Gefitinib: Difference between revisions

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{| class="wikitable" border="1" width="40%" style="text-align:center"
{| class="wikitable" border="1" width="40%" style="text-align:center"
|-
|-
!  colspan="6" align="center"| EGFR Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]] Comparison at Equivalent Dosages <ref>PMID:16609030</ref><ref>PMID:17482782</ref>
!  colspan="4" align="center"| EGFR Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]] Comparison at Equivalent Dosages <ref>PMID:16609030</ref><ref>PMID:17482782</ref><ref>D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.</ref>
|-
|-
! Parameter
! Parameter
! [[Erlotinib]] (Tarceva)
! [[Erlotinib]] (Tarceva)
! [[Gefitinib]] (Iressa)
! [[Gefitinib]] (Iressa)
 
! Lapatinib (Tykerb)
|-
|-
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)  
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)  
! 2.0
! 2.0
! 5.4
! 5.4
 
! 8.3
|-
|-
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)  
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)  
! 69.6
! 69.6
! 130
! 130
|-
|-
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
! 99
! 99
! 59
! 59
! 29-49
|-
|-
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
! 93
! 93
! 90
! 90
! 99
|-
|-
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! 9.4
! 9.4
! 26.9
! 26.9
! 29
|-
|-
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! 20577
! 20577
! 3850
! 3850
! 11040
|-
|-
! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
! 2
! 2
! 23
! 23
! 12
|-
|-
! Typical Dosage (mg)
! Typical Dosage (mg)
! 150
! 150
! 250
! 250
! 50
|-
|-
! Metabolism
! Metabolism
! Hepatic - (CYP3A4, CYP3A5, CYP2D6, CYP1A1)
! Hepatic - (CYP3A4, CYP3A5, CYP2D6, CYP1A1)
! Hepatic - (CYP3A4, CYP3A5, CYP2D6, CYP1A1, CYP1A2)
! Hepatic - (CYP3A4, CYP3A5, CYP2D6, CYP1A1, CYP1A2)
! Hepatic (CYP3A4)
|}
|}


Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

David Canner, Michal Harel, Joel L. Sussman