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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/29042753/functional-and-morphological-effects-of-diazepam-and-midazolam-on-tumor-vasculature-in-the-9l-gliosarcoma-brain-tumor-model-using-dynamic-susceptibility-contrast-mri-a-comparative-study
#1
Nuo Yan, Yuzhen Zheng, Cheng Yang
Antiangiogenic therapy attenuates tumor growth by reducing vascularization. Diazepam (DZP) and midazolam (MZL) have antiangiogenic properties in human umbilical vein endothelial cells. Thus, we investigated the antiangiogenic activity of DZP and MZL in the rat 9L gliosarcoma brain tumor model. The effect on tumor vasculature was evaluated using dynamic susceptibility contrast magnetic resonance imaging with gradient-echo (GE) and spin-echo (SE) to assess perfusion parameters, including cerebral blood volume (CBV), cerebral blood flow (CBF), mean transit time (MTT), and mean vessel diameter...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29042752/spotlight-on-perampanel-in-the-management-of-seizures-design-development-and-an-update-on-place-in-therapy
#2
REVIEW
Michele A Faulkner
PURPOSE: Perampanel is a first-in-class antiepileptic medication approved for the treatment of partial (focal) seizures, and as adjunctive treatment for primarily generalized tonic-clonic seizures. The pharmacology, efficacy data, adverse-effect profile, pharmacokinetics and place in therapy are reviewed. SUMMARY: Perampanel is indicated for use in patients with epilepsy who are 12 years of age or older. It is the first medication designed specifically to be a non-competitive antagonist at post-synaptic α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate receptors...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29042751/spotlight-on-ertugliflozin-and-its-potential-in-the-treatment-of-type-2-diabetes-evidence-to-date
#3
REVIEW
Francesca Cinti, Simona Moffa, Flavia Impronta, Chiara Ma Cefalo, Vinsin A Sun, Gian Pio Sorice, Teresa Mezza, Andrea Giaccari
Sodium-glucose cotransporter 2 (SGLT2) inhibitors are the latest therapeutic strategy in the treatment of type 2 diabetes mellitus (T2DM). Using an insulin-independent mechanism (glycosuria), they reduce glucose toxicity and improve insulin sensitivity and β-cell function. The promising results obtained in clinical trials show that SGLT2 significantly improves glycemic control and provides greater cardiovascular protection, combined with a reduction in body weight and blood pressure (BP). This review focuses on ertugliflozin, a new, highly selective, and reversible SGLT2 inhibitor...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29042750/current-perspective-on-rituximab-in-rheumatic-diseases
#4
REVIEW
Tommaso Schioppo, Francesca Ingegnoli
The steadily increasing knowledge regarding pathogenetic mechanisms in autoimmune rheumatic diseases has paved the way to different therapeutic approaches. In particular, the market entry of biologics has dramatically modified the natural history of rheumatic chronic inflammatory diseases with a meaningful impact on patients' quality of life. Among the wide spectrum of available biological treatments, rituximab (RTX), first used in the treatment of non-Hodgkin's lymphoma, was later approved for rheumatoid arthritis and anti-neutrophil cytoplasmic antibodies-associated vasculitis...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29033548/the-new-era-of-nanotechnology-an-alternative-to-change-cancer-treatment
#5
REVIEW
Ancuta Jurj, Cornelia Braicu, Laura-Ancuta Pop, Ciprian Tomuleasa, Claudia Diana Gherman, Ioana Berindan-Neagoe
In the last few years, nanostructures have gained considerable interest for the safe delivery of therapeutic agents. Several therapeutic approaches have been reported, such as molecular diagnosis, disease detection, nanoscale immunotherapy and anticancer drug delivery that could be integrated into clinical use. The current paper aims to highlight the background that supports the use of nanoparticles conjugated with different types of therapeutic agents, applicable in targeted therapy and cancer research, with a special emphasis on hematological malignancies...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29033547/new-tablet-formulation-of-tacrolimus-with-smaller-interindividual-variability-may-become-a-better-treatment-option-than-the-conventional-capsule-formulation-in-organ-transplant-patients
#6
Yu Kyong Kim, Anhye Kim, Shin Jung Park, Howard Lee
To evaluate the pharmacokinetic (PK) and tolerability profiles of a new tablet formulation of tacrolimus and its interindividual variability (IIV) in the systemic exposure, and to compare them with those of the conventional capsule formulation, a randomized, open-label, two-treatment, two-period, two-sequence, crossover study was performed in 47 healthy males. The capsule or tablet formulation of tacrolimus was orally administered, and serial blood samples were collected up to 96 hours after dosing. Whole-blood tacrolimus concentration was determined using liquid chromatography-tandem mass spectrometry...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29033546/safety-and-efficacy-profile-of-pembrolizumab-in-solid-cancer-pooled-reanalysis-based-on-randomized-controlled-trials
#7
Manni Wang, Xuelei Ma, Linghong Guo, Fan Xia
