This is the RSS news feed of one of our preset news channels on LSIS - The Life Science Infromation Service. Please visit us to find a current view of this one and many more channels via our alerting push services: http://www.lsis.com/channels/?query=100 http://www.lsis.com/goto/r100/rss 2012-02-05T11:11:03+01:00 text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Cytokines are key regulatory molecules that serve as critical mediators of cell-to-cell communication. They play a central role in immune function and are important molecular targets for drug discovery because of their dysregulation in immune disease. Initial attempts to develop agents that block the actions of cytokines focused on identifying small-molecule antagonists that would directly compete with these cytokines for their cognate receptors. These efforts were, for the most part, (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 A one-step conversion of ketones into N-acetyl enamides was developed. The process employs safe and inexpensive reagents, proceeds under mild conditions, and tolerates diverse functional groups. The addition of edte (N,N,N',N'-tetrakis(2-hydroxyethyl)ethylenediamine) prior to workup enables water solubilization of Ti alkoxides and allows a simple extractive workup. |-| Angew Chem Int Ed Engl. |-| Reeves JT, Tan Z, Han ZS, Li G, Zhang Y, Xu Y, Reeves DC, Gonnella NC, Ma S, Lee H, Lu BZ, (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 With the publication of the quality guideline ICH Q9 "Quality Risk Management" by the International Conference on Harmonization, risk management has already become a standard requirement during the life cycle of a pharmaceutical product. Failure mode and effect analysis (FMEA) is a powerful risk analysis tool that has been used for decades in mechanical and electrical industries. However, the adaptation of the FMEA methodology to biopharmaceutical processes brings about some difficulties. The (…) text/html http://www.uspto.gov/ USPTO http://www.lsis.com/channels/?query=100 United States Patent: 8106060 |-| Title: 8-(3-amino-piperidin-1-yl)-xanthines, their preparation, and their use as pharmaceuticals |-| Inventors: Pfrengle; Waldemar (Biberach, DE), Sieger; Peter (Mittelbiberach, DE) |-| Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE) |-| The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof. text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Aims - Sodium glucose cotransporter-2 (SGLT-2) is key to reabsorption of glucose in the kidney. SGLT-2 inhibitors are in clinical development for treatment of type 2 diabetes mellitus (T2DM). The mechanism may be of value also in the treatment of type 1 diabetes mellitus (T1DM). This study investigated effects of the SGLT-2 inhibitor empagliflozin, alone and in combination with insulin, on glucose homeostasis in an animal model of T1DM. Materials and Methods - Sprague-Dawley rats were (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 The apparent diffusion coefficient (ADC) of hyperpolarized (HP) gases is a parameter that reflects changes in lung microstructure. However, ADC is dependent on many physiological and experimental variables that need to be controlled or specified in order to ensure the reliability and reproducibility of this parameter. A single breath-hold experiment is desirable in order to reduce the amount of consumed HP gas. The application of a positive end-expiratory pressure (PEEP) causes an increase in (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 In clinical development, thorough QT interval/corrected QT interval (QT/QTc) studies are performed to demonstrate that new investigational drugs do not change cardiac repolarization. In addition to the analysis recommended by ICH E14, exposure-response modeling has recently gained increased scientific attention. A direct concentration-QTc relationship is usually assumed with this pharmacokinetics (PK) QT analysis. Consequently, unconsidered effect delays might lead to severe bias in (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 PURPOSE: Dabigatran etexilate is an oral, reversible, direct thrombin inhibitor licensed for the prevention of venous thromboembolism and stroke prevention in patients with atrial fibrillation. The aim of this study was to investigate whether, and to what extent, a switch from enoxparin to dabigatran etexilate affects the pharmacokinetic (PK) and pharmacodynamic (PD) parameters and safety profile