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https://www.readbyqxmd.com/read/27899405/brigatinib-effective-in-alk-nsclc
#1
(no author information available yet)
Results from a phase I/II trial indicate that the investigational ALK inhibitor brigatinib is active in patients with ALK-rearranged non-small cell lung cancer. Patients who had previously received crizotinib-as well as those who hadn't-responded to the drug, which was also active in patients with brain metastases.
November 29, 2016: Cancer Discovery
https://www.readbyqxmd.com/read/27867609/editorial-on-the-article-entitled-brigatinib-efficacy-and-safety-in-patients-with-anaplastic-lymphoma-kinase-alk-positive-non-small-cell-lung-cancer-in-a-phase-i-ii-trial
#2
EDITORIAL
Ivana Sullivan, David Planchard
No abstract text is available yet for this article.
October 2016: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/27836716/activity-and-safety-of-brigatinib-in-alk-rearranged-non-small-cell-lung-cancer-and-other-malignancies-a-single-arm-open-label-phase-1-2-trial
#3
Scott N Gettinger, Lyudmila A Bazhenova, Corey J Langer, Ravi Salgia, Kathryn A Gold, Rafael Rosell, Alice T Shaw, Glen J Weiss, Meera Tugnait, Narayana I Narasimhan, David J Dorer, David Kerstein, Victor M Rivera, Timothy Clackson, Frank G Haluska, David Ross Camidge
BACKGROUND: Anaplastic lymphoma kinase (ALK) gene rearrangements are oncogenic drivers of non-small-cell lung cancer (NSCLC). Brigatinib (AP26113) is an investigational ALK inhibitor with potent preclinical activity against ALK mutants resistant to crizotinib and other ALK inhibitors. We aimed to assess brigatinib in patients with advanced malignancies, particularly ALK-rearranged NSCLC. METHODS: In this ongoing, single-arm, open-label, phase 1/2 trial, we recruited patients from nine academic hospitals or cancer centres in the USA and Spain...
November 7, 2016: Lancet Oncology
https://www.readbyqxmd.com/read/27780853/the-potent-alk-inhibitor-brigatinib-ap26113-overcomes-mechanisms-of-resistance-to-first-and-second-generation-alk-inhibitors-in-preclinical-models
#4
Sen Zhang, Rana Anjum, Rachel Squillace, Sara Nadworny, Tianjun Zhou, Jeff Keats, Yaoyu Ning, Scott D Wardwell, David Miller, Youngchul Song, Lindsey Eichinger, Lauren Moran, Wei-Sheng Huang, Shuangying Liu, Dong Zou, Yihan Wang, Qurish Mohemmad, Hyun Gyung Jang, Emily Ye, Narayana Narasimhan, Frank Wang, Juan Miret, Xiaotian Zhu, Tim Clackson, David Dalgarno, William C Shakespeare, Victor M Rivera
PURPOSE: Non-small cell lung cancers (NSCLCs) harboring ALK gene rearrangements (ALK(+)) typically become resistant to the first-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) crizotinib through development of secondary resistance mutations in ALK or disease progression in the brain. Mutations that confer resistance to second-generation ALK TKIs ceritinib and alectinib have also been identified. Here, we report the structure and first comprehensive preclinical evaluation of the next-generation ALK TKI brigatinib...
October 25, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27682212/current-and-developing-therapies-for-the-treatment-of-non-small-cell-lung-cancer-with-alk-abnormalities-update-and-perspectives-for-clinical-practice
#5
M Caccese, R Ferrara, S Pilotto, L Carbognin, G Grizzi, A Caliò, M Brunelli, F Cuppone, S Petraglia, A Scarpa, G Tortora, E Bria
The treatment of patients with ALK-rearranged non-small-cell lung cancer was completely revolutionized by the introduction of Crizotinib, a small molecule inhibiting ALK, MET and ROS1. Given that resistance occurs within approximately 12 months, in order to develop more potent inhibitors and to increase drug penetration to CNS, innovative ALK-inhibitors were developed. Second-generation ALK inhibitors Ceritinib (LDK378), Alectinib (CH5424802/RO5424802) and Brigatinib (AP26113) have shown significant clinical activity, and were rapidly approved by regulatory agencies...
October 8, 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27413712/tackling-alk-in-non-small-cell-lung-cancer-the-role-of-novel-inhibitors
#6
REVIEW
Francesco Facchinetti, Marcello Tiseo, Massimo Di Maio, Paolo Graziano, Emilio Bria, Giulio Rossi, Silvia Novello
Crizotinib is an oral inhibitor of anaplastic lymphoma kinase (ALK) with remarkable clinical activity in patients suffering from ALK-rearranged non-small cell lung cancer (NSCLC), accounting to its superiority compared to chemotherapy. Unfortunately, virtually all ALK-rearranged tumors acquire resistance to crizotinib, frequently within one year since the treatment initiation. To date, therapeutic strategies to overcome crizotinib resistance have focused on the use of more potent and structurally different compounds...
June 2016: Translational Lung Cancer Research
https://www.readbyqxmd.com/read/27370605/identification-of-existing-drugs-that-effectively-target-ntrk1-and-ros1-rearrangements-in-lung-cancer
#7
Curtis R Chong, Magda Bahcall, Marzia Capelletti, Takayuki Kosaka, Dalia Ercan, Taebo Sim, Lynette M Sholl, Mizuki Nishino, Bruce E Johnson, Nathanael S Gray, Pasi A Janne
PURPOSE: Efforts to discover drugs that overcome resistance to targeted therapies in patients with rare oncogenic alterations, such as NTRK1- and ROS1-rearrangements, are complicated by the cost and protracted timeline of drug discovery. EXPERIMENTAL DESIGN: In an effort to identify inhibitors of NTRK1 and ROS1, which are aberrantly activated in some patients with non-small cell lung cancer (NSCLC), we created and screened a library of existing targeted drugs against Ba/F3 cells transformed with these oncogenes...
