolongation and Torsade de Pointes [see Warnings and Precautions ( 5.3 )] Hypertension [see Warnings and Precautions ( 5.4 )] Hemorrhagic Events [see Warnings and Precautions ( 5.5 )] Tumor Lysis Syndrome [see Warnings and Precautions ( 5.6 )] Thrombotic Microangiopathy [see Warnings and Precautions ( 5.7 )] Proteinuria [see Warnings and Precautions ( 5.8 )] Dermatologic Toxicities [see Warnings and Precautions ( 5.9 )] Reversible Posterior Leukoencephalopathy Syndrome [see Warnings and Precautions ( 5.10 )] Thyroid Dysfunction [see Warnings and Precautions ( 5.11 )] Hypoglycemia [see Warnings and Precautions ( 5.12 )] Osteonecrosis of the Jaw [see Warnings and Precautions ( 5.13 )] Impaired Wound Healing [see Warnings and Precautions ( 5.14 )] The most common adverse reactions (≥25%) are fatigue/asthenia, diarrhea, mucositis/stomatitis, nausea, decreased appetite/anorexia, vomiting, abdominal pain, hand-foot syndrome, hypertension, bleeding events, dysgeusia/altered taste, dyspepsia, and thrombocytopenia. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Novugen Pharma (USA) LLC at 1-888-966-8843 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Lactation : Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on animal reproduction studies and its mechanism of action, sunitinib malate can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no available data in pregnant women to inform a drug-associated risk. In animal developmental and reproductive toxicology studies, oral administration of sunitinib to pregnant rats and rabbits throughout organogenesis resulted in teratogenicity (embryolethality, craniofacial and skeletal malformations) at 5.5 times and 0.3 times the combined AUC (the combined systemic exposure of sunitinib plus its active metabolite) in patients administered the recommended daily doses (RDD) of 50 mg, respectively (see Data). Advise females of reproductive potential of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated populations are unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriages in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Metabolism

The pharmacokinetics of sunitinib and sunitinib malate have been evaluated in healthy subjects and in patients with solid tumors. Sunitinib AUC and C max increase proportionately over a dose range of 25 mg to 100 mg (0.5 times to 2 times the approved RDD of 50 mg).

Treatment of overdose with sunitinib malate should consist of general supportive measures. There is no specific antidote for overdosage with sunitinib malate. If indicated, elimination of unabsorbed drug should be achieved by emesis or gastric lavage. Cases of accidental overdose have been reported; these cases were associated with adverse reactions consistent with the known safety profile of sunitinib malate, or without adverse reactions. In nonclinical studies, mortality was observed following as few as 5 daily doses of 500 mg/kg (3,000 mg/m 2 ) in rats. At this dose, signs of toxicity included impaired muscle coordination, head shakes, hypoactivity, ocular discharge, piloerection, and gastrointestinal distress. Mortality and similar signs of toxicity were observed at lower doses when administered for longer durations.

• Jan 26, 2006NDANDA021938Cppi Cv
• Aug 16, 2021ANDAANDA213914Sun Pharm
• Nov 30, 2021ANDAANDA213803Teva Pharms Usa
• Dec 6, 2021ANDAANDA201275Mylan
• Apr 11, 2022ANDAANDA215843Dr Reddys
• Aug 21, 2023ANDAANDA218012Fosun Wanbang
• Mar 14, 2024ANDAANDA218615Eugia Pharma
• Feb 14, 2025ANDAANDA214824Msn

1. 1Death7,39919%
2. 2Diarrhoea4,41611%
3. 3Fatigue4,19011%
4. 4Disease Progression3,90610%
5. 5Nausea3,1218.0%
6. 6Asthenia2,4586.3%
7. 7Decreased Appetite2,3175.9%
8. 8Vomiting2,2105.7%
9. 9Neoplasm Progression2,0195.2%
10. 10Hypertension1,8024.6%
11. 11Dysgeusia1,6974.3%
12. 12Weight Decreased1,5884.1%
13. 13Malaise1,5824.1%
14. 14Stomatitis1,4653.8%
15. 15Palmar-plantar Erythrodysaesthesia Syndrome1,4553.7%

