Name: | sunitinib |
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PubChem Compound ID: | 10046539 |
Molecular formula: | C22H27FN4O2 |
Molecular weight: | 400.466 g/mol |
Name: | sunitinib |
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Name (isomeric): | DB01268 |
Drug Type: | small molecule |
Synonyms: |
Sutent; Sunitinib malate; SU11248
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Brand: | sunitinib, Sutent, SU-11248 |
Category: | Antineoplastic Agents, Angiogenesis Inhibitors |
CAS number: | 557795-19-4 |
Indication: | For the treatment of advanced renal cell carcinoma as well as the treatment of gastrointestinal stromal tumor after disease progression on or intolerance to imatinib mesylate. |
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Pharmacology: | Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA on January 26, 2006. |
Mechanism of Action: |
Sunitinib is a small molecule that inhibits multiple 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 (PDGFRa ...
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Absorption: | Maximum plasma concentrations (Cmax) of sunitinib are generally observed between 6 and 12 hours (Tmax) following oral administration. Food has no effect on the bioavailability of sunitinib. Sunitinib may be taken with or without food. |
Protein binding: | Binding of sunitinib and its primary metabolite to human plasma protein in vitro was 95% and 90%, respectively. |
Biotransformation: | Sunitinib is metabolized primarily by the cytochrome P450 enzyme, CYP3A4, to produce its primary active metabolite, which is further metabolized by CYP3A4. |
Route of elimination: | Sunitinib is metabolized primarily by the cytochrome P450 enzyme, CYP3A4, to produce its primary active metabolite, which is further metabolized by CYP3A4. Elimination is primarily via feces. In a human mass balance study of [14C]sunitinib, 61% of the dose was eliminated in feces, with renal elimination accounting for 16% of the administered dose. |
Half Life: | Following administration of a single oral dose in healthy volunteers, the terminal half-lives of sunitinib and its primary active metabolite are approximately 40 to 60 hours and 80 to 110 hours, respectively. |
Clearance: | Oral cl=34 - 62 L/h |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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