BACKGROUND: The aim of the present review is to systematically evaluate the efficacy and safety of pembrolizumab by analyzing survival outcomes and at the same time, to present evidence for future clinical applications of anti-programmed cell death protein 1 (anti-PD-1) antibodies by analyzing the efficacy and safety of pembrolizumab. METHODS: A comprehensive literature search of PubMed, Medline, and Embase was performed for all relevant clinical trials. In this study, adverse events of any grades and grades ≥3 were summarized and calculated for event rates...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29033545/downregulation-of-a20-increases-the-cytotoxicity-of-ifn-%C3%AE-in-hepatocellular-carcinoma-cells
#8
Lei Yin, Zheng Fang, Ning-Jia Shen, Ying-He Qiu, Ai-Jun Li, Yong-Jie Zhang
Hepatocellular carcinoma (HCC) is a highly fatal disease mandating development of novel, effective therapeutic strategy. Interferon-gamma (IFN-γ) is a pleiotropic cytokine with immunomodulatory, antiviral, and antitumor effects. Although IFN-γ is a promising antitumor agent, its application is limited by resistance in tumor cells. A20 is a zinc-finger protein that was initially identified as a gene product induced by tumor necrosis factor α in human umbilical vein endothelial cells. In this study, we found that silencing of A20 combined with IFN-γ significantly represses cell viability, and induces apoptosis and cell-cycle arrest in HCC cells...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29033544/eluxadoline-in-the-treatment-of-diarrhea-predominant-irritable-bowel-syndrome
#9
REVIEW
Ayşe Elif Özdener, Anastasia Rivkin
Eluxadoline is a novel drug approved for the management of diarrhea predominant irritable bowel syndrome (IBS-D). It has unique pharmacology and works on three different opioid receptors. Several Phase II and III clinical trials have demonstrated eluxadoline's efficacy in reducing symptoms related to IBS-D. Clinical trial results and postmarketing reports show a risk of pancreatitis in patients without a gallbladder or those abusing alcohol. This review article will include information on clinical trial results related to IBS-D management as well as eluxadoline's limitations...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29033543/effect-of-echinacoside-on-kidney-fibrosis-by-inhibition-of-tgf-%C3%AE-1-smads-signaling-pathway-in-the-db-db-mice-model-of-diabetic-nephropathy
#10
Fengjuan Tang, Yarong Hao, Xue Zhang, Jian Qin
Kidney fibrosis and renal tubular epithelial-to-mesenchymal transition (EMT) are the main pathological changes of diabetic nephropathy (DN), which eventually leads to end-stage renal disease. Previous studies have suggested that echinacoside (ECH) is antifibrotic in the liver. However, the effect of ECH on kidney fibrosis in DN and its mechanisms are unknown. This study was performed to explore the effect of ECH on kidney fibrosis and also the molecular mechanisms of ECH in a db/db mice model of DN. Our results showed that, relative to db/db mice, the mice in the ECH group had an improved general state and reduced blood glucose and 24-hour urinary protein levels...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29033542/axitinib-in-the-treatment-of-renal-cell-carcinoma-design-development-and-place-in-therapy
#11
REVIEW
Audrey Bellesoeur, Edith Carton, Jerome Alexandre, Francois Goldwasser, Olivier Huillard
Since 2005, the approved first-line treatment of metastatic renal cell carcinoma consists in tyrosine kinase inhibitors (TKIs) targeting the vascular endothelial growth factor receptors (VEGFRs). Axitinib is an oral second-generation TKI and a potent VEGFR inhibitor with a half maximal inhibitory concentration for the VEGF family receptors 10-fold lower than other TKIs. Axitinib activity in renal cell carcinoma (RCC) patients has been studied in various settings and particularly as second-line treatment. In this setting, axitinib with clinically based dose escalation compared to sorafenib has demonstrated an improvement in progression-free survival in a randomized Phase III trial leading to US Food and Drug Administration approval...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29033541/dexmedetomidine-reduces-the-neuronal-apoptosis-related-to-cardiopulmonary-bypass-by-inhibiting-activation-of-the-jak2-stat3-pathway
#12
Yanhua Chen, Xu Zhang, Bingdong Zhang, Guodong He, Lifang Zhou, Yubo Xie
Cardiopulmonary bypass (CPB) constitutes one of the primary methodologies pertaining to cardiac surgery. However, this form of surgery can cause damage to the body. Many studies have reported that dexmedetomidine confers cerebral protection. In this study, we aimed to investigate the effect and mechanism of dexmedetomidine on neuronal apoptosis caused by CPB. Here, rats were treated with different doses of dexmedetomidine by intravenous infusion 2 hours after CPB. We observed that dexmedetomidine treatment to rats reduces the S100β, NSE levels in plasma, and neuronal apoptosis following CPB in a dose-dependent manner...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29033540/assay-development-and-high-throughput-screening-for-small-molecule-inhibitors-of-a-vibrio-cholerae-stress-response-pathway
#13
Laura Stanbery, Jyl S Matson