July 1, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27198273/1330-brigatinib-efficacy-and-safety-in-patients-pts-with-anaplastic-lymphoma-kinase-alk-positive-alk-non-small-cell-lung-cancer-nsclc-in-a-phase-1-2-trial
#8
R Rosell, S N Gettinger, L A Bazhenova, C J Langer, R Salgia, A T Shaw, N I Narasimhan, D J Dorer, D Kerstein, D R Camidge
No abstract text is available yet for this article.
April 2016: Journal of Thoracic Oncology
https://www.readbyqxmd.com/read/27194112/proteome-wide-drug-screening-using-mass-spectrometric-imaging-of-bead-arrays
#9
Ying Zhou, Ziying Liu, Kenneth J Rothschild, Mark J Lim
A fundamental challenge in the drug discovery process is to develop compounds with high efficacy and minimal side-effects. We describe a new approach to proteome-wide drug screening for detection of on- and off-target binding which combines the advantages of mass spectrometry with microarray technology. The method involves matrix-assisted laser desorption/ionization mass spectrometric imaging (MALDI-MSI) of agarose micro-beads randomly arrayed at high-density in custom micro-well plates. Each bead carries a unique protein target and a corresponding photocleavable mass-tag for coding (PC-Mass-Tag)...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27144831/discovery-of-brigatinib-ap26113-a-phosphine-oxide-containing-potent-orally-active-inhibitor-of-anaplastic-lymphoma-kinase
#10
Wei-Sheng Huang, Shuangying Liu, Dong Zou, Mathew Thomas, Yihan Wang, Tianjun Zhou, Jan Romero, Anna Kohlmann, Feng Li, Jiwei Qi, Lisi Cai, Timothy A Dwight, Yongjin Xu, Rongsong Xu, Rory Dodd, Angela Toms, Lois Parillon, Xiaohui Lu, Rana Anjum, Sen Zhang, Frank Wang, Jeffrey Keats, Scott D Wardwell, Yaoyu Ning, Qihong Xu, Lauren E Moran, Qurish K Mohemmad, Hyun Gyung Jang, Tim Clackson, Narayana I Narasimhan, Victor M Rivera, Xiaotian Zhu, David Dalgarno, William C Shakespeare
In the treatment of echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase positive (ALK+) non-small-cell lung cancer (NSCLC), secondary mutations within the ALK kinase domain have emerged as a major resistance mechanism to both first- and second-generation ALK inhibitors. This report describes the design and synthesis of a series of 2,4-diarylaminopyrimidine-based potent and selective ALK inhibitors culminating in identification of the investigational clinical candidate brigatinib...
May 26, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27049722/brigatinib-an-anaplastic-lymphoma-kinase-inhibitor-abrogates-activity-and-growth-in-alk-positive-neuroblastoma-cells-drosophila-and-mice
#11
Joachim T Siaw, Haiying Wan, Kathrin Pfeifer, Victor M Rivera, Jikui Guan, Ruth H Palmer, Bengt Hallberg
Anaplastic lymphoma kinase (ALK) is a tyrosine kinase receptor which has been implicated in numerous solid and hematologic cancers. ALK mutations are reported in about 5-7% of neuroblastoma cases but the ALK-positive percentage increases significantly in the relapsed patient population. Crizotinib, the first clinically approved ALK inhibitor for the treatment of ALK-positive lung cancer has had less dramatic responses in neuroblastoma. Here we investigate the efficacy of a second-generation ALK inhibitor, brigatinib, in a neuroblastoma setting...
May 17, 2016: Oncotarget
https://www.readbyqxmd.com/read/26951079/second-and-third-generation-alk-inhibitors-for-non-small-cell-lung-cancer
#12
REVIEW
Jingjing Wu, John Savooji, Delong Liu
Crizotinib as the first-generation ALK inhibitor has shown significant activity in ALK-mutated non-small cell lung cancer (NSCLC). Second- and third-generation ALK inhibitors are entering clinical applications for ALK+ NSCLC. In addition, a third-generation ALK inhibitor, lorlatinib (PF-06463922), was reported to resensitize NSCLC to crizotinib. This review provided a summary of clinical development of alectinib, ceritinib, brigatinib (AP26113), and lorlatinib.
March 8, 2016: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/26654422/overcoming-crizotinib-resistance-in-alk-rearranged-nsclc-with-the-second-generation-alk-inhibitor-ceritinib
#13
REVIEW
Ittai B Muller, Adrianus J De Langen, Richard J Honeywell, Elisa Giovannetti, Godefridus J Peters
In up to 5% of non-small cell lung cancer (NSCLC) patients, the EML4-ALK translocation drives tumor progression. Treatment with the ALK inhibitor crizotinib is more effective than standard chemotherapy. However, resistance to crizotinib occurs after approximately 8 months. Ceritinib is the first second-generation ALK inhibitor approved for treatment of crizotinib-resistant NSCLC. Ceritinib inhibits two of the most common ALK-mutants that confer resistance to crizotinib: L1196 M and G1269A. Cells with ALK expression are more sensitive to ceritinib than crizotinib (IC50 25 nM vs...
2016: Expert Review of Anticancer Therapy
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