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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/28814836/safety-of-switching-from-brand-name-to-generic-levetiracetam-in-patients-with-epilepsy
#1
Magdalena Bosak, Agnieszka Słowik, Wojciech Turaj
PURPOSE: The approach to the use of generic antiepileptic drugs has recently evolved from major concern to general acceptance, but the evidence related specifically to the safety of switching from brand-name to generic levetiracetam (LEV) is scarce. The aim of the study was to assess the risk of increased frequency of seizures or other adverse events after replacement of a brand-name LEV with a generic one. PATIENTS AND METHODS: This retrospective analysis included 159 patients treated with LEV in a tertiary outpatient epilepsy clinic...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28814835/efficacy-and-tolerability-of-two-different-formulations-of-atorvastatin-in-korean-patients-with-hypercholesterolemia-a-multicenter-prospective-randomized-clinical-trial
#2
Ju-Hee Lee, Sang-Hyun Kim, Dong-Ju Choi, Seung-Jea Tahk, Jung-Han Yoon, Si Wan Choi, Taek-Jong Hong, Hyo-Soo Kim
PURPOSE: This study was designed to compare the efficacy and tolerability of the generic formulation (Atorva(®)) and the reference formulation (Lipitor(®)) of atorvastatin, both at a dosage of 20 mg once daily. METHODS: This study was a prospective open-label, randomized controlled study. Hypercholesterolemic patients who had not achieved low-density lipoprotein (LDL) cholesterol goals according to the National Cholesterol Education Program Adult Treatment Panel III (NCEP-ATP III) guideline were randomized to generic formulation or reference formulation of atorvastatin...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28814834/intracellular-trafficking-of-new-anticancer-therapeutics-antibody-drug-conjugates
#3
REVIEW
Muhammad Kalim, Jie Chen, Shenghao Wang, Caiyao Lin, Saif Ullah, Keying Liang, Qian Ding, Shuqing Chen, Jinbiao Zhan
Antibody-drug conjugate (ADC) is a milestone in targeted cancer therapy that comprises of monoclonal antibodies chemically linked to cytotoxic drugs. Internalization of ADC takes place via clathrin-mediated endocytosis, caveolae-mediated endocytosis, and pinocytosis. Conjugation strategies, endocytosis and intracellular trafficking optimization, linkers, and drugs chemistry present a great challenge for researchers to eradicate tumor cells successfully. This inventiveness of endocytosis and intracellular trafficking has given considerable momentum recently to develop specific antibodies and ADCs to treat cancer cells...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28814833/markers-of-oxidative-nitrosative-stress-and-inflammation-in-lung-tissue-of-rats-exposed-to-different-intravenous-iron-compounds
#4
Jorge E Toblli, Gabriel Cao, Jorge F Giani, Fernando P Dominici, Margarita Angerosa
Iron deficiency anemia is a frequent complication in clinical conditions such as chronic kidney disease, chronic heart failure, inflammatory bowel disease, cancer, and excessive blood loss. Given the ability of iron to catalyze redox reactions, iron therapy can be associated with oxidative stress. The lung is uniquely susceptible to oxidative stress, and little is known about the effects of intravenous iron treatment in this organ. This study characterized changes in markers of oxidative/nitrosative stress and inflammation in the lung of non-iron deficient, non-anemic rats treated with five weekly doses (40 mg iron per kg body weight) of low molecular weight iron dextran (LMWID), iron sucrose (IS), ferric carboxymaltose (FCM), ferumoxytol (FMX), iron isomaltoside 1000 (IIM), or saline (control)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28814832/combinatorial-and-sequential-delivery-of-gemcitabine-and-oseltamivir-phosphate-from-implantable-poly-d-l-lactic-co-glycolic-acid-cylinders-disables-human-pancreatic-cancer-cell-survival
#5
Stephanie Allison Logan, Amanda J Brissenden, Myron R Szewczuk, Ronald J Neufeld
Combination therapies against multiple targets are currently being developed to prevent resistance to a single chemotherapeutic agent and to extirpate pre-existing resistance in heterogeneous cancer cells in tumors due to selective pressure from the single agent. Gemcitabine (GEM), a chemotherapeutic agent, is the current standard of care for patients with pancreatic cancer. Patients with pancreatic cancer receiving GEM have a low progression-free survival. Given the poor response rate to GEM, cancer cells are known to develop rapid resistance to this drug...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28814831/schiff-base-derived-from-thiosemicarbazone-and-anthracene-showed-high-potential-in-overcoming-multidrug-resistance-in-vitro-with-low-drug-resistance-index
