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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/28442893/vitamin-d-deficiency-and-tuberculosis-what-about-body-mass-index
#1
COMMENT
Eduardo Hernández-Garduño
No abstract text is available yet for this article.
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28442892/bioequivalence-study-of-a-new-sildenafil-100-mg-orodispersible-film-compared-to-the-conventional-film-coated-100-mg-tablet-administered-to-healthy-male-volunteers
#2
Milko Radicioni, Chiara Castiglioni, Andrea Giori, Irma Cupone, Valeria Frangione, Stefano Rovati
A new orodispersible film formulation of the phosphodiesterase type 5 inhibitor, sildenafil, has been developed to examine the advantages of an orally disintegrating film formulation and provide an alternative to the current marketed products for the treatment of erectile dysfunction. The pharmacokinetics of the sildenafil 100 mg orodispersible film (IBSA) was compared to that of the conventional marketed 100 mg film-coated tablet (Viagra(®)) after single-dose administration to 53 healthy male volunteers (aged 18-51 years) in a randomized, open, two-way crossover bioequivalence study...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28442891/spotlight-on-nivolumab-in-the-treatment-of-renal-cell-carcinoma-design-development-and-place-in-therapy
#3
REVIEW
Vyshak Alva Venur, Monika Joshi, Kenneth G Nepple, Yousef Zakharia
Several tyrosine kinase inhibitors targeting the vascular endothelial growth factor receptors and molecules inhibiting the mammalian target of rapamycin are being used for management of metastatic renal cell carcinoma (mRCC); however, there is still a potential for improvement. Immune checkpoint inhibitors like nivolumab and other PD-1/PD-L1 inhibitors provide an alternative approach for patients with mRCC. In this article, the authors review the safety profile and outcomes of phase 1, 2, and 3 clinical trials of nivolumab in mRCC...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28442890/justification-of-disintegration-testing-beyond-current-fda-criteria-using-in-vitro-and-in-silico-models
#4
Lukas Uebbing, Lukas Klumpp, Gregory K Webster, Raimar Löbenberg
Drug product performance testing is an important part of quality-by-design approaches, but this process often lacks the underlying mechanistic understanding of the complex interactions between the disintegration and dissolution processes involved. Whereas a recent draft guideline by the US Food and Drug Administration (FDA) has allowed the replacement of dissolution testing with disintegration testing, the mentioned criteria are not globally accepted. This study provides scientific justification for using disintegration testing rather than dissolution testing as a quality control method for certain immediate release (IR) formulations...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28435228/erratum-decitabine-reverses-tgf-%C3%AE-1-induced-epithelial-mesenchymal-transition-in-non-small-cell-lung-cancer-by-regulating-mir-200-zeb-axis-corrigendum
#5
(no author information available yet)
[This corrects the article on p. 969 in vol. 11.].
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28435227/erratum-relaxin-inhibits-cardiac-fibrosis-and-endothelial-mesenchymal-transition-via-the-notch-pathway-corrigendum
#6
(no author information available yet)
[This corrects the article on p. 4599 in vol. 9.].
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28435226/inhibition-of-lymphangiogenesis-in-vitro-and-in-vivo-by-the-multikinase-inhibitor-nintedanib
#7
Tong Lin, Lan Gong
PURPOSE: To investigate the feasibility of nintedanib, a novel triple angiokinase inhibitor, for inhibiting lymphatic endothelial cell (LEC)-induced lymphangiogenesis in vitro and inflammatory corneal lymphangiogenesis in vivo. MATERIALS AND METHODS: Methylthiazolyldiphenyl-tetrazolium bromide (MTT) test, transwell system, and tube-formation assay were used to evaluate the effects of nintedanib on the proliferation, migration, and tube formation of LECs stimulated by vascular endothelial growth factor-C (VEGF-C), basic fibroblast growth factor (bFGF), or platelet-derived growth factor-BB (PDGF-BB)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28435225/association-of-genetic-variations-with-pharmacokinetics-and-lipid-lowering-response-to-atorvastatin-in-healthy-korean-subjects
#8
Hye In Woo, Suk Ran Kim, Wooseong Huh, Jae-Wook Ko, Soo-Youn Lee
BACKGROUND: Statins are effective agents in the primary and secondary prevention of cardiovascular disease, but treatment response to statins varies among individuals. We analyzed multiple genetic polymorphisms and assessed pharmacokinetic and lipid-lowering responses after atorvastatin 80 mg treatment in healthy Korean individuals. METHODS: Atorvastatin 80 mg was given to 50 healthy Korean male volunteers. Blood samples were collected to measure plasma atorvastatin and lipid concentrations up to 48 hours after atorvastatin administration...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28435224/investigation-of-triamterene-as-an-inhibitor-of-the-tgr5-receptor-identification-in-cells-and-animals
#9
Yingxiao Li, Kai Chun Cheng, Chiang-Shan Niu, Shih-Hsiang Lo, Juei-Tang Cheng, Ho-Shan Niu
BACKGROUND: G-protein-coupled bile acid receptor 1 (GPBAR1, also known as TGR5) has been shown to participate in glucose homeostasis. In animal models, a TGR5 agonist increases incretin secretion to reduce hyperglycemia. Many agonists have been developed for clinical use. However, the effects of TGR5 blockade have not been studied extensively, with the exception of studies using TGR5 knockout mice. Therefore, we investigated the potential effect of triamterene on TGR5. METHODS: We transfected the TGR5 gene into cultured Chinese hamster ovary cells (CHO-K1 cells) to express TGR5...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28435223/efficacy-of-the-dual-pi3k-and-mtor-inhibitor-nvp-bez235-in-combination-with-imatinib-mesylate-against-chronic-myelogenous-leukemia-cell-lines