of dabigatran. (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Restless legs syndrome (RLS) affects approximately 10-15% of the general population and has deleterious effects on sleep and subsequent daytime performance. The disorder may also give rise to long-term complications such as psychological distress and diminished quality of life. The condition is often unrecognized or misdiagnosed, and the magnitude of the effects of RLS on the sizeable proportion of undiagnosed (and therefore untreated) individuals has not previously been evaluated. |-| (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Vet Rec. |-| Johnston L, Narbe R. |-| IPL, Boehringer Ingelheim, Ingelheim, Germany. text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Aims: To assess the safety and tolerability of the dipeptidyl peptidase-4 inhibitor linagliptin in patients with type 2 diabetes. Methods: Data were pooled from eight randomized, double-blind, placebo-controlled Phase III clinical trials lasting ?24 weeks. Incidences were calculated with descriptive statistics for the overall population and for subgroups of elderly and renally impaired patients. Results: 2523 patients received linagliptin 5 mg once daily and 1049 patients received placebo. (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 INGELHEIM, Germany-(BUSINESS WIRE)-FOR NON-US MEDIA ONLY Boehringer Ingelheim announced today the initiation of two phase III clinical trials, LUX-Head & Neck 1 and LUX-Head & Neck 2. These trials evaluate afatinib* in patients with metastatic and recurrent head and neck cancer, and in patients with locally advanced disease, respectively. text/html http://www.sciencedaily.com ScienceDaily http://www.lsis.com/channels/?query=100 ScienceDaily (Jan. 12, 2012) A team of researchers at the California Institute of Technology (Caltech) has devised a new method for making complex molecules. The reaction they have come up with should enable chemists to synthesize new varieties of a whole subclass of organic compounds called nitrogen-containing heterocycles, thus opening up new avenues for the development of novel pharmaceuticals and natural products ranging from chemotherapeutic compounds to bioactive plant materials such as (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 Pfizer Inc. and Bristol-Myers Squibb Co. s blood-thinner apixaban won a final recommendation from the U.K. s health-cost agency. The pill, also known by the brand name Eliquis, may be used to prevent blood clots in adults who have undergone hip or knee replacement surgery, the National Institute for Health and Clinical Excellence said in a statement today. The agency, known as NICE, advises the state-run National Health Service on which treatments represent value for money. Almost 120,000 hip (…) text/html http://www.sciencedaily.com ScienceDaily http://www.lsis.com/channels/?query=100 ScienceDaily (Jan. 24, 2012) The many factors that contribute to how cells communicate and function at the most basic level are still not fully understood, but researchers at Baylor College of Medicine have uncovered a mechanism that helps explain how intracellular membranes fuse, and in the process, created a new physiological membrane fusion model. See Also: Health & Medicine Human Biology Bone and Spine Healthy Aging Plants & Animals Cell Biology Molecular Biology Biology Reference Cell (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 FORT LAUDERDALE, FL-(Marketwire - January 24, 2012) - QUMAS, the leading provider of compliance solutions to highly regulated companies, today kicked off its Worldwide User Conference, QUMAS Connect 2012 in Fort Lauderdale, Florida. The two-day event will feature 17 sessions on a wide variety of key compliance topics including Cloud Computing, Collaboration Trends with Business Partners, and leveraging Microsoft SharePoint 2010 as a Compliance Platform. Featured speakers at QUMAS Connect 2012 (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 Munich and Ingelheim, Germany, January 24, 2012 / B3C newswire / Priaxon, utilizing its proprietory PriaXplore platform for small molecule drug discovery, and Boehringer Ingelheim will prolongate their research and development collaboration on mdm2/p53 inhibitors for the treatment of cancer. The companies will continue working jointly to identify and advance drug candidates into pre-clinical development. Thereafter, Boehringer Ingelheim will drive the development and commercialisation of