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Drugs in R&D

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https://www.readbyqxmd.com/read/29214385/sealing-effects-on-the-storage-stability-of-the-cyanide-antidotal-candidate-dimethyl-trisulfide
#1
Lóránd Kiss, Anna Duke, Kristof Kovacs, Tibor Barcza, Márton Kiss, Ilona Petrikovics, David E Thompson
BACKGROUND: Dimethyl trisulfide (DMTS) is a highly lipid-soluble cyanide (CN) antidote candidate molecule. In prior studies with various US FDA-approved co-solvents, surfactants, and their combinations, aqueous solutions containing 15% polysorbate 80 (Poly80) were found to effectively solubilize DMTS in formulations for intramuscular administration. However, DMTS formulated in 15% aqueous Poly80 solutions showed gradual losses over time when stored in vials with septum-based seals. OBJECTIVE: The present study tested whether storing DMTS formulations in hermetically sealed glass ampules could mitigate storage losses...
December 6, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/29209910/efficacy-and-safety-of-nintedanib-for-the-treatment-of-idiopathic-pulmonary-fibrosis-an-update
#2
José Antonio Rodríguez-Portal
Idiopathic pulmonary fibrosis is a fatal form of progressive fibrosing interstitial pneumonia with limited treatment options. In recent years, its management has been transformed with the approval of two new antifibrotic drugs: nintedanib and pirfenidone. Nintedanib is a tyrosine kinase inhibitor that efficiently slows idiopathic pulmonary fibrosis progression and has an acceptable tolerability profile. This article reviews new available evidence on the long-term efficacy and safety of nintedanib in patients with idiopathic pulmonary fibrosis...
December 5, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/29177587/intranasal-therapy-to-stop-status-epilepticus-in-prehospital-settings
#3
REVIEW
John Benfield, Alberto Musto
Status epilepticus (SE) is a medical emergency characterized by uncontrolled, prolonged seizures with rapid and widespread neuronal damage. Patients that suffer from longer episodes of SE are more likely to have poorer clinical outcomes and a higher cost of healthcare. Understanding novel molecular mechanisms that regulate inhibitory and excitatory neurotransmission that initiate SE and the necessary medical infrastructure to stop SE could help identify targets for early intervention. Intranasal administration of benzodiazepines may shorten the time between initiation and cessation of seizures when compared to other routes of administration...
November 25, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/29168127/bioavailability-of-orally-administered-des-aspartate-angiotensin-i-in-human-subjects
#4
Kok-Onn Lee, Edmund Feng Tian, Martin Hui Cai, Hong Wang, Yiong-Huak Chan, Meng-Kwoon Sim
In an earlier single-dose escalation study to evaluate the safety and pharmacokinetics of orally administered des-aspartate-angiotensin I (DAA-I) in healthy subjects, the plasma level of DAA-I could not be determined because DAA-I is rapidly degraded in the circulation. The present study investigated the oral bioavailability of DAA-I by measuring the prostaglandin E2 metabolite (PGEM) in the plasma samples of the same trial. PGEM is a stable derivative of PGE2, which has been shown to be a biomarker of DAA-I...