#6
Jie Bai, Rui-Hui Wang, Yan Qiao, Aidong Wang, Chen-Jie Fang
Multidrug resistance (MDR) is a huge obstacle in cancer chemotherapeutics. Overcoming MDR is a great challenge for anticancer drug discovery. Here, DNA binding and cytotoxicity of Schiff base L1 and L2 were explored to assess their efficiency in fighting cancer and overcoming the MDR. L1 and L2 could treat extremely chemoresistant MCF-7/ADR cell as drug-sensitive cell, with drug resistance index (DRI) <2.13, showing high potential in overcoming the MDR. The apoptotic ratio induced by L1 and L2 was low for both MCF-7 and MCF-7/ADR cells...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28814830/comparative-analysis-of-essential-oil-composition-of-iranian-and-indian-nigella-sativa-l-extracted-using-supercritical-fluid-extraction-and-solvent-extraction
#7
Kourosh Hasanzadeh Ghahramanloo, Behnam Kamalidehghan, Hamid Akbari Javar, Riyanto Teguh Widodo, Keivan Majidzadeh, Mohamed Ibrahim Noordin
The objective of this study was to compare the oil extraction yield and essential oil composition of Indian and Iranian Nigella sativa L. extracted by using Supercritical Fluid Extraction (SFE) and solvent extraction methods. In this study, a gas chromatography equipped with a mass spectrophotometer detector was employed for qualitative analysis of the essential oil composition of Indian and Iranian N. sativa L. The results indicated that the main fatty acid composition identified in the essential oils extracted by using SFE and solvent extraction were linoleic acid (22...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28814829/antibiotic-susceptibility-heteroresistance-and-updated-treatment-strategies-in-helicobacter-pylori-infection
#8
REVIEW
Maria Teresa Mascellino, Barbara Porowska, Massimiliano De Angelis, Alessandra Oliva
In this review, we discuss the problem of antibiotic resistance, heteroresistance, the utility of cultures and antibiotic susceptibility tests in Helicobacter pylori (Hp) eradication, as well as the updated treatment strategies for this infection. The prevalence of antibiotic resistance is increasing all over the world, especially for metronidazole and clarithromycin, because of their heavy use in some geographical areas. Heteroresistance (simultaneous presence of both susceptible and resistant strains in different sites of a single stomach) is another important issue, as an isolate could be mistakenly considered susceptible if a single biopsy is used for antimicrobial tests...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28814828/comparison-of-efficacy-and-safety-of-oral-agents-for-the-treatment-of-relapsing-remitting-multiple-sclerosis
#9
REVIEW
Cristina Guarnera, Placido Bramanti, Emanuela Mazzon
In the therapeutic scenario of disease-modifying therapies for relapsing-remitting multiple sclerosis, the introduction of oral agents, starting in 2010 with fingolimod, has been a huge step forward in therapeutic options due to the easier administration route. Three oral drugs fingolimod, teriflunomide, and dimethyl fumarate, which are clinically approved for the treatment of relapsing-remitting multiple sclerosis, are reviewed in this work. Results of Phase III clinical trials and their extension studies showed that the three oral agents significantly reduced the annualized relapse rate - a superior efficacy compared to placebo...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28794616/schisandrin-b-attenuates-ccl4-induced-liver-fibrosis-in-rats-by-regulation-of-nrf2-are-and-tgf-%C3%AE-smad-signaling-pathways
#10
Qingshan Chen, Hai Zhang, Yan Cao, Ying Li, Sen Sun, Junping Zhang, Guoqing Zhang
Liver fibrosis is a major pathological feature of chronic liver diseases and there is no effective therapy program at present. Schisandrin B (Sch B) is the major bioactive ingredient of Schisandra chinensis, with antioxidative, anti-inflammatory, antitumor, and hepatoprotective properties. This study aimed to investigate the protective effect and related molecular mechanism of Sch B against carbon tetrachloride (CCl4)-induced liver fibrosis in rats. The in vivo therapeutic effect of Sch B on liver fibrosis induced by CCl4 was examined in rats...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28769554/the-modulation-of-enzyme-indoleamine-2-3-dioxygenase-from-dendritic-cells-for-the-treatment-of-type-1-diabetes-mellitus
