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Lapatinib
From Proteopedia
(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" | ||
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| - | ! 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> | + | ! 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 | ||
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! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr) | ! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr) | ||
! 4 | ! 4 | ||
| - | ! | + | ! 8 |
| - | ! | + | ! 8.3 |
|- | |- | ||
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml) | ! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml) | ||
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! Lapatinib (Tykerb) | ! Lapatinib (Tykerb) | ||
! Sunitinib (Sutent) | ! Sunitinib (Sutent) | ||
| - | ! | + | ! 29-49 |
|- | |- | ||
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ||
| - | ! | + | ! 99 |
| - | ! | + | ! 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) | ||
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|- | |- | ||
! Metabolism | ! Metabolism | ||
| - | ! | + | ! Hepatic (CYP3A4) |
| - | ! | + | ! Hepatic (CYP3A4) |
| - | ! | + | ! Hepatic (CYP3A4) |
|} | |} | ||
Revision as of 08:11, 6 December 2010
Pharmacokinetics
| Tyrosine Kinase Inhibitor Pharmacokinetics [1][2][3][4][5] | |||||
|---|---|---|---|---|---|
| Parameter | Lapatinib (Tykerb) | Sunitinib (Sutent) | Sorafenib (Nexavar) | ||
| Tmax (hr) | 4 | 8 | 8.3 | ||
| Cmax (ng/ml) | 115 | 24.6 | 460 | ||
| Bioavailability (%) | Lapatinib (Tykerb) | Sunitinib (Sutent) | 29-49 | ||
| Protein Binding (%) | 99 | 95 | 99 | ||
| T1/2 (hr) | 9.6 | 83 | 29 | ||
| AUC (ng/ml/hr) | 1429 | 1921 | 11040 | ||
| IC50 (nM) | Lapatinib (Tykerb) | Sunitinib (Sutent) | Sorafenib (Nexavar) | ||
| Dosage (mg) | 100 | 50 | 50 | ||
| Metabolism | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | ||
