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Assessment of Quercetin Isolated from Enicostemma Littorale Against Few Cancer Targets: An in Silico Approach
Published in A. K. Haghi, Ana Cristina Faria Ribeiro, Lionello Pogliani, Devrim Balköse, Francisco Torrens, Omari V. Mukbaniani, Applied Chemistry and Chemical Engineering, 2017
Gefitinib is a drug used in the treatment of certain types of cancer and like erlotinib it is an EGFR inhibitor, which interrupts signaling through the EGFR in target cells. Gefitinib is the first selective inhibitor of EGFR’s tyrosine kinase domain.75 The target protein (EGFR) is also sometimes referred to as Herl or ErbB-1 depending on the literature source. This leads to inappropriate activation of the anti-apoptotic Ras signaling cascade, eventually leading to uncontrolled cell proliferation.56 Research on gefitinib-sensitive, non-small cell lung cancers has shown that a mutation in the EGFR tyrosine kinase domain is responsible for activating anti-apoptotic pathways. These mutations tend to confer increased sensitivity to tyrosine kinase inhibitors such as gefitinib and erlotinib.70 Gefitinib inhibits EGFR tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme.53 Thus, the function of the EGFR tyrosine kinase in activating the anti-apoptotic Ras signal transduction cascade is inhibited, and malignant cells are inhibited.
Pulmonary reactions to chemotherapeutic agents: the ‘chemotherapy lung’
Published in Philippe Camus, Edward C Rosenow, Drug-induced and Iatrogenic Respiratory Disease, 2010
Fabien Maldonado, Andrew H Limper
Gefitinib is a selective tyrosine kinase inhibitor that has been primarily used in the treatment of non-small-cell lung carcinomas that are not responsive to conventional chemotherapy. It is now also used in the treatment of breast, ovarian and colon cancers. Numerous cases of gefitinib-induced respiratory failure have been reported and the overall incidence may be of the order of 1 per cent with a mortality rate approaching 30 per cent.75 Radiotherapy, prior history of lung fibrosis, or lung infection may predispose to this pulmonary complication.
Genotoxicity and in vitro investigation of Gefitinib-loaded polycaprolactone fabricated nanoparticles for anticancer activity against NCI-H460 cell lines
Published in Journal of Experimental Nanoscience, 2022
Gefitinib, a BCS class II drug used to treat non-small cell lung cancer (NSCLC) [1–5]. It works as both an EGFR inhibitor and a tyrosine kinase inhibitor (TKIs) [6]. According to new research, Gefitinib has a lower solubility and a slower onset of action in the gastric environment at pH 4–6. Gefitinib was found to have a log-P value of 4.15, indicating that it has a higher hydrophobic property [7]. Furthermore, hepatic elevations of alanine aminotransferase, anorexia, stomatitis, vomiting, diarrhea, and nausea were reported to occur with the 250 mg marketed Gefitinib tablets, which had only 44% bioavailability [8]. Moreover, despite their lack of understanding of new polymers, the effects of critical attributes and critical process parameters, and the basic criteria for polymeric nanoformulations such as smaller particle sizes, entrapment efficacy percentage, and polydispersity index, modern scientists are turning to polymeric nanotechnological approaches to tackle these issues [9, 10]. As a result, one of the goals of this study is to create a Gefitinib control release formulation that uses a quality by design approach, which could have rapid onset of action, increased drug solubility profile, and better drug entrapment efficacy [11].
A convergent fabrication of programmed pH/reduction-responsive nanoparticles for efficient dual anticancer drugs delivery for ovarian cancer treatment
Published in Journal of Experimental Nanoscience, 2023
Haiyan Zhang, Youlin Yang, Yi Chen, Xiahui Zhang, Xiaopei Chen
An anticancer drug called Gefitinib (GFT) is the first specific inhibitor of the tyrosine kinase region of the epidermal growth factor receptor (EGFR) tyrosine-kinase domain [25]. The transmembrane glycoprotein epidermal growth factor has unique tyrosine kinase receptors that govern high cellular proliferation and expression levels in cancer [26]. Solid tumors, including ovarian, lung, colorectal, and brain, will likely exhibit more elevated EGFR. To suppress cancer cell proliferation, GFT inhibits the kinase activity of wild-type and specific activating mutations of the EGF receptor, thereby blocking tyrosine residues linked with the receptor’s autophosphorylation, preventing further downstream signaling [27–29].