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Boehringer Ingelheim

Ingo Muegge, Prasenjit Mukherjee
A statistical analysis of 203 high-throughput screens was conducted studying the propensity of small molecules in the Boehringer Ingelheim screening deck to show biological activity after having tested inactive previously in a growing number of screening assays. Dark chemical matter (DCM) compounds, which have been tested and found inactive in 50 or more assays, exhibit hit rates that are comparable to those of compounds tested in much fewer assays. Only compounds tested inactive in 125 or more assays start showing a hit rate deterioration of up to 40% compared to compounds tested in less than 25 assays...
October 20, 2016: Journal of Medicinal Chemistry
Ned Stafford
No abstract text is available yet for this article.
2016: BMJ: British Medical Journal
Ingo Muegge, Andreas Bergner, Jan M Kriegl
Computer-Aided Drug Design (CADD) is an integral part of the drug discovery endeavor at Boehringer Ingelheim (BI). CADD contributes to the evaluation of new therapeutic concepts, identifies small molecule starting points for drug discovery, and develops strategies for optimizing hit and lead compounds. The CADD scientists at BI benefit from the global use and development of both software platforms and computational services. A number of computational techniques developed in-house have significantly changed the way early drug discovery is carried out at BI...
September 20, 2016: Journal of Computer-aided Molecular Design
Christian Ott, Iris Kistner, Mirjam Keller, Stefanie Friedrich, Carsten Willam, Peter Bramlage, Roland E Schmieder
AIMS/HYPOTHESIS: Endothelial dysfunction predicts cardiovascular damage and renal involvement. Animal experiments and human studies indicate an increased nitric oxide (NO) activity and endothelial NO synthase (NOS) expression in the early stage of type 2 diabetes. The aim of the study was to assess the effect of linagliptin on the endothelial function of the renal vasculature. METHODS: In this randomised, double-blind, parallel-group, investigator-initiated trial, 62 patients with type 2 diabetes were randomly assigned (by computer-generated random code) to receive linagliptin 5 mg (n = 30) or placebo (n = 32) for 4 weeks...
September 1, 2016: Diabetologia
Victoria Miller, Salim Yusuf, Clara K Chow, Mahshid Dehghan, Daniel J Corsi, Karen Lock, Barry Popkin, Sumathy Rangarajan, Rasha Khatib, Scott A Lear, Prem Mony, Manmeet Kaur, Viswanathan Mohan, Krishnapillai Vijayakumar, Rajeev Gupta, Annamarie Kruger, Lungiswa Tsolekile, Noushin Mohammadifard, Omar Rahman, Annika Rosengren, Alvaro Avezum, Andrés Orlandini, Noorhassim Ismail, Patricio Lopez-Jaramillo, Afzalhussein Yusufali, Kubilay Karsidag, Romaina Iqbal, Jephat Chifamba, Solange Martinez Oakley, Farnaza Ariffin, Katarzyna Zatonska, Paul Poirier, Li Wei, Bo Jian, Chen Hui, Liu Xu, Bai Xiulin, Koon Teo, Andrew Mente
BACKGROUND: Several international guidelines recommend the consumption of two servings of fruits and three servings of vegetables per day, but their intake is thought to be low worldwide. We aimed to determine the extent to which such low intake is related to availability and affordability. METHODS: We assessed fruit and vegetable consumption using data from country-specific, validated semi-quantitative food frequency questionnaires in the Prospective Urban Rural Epidemiology (PURE) study, which enrolled participants from communities in 18 countries between Jan 1, 2003, and Dec 31, 2013...
October 2016: Lancet Global Health
Eunice Mayumi Suenaga, Ligia de Cássia Val, Mineko Tominaga, José Homero Souza Filho, Gidel Soares, Monalisa Vioto, Clovis Ryuichi Nakaie
We have developed and validated a fast and sensitive ultra high-performance liquid chromatography with positive ion electrospray ionization tandem mass spectrometry method for determining N-butylscopolamine levels in human plasma using propranolol as an internal standard. The acquisition was set up in the multiple reaction monitoring mode with the transitions m/z 360.3 → 138.0 for N-butylscopolamine and m/z 260.2 → 116.1 for IS. This method uses a liquid-liquid extraction process with dichloromethane...
August 24, 2016: Biomedical Chromatography: BMC
Jiwoon Jeong, Kyuhyung Choi, Ikjae Kang, Changhoon Park, Chanhee Chae
Type 2 porcine reproductive and respiratory syndrome (PRRS) virus (PRRSV) was first isolated in Korea in 1994. The commercial PRRS modified live vaccine (Ingelvac(®) PRRS MLV, Boehringer Ingelheim Vetmedica Inc., St. Joseph, Missouri, USA) based on type 2 PRRSV, was first licensed for use in 3- to 18-week-old pigs in Korea in 1996. The objective of the present study was to evaluate the efficacy of this 20year old commercial PRRS modified live vaccine (MLV) against two recent PRRSV isolates. Two genetically distant type 2 PRRSV strains (SNUVR150004 for lineage 1 and SNUVR150324 for lineage 5), isolated in 2015, were used as challenge virus...
