Sorafenib: Difference between revisions
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David Canner (talk | contribs) New page: ===Pharmacokinetics=== {| class="wikitable" border="1" width="40%" style="text-align:center" |- ! colspan="6" align="center"| VEGFR Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Tran... |
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! colspan="6" align="center"| VEGFR Inhibitor [[ | ! colspan="6" align="center"| VEGFR Inhibitor [[Pharmacokinetics]] <ref>D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.</ref><ref>R. Khosravan, et al. General Poster Session, Developmental Therapeutics: Cytotoxic Chemotherapy, J Clin Oncol 26: 2008 (May 20 suppl; abstr 2578)</ref><ref>PMID:16133532</ref><ref>PMID:20821331</ref><ref>PMID:20717111</ref> | ||
|- | |- | ||
! Parameter | ! Parameter | ||
| Line 9: | Line 9: | ||
! [[Sorafenib]] (Nexavar) | ! [[Sorafenib]] (Nexavar) | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr) | ||
! 8 | ! 8 | ||
! 8.3 | ! 8.3 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml) | ||
! 24.6 | ! 24.6 | ||
! 460 | ! 460 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%) | ||
! Variable | ! Variable | ||
! 29-49 | ! 29-49 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%) | ||
! 95 | ! 95 | ||
! 99 | ! 99 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ||
! 83 | ! 83 | ||
! 29 | ! 29 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ||
! 1921 | ! 1921 | ||
! 11040 | ! 11040 | ||
Revision as of 12:53, 9 December 2010
Pharmacokinetics
| VEGFR Inhibitor Pharmacokinetics [1][2][3][4][5] | |||||
|---|---|---|---|---|---|
| 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) | |||
- ↑ 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