keyword
MENU ▼
Read by QxMD icon Read
search

Ceritinib

keyword
https://www.readbyqxmd.com/read/29774128/systematic-review-and-meta-analysis-of-selected-toxicities-of-approved-alk-inhibitors-in-metastatic-non-small-cell-lung-cancer
#1
Rubens Barros Costa, Ricardo L B Costa, Sarah M Talamantes, Jason B Kaplan, Manali A Bhave, Alfred Rademaker, Corinne Miller, Benedito A Carneiro, Devalingam Mahalingam, Young Kwang Chae
Introduction: Anaplastic lymphoma kinase ( ALK ) inhibitors are the mainstay treatment for patients with non-small cell lung carcinoma (NSCLC) harboring a rearrangement of the ALK gene or the ROS1 oncogenes. With the recent publication of pivotal trials leading to the approval of these compounds in different indications, their toxicity profile warrants an update. Materials and Methods: A systematic literature search was performed in July 2017. Studies evaluating US FDA approved doses of one of the following ALK inhibitors: Crizotinib, Ceritinib, Alectinib or Brigatinib as monotherapy were included...
April 24, 2018: Oncotarget
https://www.readbyqxmd.com/read/29765547/signature-program-a-platform-of-basket-trials
#2
Eric D Slosberg, Barinder P Kang, Julio Peguero, Matthew Taylor, Todd M Bauer, Donald A Berry, Fadi Braiteh, Alexander Spira, Funda Meric-Bernstam, Steven Stein, Sarina A Piha-Paul, August Salvado
Investigating targeted therapies can be challenging due to diverse tumor mutations and slow patient accrual for clinical studies. The Signature Program is a series of 8 phase 2, agent-specific basket protocols using a rapid study start-up approach involving no predetermined study sites. Each protocol evaluated 1 agent (buparlisib, dovitinib, binimetinib, encorafenib, sonidegib, BGJ398, ceritinib, or ribociclib) in patients with solid or hematologic malignancies and an actionable mutation. The primary endpoint of each study was the clinical benefit rate (ie, complete or partial response, or stable disease) at 16 weeks...
April 20, 2018: Oncotarget
https://www.readbyqxmd.com/read/29742496/ceritinib-enhances-the-efficacy-of-substrate-chemotherapeutic-agent-in-human-abcb1-overexpressing-leukemia-cells-in-vitro-in-vivo-and-ex-vivo
#3
Li Yang, Manjun Li, Fang Wang, Chen Zhen, Min Luo, Xiaona Fang, Hong Zhang, Jianye Zhang, Qingshan Li, Liwu Fu
BACKGROUND/AIMS: Multidrug resistance (MDR) triggered by ATP binding cassette (ABC) transporters, such as ABCB1, ABCC1, and ABCG2, is a key obstacle for successful cancer chemotherapy. There is currently no FDA-approved MDR modulator that can be used in clinic. Ceritinib, a selective ALK inhibitor, has been approved as the second-line treatment for ALK-positive non-small cell lung cancer. Here, we examined the role of ceritinib in leukemia associated MDR in therapy. METHODS: The cell proliferation was detected by MTT assay...
May 5, 2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29732013/successful-rechallenge-with-ceritinib-after-leukocytoclastic-vasculitis-during-ceritinib-treatment-for-non-small-cell-lung-cancer-harboring-the-eml4-alk-fusion-protein
#4
Tamio Okimoto, Yukari Tsubata, Takamasa Hotta, Megumi Hamaguchi, Takae Okuno, Yohei Shiratsuki, Akari Kodama, Mika Nakao, Yoshihiro Amano, Shunichi Hamaguchi, Noriaki Kurimoto, Reiko Tobita, Takeshi Isobe
Anaplastic lymphoma kinase (ALK)-tyrosine kinase inhibitors (TKIs) dramatically improve progression-free survival compared to cytotoxic agents. It is therefore important to manage patients with ALK-TKIs until drug resistance occurs. Leukocytoclastic vasculitis (LCV) is a rare complication during cancer treatment and is associated with a variety of factors. Currently, it is unclear whether we should withdraw a treatment when drug-induced LCV develops. We report a 40-year-old man with advanced pulmonary adenocarcinoma harboring the EML4-ALK fusion protein who developed LCV during ceritinib treatment...