the (…) text/html http://www.uspto.gov/ USPTO http://www.lsis.com/channels/?query=100 United States Patent: 8101765 |-| Title: Process for preparing acyclic HCV protease inhibitors |-| Inventors: Busacca; Carl Alan (Poughkeepsie, NY), Frutos; Rogelio Perez (Sandy Hook, CT), Haddad; Nizar (Danbury, CT), Kapadia; Suresh R. (Danbury, CT), Lorenz; Jon Charles (New Milford, CT), Saha; Anjan (Hamden, CT), Senanayake; Chris Hugh (Brookfield, CT), Wei; Xudong (Ridgefield, CT) |-| Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE) |-| Disclosed are highly (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 The post-trial access to investigational drugs has been the object of discussion since the late 1980s at least, initially linked to trials carried out in acquired immunodeficiency syndrome and, particularly, in developing countries, where the concern with patient vulnerability is more important. National and international guidelines do mention the subject; however, the complexity of the issue is not easily addressed and usually requires additional and specific discussions. The decision on (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Introduction.? Hypoactive Sexual Desire Disorder (HSDD) is the most common form of Female Sexual Dysfunction and is characterized by low sexual desire that causes distress. Aim.? The aim of this study was to assess the efficacy and safety of flibanserin, a postsynaptic 5-HT(1A) agonist/5-HT(2A) antagonist, in premenopausal women with HSDD. Methods.? North American premenopausal women with HSDD were randomized to 24 weeks' treatment with placebo (N?=?295), flibanserin 50?mg (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Aim:? To investigate whether hepatic impairment affects linagliptin pharmacokinetics, pharmacodynamics and tolerability. Methods:? This open-label, parallel-group, single-centre study enrolled patients with mild (n= 8), moderate (n= 9) or severe (n= 8) hepatic impairment and healthy subjects (n= 8). Groups were matched with regard to age, weight, and sex. Primary endpoints were linagliptin exposure following 5-mg linagliptin once daily for 7 days in patients with mild and moderate hepatic (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Stroke prevention with appropriate thromboprophylaxis still remains central to the management of atrial fibrillation (AF). Nonetheless, stroke risk in AF is not homogeneous, but despite stroke risk in AF being a continuum, prior stroke risk stratification schema have been used to 'artificially' categorise patients into low, moderate and high risk stroke strata, so that the patients at highest risk can be identified for warfarin therapy. Data from recent large cohort studies show that by being (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Donepezil is the current standard symptomatic treatment of mild-to-moderate Alzheimer's disease (AD) patients. It aims to compensate for the deficit in cholinergic neurotransmission by blocking acetylcholinesterase (AChE) and thus increases the concentration of extracellular acetylcholine. However, experience from clinical practice demonstrated that AChE inhibitors only have moderate treatment effects. As a potential new approach for memory enhancement, inhibition of specific (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 This article provides an overview of (i) the risk of stroke associated with vascular disease (acute coronary syndromes and peripheral artery disease) in patients with atrial fibrillation, (ii) the frequent coexistence of vascular disease in patients with atrial fibrillation and, (iii) the cardiovascular risk associated with the coexisting of the two diseases. The literature on this topic is relatively sparse, and we discuss results from both clinical trials and observational studies. There is (…) text/html http://www.uspto.gov/ USPTO http://www.lsis.com/channels/?query=100 United States Patent: 8096971 |-| Title: Dual chamber container for lyophilization, process for the filling up and use thereof |-| Inventors: Bassarab; Stefan (Biberach, DE), Bauer; Alexander (Biberach, DE), Denkinger; Nicole (Biberach, DE), Garidel; Patrick (Norderstedt, DE), Hemminger; Markus (Biberach, DE), Kern; Hans-Joachim (Mittelbiberach, DE), Langer; Andreas (Maselheim, DE), Presser; Ingo (Biberach, DE) |-| Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE) |-| (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Introduction.? Little is known about Hypoactive Sexual Desire Disorder (HSDD) in men. Aim.? To provide the first comprehensive characterization of men diagnosed with HSDD (Diagnostic and Statistical Manual of Mental Disorders, 4th Edition, Text Revision [DSM-IV-TR]) using established patient-reported outcomes (PROs) and new PROs developed in line with U.S. Food and Drug Administration (U.S. FDA) guidance. Methods.? This 4-week non-treatment study recruited men (N?