Tyrosine Kinase Inhibitor Pharmacokinetics
From Proteopedia
| Tyrosine Kinase Inhibitor Pharmacokinetics | ||||||||
|---|---|---|---|---|---|---|---|---|
| VEGFR & KIT Inhibitors | EGFR Inhibitors | BCR-Abl Inhibitor | ||||||
| Parameter | Sunitinib (Sutent) | Sorafenib (Nexavar) | Erlotinib (Tarceva) | Gefitinib (Iressa) | Lapatinib (Tykerb) | Imatinib (Gleevec) | Nilotinib (Tasigna) | Dasatinib (Sprycel) |
| Tmax (hr) | 8 | 8.3 | 2.0 | 5.4 | 4 | 3.7 | 3.0 | 1.0 |
| Cmax (ng/ml) | 24.6 | 460 | 69.6 | 130 | 115 | 2070 | 411 | 124 |
| Bioavailability (%) | Variable | 29-49 | 99 | 59 | Variable | 98 | 30 | 20 |
| Protein Binding (%) | 95 | 99 | 93 | 90 | 99 | 95 | 98 | 96 |
| T1/2 (hr) | 83 | 29 | 9.4 | 26.9 | 9.6 | 26.6 | 16.0 | 3.3 |
| AUC (ng/ml/hr) | 1921 | 11040 | 20577 | 3850 | 1429 | 4760 | 10052 | 461 |
| Dosage (mg) | 50 | 50 | 150 | 250 | 100 | 400 | 200 | 200 |
| Metabolism | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) |
For Pharmacokinetic Data References, see: References
