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=" | ! 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) | |||
|} | |} | ||