April 13, 2018: Oncotarget
https://www.readbyqxmd.com/read/29723525/alk-is-required-for-nlrp3-inflammasome-activation-in-macrophages
#5
Bibo Zhang, Wei Wei, Jiaming Qiu
The NLRP3 inflammasome is a key mediator of host immune responses through the induction of pyroptosis and the release of cytokines. Although the pathologic role of inflammasome in infection and sterile inflammation is well known, the mechanism and regulation of NLRP3 inflammasome activation remains obscure. Here, we report that anaplastic lymphoma kinase (ALK) is a novel regulator of NLRP3 inflammasome activation in macrophages. Pharmacologic or genetic inhibition of ALK through targeted drugs (ceritinib and lorlatinib) or RNAi blocked extracellular ATP-induced NLRP3 inflammasome activation in macrophages...
April 30, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29707414/treatment-patterns-clinical-and-economic-outcomes-of-patients-with-anaplastic-lymphoma-kinase-positive-non-small-cell-lung-cancer-receiving-ceritinib-a-retrospective-observational-claims-analysis
#6
Anand A Dalal, Annie Guerin, Alex Mutebi, Kenneth W Culver
Objective: To describe patient characteristics, treatment patterns, healthcare resource utilization (HRU), and costs among patients with anaplastic lymphoma kinase ( ALK )-positive non-small cell lung cancer (NSCLC) receiving ceritinib in second or later line of therapy. Methods: Adult patients with NSCLC receiving ceritinib were identified from two large US claims databases (2006-2015). Patient characteristics, comorbidity profile, treatment patterns prior to ceritinib, and ceritinib dosing patterns were described...
2018: Journal of Drug Assessment
https://www.readbyqxmd.com/read/29648831/the-molecular-mechanism-behind-resistance-of-the-g1202r-mutated-anaplastic-lymphoma-kinase-to-the-approved-drug-ceritinib
#7
Chaohong Chen, Zhifeng He, Deyao Xie, Liangcheng Zheng, Tianhao Zhao, Xinbo Zhang, Dezhi Cheng
Anaplastic lymphoma kinase (ALK) has been regarded as an essential target for the treatment of non-small cell lung cancer (NSCLC). However, the emergence of G1202R solvent front mutation that confer resistance to the drugs were reported for the first as well as the second generation ALK inhibitors. It was supposed that the G1202R solvent front mutation might hinder the drug binding. In this study, a different fact could be clarified by multiple molecular modeling methodologies through a structural analogue of ceritinib (compound 10, Cpd-10) that is reported to be a potent inhibitor against the G1202R mutation...
April 12, 2018: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/29629521/anaplastic-lymphoma-kinase-alk-expressing-lung-adenocarcinoma-with-combined-neuroendocrine-component-or-neuroendocrine-transformation-implications-for-neuroendocrine-transformation-and-response-to-alk-tyrosine-kinase-inhibitors
#8
Jongmin Sim, Hyunjin Kim, Jiyeon Hyeon, Yoon La Choi, Joungho Han
BACKGROUND: Anaplastic lymphoma kinase tyrosine kinase inhibitors (ALK-TKIs) are usually effective in lung adenocarcinoma patients with anaplastic lymphoma kinase (ALK) rearrangement. However, even after a good response to ALK-TKI therapy, most patients acquire resistance to these agents. Histological transformation is one of several suggested mechanisms of acquired resistance to ALK-TKIs. The clinicopathologic features of four patients with ALK-expressing adenocarcinoma and neuroendocrine features were analyzed...
