keyword
MENU ▼
Read by QxMD icon Read
search

Nintedanib

keyword
https://www.readbyqxmd.com/read/29152045/discovery-of-indolinone-based-multikinase-inhibitors-as-potential-therapeutics-for-idiopathic-pulmonary-fibrosis
#1
Zhenhua Huang, Heran Li, Qian Zhang, Fangzheng Lu, Mei Hong, Zhigang Zhang, Xiaocui Guo, Yuanju Zhu, Sanming Li, Hongzhuo Liu
Idiopathic pulmonary fibrosis (IPF) is a serious and deadly disease for which treatment options are limited. The recent approval of antifibrosis agent nintedanib represents one of the first therapeutic approaches for the treatment of IPF. Here, we report novel indolinone-based multikinase inhibitors that target angiogenesis and fibrosis pathways and may serve as potential therapeutics for IPF. KBP-7018 is a novel, tyrosine kinase-selective inhibitor with potent effects on three fibrotic kinases (c-KIT, PDGFR, and RET)...
November 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29133080/population-pharmacokinetics-of-nintedanib-in-patients-with-idiopathic-pulmonary-fibrosis
#2
Ulrike Schmid, Christiane Doege, Claudia Dallinger, Matthias Freiwald
BACKGROUND: Nintedanib is a potent intracellular inhibitor of tyrosine kinases, including the receptor kinases vascular endothelial growth factor, platelet-derived growth factor and fibroblast growth factor. A previous model assessed the population pharmacokinetics of nintedanib and its main metabolite BIBF 1202 in patients with non-small cell lung cancer and idiopathic pulmonary fibrosis (IPF). The objective of this analysis was to further characterise the population pharmacokinetics of nintedanib in patients with IPF by including data from the Phase III trials...
November 10, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29119292/population-pharmacokinetics-of-nintedanib-an-inhibitor-of-tyrosine-kinases-in-patients-with-non-small-cell-lung-cancer-or-idiopathic-pulmonary-fibrosis
#3
Ulrike Schmid, Karl-Heinz Liesenfeld, Angele Fleury, Claudia Dallinger, Matthias Freiwald
PURPOSE: A population pharmacokinetic model was developed for nintedanib in patients with non-small cell lung cancer (NSCLC) or idiopathic pulmonary fibrosis (IPF). The effects of intrinsic and extrinsic patient factors on exposure of nintedanib and its main metabolite BIBF 1202 were studied. METHODS: Data from 1191 patients with NSCLC (n = 849) or IPF (n = 342) treated with oral nintedanib (once- or twice-daily, dose range 50-250 mg) in 4 Phase II or III studies were combined...
November 8, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29106740/pharmacokinetics-of-nintedanib-in-subjects-with-hepatic-impairment
#4
Kristell Marzin, Gunther Kretschmar, Doreen Luedtke, Sandrine Kraemer, Raimund Kuelzer, Rozsa Schlenker-Herceg, Ulrike Schmid, David Schnell, Claudia Dallinger
Nintedanib is an intracellular inhibitor of tyrosine kinases used in the treatment of non-small cell lung cancer and idiopathic pulmonary fibrosis (IPF). This phase 1 open-label study investigated the influence of mild and moderate hepatic impairment on the pharmacokinetics (PK), safety, and tolerability of nintedanib following oral administration of a single 100-mg dose. Subjects with hepatic impairment classified as Child-Pugh A (mild hepatic impairment) or Child-Pugh B (moderate hepatic impairment) were eligible...
November 6, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29103264/suppressors-for-human-epidermal-growth-factor-receptor-2-4-her2-4-a-new-family-of-anti-toxoplasmic-agents-in-arpe-19-cells
#5
Yeong Hoon Kim, Lokraj Bhatt, Hye-Jin Ahn, Zhaoshou Yang, Won-Kyu Lee, Ho-Woo Nam
The effects of tyrosine kinase inhibitors (TKIs) were evaluated on growth inhibition of intracellular Toxoplasma gondii in host ARPE-19 cells. The number of tachyzoites per parasitophorous vacuolar membrane (PVM) was counted after treatment with TKIs. T. gondii protein expression was assessed by western blot. Immunofluorescence assay was performed using Programmed Cell Death 4 (PDCD4) and T. gondii GRA3 antibodies. The TKIs were divided into 3 groups; non-epidermal growth factor receptor (non-EGFR), anti-human EGFR 2 (anti-HER2), and anti-HER2/4 TKIs, respectively...
