PHARMACOKINETICSPROTEIN-tyrosine kinase inhibitorsPYRIMIDINESTARGETED drug deliveryNEOVASCULARIZATIONMETASTASISTUMOR growthPyrimidine (imatinib, dasatinib, nilotinib and pazopanib), pyridine (sorafenib) and pyrrole (sunitinib) tyrosine kinase inhibitors (TKIs) are multi-targeted TKIs with high activity towards ...
Pyrimidine (imatinib, dasatinib, nilotinib and pazopanib), pyridine (sorafenib) and pyrrole (sunitinib) tyrosine kinase inhibitors (TKIs) are multi-targeted TKIs with high activity towards several families of receptor and non-receptor tyrosine kinases involved in angiogenesis, tumour growth and metastatic...
Imatinib is a potent and selective inhibitor of the protein tyrosine kinase Bcr-Abl, platelet-derived growth factor receptors (PDGFRα and PDGFRβ) and KIT. Imatinib is approved for the treatment of chronic myeloid leukaemia (CML) and gastrointestinal stromal tumour (GIST), which have dysregulated...
Clinical pharmacokinetics of imatinib. Clin. Pharma- cokinet. 44, 879–894 (2005). 3 Cortes, J. E., Egorin, M. J., Guilhot, F., Molimard, M. & Mahon, F. X. Pharmacokinetic / pharmacodynamic correlation and blood-level testing in imatinib therapy for chronic myeloid leukemia. Leukemia...
Imatinib mesylate (IM) trough concentration varies among IM-treated chronic myeloid leukemia (CML) patients. Although IM pharmacokinetics is influenced by ... N Takahashi,M Miura,SA Scott,... - 《Journal of Human Genetics》 被引量: 294发表: 2010年 KRAS and BRAF mutations predict primary resist...
Phase I clinical trial combining imatinib mesylate and IL-2 in refractory cancer patients: IL-2 interferes with the pharmacokinetics of imatinib mesylate. Oncoimmunology 2013, 2, e23079. [CrossRef]Chaput N, Flament C, Locher C, Desbois M, Rey A, Rusakiewicz S, et al. Phase I clinical ...
PURPOSE: To evaluate the basic pharmacokinetic (PK) characteristics of imatinib mesylate and assess the relationship between the PK and pharmacodynamic (PD... Peng,B. - 《Journal of Clinical Oncology》 被引量: 764发表: 2004年 Pharmacokinetics and pharmacodynamics of recombinant human erythropoietin aft...
Clinical pharmacokinetics of tyrosine kinase inhibitors In the recent years, eight tyrosine kinase inhibitors (TKIs) have been approved for cancer treatment and numerous are under investigation. These drugs are ... NPV Erp,H Gelderblom,HJ Guchelaar - 《Clinical Pharmacokinetics》 被引量: 641发表: ...
No clinically significant impact of body weight, age, sex, race, and hepatic or renal impairment on the pharmacokinetics of asciminib has been observed and no dose adjustments are needed. The safety profile of asciminib is similar across all evaluated doses, showing good tolerability....
In conclusion, there are sufficient data that support TDM for imatinib and nilotinib targetingCminlevels of ≥ 1000 ng/mL and ≥ 469 ng/mL, respectively. For dasatinib, TDM could be especially useful to prevent excessive toxicity. The recommended Cminthreshold for toxicity is ≤ 2.5 ng/mL and...