November 22, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/29103081/a-randomized-multiple-dose-pharmacokinetic-study-of-a-novel-pde10a-inhibitor-tak-063-in-subjects-with-stable-schizophrenia-and-japanese-subjects-and-modeling-of-exposure-relationships-to-adverse-events
#5
Paul Goldsmith, John Affinito, Maggie McCue, Max Tsai, Stefan Roepcke, Jinhui Xie, Lev Gertsik, Thomas A Macek
BACKGROUND: Phosphodiesterase 10A (PDE10A) is selectively expressed in medium spiny neurons of the striatum. TAK-063 is a selective inhibitor of PDE10A in clinical development for the treatment of schizophrenia. OBJECTIVES: Safety, tolerability, and pharmacokinetics (PK) of TAK-063 were evaluated following multiple rising oral doses, and PK/adverse event (AE) models were developed to characterize the relationship between TAK-063 exposure and incidence of specific AEs...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/29076037/the-adherence-rate-threshold-is-drug-specific
#6
Melissa E Stauffer, Paul Hutson, Anna S Kaufman, Alan Morrison
INTRODUCTION: Patient adherence to a medication regimen is usually expressed as an adherence rate, defined as the proportion of prescribed doses actually taken. An adherence rate threshold, above which the therapeutic effect is maintained, is typically assigned an arbitrary value, commonly 0.8. OBJECTIVE: Here, we determined the value of the adherence rate threshold objectively in different drugs of the same class, using statins as an example. METHODS: We used pharmacokinetic/pharmacodynamic (PK/PD) modeling to predict serum levels of low-density lipoprotein cholesterol (LDL-C) in patients taking simvastatin 20 mg or atorvastatin 5 mg once daily for 30 days...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/29058304/serious-adverse-events-among-sprint-trial-participants-taking-statins-at-baseline
#7
Marco D Huesch
BACKGROUND: Real-world evidence of statin side effects is potentially biased because statin use is neither randomized nor unblinded. An innovative study design can mitigate these biases. For example, in the recent ASCOT-LLA trial, patient-reported adverse events such as muscle pain and weakness were higher in the non-randomized and non-blinded setting than in the randomized, blinded setting. Less optimally, secondary re-analysis of clinical trials in which statin use is recorded and in which serious adverse events (SAEs) are adjudicated may be conducted...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/29058303/transmucosal-delivery-of-nicotine-in-combination-with-tincture-of-benzoin-inhibits-apoptosis
#8
Alex Battaglia, Thanh Nguyen
BACKGROUND AND OBJECTIVE: The aim of this study was to test the hypothesis that tincture of benzoin (TOB) facilitates immediate transmucosal nicotine absorption while simultaneously promoting a safe and sustained delivery of the nicotine. METHODS: In combination with TOB, nicotine toxicity and diffusion across human mucosal cells were measured using a 3-D human mucosal tissue model. RESULTS: Nicotine was delivered 2.1 times more quickly in combination with TOB than in combination with saline (p < 0...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/29058302/switching-between-biological-treatments-in-psoriatic-arthritis-a-review-of-the-evidence
#9
REVIEW
Luisa Costa, Carlo Perricone, Maria Sole Chimenti, Antonio Del Puente, Paolo Caso, Rosario Peluso, Paolo Bottiglieri, Raffaele Scarpa, Francesco Caso
Psoriatic arthritis (PsA) is a chronic inflammatory arthropathy. Therapy with anti-tumor necrosis factor (TNF)-α agents represents the first therapeutic choice for moderate and severe forms; however, PsA patients can experience anti-TNFα failure, lack of efficacy, or adverse events. Several evidences exist on the effectiveness of switching among different TNFα inhibitors, and we reviewed the published data on the effectiveness of anti-TNFα first-, second- and third-line. Most of the studies report that the main reason for switching to a second anti-TNFα agent is represented by lack of efficacy (primary or secondary) and, more rarely, adverse events...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28905271/pharmacokinetics-of-a-new-oral-vitamin-d-receptor-activator-2-methylene-19-nor-20s-1%C3%AE-25-dihydroxyvitamin-d3-in-patients-with-chronic-kidney-disease-and-secondary-hyperparathyroidism-on-hemodialysis
#10
Richa Pandey, Julia B Zella, Jinge G Zhu, Lori A Plum, Margaret Clagett-Dame, William J Blaser, Wendy Bedale, Hector F DeLuca, Daniel W Coyne