April 9, 2018: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/29595984/exosomes-from-irradiated-non-small-cell-lung-cancer-cells-reduced-sensitivity-of-recipient-cells-to-anaplastic-lymphoma-kinase-inhibitors
#9
Hao Wu, Chao Zeng, Yiwang Ye, Jixian Liu, Zhimin Mu, Yuancai Xie, Baokun Chen, Qiaohong Nong, Da Wu
Exosomes, released from various cell types, serve as vehicles of intercellular communication. Rearranged anaplastic lymphoma kinase (ALK) has been detected in exosomes released from cancer cells in ALK-positive non-small cell lung cancer (NSCLC), however, the functional consequence of ALK in exosomes has not been studied. This study aims to address whether exosomal ALK release is affected by stress, and whether exosomal ALK can modulate survival of recipient cells in vitro and in vivo. Exosomes, isolated from ALK-containing H3122 cells with (Exo-Apo) or without (Exo-Ctrl) irradiation treatment, were transferred to recipient H3122 cells in vitro or mouse xenograft in vivo...
March 29, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29570100/inhibition-of-anaplastic-lymphoma-kinase-promotes-apoptosis-and-suppresses-proliferation-in-human-hepatocellular-carcinoma
#10
Zhen Yu, Ronglei Zhao
Our study was to examine the roles of crizotinib and ceritinib in hepatocellular carcinoma (HCC) cells and explore the possible mechanisms. MTT assay was employed to examine the proliferation of five HCC cell lines treated with various concentrations of crizotinib or ceritinib. HepG2 and HCCLM3 cells were incubated with 2 nmol/l ceritinib for 1 week, followed by crystal violet staining and cell counting. Protein amounts of t-ALK, p-ALK, t-AKT, p-AKT, t-ERK, p-ERK, Mcl-1, survivin, and XIAP in HepG2 cells under different culture conditions were evaluated by western blot...
March 21, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29568664/a-liquid-chromatography-with-tandem-mass-spectrometry-method-for-quantitating-total-and-unbound-ceritinib-in-patient-plasma-and-brain-tumor
#11
Xun Bao, Jianmei Wu, Nader Sanai, Jing Li
A rapid, sensitive, and robust reversed-phase liquid chromatography with tandem mass spectrometry method was developed and validated for the determination of total and unbound ceritinib, a second-generation ALK inhibitor, in patient plasma and brain tumor tissue samples. Sample preparation involved simple protein precipitation with acetonitrile. Chromatographic separation was achieved on a Waters ACQUITY UPLC BEH C18 column using a 4-min gradient elution consisting of mobile phase A (0.1% formic acid in water) and mobile phase B (0...
February 2018: Journal of Pharmaceutical Analysis
https://www.readbyqxmd.com/read/29507704/incidence-and-risk-of-hepatic-toxicities-associated-with-anaplastic-lymphoma-kinase-inhibitors-in-the-treatment-of-non-small-cell-lung-cancer-a-systematic-review-and-meta-analysis
#12
Bing Liu, Maoxi Yuan, Yi Sun, Ziming Cheng, Zaiyong Zhang, Shizheng Hou, Xiangdong Wang, Jingfeng Liu
Background: Two anaplastic lymphoma kinase (ALK)-tyrosine kinase inhibitors (-TKIs) have been approved for the treatment of patients with ALK-rearranged (ALK-positive) advanced non-small cell lung cancer (NSCLC). Severe hepatotoxicity has been observed in several clinical studies. We aim to assess the incidence and risk of liver toxicity with these drugs by a systematic review and meta-analysis of clinical trials. Materials and Methods: The databases of PubMed, Web of Science and abstracts presented at oncology conferences' proceedings were searched for relevant studies from January 2000 to January 2017...
February 6, 2018: Oncotarget
https://www.readbyqxmd.com/read/29506392/background-and-rationale-of-the-exalt3-trial-investigating-x-396-in-the-treatment-of-alk-non-small-cell-lung-cancer
#13
Eric K Singhi, Leora Horn
Despite significant advancements in the treatment of anaplastic lymphoma kinase (ALK) positive non-small-cell lung cancer (NSCLC) since the advent of crizotinib, the development of acquired resistance and poor CNS efficacy have necessitated the search for novel and more robust therapies. Ensartinib (X-396) is a novel second-generation ALK-tyrosine kinase inhibitor (TKI) that holds much clinical promise. Preclinical data have demonstrated increased potency of the drug as compared with crizotinib and other second-generation ALK-TKI therapies such as alectinib and ceritinib...