August 30, 2016: Veterinary Microbiology
Jeff S Healey, Jonas Oldgren, Michael Ezekowitz, Jun Zhu, Prem Pais, Jia Wang, Patrick Commerford, Petr Jansky, Alvaro Avezum, Alben Sigamani, Albertino Demasceno, Paul Reilly, Alex Grinvalds, Juliet Nakamya, Akinyemi Aje, Wael Almahmeed, Andrew Moriarty, Lars Wallentin, Salim Yusuf, Stuart J Connolly
BACKGROUND: Atrial fibrillation is an important cause of morbidity and mortality worldwide, but scant data are available for long-term outcomes in individuals outside North America or Europe, especially in primary care settings. METHODS: We did a cohort study using a prospective registry of patients in 47 countries who presented to a hospital emergency department with atrial fibrillation or atrial flutter as a primary or secondary diagnosis. 15 400 individuals were enrolled to determine the occurrence of death and strokes (the primary outcomes) in this cohort over eight geographical regions (North America, western Europe, and Australia; South America; eastern Europe; the Middle East and Mediterranean crescent; sub-Saharan Africa; India; China; and southeast Asia) 1 year after attending the emergency department...
September 17, 2016: Lancet
Michael Bieler, Michael Reutlinger, Tiago Rodrigues, Petra Schneider, Jan M Kriegl, Gisbert Schneider
We present the application of machine learning models to selecting G protein-coupled receptor (GPCR)-focused compound libraries. The library design process was realized by ant colony optimization. A proprietary Boehringer-Ingelheim reference set consisting of 3519 compounds tested in dose-response assays at 11 GPCR targets served as training data for machine learning and activity prediction. We compared the usability of the proprietary data with a public data set from ChEMBL. Gaussian process models were trained to prioritize compounds from a virtual combinatorial library...
May 2016: Molecular Informatics
Jaime Algorta, Laura Andrade, Marta Medina, Valentin Kirkov, Sacha Arsova, Fumin Li, Jingduan Chi
BACKGROUND AND OBJECTIVE: A novel tiotropium bromide monodose capsule dry powder inhaler (DPI) formulation and device have been developed. The formulation was based on a spray-dried matrix that enhances the aerosolizaton properties, allowing a less active tiotropium metered dose (13 µg/capsule) while maintaining the same delivered dose (10 µg/actuation). This study describes the pharmacokinetic bioequivalence to the reference product. METHODS: This randomized, two-stage, crossover, semi-replicate (three-way) study was performed in healthy volunteers...
September 2016: Clinical Drug Investigation
Martin J O'Donnell, Siu Lim Chin, Sumathy Rangarajan, Denis Xavier, Lisheng Liu, Hongye Zhang, Purnima Rao-Melacini, Xiaohe Zhang, Prem Pais, Steven Agapay, Patricio Lopez-Jaramillo, Albertino Damasceno, Peter Langhorne, Matthew J McQueen, Annika Rosengren, Mahshid Dehghan, Graeme J Hankey, Antonio L Dans, Ahmed Elsayed, Alvaro Avezum, Charles Mondo, Hans-Christoph Diener, Danuta Ryglewicz, Anna Czlonkowska, Nana Pogosova, Christian Weimar, Romaina Iqbal, Rafael Diaz, Khalid Yusoff, Afzalhussein Yusufali, Aytekin Oguz, Xingyu Wang, Ernesto Penaherrera, Fernando Lanas, Okechukwu S Ogah, Adesola Ogunniyi, Helle K Iversen, German Malaga, Zvonko Rumboldt, Shahram Oveisgharan, Fawaz Al Hussain, Daliwonga Magazi, Yongchai Nilanont, John Ferguson, Guillaume Pare, Salim Yusuf
BACKGROUND: Stroke is a leading cause of death and disability, especially in low-income and middle-income countries. We sought to quantify the importance of potentially modifiable risk factors for stroke in different regions of the world, and in key populations and primary pathological subtypes of stroke. METHODS: We completed a standardised international case-control study in 32 countries in Asia, America, Europe, Australia, the Middle East, and Africa. Cases were patients with acute first stroke (within 5 days of symptom onset and 72 h of hospital admission)...
August 20, 2016: Lancet
(no author information available yet)
The prevalence of type 2 diabetes is rising, and in 2015 more than 5% of adults in the UK were affected by this condition.(1,2) Management of type 2 diabetes includes encouraging lifestyle changes (increased exercise, modification of diet and smoking cessation) alongside the provision of medication to minimise long-term complications and manage blood sugar control while avoiding unwanted effects of drug treatment.(3) Of particular importance, people with type 2 diabetes are at increased risk of cardiovascular disease, and therefore the aims of treatment also include modification of associated risk factors...
July 2016: Drug and Therapeutics Bulletin
(no author information available yet)
No abstract text is available yet for this article.
