Tyrosine Kinase Inhibitor Pharmacokinetics
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! colspan="6" align="center"| Tyrosine Kinase 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><ref>PMID:16609030</ref><ref>PMID:17482782</ref><ref>D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.</ref> | ! colspan="6" align="center"| Tyrosine Kinase 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><ref>PMID:16609030</ref><ref>PMID:17482782</ref><ref>D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.</ref> | ||
Revision as of 13:21, 9 December 2010
| Tyrosine Kinase Inhibitor Pharmacokinetics [1][2][3][4][5][6][7][8] | |||||
|---|---|---|---|---|---|
| Parameter | Sunitinib (Sutent) | Sorafenib (Nexavar) | Erlotinib (Tarceva) | Gefitinib (Iressa) | Lapatinib (Tykerb) |
| Tmax (hr) | 8 | 8.3 | 2.0 | 5.4 | 4 |
| Cmax (ng/ml) | 24.6 | 460 | 69.6 | 130 | 115 |
| Bioavailability (%) | Variable | 29-49 | 99 | 59 | Variable |
| Protein Binding (%) | 95 | 99 | 93 | 90 | 99 |
| T1/2 (hr) | 83 | 29 | 9.4 | 26.9 | 9.6 |
| AUC (ng/ml/hr) | 1921 | 11040 | 20577 | 3850 | 1429 |
| Dosage (mg) | 50 | 50 | 150 | 250 | 100 |
| Metabolism | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic - (CYP3A4) | Hepatic - (CYP3A4) | Hepatic - (CYP3A4) |