March 6, 2018: Future Oncology
https://www.readbyqxmd.com/read/29505033/shp2-inhibition-restores-sensitivity-in-alk-rearranged-non-small-cell-lung-cancer-resistant-to-alk-inhibitors
#14
Leila Dardaei, Hui Qin Wang, Manrose Singh, Paul Fordjour, Katherine X Shaw, Satoshi Yoda, Grainne Kerr, Kristine Yu, Jinsheng Liang, Yichen Cao, Yan Chen, Michael S Lawrence, Adam Langenbucher, Justin F Gainor, Luc Friboulet, Ibiayi Dagogo-Jack, David T Myers, Emma Labrot, David Ruddy, Melissa Parks, Dana Lee, Richard H DiCecca, Susan Moody, Huaixiang Hao, Morvarid Mohseni, Matthew LaMarche, Juliet Williams, Keith Hoffmaster, Giordano Caponigro, Alice T Shaw, Aaron N Hata, Cyril H Benes, Fang Li, Jeffrey A Engelman
Most anaplastic lymphoma kinase (ALK)-rearranged non-small-cell lung tumors initially respond to small-molecule ALK inhibitors, but drug resistance often develops. Of tumors that develop resistance to highly potent second-generation ALK inhibitors, approximately half harbor resistance mutations in ALK, while the other half have other mechanisms underlying resistance. Members of the latter group often have activation of at least one of several different tyrosine kinases driving resistance. Such tumors are not expected to respond to lorlatinib-a third-generation inhibitor targeting ALK that is able to overcome all clinically identified resistant mutations in ALK-and further therapeutic options are limited...
May 2018: Nature Medicine
https://www.readbyqxmd.com/read/29490295/inhibition-of-collagen-related-peptide-induced-platelet-activation-and-apoptosis-by-ceritinib
#15
Hang Cao, Anja T Umbach, Rosi Bissinger, Meinrad Gawaz, Florian Lang
BACKGROUND/AIMS: The anaplastic lymphoma (tyrosine) kinase (ALK) inhibitor ceritinib triggers apoptosis of tumor cells and eryptosis of erythrocytes. Blood platelets may similarly enter a state resembling apoptosis, which could be triggered by activation with collagen related peptide (CRP). CRP-induced platelet apoptosis is characterized by cell membrane scrambling with phosphatidylserine exposure to the platelet surface and cell shrinkage, preceded by externalization of Ca2+ channel Orai1, increase of cytosolic Ca2+-activity ([Ca2+]i), formation of reactive oxygen species (ROS), and caspase activation...
2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29483416/-result-of-clinical-trials-of-ceritinib-in-patients-with-alk-rearranged-non-small-cell-lung-cancer-and-management-of-the-adverse-events
#16
Miyako Satouchi, Makoto Nishio, Toyoaki Hida, Kazuhiko Nakagawa
The advent of anaplastic lymphoma kinase(ALK)inhibitors has revolutionized treatment of ALK fusion gene-positive nonsmall cell lung cancer(NSCLC). Nevertheless, it has become clear that cases refractory and resistant to ALK inhibitors occur at a certain incidence, and how to treat such cases is a current issue. Following crizotinib and alectinib, ceritinib(Zykadia® capsules)is the third ALK inhibitor approved in Japan, and it is expected to be useful for patients who have developed crizotinib resistance. However, ceritinib has been pointed out to have a high incidence of gastrointestinal adverse events that impact patients' quality of life...
