Sunitinib Malate
Generic Name: sunitinib malate
Brand Names:
Sutent
11 DESCRIPTION Sunitinib is a kinase inhibitor present in SUTENT capsules as the malate salt. Sunitinib malate is described chemically as (2 S )-2-hydroxybutanedoic acid with N -[2-(diethylamino)ethyl]-5-[( Z )-(5-fluoro-1,2-dihydro-2-oxo- 3H -indol-3-ylidine)methyl]-2,4-dimethyl- 1H -pyrrole-3-carboxamide (1:1). The molecular formula is C 22 H 27 FN 4 O 2 ∙ C 4 H 6 O 5 and the molecular weight is 532.6 Daltons.
Overview
11 DESCRIPTION Sunitinib is a kinase inhibitor present in SUTENT capsules as the malate salt. Sunitinib malate is described chemically as (2 S )-2-hydroxybutanedoic acid with N -[2-(diethylamino)ethyl]-5-[( Z )-(5-fluoro-1,2-dihydro-2-oxo- 3H -indol-3-ylidine)methyl]-2,4-dimethyl- 1H -pyrrole-3-carboxamide (1:1). The molecular formula is C 22 H 27 FN 4 O 2 ∙ C 4 H 6 O 5 and the molecular weight is 532.6 Daltons.
Uses
1 INDICATIONS AND USAGE SUTENT 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). ( 1.2 ) • adjuvant treatment of adult patients at high risk of recurrent RCC following nephrectomy. ( 1.3 ) • treatment of progressive, well-differentiated pancreatic neuroendocrine tumors (pNET) in adult patients with unresectable locally advanced or metastatic disease. ( 1.4 ) 1.1 Gastrointestinal Stromal Tumor SUTENT is indicated for the treatment of adult patients with gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib mesylate.
Dosage
2 DOSAGE AND ADMINISTRATION 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 SUTENT 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. SUTENT may be taken with or without food.
Side Effects
6 ADVERSE REACTIONS 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 Warni...
Interactions
7 DRUG INTERACTIONS • CYP3A4 Inhibitors : Consider dose reduction of SUTENT when administered with strong CYP3A4 inhibitors. ( 7.1 ) • CYP3A4 Inducers : Consider dose increase of SUTENT when administered with strong CYP3A4 inducers. ( 7.1 ) 7.1 Effect of Other Drugs on SUTENT Strong CYP3A4 Inhibitors Co-administration with strong CYP3A4 inhibitors may increase sunitinib plasma concentrations [see Clinical Pharmacology (12.3) ] . Select an alternate concomitant medication with no or minimal enzyme inhibition potential. Consider a dose reduction for SUTENT when it is co-administered with strong CYP3A4 inhibitors [see Dosage and Administration (2.5) ] .
Warnings
WARNING: HEPATOTOXICITY Hepatotoxicity may be severe, and in some cases, fatal. Monitor hepatic function and interrupt, dose reduce, or discontinue SUTENT as recommended [see Warnings and Precautions (5.1) ] . WARNING: HEPATOTOXICITY See full prescribing information for complete boxed warning. Hepatotoxicity may be severe, and in some cases fatal. Monitor hepatic function and interrupt, dose reduce, or discontinue SUTENT as recommended [see Warnings and Precautions (5.1) ]. 5 WARNINGS AND PRECAUTIONS • Hepatotoxicity : Fatal liver failure has been observed. Monitor liver function tests at baseline, during each cycle, and as clinically indicated. Interrupt SUTENT for Grade 3 hepatotoxicity until resolution to Grade ≤1 or baseline and resume SUTENT at a reduced dose; discontinue if no resolution. Discontinue SUTENT 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. 4 CONTRAINDICATIONS None. None ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary Based on animal reproduction studies and its mechanism of action, SUTENT 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.
Storage
Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].
Frequently Asked Questions
What is Sunitinib Malate used for?▼
1 INDICATIONS AND USAGE SUTENT 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). ( 1.2 ) • adjuvant treatment of adult patients at high risk of recurrent RCC following nephrectomy. ( 1.3 ) • treatment of progressive, well-differentiated pancreatic neuroendocrine tumors (pNET) in adult patients with unresectable locally advanced or metastatic disease. ( 1.4 ) 1.1 Gastrointestinal Stromal Tumor SUTENT is indicated for the treatment of adult patients with gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib mesylate.
What are the side effects of Sunitinib Malate?▼
6 ADVERSE REACTIONS 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 Warni...
Can I take Sunitinib Malate during pregnancy?▼
8.1 Pregnancy Risk Summary Based on animal reproduction studies and its mechanism of action, SUTENT 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.
What are the important warnings for Sunitinib Malate?▼
WARNING: HEPATOTOXICITY Hepatotoxicity may be severe, and in some cases, fatal. Monitor hepatic function and interrupt, dose reduce, or discontinue SUTENT as recommended [see Warnings and Precautions (5.1) ] . WARNING: HEPATOTOXICITY See full prescribing information for complete boxed warning. Hepatotoxicity may be severe, and in some cases fatal. Monitor hepatic function and interrupt, dose reduce, or discontinue SUTENT as recommended [see Warnings and Precautions (5.1) ]. 5 WARNINGS AND PRECAUTIONS • Hepatotoxicity : Fatal liver failure has been observed. Monitor liver function tests at baseline, during each cycle, and as clinically indicated. Interrupt SUTENT for Grade 3 hepatotoxicity until resolution to Grade ≤1 or baseline and resume SUTENT at a reduced dose; discontinue if no resolution. Discontinue SUTENT 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. 4 CONTRAINDICATIONS None. None ( 4 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.