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Erlotinib AND cancer

Dorra Amor, Sébastien Goutal, Solène Marie, Fabien Caillé, Martin Bauer, Oliver Langer, Sylvain Auvity, Nicolas Tournier
BACKGROUND: Erlotinib is an epidermal growth factor receptor (EGFR)-targeting tyrosine kinase inhibitor approved for treatment of non-small cell lung cancer. The wide inter-individual pharmacokinetic (PK) variability of erlotinib may impact treatment outcome and/or toxicity. Recent in vivo studies reported a nonlinear uptake transport of erlotinib into the liver, suggesting carrier-mediated system(s) to mediate its hepatobiliary clearance. Erlotinib has been identified in vitro as a substrate of organic anion-transporting polypeptide (OATP) transporters which expression does not restrict to hepatocytes and may impact the tissue uptake of erlotinib in vivo...
August 16, 2018: EJNMMI Research
Hironori Uruga, Shuhei Moriguchi, Yui Takahashi, Kazumasa Ogawa, Kyoko Murase, Sayaka Mochizuki, Shigeo Hanada, Hisashi Takaya, Atsushi Miyamoto, Nasa Morokawa, Kazuma Kishi
BACKGROUND: Pneumatosis intestinalis (PI) is a rare complication of chemotherapy, characterized by multiple gas accumulations within the bowel wall. CASE PRESENTATION: A 71-year-old woman with epidermal growth factor receptor (EGFR) mutation-positive lung adenocarcinoma was admitted to our hospital because of reduced consciousness. She was diagnosed as having leptomeningeal carcinomatosis (LM) using lumbar puncture. Because she could not swallow a tablet, erlotinib was administered via a feeding tube...
August 16, 2018: BMC Cancer
Junjun Li, Xiaomei Liu, Caijun Yuan
Epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) are effective in the treatment of advanced non-small-cell lung cancer (NSCLC) with leptomeningeal metastases (LM); however, a proportion of the patients with resistant tumors do not benefit from EGFR-TKI treatment. In the present study the case of a female patient with advanced lung adenocarcinoma harboring the EGFR L858R mutation (encoded in exon 21) who developed intracranial metastases following treatment with erlotinib after gefitinib failure is reported...
September 2018: Molecular and Clinical Oncology
Alexandria C McGrath, Geeta Sandhu, Euan Walpole, Elizabeth McCaffrey, Samantha A Hollingworth
Erlotinib is used to treat non-small-cell lung cancer (NSCLC). Erlotinib was subsidized on the Pharmaceutical Benefits Schedule in Australia for the treatment of advanced stage (IIIB or IV) NSCLC (August 2008). In the pivotal trial supporting initial subsidy, erlotinib increased overall survival (OS) by 2 months compared with placebo (adjusted hazard ratio, 0.70; 95% confidence interval: 0.58-0.85). We examined the effectiveness of erlotinib in a 'real-world' setting by measuring survival outcomes in NSCLC patients treated in two tertiary metropolitan public hospitals in Queensland...
September 2018: Anti-cancer Drugs
Bi-Sheng Liu, Xin-Yu Dai, Hong-Wei Xia, Huan-Ji Xu, Qiu-Lin Tang, Qi-Yong Gong, Yong-Zhan Nie, Feng Bi
Dysregulation of epidermal growth factor receptor (EGFR) signaling is responsible for the resistance to EGFR tyrosine kinase inhibitors (TKIs), such as gefitinib and erlotinib, and is thereby associated with the progression of tumors in non‑small cell lung cancers (NSCLCs). Immunoblotting results revealed that geranylgeranyl transferase 1 inhibitor (GGTI)‑298, a geranylgeranyl transferase 1 inhibitor with potential antitumor effects, effectively inhibited the phosphorylation of EGFR and its downstream target protein kinase B (AKT)...