BACKGROUND: 2-Methylene-19-nor-(20S)-1α,25-dihydroxyvitamin D3 (DP001 or 2MD) is a novel, potent 1α-hydroxylated vitamin D analog that binds to the vitamin D receptor and suppresses parathyroid hormone synthesis and secretion with potential for an improved safety profile compared to existing active vitamin D analogs. The purpose of this study was to evaluate the pharmacokinetics of DP001 given orally after hemodialysis. METHODS: DP001 (550 ng) was given orally to 11 hemodialysis patients with secondary hyperparathyroidism after each dialysis session (3 times/week) for 4 weeks...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28895069/feasibility-safety-and-efficacy-of-an-alternative-schedule-of-sunitinib-for-the-treatment-of-patients-with-metastatic-renal-cell-carcinoma-a-retrospective-study
#11
Sebastiano Buti, Maddalena Donini, Melissa Bersanelli, Alessia Gattara, Francesco Leonardi, Rodolfo Passalacqua
BACKGROUND: Standard treatment with sunitinib for patients with metastatic renal cancer provides an 'on-off' schedule (daily administration of a 50-mg capsule for 4 weeks, followed by a 2-week break; consecutive 6-week cycles). We developed an alternative intermittent schedule to reduce the toxicity and symptoms of tumor regrowth during the rest period and to allow prolonged continuation of therapy, maintaining dose intensity. OBJECTIVE: The objective of this study was to provide a retrospective evaluation of the feasibility, safety, and efficacy of an alternative schedule of sunitinib in patients who did not tolerate classical treatment...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28879645/pharmacokinetic-effects-of-antidrug-antibodies-occurring-in-healthy-subjects-after-a-single-dose-of-intravenous-infliximab
#12
Eli D Ehrenpreis
BACKGROUND: Infliximab pharmacokinetic studies have been performed in patients receiving chronic infliximab therapy. In these patients, infliximab antidrug antibodies (ADAs) increase infliximab clearance and decrease serum levels and drug efficacy. OBJECTIVE: This study analyzed the pharmacokinetic effect of infliximab ADAs in healthy subjects receiving a single dose of intravenous infliximab. METHODS: Data were obtained from a single-blind, parallel-group, single-dose study of healthy subjects receiving 5 mg/kg of intravenous SB2 (infliximab biosimilar), EU-sourced Remicade (EU-IFX) or US-sourced Remicade (US-IFX)...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28879638/impact-of-etoposide-on-brca1-expression-in-various-breast-cancer-cell-lines
#13
Xi Zhang, Simone Hofmann, Nadia Harbeck, Udo Jeschke, Sophie Sixou
Breast cancer 1 (BRCA1), as a tumor suppressor, exerts an effective influence on protecting DNA integrity to suppress the development of breast cancer (BC). BRCA1 expression is induced in response to DNA-damaging agents such as etoposide. Germline BRCA1 gene mutations are associated with development of hereditary BC. However, besides BRCA-mutated BCs, some sporadic cancers may also exhibit a BRCA-like phenotype, displaying so-called 'BRCAness'. This common phenotype may respond to similar therapeutic approaches as BRCA-mutated tumors and may thus have important implications for the clinical management of these cancers...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28879584/adverse-event-profile-of-pyrimethamine-based-therapy-in-toxoplasmosis-a-systematic-review
#14
REVIEW
Ruben R Ben-Harari, Elizabeth Goodwin, Julio Casoy
INTRODUCTION: Approximately a third of the population worldwide is chronically infected with Toxoplasma gondii. Pyrimethamine-based regimens are recommended for the treatment of toxoplasmosis. OBJECTIVE: The aim was to evaluate the safety profile of pyrimethamine-based treatment for the three main Toxoplasma manifestations: toxoplasmic encephalitis (TE), ocular toxoplasmosis, and congenital toxoplasmosis. METHODS: PubMed, Cochrane Library, and Google Scholar databases were searched through August 1, 2016...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28875397/boceprevir-and-antiretroviral-pharmacokinetic-interactions-in-hiv-hcv-co-infected-persons-aids-clinical-trials-group-study-a5309s
#15
Jennifer J Kiser, Darlene Lu, Susan L Rosenkranz, Gene D Morse, Robin DiFrancesco, Kenneth E Sherman, Adeel A Butt
OBJECTIVE: The objective of this study was to determine the magnitude of drug interactions between the hepatitis C virus (HCV) protease inhibitor boceprevir (BOC) and antiretroviral (ARV) agents in persons with HIV/HCV co-infection. METHODS: Participants taking two nucleos(t)ide analogs with either efavirenz, raltegravir, or ritonavir-boosted atazanavir, darunavir, or lopinavir underwent intensive pharmacokinetic (PK) sampling for ARV 2 weeks before (week 2) and 2 weeks after initiating BOC (week 6) and for BOC at week 6...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28865038/benzodiazepines-and-z-drugs-an-updated-review-of-major-adverse-outcomes-reported-on-in-epidemiologic-research
