The human breast cancer resistance protein (BCRP, gene symbol ABCG2) is an ATP-
binding cassette (ABC) efflux transporter. It was so named because it was initially cloned …

Imatinib, nilotinib, and dasatinib are tyrosine kinase inhibitors (TKIs) that have become first-
line treatments for Philadelphia chromosome-positive chronic myeloid leukemia (CML) …

Several cytochrome P450 (CYP) CYP3A polymorphisms were associated with reduced
enzyme function. We aimed to evaluate the influence of these alleles on the …

Introduction Interindividual differences in drug response are a frequent clinical challenge
partly due to variation in pharmacokinetics. ATP-binding cassette (ABC) transporters are …

Cytochrome P450 3A4 (CYP3A4), one of the most important members of the cytochrome
P450 subfamily, is a crucial catalyst in the metabolism of numerous drugs. As it catalyzes …

The human breast cancer resistance protein (BCRP/ABCG2) is an ATP-binding cassette
efflux transporter that uses ATP hydrolysis to expel xenobiotics from cells, including anti …

Small-molecule inhibitors of tyrosine kinases (TKIs) are the mainstay of treatment for many
malignancies and represent novel treatment options for other diseases such as idiopathic …

The widespread expression and polyspecificity of the multidrug ABCG2 efflux transporter
make it an important determinant of the pharmacokinetics of a variety of substrate drugs. Null …

Highlights•Complete overview on exposure–response relationships for TKIs used in solid
tumors.•Dose individualization is expected to minimize toxicity and improve efficacy.•For …

Cancer treatment is becoming more and more individually based as a result of the large
inter-individual differences that exist in treatment outcome and toxicity when patients are …