August 9, 2018: Molecular Medicine Reports
Yang-Ling Li, Xiu Hu, Qing-Yu Li, Fei Wang, Bo Zhang, Ke Ding, Bi-Qin Tan, Neng-Ming Lin, Chong Zhang
As patients with non‑small cell lung cancer (NSCLC) and wild‑type epidermal growth factor receptor (EGFR) are resistant to treatment with erlotinib or gefitinib, potential chemosensitizers are required to potentiate wild‑type EGFR NSCLC cells to erlotinib/gefitinib treatment. The present study reported that shikonin could sensitize the anticancer activity of erlotinib/gefitinib in wild‑type EGFR NSCLC cells. Furthermore, shikonin could potentiate mitochondrial‑mediated apoptosis induced by erlotinib/gefitinib in wild‑type EGFR NSCLC cells...
August 3, 2018: Molecular Medicine Reports
Kazuo Tsuchiya, Masato Karayama, Hideki Yasui, Hironao Hozumi, Yuzo Suzuki, Kazuki Furuhashi, Noriyuki Enomoto, Tomoyuki Fujisawa, Yutaro Nakamura, Naoki Inui, Takafumi Suda
A 53-year-old man with advanced lung adenocarcinoma harboring epidermal growth factor receptor (EGFR) exon 19 deletion received erlotinib. After 12 months of disease control with erlotinib monotherapy, leptomeningeal metastases (LM) occurred. A cerebrospinal fluid examination demonstrated a pre-existing EGFR exon 19 deletion. Bevacizumab was combined with erlotinib, and the LM improved. After six months of combination therapy, however, the LM was exacerbated. A re-examination of the cerebrospinal fluid revealed a T790M mutation and exon 19 deletion...
August 10, 2018: Internal Medicine
Mitsuo Sato, Akira Matsui, Yoshie Shimoyama, Norihito Omote, Masahiro Morise, Tetsunari Hase, Ichidai Tanaka, Kojiro Suzuki, Yoshinori Hasegawa
Squamous cell carcinoma (SCC) transformation has been identified as a mechanism of resistance to first-generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs), gefitinib or erlotinib, in EGFR-mutated lung cancer. However, whether second- or third-generation TKIs can overcome resistance due to SCC transformation remains unclear. We herein report an EGFR-mutated lung adenocarcinoma undergoing transformation into SCC that exhibited a durable response to afatinib, which is a second-generation irreversible EGFR-TKI...
August 10, 2018: Internal Medicine
Giovanni Ribaudo, Enrico Zanforlin, Giuseppe Zagotto
The introduction of tyrosine kinase inhibitors (TKIs) in the clinical management of oncological patients spread the light on the use of selective, rationally designed small molecules for the treatment of cancer. First-generation TKIs bared high response against these malignancies, although the unavoidable shadow of resistance limits their long-term efficacy. Non-small-cell lung cancer (NSCLC) accounts for 85% of lung cancer cases, and it is the first cause of cancer deaths worldwide for men and women. Traditional chemotherapy is marginally effective against this form, and erlotinib and gefitinib were introduced as first-line treatments based on the observation that the epidermal growth factor receptor (EGFR), a receptor tyrosine kinase (RTK), is mutated in several cases and, thus, represents a druggable target...
August 12, 2018: Archiv der Pharmazie
M Kimura, F Yasue, E Usami, S Kawachi, M Iwai, M Go, Y Ikeda, T Yoshimura
Epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), including gefitinib, erlotinib and afatinib are standard first-line treatments for EGFR gene mutation-positive non-small cell lung cancer. The present study aimed to compare the cost-effectiveness of using erlotinib, afatinib or gefitinib. The safety of EGFR-TKIs was also investigated. Expected costs were calculated based on data from patients with advanced EGFR mutation-positive non-small-cell lung cancer who were treated with gefitinib, erlotinib or afatinib...
