Sunitinib

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spinqualitylabelsall models Sunitinib, also known as Sutent, (3g0e) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Better Known as: Sutent

• Marketed By: Pfizer
  
• Major Indication: Renal Cell Carcinoma & Stomach Cancer
  
• Drug Class: Receptor Tyrosine Kinase (Including VEGFR & PDGFR) Inhibitor
• Date of FDA Approval (Patent Expiration): 2006 (2020)
  
• 2009 Sales: $964 Million ^[1]
• Importance:
• See Pharmaceutical Drugs for more information about other drugs and disorders.

Mechanism of Action

Pharmacokinetics

VEGFR Inhibitor Pharmacokinetics [2][3][4][5][6]
Parameter	Sunitinib (Sutent)	Sorafenib (Nexavar)
Tmax (hr)	8	8.3
Cmax (ng/ml)	24.6	460
Bioavailability (%)	Variable	29-49
Protein Binding (%)	95	99
T1/2 (hr)	83	29
AUC (ng/ml/hr)	1921	11040
Dosage (mg)	50	50
Metabolism	Hepatic (CYP3A4)	Hepatic (CYP3A4)

References

1. ↑ http://www.inpharm.com/news/101125/renal-cell-carcinoma-market-votrient-sutent
2. ↑ D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.
3. ↑ R. Khosravan, et al. General Poster Session, Developmental Therapeutics: Cytotoxic Chemotherapy, J Clin Oncol 26: 2008 (May 20 suppl; abstr 2578)
4. ↑ Lathia C, Lettieri J, Cihon F, Gallentine M, Radtke M, Sundaresan P. Lack of effect of ketoconazole-mediated CYP3A inhibition on sorafenib clinical pharmacokinetics. Cancer Chemother Pharmacol. 2006 May;57(5):685-92. Epub 2005 Aug 25. PMID:16133532 doi:10.1007/s00280-005-0068-6
5. ↑ Brendel E, Ludwig M, Lathia C, Robert C, Ropert S, Soria JC, Armand JP. Pharmacokinetic results of a phase I trial of sorafenib in combination with dacarbazine in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2010 Sep 7. PMID:20821331 doi:10.1007/s00280-010-1423-9
6. ↑ Boven E, Massard C, Armand JP, Tillier C, Hartog V, Brega NM, Countouriotis AM, Ruiz-Garcia A, Soria JC. A phase I, dose-finding study of sunitinib in combination with irinotecan in patients with advanced solid tumours. Br J Cancer. 2010 Sep 28;103(7):993-1000. Epub 2010 Aug 17. PMID:20717111 doi:10.1038/sj.bjc.6605852