October 2017: Korean Journal of Parasitology
https://www.readbyqxmd.com/read/29101500/early-clinical-experiences-with-nintedanib-in-three-uk-tertiary-interstitial-lung-disease-centres
#6
Hannah Toellner, G Hughes, W Beswick, M G Crooks, C Donaldson, I Forrest, S P Hart, C Leonard, M Major, A J Simpson, N Chaudhuri
BACKGROUND: Nintedanib has been shown to slow disease progression in patients with idiopathic pulmonary fibrosis (IPF). It was approved by the National Institute for Health and Care Excellence (NICE) in January 2016 for IPF patients with a forced vital capacity (FVC) of 50-80% in the United Kingdom (UK). AIM: To report real world data about our early clinical experience using nintedanib in 187 patients with a multi-disciplinary (MDT) diagnosis of IPF in a manufacturer funded patient in need scheme (three UK centres) prior to NICE approval...
November 3, 2017: Clinical and Translational Medicine
https://www.readbyqxmd.com/read/29101238/glucocorticoid-resistance-is-reverted-by-lck-inhibition-in-pediatric-t-cell-acute-lymphoblastic-leukemia
#7
Valentina Serafin, Giorgia Capuzzo, Gloria Milani, Sonia Anna Minuzzo, Marica Pinazza, Roberta Bortolozzi, Silvia Bresolin, Elena Porcù, Chiara Frasson, Stefano Indraccolo, Giuseppe Basso, Benedetta Accordi
Pediatric T-acute lymphoblastic leukemia (T-ALL) patients often display resistance to glucocorticoid (GC) treatment. These patients, classified as Prednisone Poor Responders (PPR), have poorer outcome compared to the other pediatric T-ALL patients receiving a high-risk adapted therapy. Since glucocorticoids are administered to ALL patients during all the different phases of therapy, GC resistance represents an important challenge to be addressed in order to improve the outcome for these patients. Mechanisms underlying resistance are not yet fully unraveled, thus our research focused on the identification of deregulated signaling pathways to point out new targeted approaches...
November 3, 2017: Blood
https://www.readbyqxmd.com/read/29074545/idiopathic-pulmonary-fibrosis-lessons-from-clinical-trials-over-the-past-25%C3%A2-years
#8
REVIEW
Ganesh Raghu
Idiopathic pulmonary fibrosis (IPF) is a progressive and ultimately fatal disease. A major breakthrough in treatment came when, after decades of clinical trials which failed to identify an efficacious treatment regimen, two therapies were successful in Phase-III trials. The advent of these therapies, nintedanib and pirfenidone, meant that for the first time IPF patients had two treatment options that could reduce disease progression. This review summarises the key lessons to be obtained from the clinical trials that led to the current international clinical practice guidelines for the treatment of IPF and provides insights for the design of future clinical trials that are needed if we are to improve outcomes that are clinically meaningful to IPF patients...
October 2017: European Respiratory Journal: Official Journal of the European Society for Clinical Respiratory Physiology
https://www.readbyqxmd.com/read/29052582/idiopathic-pulmonary-fibrosis
#9
REVIEW
Fernando J Martinez, Harold R Collard, Annie Pardo, Ganesh Raghu, Luca Richeldi, Moises Selman, Jeffrey J Swigris, Hiroyuki Taniguchi, Athol U Wells
Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive lung disease characterized by progressive lung scarring and the histological picture of usual interstitial pneumonia (UIP). It is associated with increasing cough and dyspnoea and impaired quality of life. IPF affects ∼3 million people worldwide, with incidence increasing dramatically with age. The diagnostic approach includes the exclusion of other interstitial lung diseases or overlapping conditions and depends on the identification of the UIP pattern, usually with high-resolution CT; lung biopsy might be required in some patients...
October 20, 2017: Nature Reviews. Disease Primers
https://www.readbyqxmd.com/read/29038968/anti-fibrotic-nintedanib-a-new-opportunity-for-systemic-sclerosis-patients
#10
REVIEW
Ana Catarina Duarte, Maria José Santos, Ana Cordeiro
Systemic sclerosis is a connective tissue disease characterized by progressive skin thickening and a wide spectrum of internal organ involvement. Pathogenesis includes vasculopathy, inflammation, and fibrosis. Although immunosuppressants such as cyclophosphamide and mycophenolate mofetil have shown some benefit in interstitial lung disease management, it is still a major cause of morbi-mortality in these patients. Therefore, there is a current need for new therapies. Here, we report a 65-year-old female patient with limited cutaneous systemic sclerosis, anti-topoisomerase-positive and extensive lung disease...