August 2018: Molecular and Clinical Oncology
Solange Peters, Alessandra Curioni-Fontecedro, Hovav Nechushtan, Jin-Yuan Shih, Wei-Yu Liao, Oliver Gautschi, Vito Spataro, Mojca Unk, James Chih-Hsin Yang, Robert M Lorence, Philippe Carrière, Agnieszka Cseh, Gee-Chen Chang
INTRODUCTION: Approximately 1-4% of non-small-cell lung cancer (NSCLC) tumors harbor a human epidermal growth factor receptor 2 (HER2) mutation; there is no approved targeted treatment for this subgroup. METHODS: Patients with stage IV NSCLC that progressed after clinical benefit on erlotinib/gefitinib and/or had activating epidermal growth factor receptor (EGFR) or HER2 mutations, had exhausted other treatments, and were ineligible for afatinib trials, were enrolled in a named patient use (NPU) program, receiving afatinib 30-50 mg/day on a compassionate basis within routine clinical practice...
August 7, 2018: Journal of Thoracic Oncology
Edward B Garon, Jill M Siegfried, Laura P Stabile, Patricia A Young, Diana C Marquez-Garban, David J Park, Ravi Patel, Eddie H Hu, Saeed Sadeghi, Rupesh J Parikh, Karen L Reckamp, Brad Adams, Robert M Elashoff, David Elashoff, Tristan Grogan, He-Jing Wang, Sanja Dacic, Meghan Brennan, Yacgley Valdes, Simon Davenport, Steven M Dubinett, Michael F Press, Dennis J Slamon, Richard J Pietras
OBJECTIVES: This open-label, randomized phase II trial evaluated antitumor efficacy of an antiestrogen, fulvestrant, in combination with human epidermal growth factor receptor (EGFR) inhibitor, erlotinib, in advanced non-small cell lung cancer (NSCLC) patients. MATERIALS AND METHODS: Patients with advanced or metastatic NSCLC, ECOG 0-2, previous chemotherapy unless patient refusal, and no prior EGFR-directed therapy were randomized 2:1 to erlotinib 150 mg oral daily plus 500 mg intramuscular fulvestrant on day 1, 15, 29 and every 28 days thereafter or erlotinib alone 150 mg oral daily...
September 2018: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
Chong Hyun Suh, Hye Sun Park, Kyung Won Kim, Junhee Pyo, Hiroto Hatabu, Mizuki Nishino
PURPOSE: Pneumonitis is a significant toxicity of EGFR tyrosine kinase inhibitors (EGFR-TKI) in non-small-cell lung cancer (NSCLC) patients. We studied the incidence of pneumonitis in clinical trials of EGFR-TKI published in 2003-2017, and performed subgroups analyses to identity predisposing factors. METHODS: Ovid-MEDLINE and EMBASE search up to 4/17/17 using the keywords, "erlotinib", "gefitinib", "afatinib", "osimertinib", and "lung cancer", resulted in a total of 153 eligible trial cohorts with 15,713 advanced NSCLC patients treated with EGFR-TKI...
September 2018: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
Yuzhou Shen, Wentao Li
Background: Aim of this study was to prepare the hyaluronic acid and human serum albumin modified erlotinib nanoparticles (ERT-HSA-HA NPs) delivery system by a precipitation method. Methods: ERT-HSA-HA NPs were characterized for physical properties, such as morphology and particle size, and in vitro drug release. Moreover, the cytotoxicity, cellular uptake, in vivo studies of ERT-HSA-HA nanoparticle were investigated and compared in A549 cells. Results: The ERT-HSA-HA NPs showed spherical morphology, and their hydrodynamic diameter was 112...
2018: Drug Design, Development and Therapy
Masashi Fukuoka, Katsuji Yoshioka, Hirohiko Hohjoh
Gefitinib and erlotinib are epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs). Although EGFR-TKIs are effective as anti-cancer drugs, cancer cells sometimes gain tolerance to the drugs. Previous studies suggested that the fibroblast growth factor receptor (FGFR)-signaling pathway could serve as compensation for the EGFR-signaling pathway inhibited by EGFR-TKIs. Our study further suggested that FGF2, a FGFR ligand, leaked out from naïve cells killed by gefitinib could initiate the FGFR-signaling pathway in surviving cells; i...