February 2018: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/29474558/phase-3-study-of-ceritinib-vs-chemotherapy-in-alk-rearranged-nsclc-patients-previously-treated-with-chemotherapy-and-crizotinib-ascend-5-japanese-subset
#17
Katsuyuki Kiura, Fumio Imamura, Hiroshi Kagamu, Shingo Matsumoto, Toyoaki Hida, Kazuhiko Nakagawa, Miyako Satouchi, Isamu Okamoto, Mitsuhiro Takenoyama, Yasuhito Fujisaka, Takayasu Kurata, Masayuki Ito, Kota Tokushige, Ben Hatano, Makoto Nishio
Background: In the global, Phase 3, ASCEND-5 study, ceritinib improved progression-free survival (PFS) vs chemotherapy in patients with anaplastic lymphoma kinase (ALK)-rearranged non-small cell lung cancer (NSCLC) who had previously progressed on crizotinib and platinum-based chemotherapy. Here, we report efficacy and safety in a subset of Japanese patients from the ASCEND-5 study. Methods: Patients with advanced ALK-rearranged NSCLC received oral ceritinib 750 mg/day or chemotherapy (intravenous pemetrexed 500 mg/m2 or docetaxel 75 mg/m2 [investigator's choice], every 21 days)...
April 1, 2018: Japanese Journal of Clinical Oncology
https://www.readbyqxmd.com/read/29458783/precision-medicine-in-alk-rearranged-nsclc-a-rapidly-evolving-scenario
#18
REVIEW
Alfredo Addeo, Fabrizio Tabbò, Tim Robinson, Lucio Buffoni, Silvia Novello
IMPORTANCE: The identification of anaplastic lymphoma kinase (ALK) rearrangements in 2-5% of non-small cell lung cancer (NSCLC) patients led to the rapid clinical development of its oral tyrosine kinase inhibitor (TKI). Crizotinib was the first ALK inhibitor approved and utilised in the treatment of ALK+ NSCLC patients in the second line setting first and subsequently in the first line one. Since then many other ALK inhibitors have been developed (ceritinib, alectinib, brigatinib, lorlatinib,etc) and the treatment paradigm of these patients has considerably drifted...
February 2018: Critical Reviews in Oncology/hematology
https://www.readbyqxmd.com/read/29458286/cost-effectiveness-of-ceritinib-in-previously-untreated-anaplastic-lymphoma-kinase-positive-metastatic-non-small-cell-lung-cancer-in-the-united-states
#19
Zheng-Yi Zhou, Alex Mutebi, Simeng Han, Arielle G Bensimon, Marie Louise Ricculli, Jipan Xie, Anand Dalal, Ken Culver
AIMS: To assess the cost-effectiveness of first-line ceritinib vs crizotinib and platinum doublet chemotherapy for anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) from a US third-party payer's perspective. MATERIALS AND METHODS: A partitioned survival model with three health states (stable disease, progressive disease, death) was developed over a 20-year time horizon. Ceritinib's efficacy inputs (progression-free and overall survival) were estimated from ASCEND-4; parametric survival models extrapolated data beyond the trial period...
March 12, 2018: Journal of Medical Economics
https://www.readbyqxmd.com/read/29458018/5-chloro-n4-2-isopropylsulfonyl-phenyl-n2-2-methoxy-4-4-4-methylpiperazin-1-yl-methyl-1h-1-2-3-triazol-1-yl-phenyl-pyrimidine-2-4-diamine-wy-135-a-novel-alk-inhibitor-induces-cell-cycle-arrest-and-apoptosis-through-inhibiting-alk-and-its-downstream-pathways
#20
Mengting Han, Jiwei Shen, Lijing Wang, Yu Wang, Xin Zhai, Yao Li, Meiqiao Liu, Zengqiang Li, Daiying Zuo, Yingliang Wu
Anaplastic lymphoma kinase (ALK)-positive cancers have rising morbidity and mortality in recent years, and novel chemotherapeutic drugs with no drug resistance and high activity for treating ALK-positive cancers are needed urgently. In this study, we investigated the anti-cancer effect of 5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-((4-methylpiperazin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)pyrimidine-2,4-diamine (WY-135), a novel ALK inhibitor, on nucleophosmin-anaplastic lymphoma kinase (NPM-ALK) positive cancer cell line Karpas299 and echinoderm microtubule associated protein like 4-anaplastic lymphoma kinase (EML4-ALK) positive cancer cell line H2228...
March 25, 2018: Chemico-biological Interactions
keyword
keyword
18630
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"