This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
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