2018: PloS One
Marie-Rose B S Crombag, Jacobine G C van Doremalen, Julie M Janssen, Hilde Rosing, Jan H M Schellens, Jos H Beijnen, Neeltje Steeghs, Alwin D R Huitema
AIM: Pharmacokinetics of small molecule kinase inhibitors (KIs) used in cancer treatment may alter with increasing age, but results are conflicting. This study aims to compare exposure to KIs between older and younger patients (<70 and ≥70 years) in clinical practice. METHODS: KI plasma concentrations of routinely treated patients were measured using validated assays. Calculated dose-normalized trough concentrations were compared in both age groups. For KIs with a clinically meaningful target concentration (erlotinib, imatinib, pazopanib, sunitinib, and vemurafenib), influence of older age on target attainment was assessed...
August 1, 2018: British Journal of Clinical Pharmacology
Wang Jing, Haiyong Wang, Li Kong, Jinming Yu, Hui Zhu
Leptomeningeal metastases (LMs) were devastating metastatic complications of non-small cell lung cancer (NSCLC). Management of LMs relied on conventional therapy but with poor survival, lacking effective treatment strategies. We present the case of a 52-year-old female non-smoker with advanced lung adenocarcinoma and initially positive EGFR-mutation, who failed to the treatment of standard first-line chemotherapy (pemetrexed plus cisplatin) and bevacizumab (BEV), and maintenance therapy with pemetrexed plus BEV...
August 1, 2018: Cancer Biology & Therapy
Zahra Haghighijoo, Zahra Rezaei, Mansooreh Jaberipoor, Samaneh Taheri, Meysam Jani, Soghra Khabnadideh
Quinazoline is one of the most widespread scaffolds amongst natural and synthetic bioactive compounds. Recently the quinazoline derivatives and in particular the 4-anilinoquinazolines have attracted much attention for their anticancer properties due to their capability to stabilize the kinase activity of epidermal growth factor receptor (EGFR). A series of fifteen previously designed and synthesized 4-anilinoquinazoline analogs (4-18) were evaluated for cytotoxic activity on two breast cancer cell lines (MCF-7 and MDA-MB-468)...
August 2018: Research in Pharmaceutical Sciences
Malose J Mphahlele, Mmakwena M Mmonwa, Abimbola Aro, Lyndy J McGaw, Yee Siew Choong
A series of indole-aminoquinazolines was prepared via amination of the 2-aryl-4-chloroquinazolines with the 7-amino-2-aryl-5-bromoindoles. It was then evaluated for cytotoxicity in vitro against human lung cancer (A549), epithelial colorectal adenocarcinoma (Caco-2), hepatocellular carcinoma (C3A), breast adenocarcinoma (MCF-7), and cervical cancer (HeLa) cells. A combination on the quinazoline and indole moieties of a 2-phenyl and 2-(4-fluorophenyl) rings in compound 4b ; 2-(4-fluorophenyl) and 3-chlorophenyl rings in compound 4f ; or the two 2-(4-fluorophenyl) rings in compound 4g , resulted in significant and moderate activity against the Caco-2 and C3A cell lines...
July 31, 2018: International Journal of Molecular Sciences
Rosalin Mishra, Hima Patel, Samar Alanazi, Long Yuan, Joan T Garrett
ERBB family members including epidermal growth factor receptor (EGFR) also known as HER1, ERBB2/HER2/Neu, ERBB3/HER3 and ERBB4/HER4 are aberrantly activated in multiple cancers and hence serve as drug targets and biomarkers in modern precision therapy. The therapeutic potential of HER3 has long been underappreciated, due to impaired kinase activity and relatively low expression in tumors. However, HER3 has received attention in recent years as it is a crucial heterodimeric partner for other EGFR family members and has the potential to regulate EGFR/HER2-mediated resistance...
January 30, 2018: Oncology Reviews
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