October 16, 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/29035589/the-activity-of-nintedanib-in-an-animal-model-of-allogenic-left-lung-transplantation-resembling-aspects-of-allograft-rejection
#11
Marietta von Suesskind-Schwendi, Elke Boxhammer, Stephan W Hirt, Stephan Schreml, Christof Schmid, Lutz Wollin, Karla Lehle
AIM OF THE STUDY: The prevention and treatment of chronic lung allograft dysfunction (CLAD) after lung transplantation (LTx) remain unsatisfactory. Growth factors may play an important role in the development of CLAD. This study evaluated the effects of nintedanib, a receptor tyrosine kinase inhibitor, in the treatment of CLAD after experimental LTx. MATERIALS AND METHODS: A rat model of left lung allo-transplantation (Fisher 344 to Wistar Kyoto) was used to evaluate the effect of nintedanib (50 mg/kg per day) on the development of CLAD...
October 16, 2017: Experimental Lung Research
https://www.readbyqxmd.com/read/29034773/substrate-dependent-effects-of-molecular-targeted-anticancer-agents-on-activity-of-organic-anion-transporting-polypeptide-1b1
#12
Hiroyoshi Koide, Masayuki Tsujimoto, Ai Takeuchi, Miyu Tanaka, Yoko Ikegami, Mayu Tagami, Syoko Abe, Miki Hashimoto, Tetsuya Minegaki, Kohshi Nishiguchi
1. Organic anion-transporting polypeptide 1B1 (OATP1B1) plays an important role in the hepatic uptake of a broad range of substrate drugs. In vitro experiments show that molecular-targeted agents do not always have similar effects on OATP1B1 activity. 2. The purpose of this study was to clarify whether the effects of molecular-targeted agents on OATP1B1 are substrate-dependent. We used OATP1B1-transfected cells to compare the effects of molecular-targeted agents on OATP1B1-mediated uptake of fluorescein (FL), 2',7'-dichlorofluorescein (DCF), atorvastatin, SN-38, and valsartan...
October 16, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29018526/design-of-the-pf-ild-trial-a-double-blind-randomised-placebo-controlled-phase-iii-trial-of-nintedanib-in-patients-with-progressive-fibrosing-interstitial-lung-disease
#13
Kevin R Flaherty, Kevin K Brown, Athol U Wells, Emmanuelle Clerisme-Beaty, Harold R Collard, Vincent Cottin, Anand Devaraj, Yoshikazu Inoue, Florence Le Maulf, Luca Richeldi, Hendrik Schmidt, Simon Walsh, William Mezzanotte, Rozsa Schlenker-Herceg
600 patients aged ≥18 years will be randomised in a 1:1 ratio to nintedanib or placebo. Patients with diagnosis of IPF will be excluded. The study population will be enriched with two-thirds having a usual interstitial pneumonia-like pattern on HRCT. The primary endpoint is the annual rate of decline in forced vital capacity over 52 weeks. The main secondary endpoints are the absolute change from baseline in King's Brief Interstitial Lung Disease Questionnaire total score, time to first acute interstitial lung disease exacerbation or death and time to all-cause mortality over 52 weeks...
2017: BMJ Open Respiratory Research
https://www.readbyqxmd.com/read/29017422/nintedanib-for-idiopathic-pulmonary-fibrosis
#14
Abisola Tepede, Dinesh Yogaratnam
OBJECTIVE: To review the pharmacology, safety, and efficacy of nintedanib for the treatment of idiopathic pulmonary fibrosis (IPF). METHODS: A literature search was conducted via PubMed using the MeSH term "idiopathic pulmonary fibrosis" combined with the key word "nintedanib." Additional online searches using Google Scholar, Micromedex, and PubMed were performed to obtain prescribing and cost information. RESULTS: One phase II and 2 replicate phase III clinical trials that examined the safety and efficacy of nintedanib for IPF were identified...
January 1, 2017: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/28993537/long-term-treatment-of-patients-with-idiopathic-pulmonary-fibrosis-with-nintedanib-results-from-the-tomorrow-trial-and-its-open-label-extension
#15
Luca Richeldi, Michael Kreuter, Moisés Selman, Bruno Crestani, Anne-Marie Kirsten, Wim A Wuyts, Zuojun Xu, Katell Bernois, Susanne Stowasser, Manuel Quaresma, Ulrich Costabel
The TOMORROW trial of nintedanib comprised a randomised, placebo-controlled, 52-week period followed by a further blinded treatment period and an open-label extension. We assessed outcomes across these periods in patients randomised to nintedanib 150 mg twice daily or placebo at the start of TOMORROW. The annual rate of decline in FVC was -125.4 mL/year (95% CI -168.1 to -82.7) in the nintedanib group and -189.7 mL/year (95% CI -229.8 to -149.6) in the comparator group. The adverse event profile of nintedanib remained consistent throughout the studies...
