Malate

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
• Jul 7, 2015ANDAANDA078027Teva Pharms Usa
• May 28, 2021NDANDA213378Alkermes Inc
• Aug 16, 2021ANDAANDA213914Sun Pharm
• Nov 30, 2021ANDAANDA213803Teva Pharms Usa
• Dec 6, 2021ANDAANDA201275Mylan
• Apr 11, 2022ANDAANDA215843Dr Reddys
• Aug 21, 2023ANDAANDA218012Fosun Wanbang

1. 1Death7,41418%
2. 2Diarrhoea4,44511%
3. 3Fatigue4,27710%
4. 4Disease Progression3,9129.5%
5. 5Nausea3,4718.5%
6. 6Asthenia2,4876.1%
7. 7Decreased Appetite2,3715.8%
8. 8Vomiting2,2845.6%
9. 9Neoplasm Progression2,0194.9%
10. 10Hypertension1,8094.4%
11. 11Dysgeusia1,6994.1%
12. 12Weight Decreased1,6614.1%
13. 13Malaise1,6304.0%
14. 14Stomatitis1,4653.6%
15. 15Palmar-plantar Erythrodysaesthesia Syndrome1,4553.5%

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

• Targeting of Staphyloxanthin and α-Hemolysin by Natural Compound L-Malic Acid Suppresses Staphylococcus aureus Virulence.
  FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2026 · Shen L, Wang B, Yang J, et al.
  PMID 42216777DOI 10.1096/fj.202600917R
• Aspartate-Glutamate Carrier 1 (SLC25A12) Deficiency: Malate-Aspartate Shuttle Failure, Neurodevelopmental Epileptic Encephalopathy, and Ketone-Based Metabolic Therapy.
  International journal of molecular sciences · 2026 · Murano M, Iaconisi GN, Monné M, et al.
  PMID 42196434DOI 10.3390/ijms27104455
• Simultaneous enhancement of porosity and thermal stability in hydroxyethyl cellulose membranes via malic acid incorporation and non-solvent induced phase separation.
  International journal of biological macromolecules · 2026 · Ryu H, Kang SW
  PMID 42092651DOI 10.1016/j.ijbiomac.2026.152377
• Optimization and scale up of L-malic acid production from methanol by the methylotrophic yeast Ogataea polymorpha.
  FEMS yeast research · 2026 · Mauri A, Yovcheva M, Demling P, et al.
  PMID 42080835DOI 10.1093/femsyr/foag017
• VcNADP-ME4 positively regulates malic acid degradation in blueberry fruit as modulated by two bZIPs.
  Journal of plant physiology · 2026 · Dai Y, Min Y, Leng Y, et al.
  PMID 42068770DOI 10.1016/j.jplph.2026.154786
• Raman Spectroscopy-Based Glucose Feed Control Automates Malic Acid Fermentation.
  Biotechnology and bioengineering · 2026 · Grebe LA, Hürter K, Engel D, et al.
  PMID 42057341DOI 10.1002/bit.70211
• Organic acids counteract the determinate root development induced by phosphate deprivation in Arabidopsis thaliana.
  Plant signaling & behavior · 2026 · Corona-Sánchez I, López-Bucio J, Villalobos-Escobedo JM, et al.
  PMID 42026737DOI 10.1080/15592324.2026.2662710
• Advancing Malic Acid Production of Aspergillus oryzae: Combined Process Optimization and Application of Various Substrates.
  Biotechnology and bioengineering · 2026 · Hartmann L, Neumann A, Holtmann D, et al.
  PMID 41981792DOI 10.1002/bit.70201

The 10 most recently updated of 326 ClinicalTrials.gov registrations naming Malate as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• 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
• A Study to Test the Addition of the Drug Cabozantinib to Chemotherapy in Patients With Newly Diagnosed Osteosarcoma
  Recruiting · Phase 2 · Phase 3 · Interventional · 1,122 enrolled · National Cancer Institute (NCI)
  NCT05691478updated 2026-06-12
• Testing Nivolumab and Ipilimumab Immunotherapy With or Without the Targeted Drug Cabozantinib in Recurrent, Metastatic, or Incurable Nasopharyngeal Cancer
  Recruiting · Phase 2 · Interventional · 50 enrolled · National Cancer Institute (NCI)
  NCT05904080updated 2026-06-12
• Cabozantinib S-malate in Treating Patients With Relapsed Osteosarcoma or Ewing Sarcoma
  Active not recruiting · Phase 2 · Interventional · 90 enrolled · National Cancer Institute (NCI)
  NCT02243605updated 2026-06-12
• Testing the Addition of the Anti-cancer Drug, Cabozantinib, to the Usual Immunotherapy Treatment, Avelumab, in Patients With Metastatic Urothelial Cancer, MAIN-CAV Study
  Active not recruiting · Phase 3 · Interventional · 654 enrolled · National Cancer Institute (NCI)
  NCT05092958updated 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
• Using Nivolumab Alone or With Cabozantinib to Prevent Mucosal Melanoma Return After Surgery
  Active not recruiting · Phase 2 · Interventional · 101 enrolled · National Cancer Institute (NCI)
  NCT05111574updated 2026-06-11
• Cabozantinib-S-Malate in Treating Younger Patients With Recurrent, Refractory, or Newly Diagnosed Sarcomas, Wilms Tumor, or Other Rare Tumors
  Active not recruiting · Phase 2 · Interventional · 109 enrolled · National Cancer Institute (NCI)
  NCT02867592updated 2026-06-11
• Losartan + Sunitinib in Treatment of Osteosarcoma
  Recruiting · Phase 1 · Interventional · 41 enrolled · University of Colorado, Denver
  NCT03900793updated 2026-06-11
• Testing the Effectiveness of Two Immunotherapy Drugs (Nivolumab and Ipilimumab) With One Anti-cancer Targeted Drug (Cabozantinib) for Rare Genitourinary Tumors
  Recruiting · Phase 2 · Interventional · 314 enrolled · National Cancer Institute (NCI)
  NCT03866382updated 2026-06-11

Frequently asked questions

How does Malate 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 Malate used for?

According to FDA labeling, Malate 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 are the contraindications for Malate?

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