Overcoming ABC transporter-mediated multidrug resistance: The dual role of tyrosine kinase inhibitors as multitargeting agents

GL Beretta, G Cassinelli, M Pennati, V Zuco… - European journal of …, 2017 - Elsevier
Resistance to conventional and target specific antitumor drugs still remains one of the major
cause of treatment failure and patience death. This condition often involves ATP-binding …

Imatinib, sunitinib and pazopanib: from flat‐fixed dosing towards a pharmacokinetically guided personalized dose

K Westerdijk, IME Desar, N Steeghs… - British journal of …, 2020 - Wiley Online Library
Tyrosine kinase inhibitors (TKIs) are anti‐cancer drugs that target tyrosine kinases, enzymes
that are involved in multiple cellular processes. Currently, multiple oral TKIs have been …

Individualized dosing of tyrosine kinase inhibitors: are we there yet?

D de Wit, HJ Guchelaar, J den Hartigh… - Drug discovery today, 2015 - Elsevier
Highlights•Complete overview on exposure–response relationships for TKIs used in solid
tumors.•Dose individualization is expected to minimize toxicity and improve efficacy.•For …

[HTML][HTML] Pharmacokinetically guided sunitinib dosing: a feasibility study in patients with advanced solid tumours

NAG Lankheet, JSL Kloth… - British journal of …, 2014 - nature.com
Background: Plasma exposure of sunitinib shows large inter-individual variation. Therefore,
a pharmacokinetic (PK) study was performed to determine safety and feasibility of sunitinib …

CYP3A5 and ABCB1 polymorphisms as predictors for sunitinib outcome in metastatic renal cell carcinoma

MHM Diekstra, JJ Swen, E Boven, D Castellano… - European urology, 2015 - Elsevier
Background In our exploratory studies, we associated single nucleotide polymorphisms
(SNPs) in candidate genes with the efficacy and toxicities of sunitinib in metastatic renal cell …

Association analysis of genetic polymorphisms in genes related to sunitinib pharmacokinetics, specifically clearance of sunitinib and SU12662

MHM Diekstra, HJ Klümpen, M Lolkema… - Clinical …, 2014 - Wiley Online Library
Interpatient variability in the pharmacokinetics (PK) of sunitinib is high. Single nucleotide
polymorphisms (SNPs) in PK candidate genes have been associated with the efficacy and …

CYP3A activity: towards dose adaptation to the individual

N Hohmann, WE Haefeli, G Mikus - Expert opinion on drug …, 2016 - Taylor & Francis
Introduction: Co-medication, gene polymorphisms and co-morbidity are main causes for
high variability in expression and function of the CYP3A isoenzymes. Pharmacokinetic …

Kinase inhibitor pharmacokinetics: comprehensive summary and roadmap for addressing inter-individual variability in exposure

A Rowland, M Van Dyk, AA Mangoni… - Expert Opinion on …, 2017 - Taylor & Francis
Introduction: Small molecule protein kinase inhibitors (KIs) are a class of drugs with complex
and unconventional physiochemical and pharmacokinetic characteristics. Cytochrome P450 …

Interindividual variability in cytochrome P450 3A and 1A activity influences sunitinib metabolism and bioactivation

EA Burnham, AA Abouda, JE Bissada… - Chemical research in …, 2022 - ACS Publications
Sunitinib is an orally administered tyrosine kinase inhibitor associated with idiosyncratic
hepatotoxicity; however, the mechanisms of this toxicity remain unclear. We have previously …

[HTML][HTML] Dietary sodium restriction prevents vascular endothelial growth factor inhibitor-induced hypertension

L van Doorn, WJ Visser, DCH van Dorst… - British Journal of …, 2023 - nature.com
Background Vascular endothelial growth factor inhibitors (VEGFIs) are effective anticancer
agents which often induce hypertension. VEGFI-induced hypertension is sodium-sensitive in …