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Drugs in R&D

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https://www.readbyqxmd.com/read/29737467/correction-to-the-many-faces-of-apomorphine-lessons-from-the-past-and-challenges-for-the-future
#1
Manon Auffret, Sophie Drapier, Marc Vérin
In the original publication, the name of the author in T.
May 8, 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29671128/a-phase-i-study-of-the-pharmacokinetics-and-pharmacodynamics-of-intranasal-doxylamine-in-subjects-with-chronic-intermittent-sleep-impairment
#2
Mark Allison, Cecilia Hale
INTRODUCTION: Doxylamine tablets are approved as an over-the-counter sleep aid. We developed a doxylamine succinate intranasal metered-dose delivery system with the expectation of a more rapid onset of action with reduced side-effect potential compared with the oral tablet. METHODS: This phase I study randomized 24 adults with chronic intermittent sleep impairment to receive either single doses of intranasal doxylamine succinate 3.2, 6.3, or 12.7 mg or doxylamine succinate 25-mg oral tablet...
April 18, 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29572732/efficacy-and-safety-of-sublingual-fentanyl-tablets-in-breakthrough-cancer-pain-management-according-to-cancer-stage-and-background-opioid-medication
#3
Jordi Guitart, María Isabel Vargas, Vicente De Sanctis, Jordi Folch, Rafael Salazar, José Fuentes, Joan Coma, Julia Ferreras, Jordi Moya, Albert Tomás, Pere Estivill, Francisco Rodelas, Antonio Javier Jiménez, Almudena Sanz
OBJECTIVE: Our objective was to assess the effect of sublingual fentanyl tablets (SFTs) on pain relief, quality of life, and adverse effects in patients with cancer pain, according to cancer stage and background opioid regimen. METHODS: Subgroup analyses from a recently completed study were performed according to cancer stage (locally advanced cancer [LAC] vs. metastatic cancer) and most frequent background opioid medication (fentanyl vs. oxycodone/naloxone). The efficacy and safety of SFTs were evaluated, recording pain intensity (PI), onset of pain relief, and adverse events (AEs)...
March 23, 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29546602/the-many-faces-of-apomorphine-lessons-from-the-past-and-challenges-for-the-future
#4
REVIEW
Manon Auffret, Sophie Drapier, Marc Vérin
Apomorphine is now recognized as the oldest antiparkinsonian drug on the market. Though still underused, it is increasingly prescribed in Europe for patients with advanced Parkinson's disease (PD) with motor fluctuations. However, its history is far from being limited to movement disorders. This paper traces the history of apomorphine, from its earliest empirical use, to its synthesis, pharmacological development, and numerous indications in human and veterinary medicine, in light of its most recent uses and newest challenges...
March 15, 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29488154/evaluation-of-the-pharmacokinetics-and-safety-of-a-single-oral-dose-of-fasiglifam-in-subjects-with-mild-or-moderate-hepatic-impairment
#5
John Marcinak, Majid Vakilynejad, Akifumi Kogame, Yoshihiko Tagawa
BACKGROUND AND AIMS: Fasiglifam, a potent, selective novel agonist of G protein-coupled receptor 40, stimulates insulin secretion at elevated blood glucose levels in a glucose-dependent manner. This study evaluated the potential effect of hepatic impairment on the pharmacokinetics and safety of a single dose of fasiglifam and its metabolite M-I. Fasiglifam's clinical development was halted due to liver safety concerns. METHODS: In this phase I, open-label study, subjects with mild or moderate hepatic impairment, along with matched controls (gender, weight, age, and smoking status), received a single, 25-mg oral dose of fasiglifam...
February 27, 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29468559/15-years-of-experience-with-biphasic-insulin-aspart-30-in-type-2-diabetes
#6
REVIEW
Andreas Liebl, Viswanathan Mohan, Wenying Yang, Krzysztof Strojek, Sultan Linjawi
Since clinical experience with biphasic insulin aspart 30 (BIAsp 30) in type 2 diabetes mellitus (T2DM) was reviewed in 2012 after 10 years of use worldwide, additional studies have been published that highlight new aspects, including use in real-world populations. Evidence from 35 new studies confirms and builds upon previous work indicating that BIAsp 30 continues to have pharmacodynamic and clinical advantages over biphasic human insulin (BHI 30), including in real-world practice with unselected populations of patients...
March 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29404858/bayesian-networks-a-new-approach-to-predict-therapeutic-range-achievement-of-initial-cyclosporine-blood-concentration-after-pediatric-hematopoietic-stem-cell-transplantation
#7
Vincent Leclerc, Michel Ducher, Nathalie Bleyzac
BACKGROUND: Pediatric hematopoietic stem cell transplantation (HSCT) allows the treatment of numerous diseases, both malignant and non-malignant. Cyclosporine, a narrow therapeutic index drug, is the major immunosuppressant used to prevent graft-versus-host disease (GVHD), but may also cause severe adverse effects in case of overdosing. OBJECTIVE: The objective of this study is to predict the initial cyclosporine residual blood concentration value after pediatric HSCT, and consequently the dose necessary to reach the therapeutic range, using a mathematical individual predictive model...