#16
REVIEW
Jaden Brandt, Christine Leong
Various adverse events resulting from, or associated with, benzodiazepine and/or Z-drug use have been extensively reported on and discussed in great detail within the biomedical literature. It is widely accepted that motor vehicle accidents and falls leading to fractures in older adults are major adverse events that have been shown to occur more frequently in users of sedative-hypnotic medication, especially of the benzodiazepine and related Z-drug variety. However, the last few years have seen increasing reports in the literature raising the issue of benzodiazepine and Z-drug exposure in the development of other serious medical issues including dementia, infections, respiratory disease exacerbation, pancreatitis, and cancer...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28828595/the-egfr-inhibitor-gefitinib-enhanced-the-response-of-human-oral-squamous-cell-carcinoma-to-cisplatin-in-vitro
#17
Ashraf Khalil, Mark J Jameson
INTRODUCTION: The epidermal growth factor receptor (EGFR) is highly expressed in a variety of solid tumors including oral cavity squamous cell carcinoma (OSCC) and has been implicated in the resistance of these tumors to cisplatin. This study was performed to determine if the EGFR tyrosine kinase inhibitor gefitinib could enhance the cytotoxic effect of cisplatin on OSCC cells in vitro. METHODS: The expression of EGFR and the phosphorylation of its downstream signaling to ERK, and AKT pathway were detected by Western blotting...
December 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28905245/identification-of-polymorphic-forms-of-active-pharmaceutical-ingredient-in-low-concentration-dry-powder-formulations-by-synchrotron-x-ray-powder-diffraction
#18
Kenji Egusa, Fumiaki Okazaki, Joerg Schiewe, Ulrike Werthmann, Markus Wolkenhauer
BACKGROUND: The identification of different (pseudo) polymorphs of an active pharmaceutical ingredient in dry powder formulations is of importance during development and entire product lifecycle, e.g., quality control. Whereas determination of polymorphic differences of pure substances is rather easy, in dry powder formulations, it is generally difficult and the difficulties increase particularly, if the substance of interest is present only in low concentrations in the formulation. Such a formulation is Spiriva(®) inhalation powder (Boehringer Ingelheim), which contains only 0...
September 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28831752/longitudinal-assessment-of-the-effect-of-atrasentan-on-thoracic-bioimpedance-in-diabetic-nephropathy-a-randomized-double-blind-placebo-controlled-trial
#19
David J Webb, Blai Coll, Hiddo J L Heerspink, Dennis Andress, Yili Pritchett, John J Brennan, Mark Houser, Ricardo Correa-Rotter, Donald Kohan, Hirofumi Makino, Vlado Perkovic, Giuseppe Remuzzi, Sheldon W Tobe, Robert Toto, Robert Busch, Pablo Pergola, Hans-Henrik Parving, Dick de Zeeuw
BACKGROUND: Fluid retention is a common adverse event in patients who receive endothelin (ET) receptor antagonist therapy, including the highly selective ETA receptor antagonist, atrasentan. OBJECTIVE: We performed longitudinal assessments of thoracic bioimpedance in patients with type 2 diabetes mellitus and nephropathy to determine whether a decrease in bioimpedance accurately reflected fluid retention during treatment with atrasentan. STUDY DESIGN: We conducted a randomized, double-blind, placebo-controlled study in 48 patients with type 2 diabetes mellitus and nephropathy who were receiving stable doses of renin angiotensin system inhibitors and diuretics...
September 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28815425/methodological-study-of-vancomycin-dosing-in-elderly-patients-using-actual-serum-creatinine-versus-rounded-serum-creatinine
#20
Tramaine Young, Matt Daniel, Stephanie Baumhover, Duke Eidson, Jane Green
PURPOSE: The practice of intentional rounding up of serum creatinine (SCr) in elderly patients with low measured values can lead to an underestimation of creatinine clearance and subsequent inaccurate dosing of medications. Thus, the purpose of this study was to evaluate the accuracy of vancomycin dose calculations for patients aged ≥65 years using an SCr rounded up to 1 mg/dL versus actual SCr. METHODS: This study compared the difference between measured steady-state vancomycin trough concentrations with predicted trough concentrations that have been calculated using rounded SCr and actual SCr...
September 2017: Drugs in R&D
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