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https://www.readbyqxmd.com/read/28680831/a-crowded-but-still-varied-space-brigatinib-in-anaplastic-lymphoma-kinase-rearranged-non-small-cell-lung-cancer
#1
COMMENT
Sawsan Rashdan, David E Gerber
No abstract text is available yet for this article.
February 2017: Translational Cancer Research
https://www.readbyqxmd.com/read/28628492/complete-remission-of-intrathecal-metastases-with-lorlatinib-therapy-in-a-heavily-pretreated-alk-positive-lung-cancer-patient
#2
Maximilian J Hochmair, Sophia Schwab, Helmut Prosch
Patients with lung cancer who show EML4-ALK translocation are routinely treated with ALK tyrosine kinase inhibitors, although in the majority of cases, these patients develop resistance over time. The central nervous system is a common of site of recurrence in this population, which calls for next-generation drugs that can penetrate into the brain and achieve clinically meaningful central nervous system activity. Here, I report the case of a female patient diagnosed with adenocarcinoma of the lung in 2005, at the age of 46 years, who underwent lobectomy and then experienced a series of progression episodes 6 years later...
September 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28597393/brigatinib-first-global-approval
#3
REVIEW
Anthony Markham
Brigatinib (ALUNBRIG™) is a small molecule antineoplastic anaplastic lymphoma kinase (ALK) inhibitor being developed by ARIAD Pharmaceuticals (a wholly-owned subsidiary of Takeda Pharmaceutical Company). In April 2017 brigatinib received accelerated approval in the USA for the treatment of patients with ALK-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. The development of resistance to crizotinib is a therapeutic challenge that has led to the development of second-generation ALK-inhibitors such as brigatinib, which have activity against treatment-resistant ALK mutants...
July 2017: Drugs
https://www.readbyqxmd.com/read/28536155/brigatinib-approved-but-treatment-role-uncertain
#4
(no author information available yet)
The FDA has approved the ALK inhibitor brigatinib for patients with metastatic non-small cell lung cancer who cannot take crizotinib or whose disease worsened despite its use. The decision was based upon results of a phase II study that assessed two drug doses, with overall response rates of 45% and 56% respectively. The drug's effect on overall survival remains unclear, as does the optimal sequence of brigatinib and the three other ALK inhibitors.
July 2017: Cancer Discovery
https://www.readbyqxmd.com/read/28526734/brigatinib-achieves-whole-body-and-intracranial-responses
#5
(no author information available yet)
Brigatinib is tolerable and has antitumor activity in crizotinib-resistant ALK-positive NSCLC.
May 19, 2017: Cancer Discovery
https://www.readbyqxmd.com/read/28506557/brigatinib-effective-in-alk-positive-non-small-cell-lung-cancer
#6
Manjulika Das
No abstract text is available yet for this article.
May 11, 2017: Lancet Oncology
https://www.readbyqxmd.com/read/28475456/brigatinib-in-patients-with-crizotinib-refractory-anaplastic-lymphoma-kinase-positive-non-small-cell-lung-cancer-a-randomized-multicenter-phase-ii-trial
#7
Dong-Wan Kim, Marcello Tiseo, Myung-Ju Ahn, Karen L Reckamp, Karin Holmskov Hansen, Sang-We Kim, Rudolf M Huber, Howard L West, Harry J M Groen, Maximilian J Hochmair, Natasha B Leighl, Scott N Gettinger, Corey J Langer, Luis G Paz-Ares Rodríguez, Egbert F Smit, Edward S Kim, William Reichmann, Frank G Haluska, David Kerstein, D Ross Camidge
Purpose Most crizotinib-treated patients with anaplastic lymphoma kinase gene ( ALK)-rearranged non-small-cell lung cancer (ALK-positive NSCLC) eventually experience disease progression. We evaluated two regimens of brigatinib, an investigational next-generation ALK inhibitor, in crizotinib-refractory ALK-positive NSCLC. Patients and Methods Patients were stratified by brain metastases and best response to crizotinib. They were randomly assigned (1:1) to oral brigatinib 90 mg once daily (arm A) or 180 mg once daily with a 7-day lead-in at 90 mg (180 mg once daily [with lead-in]; arm B)...
August 1, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28435288/the-activity-safety-and-evolving-role-of-brigatinib-in-patients-with-alk-rearranged-non-small-cell-lung-cancers
#8
REVIEW
Joshua K Sabari, Fernando C Santini, Alison M Schram, Isabella Bergagnini, Ruqin Chen, Chebli Mrad, W Victoria Lai, Kathryn C Arbour, Alexander Drilon
Brigatinib (AP26113) is a dimethylphosphine oxide group-containing tyrosine kinase inhibitor (TKI) constructed around a bisanilinopyrimidine scaffold with potent activity against the anaplastic lymphoma kinase (ALK) and several other targets. Despite the activity of first- and second-generation ALK inhibitors in advanced ALK-rearranged lung cancers, the development of acquired resistance represents an ongoing challenge. Later generation ALK inhibitors such as brigatinib are important potential tools in the management of patients with acquired resistance characterized by continued dependency on ALK...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28427013/the-accelerated-path-of-ceritinib-translating-pre-clinical-development-into-clinical-efficacy
#9
REVIEW
Tony S K Mok, Lucio Crino, Enriqueta Felip, Ravi Salgia, Tommaso De Pas, Daniel S W Tan, Laura Q M Chow
The discovery of anaplastic lymphoma kinase (ALK)-rearranged non-small-cell lung cancer (NSCLC) in 2007 led to the development and subsequent approval of the ALK inhibitor crizotinib in 2011. However, despite its clinical efficacy, resistance to crizotinib invariably develops. There is now a next generation of ALK inhibitors, including two that have been approved-ceritinib and alectinib-and others that are in development-brigatinib, lorlatinib and X-396. Ceritinib and the other next-generation ALK inhibitors are more potent than crizotinib and can overcome tumor cell resistance mechanisms...
April 2017: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/28287083/brigatinib-combined-with-anti-egfr-antibody-overcomes-osimertinib-resistance-in-egfr-mutated-non-small-cell-lung-cancer
#10
Ken Uchibori, Naohiko Inase, Mitsugu Araki, Mayumi Kamada, Shigeo Sato, Yasushi Okuno, Naoya Fujita, Ryohei Katayama
Osimertinib has been demonstrated to overcome the epidermal growth factor receptor (EGFR)-T790M, the most relevant acquired resistance to first-generation EGFR-tyrosine kinase inhibitors (EGFR-TKIs). However, the C797S mutation, which impairs the covalent binding between the cysteine residue at position 797 of EGFR and osimertinib, induces resistance to osimertinib. Currently, there are no effective therapeutic strategies to overcome the C797S/T790M/activating-mutation (triple-mutation)-mediated EGFR-TKI resistance...
March 13, 2017: Nature Communications
https://www.readbyqxmd.com/read/27899405/brigatinib-effective-in-alk-nsclc
#11
(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.
January 2017: 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
#12
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
#13
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...
December 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
#14
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...
November 15, 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
#15
REVIEW
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...
December 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27413712/tackling-alk-in-non-small-cell-lung-cancer-the-role-of-novel-inhibitors
#16
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
#17
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 Jänne
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...
January 1, 2017: 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
#18
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
#19
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
#20
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
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