Recent PubMed references pinned to Sunitinib as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• [(177)Lu]Lu-dota-tate versus sunitinib in patients with metastatic progressive neuroendocrine tumours of the pancreas (OCLURANDOM): a randomised, controlled, phase 2 trial.
  The Lancet. Oncology · 2026 · Baudin E, Durand A, Beron A, et al.
  PMID 42225102DOI 10.1016/S1470-2045(26)00108-7
• PYCR2 contributes to sunitinib resistance in hepatocellular carcinoma by activating the PPAR signaling pathway.
  Biochemical and biophysical research communications · 2026 · Zheng X, Jiang Y, Liu B, et al.
  PMID 42155340DOI 10.1016/j.bbrc.2026.153971
• Design, synthesis and anti-necroptosis evaluation of RIPK1 inhibitors derived from sunitinib.
  European journal of medicinal chemistry · 2026 · Jiang Y, Zheng Y, Zou M, et al.
  PMID 42140113DOI 10.1016/j.ejmech.2026.118925
• USP15 stabilizes c-Myc to drive sunitinib resistance by suppressing cuproptosis in clear cell renal cell carcinoma.
  Cell reports · 2026 · Chen Y, Huang S, Wang L, et al.
  PMID 42054210DOI 10.1016/j.celrep.2026.117328
• Stereotactic body radiotherapy plus sunitinib vs. sunitinib alone in treatment-naive oligometastatic renal cell carcinoma: A phase 2 clinical trial.
  Cell reports. Medicine · 2026 · Liu Y, Zhang XY, Wei WS, et al.
  PMID 42013852DOI 10.1016/j.xcrm.2026.102747
• Synergistic induction of ferroptosis by paclitaxel and sunitinib is mediated through SLC7A11 in lung cancer.
  International immunopharmacology · 2026 · Jin M, Hu J, Zheng A, et al.
  PMID 41955701DOI 10.1016/j.intimp.2026.116595
• Elucidating the binding and metabolic interactions of sunitinib and sorafenib with Cytochrome P450s CYP2U1 and CYP2D6.
  Molecular pharmacology · 2026 · Tang TY, Li Y, Chapman P, et al.
  PMID 41946119DOI 10.1016/j.molpha.2026.100114
• PABPC1-induced stabilization of PGK1 mRNA reduces apoptosis and sunitinib sensitivity in renal cell carcinoma by suppressing endoplasmic reticulum stress.
  Cell death & disease · 2026 · Chen X, Cao S, Jia T, et al.
  PMID 41932875DOI 10.1038/s41419-026-08676-3

The 10 most recently updated of 596 ClinicalTrials.gov registrations naming Sunitinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of IDRX-42 (GSK6042981) Versus (vs) Sunitinib in Participants With Gastrointestinal Stromal Tumors After Imatinib Therapy
  Recruiting · Phase 3 · Interventional · 450 enrolled · GlaxoSmithKline
  NCT07218926updated 2026-06-12
• Pre-Surgical Sutent in Renal Cell Carcinoma (RCC)
  Active not recruiting · Phase 2 · Interventional · 50 enrolled · M.D. Anderson Cancer Center
  NCT00715442updated 2026-06-12
• Sunitinib Malate With Hormonal Ablation for Patients Who Will Have Prostatectomy
  Active not recruiting · Phase 2 · Interventional · 64 enrolled · M.D. Anderson Cancer Center
  NCT00329043updated 2026-06-12
• Losartan + Sunitinib in Treatment of Osteosarcoma
  Recruiting · Phase 1 · Interventional · 41 enrolled · University of Colorado, Denver
  NCT03900793updated 2026-06-11
• Pan Tumor Rollover Study
  Recruiting · Phase 2 · Interventional · 1,500 enrolled · Bristol-Myers Squibb
  NCT03899155updated 2026-06-03
• Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
  Active not recruiting · Phase 2 · Interventional · 6,452 enrolled · National Cancer Institute (NCI)
  NCT02465060updated 2026-06-03
• Comparing Retreatment of 177Lu-DOTATATE PRRT Versus the Usual Treatment in Patients With Metastatic Unresectable Gastroenteropancreatic Neuroendocrine Tumors, NET RETREAT Trial
  Recruiting · Phase 2 · Interventional · 100 enrolled · National Cancer Institute (NCI)
  NCT05773274updated 2026-06-03
• TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer
  Recruiting · Phase 2 · Interventional · 4,200 enrolled · American Society of Clinical Oncology
  NCT02693535updated 2026-05-29
• Expanded Access to Bezuclastinib to be Coadministered With Sunitinib for Patients With Gastrointestinal Stromal Tumors
  Available · Expanded access · Cogent Biosciences, Inc.
  NCT06948955updated 2026-05-28
• Testing Sunitinib as Potentially Targeted Treatment in Cancers With cKIT Genetic Changes (MATCH - Subprotocol V)
  Active not recruiting · Phase 2 · Interventional · 10 enrolled · National Cancer Institute (NCI)
  NCT06390826updated 2026-05-28

Frequently asked questions

How does Sunitinib work?

Sunitinib is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs), some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Sunitinib was evaluated for its inhibitory activity against a variety of kinases (>80 kinases) and was identified as an inhibitor of platelet-derived growth factor receptors (PDGFRα and PDGFRβ), vascular endothelial growth factor receptors (VEGFR1, VEGFR2, and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor Type 1 (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET).

What is Sunitinib used for?

According to FDA labeling, Sunitinib carries indications including: Sunitinib malate is a kinase inhibitor indicated for: treatment of adult patients with gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib mesylate. ( 1.1 ) treatment of adult patients with advanced renal cell carcinoma (RCC).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Sunitinib?

Sunitinib is classified as Other protein kinase inhibitors, Kinase Inhibitor, Protein Kinase Inhibitors, Receptor Tyrosine Kinase Inhibitors, Vascular Growth Decrease.

What are the brand names for Sunitinib?

Sunitinib is marketed under brand names including Sutent.

What are the contraindications for Sunitinib?

Sunitinib labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.