Abstract The 4-anilinoquinazolines (gefitinib, erlotinib and lapatinib) are members of a class
of potent and selective inhibitors of the human epidermal growth factor receptor (HER) family …

Importance of the field: A concerted effort by the pharmaceutical industry over the last
decade has led to the successful clinical development of protein kinase inhibitors as …

In the recent years, eight tyrosine kinase inhibitors (TKIs) have been approved for cancer
treatment and numerous are under investigation. These drugs are rationally designed to …

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

Background: Gefitinib is an orally active inhibitor of epidermal growth factor receptor (EGFR)
tyrosine kinase (TK) with activity in non–small-cell lung cancer. The response to gefitinib is …

1. The pharmacokinetics of gefitinib and its metabolites in rat and dog were investigated in
preclinical studies conducted to support the safety evaluation and clinical development of …

Purpose: To examine the enzyme kinetics of gefitinib and erlotinib metabolism by individual
cytochrome P450 (CYP) enzymes, and to compare their effects on CYP3A activity, with the …

Gefitinib (Iressa, AstraZeneca) has been widely used for the treatment of locally advanced or
metastatic non-small cell lung cancer. A number of studies have been reported on its …

Background and objectives: Gefitinib (IRESSA®, ZD1839), an epidermal growth factor
receptor tyrosine kinase inhibitor, has been approved in several countries for the treatment …

Background and objectives Exposure to gefitinib (IRESSA®, ZD1839), an epidermal growth
factor receptor-tyrosine kinase inhibitor, is highly variable between subjects. In an attempt to …