scholarly journals Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors

2021 ◽  
Author(s):  
Karima Alim ◽  
Amélie Moreau ◽  
Arnaud Bruyère ◽  
Elodie Jouan ◽  
Claire Denizot ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors ◽  
Organic Cation ◽  
Organic Cation Transporter ◽  
Organic Cation Transporter 3

scholarly journals Transport of six tyrosine kinase inhibitors: active or passive?

ADMET & DMPK ◽  
2016 ◽  
Vol 4 (1) ◽  
pp. 23 ◽  
Author(s):  
Richard J. Honeywell ◽  
Sarina Hitzerd ◽  
Ietje Kathmann ◽  
Godefridus J. Peters
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Intestinal Epithelium ◽  
Kinase Inhibitors ◽  
Organic Cation ◽  
Organic Cation Transporter ◽  
Passive Transport ◽  
Intracellular Accumulation ◽  
Transwell System

<p class="ADMETabstracttext">Transport of erlotinib, gefitinib, sorafenib, sunitinib, dasatinib and crizotinib can be active or passive, which was studied by measuring uptake  at low (4 °C; passive) and normal temperature (37 °C; active and passive) and by the use of specific organic cation transporter (OCT) inhibitors. Intracellular accumulation was determined using Caco-2 as monolayers, while for gut permeation we used differentiated Caco-2 as model for intestinal epithelium in the Transwell system. Sorafenib and crizotinib uptake are likely to be dependent on passive transport. Gefitinib, dasatinib and sunitinib uptake seem to be active. Erlotinib’s transport also seems to be active. This study suggests that hOCTs might be involved in the apical to basolateral transport of gefitinib and crizotinib. Overall it can be concluded that the accumulation and transport of these six TKIs are very different, despite the fact that they are all tyrosine kinase inhibitors.</p>

Side effects of tyrosine kinase inhibitors (TKIs) on bone remodelling

2012 ◽  
Vol 224 (03) ◽  
Author(s):  
JT Tauer ◽  
A Ulmer ◽  
LC Hofbauer ◽  
M Suttorp
Keyword(s):  
Side Effects ◽  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors ◽  
Bone Remodelling

Organic cation transporter 3 ist im hepatischen Kupfermetabolismus involviert

2018 ◽  
Vol 56 (08) ◽  
pp. e250-e250
Author(s):  
S Guttmann ◽  
S Reinartz Groba ◽  
C Niemietz ◽  
V Sandfort ◽  
A Zibert ◽  
...  
Keyword(s):  
Organic Cation ◽  
Organic Cation Transporter ◽  
Organic Cation Transporter 3

A framework for risk stratification in EGFR+ lung adenocarcinoma treated with tyrosine kinase inhibitors

2019 ◽  
Author(s):  
P Christopoulos ◽  
M Kirchner ◽  
F Bozorgmehr ◽  
N Magios ◽  
AL Volckmar ◽  
...  
Keyword(s):  
Risk Stratification ◽  
Tyrosine Kinase ◽  
Lung Adenocarcinoma ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors
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