July 9, 2016: Veterinary Record
K Kempf, S Martin, C Döhring, K Dugi, B Haastert, M Schneider
BACKGROUND: Cardiovascular disease (CVD) may cause an economic burden to companies, but CVD risk estimations specific to working populations are lacking. AIMS: To estimate the 10-year CVD risk in the Boehringer Ingelheim (BI) employee cohort and analyse the potential effect of hypothetical risk reduction interventions. METHODS: We estimated CVD risk using the Framingham (FRS), PROCAM (PRS) and Reynolds (RRS) risk scores, using cross-sectional baseline data on BI Pharma employees collected from 2005 to 2011...
October 2016: Occupational Medicine
Esther S Kim
Olmutinib (Olita(TM)) is an oral, third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) that is being developed by Boehringer Ingelheim and Hanmi Pharmaceutical Co. Ltd for the treatment of non-small cell lung cancer (NSCLC). Third-generation EGFR TKIs with covalent binding to the receptors demonstrate irreversible enzymatic inhibition of activating EGFR mutations and T790M mutation (a common reason for acquired EGFR TKI resistance), while sparing wild-type EGFR. In December 2015, olmutinib was granted breakthrough therapy designation in NSCLC by the US FDA...
July 2016: Drugs
Wijdan H Ramadan, Wissam K Kabbara, Rosa M Abilmona
PURPOSE: Published data on the pharmacology, pharmacokinetics, efficacy, and safety of the once-daily, long-acting β2-agonist (LABA) olodaterol are reviewed. SUMMARY: Olodaterol (Striverdi Respimat, Boehringer Ingelheim), a LABA with high selectivity for β2-adrenergic receptors, is indicated for the treatment of chronic obstructive pulmonary disease (COPD); the recommended dose is 5 μg, to be delivered once daily via the Respimat inhaler. In 48- and 6-week Phase III clinical trials of olodaterol evaluating various lung function and symptomatic outcomes in patients with moderate to very severe COPD, olodaterol use was associated with significant improvements in spirometry outcomes, such as postbronchodilator forced expiratory volume in one second (FEV1), as well as dyspnea severity and quality-of-life measures...
August 1, 2016: American Journal of Health-system Pharmacy: AJHP
(no author information available yet)
UNLABELLED: The Food and Drug Administration Modernization Act (FDAMA) of 1997 included Section 114 as a regulatory safe harbor with the goal of increasing the dissemination of health care economic information (HCEI) to those responsible for formulary decision making. HCEI is typically not included within FDA-approved labeling. Although it has been nearly 20 years since passage and enactment of Section 114, proactive distribution of HCEI has been underutilized by biopharmaceutical companies partly because of (a) vague wording in the statute and (b) the absence of FDA-implementing regulations...
July 2016: Journal of Managed Care & Specialty Pharmacy
Kyle T Baron, Sreeraj Macha, Uli C Broedl, Valerie Nock, Silke Retlich, Matthew Riggs
INTRODUCTION: The aim of the analysis was to characterize the population pharmacokinetics (PKs) and exposure-response (E-R) for efficacy (fasting plasma glucose, glycated hemoglobin) and safety/tolerability [hypoglycemia, genital infections, urinary tract infection (UTI), and volume depletion] of the sodium glucose cotransporter 2 inhibitor, empagliflozin, in patients with type 2 diabetes mellitus. This study extends the findings of previous analyses which described the PK and pharmacodynamics (PD) using early clinical studies of up to 12 weeks in duration...
September 2016: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
Christoph Wanner, Silvio E Inzucchi, John M Lachin, David Fitchett, Maximilian von Eynatten, Michaela Mattheus, Odd Erik Johansen, Hans J Woerle, Uli C Broedl, Bernard Zinman
BACKGROUND: Diabetes confers an increased risk of adverse cardiovascular and renal events. In the EMPA-REG OUTCOME trial, empagliflozin, a sodium-glucose cotransporter 2 inhibitor, reduced the risk of major adverse cardiovascular events in patients with type 2 diabetes at high risk for cardiovascular events. We wanted to determine the long-term renal effects of empagliflozin, an analysis that was a prespecified component of the secondary microvascular outcome of that trial. METHODS: We randomly assigned patients with type 2 diabetes and an estimated glomerular filtration rate of at least 30 ml per minute per 1...
July 28, 2016: New England Journal of Medicine
Julia Stadler, Susanne Zoels, Matthias Eddicks, Christian Kraft, Mathias Ritzmann, Andrea Ladinig
The objective of the present study was to assess safety and efficacy of a new modified live-virus porcine reproductive and respiratory syndrome (PRRS) genotype 1 vaccine in pregnant sows at various stages of gestation under field conditions. A total of 505 sows and gilts were allocated to two treatment groups and maintained in separate facilities. Animals of group 1 were vaccinated with a commercial modified live genotype 1 PRRSV vaccine (control product, CP), while animals of group 2 were immunized with a new modified live genotype 1 PRRSV vaccine (investigational veterinary product, IVP) (ReproCyc® PRRS EU, Boehringer Ingelheim Vetmedica GmbH)...
July 19, 2016: Vaccine
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