March 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29392574/comparison-of-the-pharmacokinetics-of-droxidopa-after-dosing-in-the-fed-versus-fasted-state-and-with-3-times-daily-dosing-in-healthy-elderly-subjects
#8
Jack J Chen, L Arthur Hewitt
BACKGROUND: Droxidopa is an oral prodrug of norepinephrine approved for the treatment of symptomatic neurogenic orthostatic hypotension. This two-part, randomized, crossover study evaluated the 24-h pharmacokinetic profile of droxidopa in 24 healthy elderly subjects. METHODS: Noncompartmental analysis was used to calculate the area under the plasma concentration-time curve (AUC), maximum plasma concentration (Cmax ), time of Cmax (tmax ), and elimination half-life (t½e ) of droxidopa and metabolites...
March 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29374829/in-vitro-safety-pharmacology-profiling-of-topical-%C3%AE-adrenergic-agonist-treatments-for-erythema-of-rosacea
#9
David Piwnica, Atul Pathak, Gregor Schäfer, James R Docherty
BACKGROUND: Topical α-adrenergic agonist therapy has been developed to treat the persistent erythema of rosacea patients. Brimonidine and oxymetazoline are both topical α-adrenergic agonists. OBJECTIVES: The objective of this in vitro safety pharmacology study was to compare the potential safety profiles of brimonidine and oxymetazoline. METHODS: Brimonidine and oxymetazoline underwent pharmacological profiling with a standard panel of 151 assays, including α-adrenergic receptors and 5-hydroxytryptamine (5-HT) receptors...
March 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29330776/second-hand-exposure-of-staff-administering-vaporised-cannabinoid-products-to-patients-in-a-hospital-setting
#10
Nadia Solowij, Peter Galettis, Samantha J Broyd, Peter de Krey, Jennifer H Martin
BACKGROUND: In many health settings, administration of medicinal cannabis poses significant implementation barriers including drug storage and safety for administering staff and surrounding patients. Different modes of administration also provide different yet potentially significant issues. One route that has become of clinical interest owing to the rapid onset of action and patient control of the inhaled amount (via breath timing and depth) is that of vaporisation of cannabinoid products...
March 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29260458/the-risk-of-thrombocytopenia-during-valproic-acid-therapy-a-critical-summary-of-available-clinical-data
#11
Massimiliano Buoli, Marta Serati, Andrea Botturi, A Carlo Altamura
Valproate is an effective anti-epileptic and mood stabilizer drug, but its prescription may be complicated by the development of thrombocytopenia. The purpose of the present manuscript is to provide a critical overview about the risk of thrombocytopenia during treatment with valproate. A search of the main database sources has been conducted to identify relevant papers about the topic. In the studies with a larger sample size (> 150 subjects), thrombocytopenia occurred in 12-18% of subjects receiving treatment with valproate...
March 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29255971/effects-of-a-fixed-dose-co-formulation-of-daclatasvir-asunaprevir-and-beclabuvir-on-the-pharmacokinetics-of-a-cocktail-of-cytochrome-p450-and-drug-transporter-substrates-in-healthy-subjects
#12
Tushar Garimella, Xiaolu Tao, Karen Sims, Yi-Ting Chang, Jignasa Rana, Elsa Myers, Megan Wind-Rotolo, Rahul Bhatnagar, Timothy Eley, Frank LaCreta, Malaz AbuTarif
BACKGROUND: A fixed-dose combination of daclatasvir (DCV; hepatitis C virus NS5A inhibitor), asunaprevir (ASV; non-structural protein 3 inhibitor), and beclabuvir (BCV; non-structural protein 5B inhibitor) is approved in Japan for hepatitis C virus genotype 1. OBJECTIVE: The objective of this study was to assess the combination's drug-drug interaction potential in vivo using a validated cocktail of eight cytochrome P450 (CYP) and transporter probes. METHODS: We conducted an open-label single-sequence study in healthy adults (n = 20) given single-dose caffeine (CYP1A2 substrate), metoprolol (CYP2D6), flurbiprofen (CYP2C9), montelukast (CYP2C8), omeprazole (CYP2C19), midazolam (CYP3A4), digoxin (P-glycoprotein), and pravastatin (organic anion-transporting polypeptide), alone or with steady-state twice-daily DCV/ASV/BCV 30/200/75 mg (with or without additional BCV 75 mg to adjust for higher exposure in hepatitis C virus infection)...
March 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29214385/sealing-effects-on-the-storage-stability-of-the-cyanide-antidotal-candidate-dimethyl-trisulfide
#13
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...
March 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29209910/efficacy-and-safety-of-nintedanib-for-the-treatment-of-idiopathic-pulmonary-fibrosis-an-update
#14
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...
March 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29177587/intranasal-therapy-to-stop-status-epilepticus-in-prehospital-settings
#15
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...
March 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29168127/bioavailability-of-orally-administered-des-aspartate-angiotensin-i-in-human-subjects
#16
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...
March 2018: 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
#17
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
#18
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
#19
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
#20
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
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