October 9, 2017: Thorax
https://www.readbyqxmd.com/read/28980742/nintedanib-treatment-delays-prostate-dorsolateral-lobe-cancer-progression-in-the-tramp-model-contribution-to-the-epithelial-stromal-interaction-balance
#16
Ellen Nogueira Pangrazi, Raquel Frenedoso da Silva, Larissa Akemi Kido, Fabio Montico, Valéria Helena Alves Cagnon
Prostate cancer progression mechanism has been linked to epithelial proliferation, tumor invasion ability and growth factors. Nintedanib (BIBF 1120) has been reported as being FGF and VEGF pathway inhibitors, exhibiting antitumor activity. Thus, the objective herein was to characterize the early Nintedanib treatment effects on the structure and molecules involved in the basal membrane, the extracellular matrix maintenance, in addition to the angiogenesis and mitogenic processes at different grades of prostatic tumor development in TRAMP mice...
October 5, 2017: Cell Biology International
https://www.readbyqxmd.com/read/28978214/strategies-to-manage-costs-in-idiopathic-pulmonary-fibrosis
#17
Gary M Owens
Idiopathic pulmonary fibrosis (IPF) is a diagnostically challenging disease. Clinicians are faced with the need to exclude alternative diagnoses, limited treatment and management guidelines, and few treatment options. Patients with IPF have significantly increased healthcare usage compared with similar patients without the disease. Medicare estimates for this disease are as high as $3 billion, not including cost of treatment. The disease, characterized by worsening dyspnea, declining lung function, nonspecific respiratory symptoms, and a varied clinical course randomly punctuated by episodes of acute exacerbations, is also accompanied by a host of comorbid conditions that contribute significantly to increased healthcare usage and cost...
July 2017: American Journal of Managed Care
https://www.readbyqxmd.com/read/28978213/evaluating-new-treatment-options
#18
Steven D Nathan
Idiopathic pulmonary fibrosis (IPF) is the most prevalent type of idiopathic interstitial pneumonia, accounting for at least half of all diagnosed cases. Because it lacks a cure, the goal of treatment for IPF is to stabilize or reduce the rate of disease progression. Nonpharmacologic treatment options for IPF consist of long-term oxygen treatment, lung transplantation, and pulmonary rehabilitation. In the past, pharmacologic therapies for IPF included anticoagulants and anti-inflammatory or immunosuppressive agents...
July 2017: American Journal of Managed Care
https://www.readbyqxmd.com/read/28978212/overview-of-idiopathic-pulmonary-fibrosis-ipf-and-evidence-based-guidelines
#19
Roozbeh Sharif
Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive form of interstitial lung disease (ILD), characterized by fibrosis and worsening lung function, that primarily occurs in those 50 years and older. Various causes including genetic susceptibility, environmental risk factors, and exposures have been suggested in the literature. All of these cause repetitive micro-injury to the lung tissue and vasculature, which triggers a cascade of inflammatory response and fibrosis. Symptoms are nonspecific and most patients present several years after the initial radiographic changes occur...
July 2017: American Journal of Managed Care
https://www.readbyqxmd.com/read/28965421/safety-and-efficacy-of-nintedanib-for-the-treatment-of-metastatic-colorectal-cancer
#20
REVIEW
Maria Carmen Riesco-Martinez, Ana Sanchez-Torre, Rocio Garcia-Carbonero
Nintedanib (BIBF 1200) is an oral tyrosine kinase inhibitor that targets the vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR) and fibroblast growth factor (FGFR) receptors. It is approved in Europe in combination with docetaxel for patients with advanced lung adenocarcinoma who have progressed to first-line chemotherapy. However, its role in the treatment of metastatic colorectal cancer (mCRC) is uncertain. Recent results from the LUME-Colon 1 pivotal phase III trial showed only a marginal increase in progression free survival over placebo in refractory mCRC patients, with a toxicity profile similar to other antiangiogenic agents, and no benefit in overall survival...
November 2017: Expert Opinion on Investigational Drugs
keyword
keyword
6846
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"