Sunitinib
|
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
- ↑ http://www.inpharm.com/news/101125/renal-cell-carcinoma-market-votrient-sutent
- ↑ D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.
- ↑ R. Khosravan, et al. General Poster Session, Developmental Therapeutics: Cytotoxic Chemotherapy, J Clin Oncol 26: 2008 (May 20 suppl; abstr 2578)
- ↑ 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
- ↑ 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
- ↑ 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