#11
REVIEW
Débora Moitinho Abram, Luis Gustavo Romani Fernandes, Antônio Celso Saragossa Ramos Filho, Patrícia Ucelli Simioni
Diabetes mellitus type 1 (DM1) is an autoimmune disease in which β-cells of the pancreas islet are destroyed by T lymphocytes. Specific T cells are activated by antigen-presenting cells, mainly dendritic cells (DCs). It is already known that the regulation of tryptophan pathway in DC can be a mechanism of immunomodulation. The enzyme indoleamine 2,3-dioxygenase (IDO) is present in many cells, including DC, and participates in the metabolism of the amino acid tryptophan. Recent studies suggest the involvement of IDO in the modulation of immune response, which became more evident after the in vitro demonstration of IDO production by DC and of the ability of these cells to inhibit lymphocyte function through the control of tryptophan metabolism...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28769553/clinical-utility-of-alpha-1-proteinase-inhibitor-in-the-management-of-adult-patients-with-severe-alpha-1-antitrypsin-deficiency-a-review-of-the-current-literature
#12
REVIEW
David G Parr, Beatriz Lara
Alpha-1 antitrypsin (AAT) functions primarily to inhibit neutrophil elastase, and its deficiency predisposes individuals to the development of chronic obstructive pulmonary disease (COPD). The putative protective serum concentration is generally considered to be above a threshold of 11 μM/L, and therapeutic augmentation of AAT above this value is believed to retard the progression of emphysema. Several AAT preparations, all derived from human donor plasma, have been commercialized since approval by the US Food and Drug Administration (FDA) in 1987...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28761332/using-dezocine-to-prevent-etomidate-induced-myoclonus-a-meta-analysis-of-randomized-trials
#13
Yu Zhu, Yuting Yang, Chengmao Zhou, Zeqing Bao
OBJECTIVE: This study was designed to evaluate the efficacy and safety of preinjection of dezocine in preventing etomidate-induced myoclonus. METHODS: PubMed, Embase, The Cochrane Library, and China National Knowledge Infrastructure (CNKI) were searched to collect relevant randomized controlled trials (RCTs) from inception to July 2016 on the preinjection of dezocine in preventing etomidate-induced myoclonus. Two researchers independently screened literature, extracted data, and evaluated bias risks in accordance with inclusion and exclusion criteria, and then used RevMan 5...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28761331/antiglycation-radical-scavenging-and-semicarbazide-sensitive-amine-oxidase-inhibitory-activities-of-acetohydroxamic-acid-in-vitro
#14
Yuh-Hwa Liu, Yeh-Lin Lu, Der-Zen Liu, Wen-Chi Hou
Advanced glycation endproducts (AGEs) can promote intracellular reactive oxygen species production, and the levels of AGEs are highly correlated with cardiovascular disease and diabetes complications. Acetohydroxamic acid (acetH) is a bacterial urease inhibitor drug used to treat kidney stones and infections in the urinary tract, and hydroxyurea (HU) is a drug used for antineoplasm and sickle cell diseases. Both acetH and HU are hydroxamic acid derivatives. It was found that acetH and HU at 2.5 or 5 mM showed anti-AGE formation by lowering the AGEs' fluorescent intensities and N(ε)-(carboxymethyl)lysine formation in bovine serum albumin/galactose models, and both showed better and significant differences (P<0...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28744104/efficacy-and-safety-of-direct-acting-antiviral-therapy-in-previous-hard-to-treat-patients-with-recurrent-hepatitis-c-virus-infection-after-liver-transplantation-a-real-world-cohort
#15
Sebastian Bernuth, Daniel Grimm, Johanna Vollmar, Felix Darstein, Jens Mittler, Michael Heise, Maria Hoppe-Lotichius, Peter R Galle, Hauke Lang, Tim Zimmermann