=?200) with or (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Introduction.? Hypoactive Sexual Desire Disorder (HSDD) is characterized by low sexual desire that causes marked distress or interpersonal difficulty. Aim.? To assess the efficacy and tolerability of flibanserin, a postsynaptic 5-HT1A agonist/5-HT2A antagonist, in the treatment of premenopausal women with HSDD. Methods.? North American premenopausal women with HSDD (mean age 35?years) were randomized to 24?weeks' treatment with flibanserin 25?mg twice daily (N?=?396), 50?mg (…) text/html http://www.sciencedaily.com ScienceDaily http://www.lsis.com/channels/?query=100 ScienceDaily (Jan. 12, 2012) Investigators in the Massachusetts General Hospital (MGH) Center for Systems Biology have discovered a previously unknown type of immune cell, a B cell that can produce the important growth factor GM-CSF, which stimulates many other immune cells. They also found that these novel cells may help protect against the overwhelming, life-threatening immune reaction known as sepsis. See Also: Health & Medicine Immune System Lymphoma Stem Cells Brain Tumor Nervous System (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 The objective of the present study was to determine if the European porcine reproductive and respiratory syndrome virus (PRRSV) can be transmitted via spiked semen to preimmunized sows and induce reproductive failure. Sows were immunized with the North American PRRSV-based modified live vaccine (Ingelvac PRRS MLV, Boehringer Ingelheim Animal Health, St. Joseph, MO, USA) and were artificially inseminated. The sows were randomly divided into three groups. The vaccinated (group 2) and (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 GHENT, BELGIUM-(Marketwire - January 10, 2012) - GHENT, Belgium, 10 January 2012 - Ablynx [Euronext Brussels: ABLX] today announced that it has been granted an extended Certificate of Good Manufacturing Practice (GMP) from the Federal Agency for Medicines and Health Products (FAMHP) in Belgium for its new GMP unit at its headquarters in Ghent, after having been inspected in November 2011. Having received this accreditation, Ablynx's GMP unit will now perform release- testing on Drug Substance (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 HAMBURG, Germany, Jan. 11, 2012 (GLOBE NEWSWIRE) - Evotec AG (Frankfurt:EVT) (TecDAX) today announced that its research alliance with Boehringer Ingelheim has achieved a milestone triggering a payment of ¬ 2.5 million to Evotec. The milestone was achieved for the identification and selection of a compound to be advanced into extended profiling prior to pre-clinical development within an oncology programme. This is the fourth milestone achieved in 2011 and represents a total of ¬ 10.5 (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 The objective of the present study was to assess the suitability of an accurate, sensitive, standardized, chronometric blood coagulation test to determine the anticoagulation activity of dabigatran and to quantify concentrations of dabigatran in plasma. Dabigatran was spiked at increasing concentrations in pooled citrated normal human plasma to measure diluted thrombin time with the HEMOCLOT THROMBIN INHIBITOR assay. Calibration curve linearity, inter-assay and intra-assay precision, and assay (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 Boehringer Ingelheim GmbH s anti- coagulant Pradaxa increases a patient s risk of heart attack or severe chest pain, according to a review of studies conducted on the drug. An analysis of seven clinical trials found that it was œsignificantly associated with a higher risk  of heart attacks and acute coronary syndrome, or ACS, a designation that includes heart attacks and chest pain, researchers wrote in a report published today in the Archives of Internal Medicine. The potential risk of (…) text/html http://www.uspto.gov/ USPTO http://www.lsis.com/channels/?query=100 United States Patent: 8093266 |-| Title: Rho kinase inhibitors |-| Inventors: Dahmann; Georg (Attenweiler, DE), Hickey; Eugene Richard (Danbury, CT), Li; Xiang (Danbury, CT), Mao; Wang (Milford, CT), Marshall; Daniel R. (Sandy Hook, CT), Morwick; Tina M. (New Milford, CT), Sibley; Robert (North Haven, CT), Snow; Roger John (Danbury, CT), Sorcek; Ronald J. (Bethel, CT), Wu; Frank (Ridgefield, CT), Young; Erick Richard Roush (Danbury, CT) |-| Assignee: Boehringer Ingelheim International GmbH (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 CHICAGO, Illinois, January 9, 2012 - Only 10% of molecules that enter Phase II will reach market, according to recent analysis by the Pharmaceutical Benchmarking Forum (PBF). And that is on top of growing attrition rates in earlier phases for preclinical and initial human studies that make the overall challenge of bringing drugs through Development even greater. This analysis is based on very detailed data from the PBF - which consists of the leading pharmaceutical companies - and offers the (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 There is an increasing demand for quantitative data on metabolite exposure triggered by regulatory guidances. This contribution describes the accuracy of nanoelectrospray ionization mass spectrometry response of drug compounds and their metabolites from biological matrices compared with radiometric quantification. This is a comprehensive investigation of a set of real-life pharmaceutical compounds in relevant matrices such as urine, bile, feces and plasma. The data suggest that (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 A wide range of polymorphisms have been reported in muscarinic receptor subtype genes, mostly in M(1) and M(2) and, to a lesser extent, M(3) receptors. Most studies linking such genetic variability to phenotype have been performed for brain functions, but a more limited amount of information is also available for cardiac and airway function. Unfortunately, for none of the phenotypes under investigation a robust association with genotype has emerged. Moreover, it remains mostly unclear whether (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 WATERTOWN, Mass.-(BUSINESS WIRE)- FORMA Therapeutics announced today that the Company has entered into a research and development collaboration with Boehringer Ingelheim to discover and develop novel drug candidates for the treatment of cancer. The agreement will focus on discovering small molecule drugs against oncology-relevant protein-protein interactions. Under the terms of the collaboration, FORMA will receive a total of $65 million in up-front payments and research funding to screen (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 J Thromb Haemost. |-| Liesenfeld KH, Lehr T, Dansirikul C, Reilly PA, Connolly SJ, Ezekowitz MD, Yusuf S, Wallentin L, Haertter S, Staab A. |-| Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach, Germany Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT, USA Population Health Research Institute, McMaster University, Hamilton, ON, Canada Lankenau Institute for Medical Research and the Heart Center, Wynnewood, PA, USA Uppsala Clinical (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Sodium-dependent sugar transporters (SGLT) actively catalyse carbohydrate transport across cellular membranes. Six of the 12 known SGLT family members have the capacity to bind and/or transport monosaccharides (SGLT-1 to 6); of these, all but SGLT-5 have been characterised. Here we demonstrate that human SGLT-5 is exclusively expressed in the kidney. Four splice variants were detected and the most abundant SGLT-5-mRNA was functionally characterised. SGLT-5 mediates sodium-dependent (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 GHENT, BELGIUM-(Marketwire - January 04, 2012) - Ablynx [Euronext Brussels: ABLX] today announced that it plans to webcast its corporate presentation at the 30(th) Annual J.P. Morgan Healthcare Conference on Wednesday, 11 January 2012 at 03:30 p.m. PST / 00:30 a.m. CET. The presentation, followed by a Q&A, will be hosted by Dr Edwin Moses, CEO and Chairman of Ablynx. The presentation will be webcast live and may be accessed on the home page of the Ablynx website at www.ablynx.com. Shortly (…) text/html http://www.uspto.gov/ USPTO http://www.lsis.com/channels/?query=100 United States Patent: 8088769 |-| Title: Cyanopyrimidinones |-| Inventors: Hendrix; Martin (Odenthal, DE), Barfacker; Lars (Oberhausen, DE), Heckroth; Heike (Odenthal, DE), Karthaus; Dagmar (Solingen, DE), Tersteegen; Adrian (Wuppertal, DE) |-| Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE) |-| The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 PURPOSE: To investigate the pharmacokinetics, metabolism and tolerability of afatinib (BIBW 2992), an oral irreversible ErbB family blocker, in healthy male volunteers. METHODS: In this open-label, single-center study, 8 healthy male volunteers received a single oral dose of 15 mg [(14)C]-radiolabeled afatinib (equivalent to 22.2 mg of the dimaleinate salt) as a solution. Blood, urine and fecal samples were (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Linagliptin is a selective, competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, recently approved in the USA, Japan and Europe for the treatment of type 2 diabetes. It has non-linear pharmacokinetics and, unlike other DPP-4 inhibitors, a largely non-renal excretion route. It was hypothesised that P-glycoprotein (P-gp)-mediated intestinal transport could influence linagliptin bioavailability, and might contribute to its elimination. Two studies evaluated the role of P-gp-mediated transport in (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Ethnic differences in drug disposition may potentially influence therapeutic response to dabigatran, a reversible direct thrombin inhibitor used for the prevention and/or treatment of various thromboembolic disorders. This analysis of data from 18 clinical studies in healthy volunteers and patients with non-valvular atrial fibrillation (AF) or undergoing knee or hip arthroplasty investigated whether there were any clinically relevant differences in the pharmacokinetics and pharmacodynamics of (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 The National Institute for Health and Clinical Excellence (NICE) invited Boehringer Ingelheim GmbH, the manufacturer of dabigatran etexilate (DBG), to submit evidence on the clinical and cost effectiveness of this drug for the primary prevention of venous thromboembolism (VTE) in adult patients who have undergone total hip replacement (THR) or total knee replacement (TKR) surgery, as part of NICE's single technology appraisal process. The comparators were enoxaparin and fondaparinux, as (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 This contribution describes the combination of whole body autoradiography with liquid extraction surface analysis (LESA) and mass spectrometry (MS) to study the distribution of the tachykinin NK(1) antagonist figopitant and its metabolites in tissue sections of rats after intravenous administration of 5.0 mg/kg figopitant. An overview of autoradiography results is presented together with mass spectrometric identification and semi-quantification of parent drug and its metabolites based on (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 ABSTRACT: The strategic integration of in vivo cardiovascular models is important during lead optimization (LO) to enable a wide therapeutic-index for cardiovascular safety. However, under what conditions (e.g. species, route-of-administration, anesthesia) studies should be performed to drive go/no-go is open to interpretation. Two compounds, torcetrapib and a novel steroid-hormone mimetic (SHM-1121X), both with off-target cardiovascular liabilities, were profiled in four in vivo (…) text/html http://www.biospace.com BioSpace http://www.lsis.com/channels/?query=100 December 17, 2011 - Simcere will develop a cardiovascular molecule with Bristol-Myers Squibb; China Sky One Medical and three partners will invest $36.3 million to create a stem cell company; ICON acquired a China clinical-stage CRO, BeijingWits Medical Consulting; Jilin Aodong Medicine put a hold on its $25 million Vital Therapies investment; Boehringer Ingelheim announced a $91 million expansion of its Shanghai manufacturing facility; Pfizer executives said the company has a two-fold R&D (…) text/html http://www.ncbi.nlm.nih.gov NCBI PubMed http://www.lsis.com/channels/?query=100 Aim: The aim was to assess the performance of the Visual Analogue Scale (VAS) in patients recruited in a clinical trial with over the counter analgesics in headache.Methods: The Thomapyrin Study showed the significant superiority of the fixed combination of acetylsalicylic acid + paracetamol + caffeine over the combination without caffeine, the single preparations, and placebo in the treatment of headache. Patients enrolled into the study were trained in the handling of the VAS by naming (…)