… studies on the human serum albumin binding of the clinically approved EGFR inhibitors gefitinib, erlotinib, afatinib, osimertinib and the investigational inhibitor …

O Dömötör, K Pelivan, A Borics, BK Keppler… - Journal of …, 2018 - Elsevier
… between human serum albumin (HSA) and four approved epidermal growth factor receptor
(EGFR) inhibitors gefitinib (… The EGFR inhibitors were predominantly presented in their single …

Human serum albumin nanoparticulate system with encapsulation of gefitinib for enhanced anti-tumor effects in non-small cell lung cancer

X Pang, P Yang, L Wang, J Cao, Y Cheng… - … of Drug Delivery Science …, 2019 - Elsevier
Gefitinib, a selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, has
… non-small cell lung cancer patients with tumors carrying sensitive EGFR mutation. However, …

Human serum albumin binding and synergistic effects of gefitinib in combination with regorafenib on colorectal cancer cell lines

H Tanzadehpanah, H Mahaki, M Moradi… - Colorectal …, 2018 - Future Medicine
… Thus, in this study, the interaction between EGFR inhibitor (small molecule TKIs such as
GEF) and multikinase inhibitor (REG) was suggested to represent a promising combination for …

[HTML][HTML] Spectroscopic and molecular docking studies of binding interaction of gefitinib, lapatinib and sunitinib with bovine serum albumin (BSA)

GF Shen, TT Liu, Q Wang, M Jiang, JH Shi - Journal of Photochemistry and …, 2015 - Elsevier
… kinase inhibitors (TKIs), such as gefitinib, lapatinib and sunitinib, with bovine serum albumin
(BSA) … and configuration with human serum albumin (HSA), clear structure and low cost [8]. …

Interaction of an anticancer drug, gefitinib with human serum albumin: insights from fluorescence spectroscopy and computational modeling analysis

MZ Kabir, WV Tee, SB Mohamad, Z Alias, S Tayyab - RSC advances, 2016 - pubs.rsc.org
… Among the wide variety of anticancer drugs used in clinical routine, gefitinib (GEF) is one
of … 1) competes with ATP for the ATP-binding site of the epidermal growth factor receptor (EGFR

Gefitinib

AFMM Rahman, HM Korashy, MG Kassem - … of drug substances, excipients …, 2014 - Elsevier
Gefitinib (Iressa®) is a selective inhibitor of epidermal growth … as gefitinib (Iressa®), that
inhibit the kinase activity of EGFRGefitinib is highly bound to human plasma albumin and α1-…

Binding of gefitinib, an inhibitor of epidermal growth factor receptor-tyrosine kinase, to plasma proteins and blood cells: in vitro and in cancer patients

J Li, J Brahmer, W Messersmith, M Hidalgo… - Investigational new …, 2006 - Springer
… and 78% of gefitinib was bound to human serum albumin (HSA) … gefitinib is highly protein
bound (∼ 97%) in human plasma. … Gefitinib targets the ATP cleft within the EGFR-TK to prevent …

Binding site identification of anticancer drug gefitinib to HSA and DNA in the presence of five different probes

H Tanzadehpanah, H Mahaki… - Journal of …, 2019 - Taylor & Francis
… evaluate the binding interaction of gefitinib (GEF) with human serum albumin (HSA) and calf
… binding between anticancer drug gefitinib as a tyrosine kinase inhibitor with HSA and DNA …

… (EGFR) tyrosine kinase inhibitor gefitinib (ZD1839, Iressa) in non–small cell lung cancer cell lines correlates with gene copy number and EGFR Mutations but not …

BA Helfrich, D Raben, M Varella-Garcia… - Clinical cancer …, 2006 - AACR
… effects of gefitinib on cell cycle were determined by flow cytometry and the molecular effects
of gefitinib EGFR inhibition on downstream signal proteins by Western blotting. Gefitinib in …

Physicochemical properties of epidermal growth factor receptor inhibitors and development of a nanoliposomal formulation of gefitinib

BJ Trummer, V Iyer, SV Balu-Iyer, R O'Connor… - Journal of …, 2012 - Elsevier
… Although the EGFR inhibitors are orally active and have … the efficacy of combination therapies
with EGFR inhibitors. … saline containing 450 nM bovine serum albumin (BSA). Excitation …