Sorafenib: Difference between revisions

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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 [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|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>
!  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>
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! Parameter
! Parameter
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! [[Sorafenib]] (Nexavar)
! [[Sorafenib]] (Nexavar)
|-
|-
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)  
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)  
! 8
! 8
! 8.3
! 8.3
|-
|-
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)  
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)  
! 24.6
! 24.6
! 460
! 460
|-
|-
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
! Variable
! Variable
! 29-49
! 29-49
|-
|-
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
! 95
! 95
! 99
! 99
|-
|-
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! 83
! 83
! 29
! 29
|-
|-
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! [[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)
  1. ↑ D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.
  2. ↑ R. Khosravan, et al. General Poster Session, Developmental Therapeutics: Cytotoxic Chemotherapy, J Clin Oncol 26: 2008 (May 20 suppl; abstr 2578)
  3. ↑ 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
  4. ↑ 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
  5. ↑ 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

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