Chronic Myeloid Leukemia (CML) is a clonal disease characterized by the presence of the
Philadelphia (Ph+) chromosome and its oncogenic product, BCR-ABL, a constitutively active …

Pyrimidine (imatinib, dasatinib, nilotinib and pazopanib), pyridine (sorafenib) and pyrrole
(sunitinib) tyrosine kinase inhibitors (TKIs) are multi-targeted TKIs with high activity towards …

Introduction: Because of their important roles in disease and excellent 'druggability', kinases
have become the second largest drug target family. The great success of the BCR-ABL …

The use of small molecules became one key cornerstone of targeted anti-cancer therapy.
Among them, tyrosine kinase inhibitors (TKIs) are especially important, as they were the first …

Imatinib has so far been the first-choice treatment in chronic myeloid leukemia with excellent
results. However, only a proportion of patients achieve major molecular response–hence the …

Background This study explored the impact of genetic polymorphisms in cytochrome P450
(CYP) enzymes and transporters on the plasma trough concentration of imatinib mesylate …

Introduction: Co-medication, gene polymorphisms and co-morbidity are main causes for
high variability in expression and function of the CYP3A isoenzymes. Pharmacokinetic …

Abstract Heme oxygenase-1 (HO-1) is the enzyme catalyzing the rate-limiting oxidative
degradation of cellular heme into free iron, carbon monoxide (CO), and biliverdin, which is …

Pharmacogenomics is based on the understanding of the individual differences in drug use,
the response to drug therapy (efficacy and toxicity), and the mechanisms underlying variable …

Small molecule therapy is a critical component of targeted anticancer treatment, with
tyrosine kinase inhibitors (TKIs) being the first compounds to treat the clonal Chronic …