Antibiotics are important adjuncts to oral rehydration therapy in cholera disease management. However, due to the rapid emergence of resistance to the antibiotics used to treat cholera, therapeutic options are becoming limited. Therefore, there is a critical need to develop additional therapeutics to aid in the treatment of cholera. Previous studies showed that the extracytoplasmic stress response (σ(E)) pathway of Vibrio cholerae is required for full virulence of the organism. The pathway is also required for bacterial growth in the presence of ethanol...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28979099/investigating-isoquinoline-derivatives-for-inhibition-of-inhibitor-of-apoptosis-proteins-for-ovarian-cancer-treatment
#14
Chen Chen, Jie Wu, Pengfei Zhu, Congjian Xu, Liangqing Yao
OBJECTIVE: To discover novel isoquinoline derivatives for inhibition of inhibitor of apoptosis proteins (IAP) for the treatment of ovarian cancer. METHODS: We first synthesized 533 isoquinoline derivatives, and screened them using CCK-8 to measure their antiproliferative activity. These compounds were further tested by Hoechst staining and flow cytometric analysis to assess proapoptotic activity. The in vivo antitumor efficacy and safety of the screened compounds were evaluated on the xenograft mouse model...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28979098/metal-organic-frameworks-as-a-drug-delivery-system-for-flurbiprofen
#15
Muder Al Haydar, Hussein Rasool Abid, Bruce Sunderland, Shaobin Wang
BACKGROUND: Metal organic frameworks (MOFs) have attracted more attention in the last decade because of a suitable pore size, large surface area, and high pore volume. Developing biocompatible MOFs such as the MIL family as a drug delivery system is possible. PURPOSE: Flurbiprofen (FBP), a nonsteroidal anti-inflammatory agent, is practically insoluble in aqueous solution, and, therefore, needs suitable drug delivery systems. Different biocompatible MOFs such as Ca-MOF and Fe-MILs (53, 100, and 101) were synthesized and employed for FBP delivery...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28979097/erratum-cissus-quadrangularis-inhibits-il-1%C3%AE-induced-inflammatory-responses-on-chondrocytes-and-alleviates-bone-deterioration-in-osteotomized-rats-via-p38-mapk-signaling-corrigendum
#16
(no author information available yet)
[This corrects the article on p. 2927 in vol. 9.].
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28919718/extended-infusion-versus-intermittent-infusion-of-imipenem-in-the-treatment-of-ventilator-associated-pneumonia
#17
Mohamed M Ibrahim, Tarek Fouad Tammam, Mohy El Deen Ebaed, Hatem A Sarhan, Gamal F Gad, Amal K Hussein
BACKGROUND: Mechanical ventilation support can be the main source of ventilator-associated pneumonia (VAP). VAP is a serious infection that may be associated with dangerous gram-negative bacteria mainly, and it leads to an increase in the mortality in the intensive care unit (ICU). Imipenem is one of the strongest antibiotics now available for treating VAP which is associated with gram-negative and gram-positive bacteria, and it belongs to beta-lactam antibiotic group (carbapenem). OBJECTIVE: This study tried to investigate the efficacy of imipenem against VAP when it was infused within 180 min versus the efficacy when it was infused within 30-60 min...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28919717/the-influence-of-goal-directed-fluid-therapy-on-the-prognosis-of-elderly-patients-with-hypertension-and-gastric-cancer-surgery-retraction
#18
(no author information available yet)
[This retracts the article on p. 2113 in vol. 8.].
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28919716/palatability-and-physical-properties-of-potassium-binding-resin-rdx7675-comparison-with-sodium-polystyrene-sulfonate
#19
Vanessa Zann, John McDermott, Jeffrey W Jacobs, James P Davidson, Fangling Lin, Paul Korner, Robert C Blanks, David P Rosenbaum
BACKGROUND: Hyperkalemia is a potentially life-threatening condition that patients with heart failure or chronic kidney disease, especially those taking renin-angiotensin-aldosterone system inhibitors, are at high risk of developing. Sodium polystyrene sulfonate (SPS), a current treatment, binds potassium within the gastrointestinal tract to reduce potassium absorption. However, poor palatability limits its long-term use. RDX7675, a novel potassium binder in development for the treatment of hyperkalemia, is a calcium salt of a reengineered polystyrene sulfonate-based resin designed to have enhanced palatability...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28919715/in-vitro-inhibitory-activities-of-magnolol-against-candida-spp
#20
Peiru Zhou, Jingya Fu, Hong Hua, Xiaosong Liu
Candida spp. cause various infections involving the skin, mucosa, deep tissues, and even life-threatening candidemia. They are regarded as an important pathogen of nosocomial bloodstream infection, with a high mortality rate. As a result of prolonged exposure to azoles, the therapeutic failure associated with azoles resistance has become a serious challenge in clinical situations. Therefore, novel, alternative antifungals are required urgently. In the present study, the CLSI M-27A broth microdilution method and the 2,3-Bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction assay were used to evaluate the antifungal effects of magnolol against various standard Candida strains in planktonic mode and biofilm formation, respectively...
2017: Drug Design, Development and Therapy
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