BACKGROUND: Recurrent hepatitis C virus (HCV) infection after liver transplantation (LT) has been a frequent and relevant problem in the past two decades. This analysis evaluated the efficacy and safety of new interferon (IFN)-free direct-acting antiviral (DAA) therapies in a large real-world cohort of HCV patients after LT. METHODS: We retrospectively analyzed a cohort of 157 patients infected with HCV who underwent deceased donor LT between 1997 and 2014. Patient survival, outcome, and side effects of antiviral therapy were assessed...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28744103/clinical-utility-of-evolocumab-in-the-management-of-hyperlipidemia-patient-selection-and-follow-up
#16
REVIEW
Dave L Dixon, Leo F Buckley, Cory R Trankle, Dinesh Kadariya, Antonio Abbate
Inhibition of PCSK9 is a novel therapeutic strategy aimed at reducing low-density-lipoprotein cholesterol (LDL-C) and cardiovascular risk. Evolocumab is a fully humanized monoclonal antibody that inhibits PCSK9, an enzyme that binds to LDL receptors and prevents them from recycling to the hepatocyte surface. Clinical trials have demonstrated 50%-70% reductions in LDL-C with evolocumab when used in combination with statin therapy. The recent FOURIER trial demonstrated that evolocumab further reduces cardiovascular events, but not mortality, in high-risk patients already receiving statin therapy...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28744102/bioequivalence-of-generic-alendronate-sodium-tablets-70-mg-to-fosamax-%C3%A2-tablets-70-mg-in-fasting-healthy-volunteers-a-randomized-open-label-three-way-reference-replicated-crossover-study
#17
Yifan Zhang, Xiaoyan Chen, Yunbiao Tang, Youming Lu, Lixia Guo, Dafang Zhong
PURPOSE: The aim of this study was to evaluate the bioequivalence of a generic product 70 mg alendronate sodium tablets with the reference product Fosamax(®) 70 mg tablet. MATERIALS AND METHODS: A single-center, open-label, randomized, three-period, three-sequence, reference-replicated crossover study was performed in 36 healthy Chinese male volunteers under fasting conditions. In each study period, the volunteers received a single oral dose of the generic or reference product (70 mg)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28744101/a-6-month-mixed-effect-pharmacokinetic-model-for-post-transplant-intravenous-anti-hepatitis-b-immunoglobulin-prophylaxis
#18
Seunghoon Han, Gun Hyung Na, Dong-Goo Kim
BACKGROUND: Although individualized dosage regimens for anti-hepatitis B immunoglobulin (HBIG) therapy have been suggested, the pharmacokinetic profile and factors influencing the basis for individualization have not been sufficiently assessed. We sought to evaluate the pharmacokinetic characteristics of anti-HBIG quantitatively during the first 6 months after liver transplantation. METHODS: Identical doses of 10,000 IU HBIG were administered to adult liver transplant recipients daily during the first week, weekly thereafter until 28 postoperative days, and monthly thereafter...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28744100/evaluation-of-the-stability-of-linezolid-in-aqueous-solution-and-commonly-used-intravenous-fluids
#19
Rachel Taylor, Bruce Sunderland, Giuseppe Luna, Petra Czarniak
PURPOSE: The aim was to evaluate the stability of linezolid in commonly used intravenous fluids and in aqueous solution to determine the kinetics of degradation and shelf-life values at alkaline pH values. METHODS: Forced degradation studies were performed on linezolid in solution to develop a validated high-performance liquid chromatography analysis. Sodium chloride 0.9%, sodium lactate, and glucose 5% and glucose 10% solution containing 2.0 mg/mL linezolid were stored at 25...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28744099/pharmacokinetics-pharmacodynamics-and-tolerability-of-verinurad-a-selective-uric-acid-reabsorption-inhibitor-in-healthy-adult-male-subjects
#20
Zancong Shen, Michael Gillen, Jeffrey N Miner, Gail Bucci, David M Wilson, Jesse W Hall
PURPOSE: Verinurad (RDEA3170) is a selective uric acid reabsorption inhibitor in clinical development for the treatment of gout and asymptomatic hyperuricemia. The aim of this study was to evaluate the pharmacokinetics, pharmacodynamics, and tolerability of verinurad in healthy adult males. SUBJECTS AND METHODS: This was a Phase I, randomized, double-blind, placebo-controlled, single and multiple ascending dose study. Panels of eight male subjects received a single oral dose of verinurad or placebo in either a fasted or fed state; panels of 10-12 male subjects received ascending doses of once-daily verinurad or placebo in a fasted state for 10 days...
2017: Drug Design, Development and Therapy
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