Sunitinib
- Atc Codes:L01XE04
- CAS Codes:557795-19-4#341031-54-7
- PHARMGKB ID:557795-19-4#341031-54-7
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Sutent; Belgium: Sutent; Bulgaria: Sutent; Cyprus: Sutent; Czech Republic: Sutent; Denmark: Sutent; Estonia: Sutent; Finland: Sutent; France: Sutent; Germany: Sutent; Greece: Sutent; Hungary: Sutent; Ireland: Sutent; Italy: Sutent; Latvia: Sutent; Lithuania: Sutent; Luxembourg: Sutent; Malta: Sutent; Netherlands: Sutent; Poland: Sutent; Portugal: Sutent; Romania: Sutent; Slovakia: Sutent; Slovenia: Sutent; Spain: Sutent; Sweden: Sutent; UK: Sutent.
North America
Canada: Sutent; USA: Sutent.
Latin America
Argentina: Sutent; Brazil: Sutent; Mexico: Sutent.
Asia
Japan: Sutent.
Drug combinations
Chemistry
Sunitinib: C~22~H~27~FN~4~O~2~. Mw: 398.47. N-(2-Diethylaminoethyl)-5-[(Z)-(5-fluoro-2-oxo-indolin-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide. CAS-557795-19-4.
Sunitinib Malate: C~22~H~27~FN~4~O~2~ C~4~H~6~O~5~. Mw: 532.60. Butanedioic acid, hydroxy-, (2S)-, compound 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). CAS-341031-54-7 (2006).
Pharmacologic Category
Other Antineoplastic Agents; Protein Kinase Inhibitors. Tyrosine Kinase Inhibitor. Vascular Endothelial Growth Factor Inhibitor. (ATC-Code: L01XE04).
Mechanism of action
Exhibits antitumor and antiangiogenic properties by inhibiting multiple receptor tyrosine kinases, including platelet-derived growth factors (PDGFR-α and PDGFR-β), vascular endothelial growth factors (VEGFR-1, VEGFR-2, and VEGFR-3), FMS-like tyrosine kinase-3 (FLT3), colony-stimulating factor type 1 (CSF-1R), and glial cell-line-derived neurotrophic factor receptor.
Therapeutic use
Gastrointestinal stromal tumor. Advanced renal cell cancer.
Pregnancy and lactiation implications
Animal studies demonstrated teratogenicity and fetal loss. There are no adequate studies in pregnant women. Excretion in breast milk unknown (not recommended in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to sunitinib or any component of the formulation, or pregnancy.
Warnings and precautions
Adrenal toxicity reported. Hemorrhagic events reported. May cause skin and/or hair depigmentation or discoloration. Serious and fatal GI complications occurred. May cause hypertension. May cause decrease in left ventricular ejection fraction. QTc prolongation and torsade de pointes observed (use caution in history of QTc prolongation, with medications known to increase sunitinib levels or prolong QT interval, or pre-existing (relevant) cardiac disease, bradycardia, or electrolyte imbalance). Reversible posterior leukoencephalopathy syndrome reported (confusion, headache, hypertension, lethargy, seizure, blindness and/or other vision, or neurologic disturbances). Hypothyroidism may occur. Hyperthyroidism, sometimes followed by hypothyroidism, also reported. Microangiopathic hemolytic anemia reported when sunitinib used in combination with bevacizumab. Use with caution in patients concurrently taking strong CYP3A4 inhibitors (may increase sunitinib levels) or inducers (may decrease sunitinib levels).