Lapatinib
From Proteopedia
(Difference between revisions)
| Line 3: | Line 3: | ||
{| class="wikitable" border="1" width="40%" style="text-align:center" | {| class="wikitable" border="1" width="40%" style="text-align:center" | ||
|- | |- | ||
| - | ! colspan="6" align="center"| | + | ! colspan="6" align="center"| Tyrosine Kinase 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> |
|- | |- | ||
! Parameter | ! Parameter | ||
| Line 10: | Line 10: | ||
|- | |- | ||
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr) | ! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr) | ||
| - | ! 4 | ||
! 8 | ! 8 | ||
| + | ! 8.3 | ||
|- | |- | ||
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml) | ! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml) | ||
| - | ! 115 | ||
! 24.6 | ! 24.6 | ||
| + | ! 460 | ||
|- | |- | ||
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%) | ! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%) | ||
| - | ! Lapatinib (Tykerb) | ||
! Sunitinib (Sutent) | ! Sunitinib (Sutent) | ||
| + | ! 29-49 | ||
|- | |- | ||
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ||
| - | ! 99 | ||
! 95 | ! 95 | ||
| + | ! 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) | ||
| - | ! 9.6 | ||
! 83 | ! 83 | ||
| + | ! 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) | ||
| - | ! 1429 | ||
! 1921 | ! 1921 | ||
| + | ! 11040 | ||
|- | |- | ||
! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM) | ! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM) | ||
| - | ! Lapatinib (Tykerb) | ||
! Sunitinib (Sutent) | ! Sunitinib (Sutent) | ||
| + | ! Sorafenib (Nexavar) | ||
|- | |- | ||
! Dosage (mg) | ! Dosage (mg) | ||
| - | ! | + | ! 50 |
! 50 | ! 50 | ||
|- | |- | ||
Revision as of 08:38, 6 December 2010
Pharmacokinetics
| Tyrosine Kinase Inhibitor Pharmacokinetics [1][2][3][4][5] | |||||
|---|---|---|---|---|---|
| Parameter | Sunitinib (Sutent) | Sorafenib (Nexavar) | |||
| Tmax (hr) | 8 | 8.3 | |||
| Cmax (ng/ml) | 24.6 | 460 | |||
| Bioavailability (%) | Sunitinib (Sutent) | 29-49 | |||
| Protein Binding (%) | 95 | 99 | |||
| T1/2 (hr) | 83 | 29 | |||
| AUC (ng/ml/hr) | 1921 | 11040 | |||
| IC50 (nM) | Sunitinib (Sutent) | Sorafenib (Nexavar) | |||
| Dosage (mg) | 50 | 50 | |||
| Metabolism | Hepatic (CYP3A4) | Hepatic (CYP3A4) | |||
