Ceritinib in patients with advanced, crizotinib-treated, anaplastic lymphoma kinase-rearranged NSCLC: Japanese subset

ConclusionsThis study demonstrates the clinical activity and manageable tolerability of ceritinib in a Japanese subset of chemotherapy- and crizotinib-pretreated patients withALK-rearranged non-small cell lung cancer who progressed on crizotinib, as was shown in the whole ASCEND-2 study population.ClinicalTrials.gov identifier: NCT01685060
Source: Japanese Journal of Clinical Oncology - Category: Cancer & Oncology Source Type: research

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Publication date: Available online 16 October 2019Source: Biocatalysis and Agricultural BiotechnologyAuthor(s): V. Arpudhamary, S. Priya, Muhammed A.P. Manzoor, D. Mubarakali, S. HemalathaAbstractCancer is a group of diseases characterized by the rapid creation of abnormal cells. Cancer is one of the leading causes of death in humans, affecting millions of people per year. Cembranoids are carbocyclic diterpenes composed of 14-membered ring, mainly present in the genera Nicotiana and Pinus in plants, and soft coral and other organisms. Cembranoids are cytotoxic and inhibit phospholipid metabolism. The present study is focus...
Source: Biocatalysis and Agricultural Biotechnology - Category: Biotechnology Source Type: research
In this study, 3D Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA) were employed to construct quantitative structure-activity relationship (QSAR) models of a series of niacinamide analogues as antiandrogens. The obtained models have good reliability and predictivity. In addition, the contour maps from the models can intuitively aid to understand the vital structural characteristics of niacinamides related with the AR antagonistic activities. Our study provides important guidance for the rational design and screening of highly potential active antiandrogens.
Source: Journal of Molecular Structure - Category: Molecular Biology Source Type: research
In conclusion, we showed hypermethylation of CpGs as a novel mechanism of action for DNMTi agents and identified 638 hypermethylated molecular targets (CpGs) common to decitabine and azacytidine therapy. These novel results suggest that hypermethylation of CpGs should be considered when predicting the DNMTi responses and side effects in cancer patients. Introduction DNA methyltransferase inhibitors (DNMTi) are widely used as chemical tools for hypomethylating the genome, with an aim to understand the role of DNA methylation in multiple processes (e.g., X-chromosome inactivation and DNA imprinting) and as an anti-ca...
Source: Frontiers in Pharmacology - Category: Drugs & Pharmacology Source Type: research
Conclusion The expression of the components of the PTN-MK-RPTPβ/ζ axis in immune cells and in inflammatory diseases suggests important roles for this axis in inflammation. Pleiotrophin has been recently identified as a limiting factor of metainflammation, a chronic pathological state that contributes to neuroinflammation and neurodegeneration. Pleiotrophin also seems to potentiate acute neuroinflammation independently of the inflammatory stimulus while MK seems to play different -even opposite- roles in acute neuroinflammation depending on the stimulus. Which are the functions of MK and PTN in chronic neuroinfla...
Source: Frontiers in Pharmacology - Category: Drugs & Pharmacology Source Type: research
ConclusionCrizotinib was effective and well tolerated in Chinese patients withROS1-positive advanced NSCLC in real-world clinical practice. The progression sites and patterns, as well as treatments after first disease progression on crizotinib were diverse. Crizotinib beyond progressive disease and local therapy after failure of crizotinib treatment were feasible and effective in clinical practice.
Source: Targeted Oncology - Category: Cancer & Oncology Source Type: research
Abstract Lorlatinib, a novel generation oral anaplastic lymphoma kinase (ALK) and ROS1 inhibitor with high membrane and blood-brain barrier permeability, recently received accelerated approval for treatment of ALK-rearranged non-small-cell lung cancer (NSCLC), and its further clinical development is ongoing. We previously found that the efflux transporter P-glycoprotein (MDR1/ABCB1) restricts lorlatinib brain accumulation and that the drug-metabolizing enzyme cytochrome P450-3A (CYP3A) limits its oral availability. Using genetically modified mouse models, we investigated the impact of targeted pharmacological inhi...
Source: European Journal of Pharmaceutics and Biopharmaceutics - Category: Drugs & Pharmacology Authors: Tags: Eur J Pharm Biopharm Source Type: research
Publication date: November 2018Source: Pharmacological Research, Volume 137Author(s): Wenlong Li, Rolf W. Sparidans, Yaogeng Wang, Maria C. Lebre, Jos H. Beijnen, Alfred H. SchinkelAbstractBrigatinib is an FDA-approved oral anaplastic lymphoma kinase (ALK) inhibitor for treatment of metastatic non-small cell lung cancer (NSCLC). Using genetically modified mouse models, we investigated the roles of the multidrug efflux transporters ABCB1 and ABCG2, and the multispecific drug-metabolizing enzyme CYP3 A in plasma pharmacokinetics and tissue distribution of brigatinib. In vitro, brigatinib was exceptionally well transpo...
Source: Pharmacological Research - Category: Drugs & Pharmacology Source Type: research
AbstractThe identification of anaplastic lymphoma kinase rearrangements in 2 –5% of patients with non-small-cell lung cancer led to rapid advances in the clinical development of oral tyrosine kinase inhibitors. Anaplastic lymphoma kinase inhibitors are an effective treatment in preclinical models and patients with anaplastic lymphoma kinase-translocated cancers. Four anapl astic lymphoma kinase inhibitors (crizotinib, ceritinib, alectinib, and brigatinib) have recently been approved. Post-marketing studies provided additional pharmacokinetic information on their pharmacokinetic parameters. The pharmacokinetic propert...
Source: Clinical Pharmacokinetics - Category: Drugs & Pharmacology Source Type: research
Publication date: Available online 24 January 2017 Source:The Lancet Author(s): Jean-Charles Soria, Daniel S W Tan, Rita Chiari, Yi-Long Wu, Luis Paz-Ares, Juergen Wolf, Sarayut L Geater, Sergey Orlov, Diego Cortinovis, Chong-Jen Yu, Maximillian Hochmair, Alexis B Cortot, Chun-Ming Tsai, Denis Moro-Sibilot, Rosario G Campelo, Tracey McCulloch, Paramita Sen, Margaret Dugan, Serafino Pantano, Fabrice Branle, Cristian Massacesi, Gilberto de Castro Background The efficacy of ceritinib in patients with untreated anaplastic lymphoma kinase (ALK)-rearranged non-small-cell lung cancer (NSCLC) is not known. We assessed the efficac...
Source: The Lancet - Category: Journals (General) Source Type: research
Eric S Schaefer,1 Christina Baik2 1Section of Medical Oncology, Highlands Oncology Group, Fayetteville, AR, 2Department of Medicine, Medical Oncology Division, University of Washington School of Medicine, Seattle, WA, USA Abstract: Anaplastic lymphoma kinase (ALK) gene fusions occur in 3%–7% of non-small-cell lung cancer (NSCLC) cases. Ceritinib, a once-daily, oral ALK inhibitor, has activity against crizotinib-resistant and crizotinib-naïve NSCLC, including brain metastases. Ceritinib (Zykadia™) was granted accelerated approval by the US Food and Drug Administration in 2014 for treating crizotinib-resista...
Source: Cancer Management and Research - Category: Cancer & Oncology Tags: Cancer Management and Research Source Type: research
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