#10
Pengliang Xin, Chuntuan Li, Yan Zheng, Qunyi Peng, Huifang Xiao, Yuanling Huang, Xiongpeng Zhu
BACKGROUND: Phosphatidylinositol 3-kinase/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR) pathway is a therapy target of cancer. We aimed to confirm the effect of dual PI3K/mTOR inhibitor NVP-BEZ235 on proliferation, apoptosis, and autophagy of chronic myelogenous leukemia (CML) cells and sensitivity of tyrosine kinase inhibitor in vitro. METHODS: Two human CML cell lines, K562 and KBM7R (T315I mutant strain), were used. The proliferation of CML cells was detected by MTS (Owen's reagent) assay...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28435222/effects-of-intrathecal-dexmedetomidine-on-shivering-after-spinal-anesthesia-for-cesarean-section-a-double-blind-randomized-clinical-trial
#11
Karim Nasseri, Negin Ghadami, Bijan Nouri
BACKGROUND: Shivering is among the common troublesome complications of spinal anesthesia (SA), and causes discomfort and discontentment in parturients undergoing cesarean sections (CSs). The aim of this study was to investigate the effects of intrathecal dexmedetomidine in the prevention of shivering in those who underwent CS under SA. SUBJECTS AND METHODS: Fifty parturients planned for elective CSs under SA were enrolled in this prospective, double-blinded, controlled study and randomly divided into two equal groups...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28435221/phenotypic-evaluation-and-in-silico-admet-properties-of-novel-arylimidamides-in-acute-mouse-models-of-trypanosoma-cruzi-infection
#12
Cristiane França da Silva, Denise da Gama Jaén Batista, Julianna Siciliano de Araújo, Edézio Ferreira Cunha-Junior, Chad E Stephens, Moloy Banerjee, Abdelbasset A Farahat, Senol Akay, Mary K Fisher, David W Boykin, Maria de Nazaré Correia Soeiro
Arylimidamides (AIAs), previously termed as reversed amidines, present a broad spectrum of activity against intracellular microorganisms. In the present study, three novel AIAs were evaluated in a mouse model of Trypanosoma cruzi infection, which is the causative agent of Chagas disease. The bis-AIAs DB1957, DB1959 and DB1890 were chosen based on a previous screening of their scaffolds that revealed a very promising trypanocidal effect at nanomolar range against both the bloodstream trypomastigotes (BTs) and the intracellular forms of the parasite...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28435220/formulation-release-characteristics-and-bioavailability-study-of-gastroretentive-floating-matrix-tablet-and-floating-raft-system-of-mebeverine-hcl
#13
Mohamed A El Nabarawi, Mahmoud H Teaima, Rehab A Abd El-Monem, Nagla A El Nabarawy, Dalia A Gaber
To prolong the residence time of dosage forms within the gastrointestinal tract until all drug is released at the desired rate is one of the real challenges for oral controlled-release drug delivery systems. This study was designed to develop a controlled-release floating matrix tablet and floating raft system of Mebeverine HCl (MbH) and evaluate different excipients for their floating behavior and in vitro controlled-release profiles. Oral pharmacokinetics of the optimum matrix tablet, raft system formula, and marketed Duspatalin(®) 200 mg retard as reference were studied in beagle dogs...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28424540/mc-ppea-as-a-new-and-more-potent-inhibitor-of-clp-induced-sepsis-and-pulmonary-inflammation-than-fk866
#14
Peixin Huang, Mark W Lee, Keivan Sadrerafi, Daniel P Heruth, Li Q Zhang, Dev Maulik, Shui Qing Ye
Our previous study indicated that overexpression of nicotinamide phosphoribosyltransferase (NAMPT) aggravated acute lung injury, while knockdown of NAMPT expression attenuated ventilator-induced lung injury. Recently, we found that meta-carborane-butyl-3-(3-pyridinyl)-2E-propenamide (MC-PPEA, MC4), in which the benzoylpiperidine moiety of FK866 has been replaced by a carborane, displayed a 100-fold increase in NAMPT inhibition over FK866. Here, we determined the effects of MC4 and FK866 on cecal ligation and puncture (CLP) surgery-induced sepsis in C57BL/6J mice...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28424539/%C3%AE-3-adrenoceptor-activation-upregulates-apolipoprotein-a-i-expression-in-hepg2-cells-which-might-further-promote-cholesterol-efflux-from-macrophage-foam-cells
#15
Xia-Qing Gao, Yan-Fang Li, Zhi-Li Jiang
OBJECTIVE: The aim of this study was to explore the effects of β3-adrenoceptor (β3-AR) activation on HepG2 cells and its influence on cholesterol efflux from macrophage foam cells. MATERIALS AND METHODS: HepG2 cells were cultured and treated with the β3-AR agonist, BRL37344, and antagonist, SR52390A, and the expression of apolipoprotein (Apo) A-I, ApoA-II, ApoB, and β3-AR in the supernatants and cells was determined. The expression of peroxisome proliferator-activated receptor (PPAR) γ and PPARα in the HepG2 cells was also assessed...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28424538/metal-complexes-in-cancer-therapy-an-update-from-drug-design-perspective
#16
REVIEW
Umar Ndagi, Ndumiso Mhlongo, Mahmoud E Soliman
In the past, metal-based compounds were widely used in the treatment of disease conditions, but the lack of clear distinction between the therapeutic and toxic doses was a major challenge. With the discovery of cisplatin by Barnett Rosenberg in 1960, a milestone in the history of metal-based compounds used in the treatment of cancers was witnessed. This forms the foundation for the modern era of the metal-based anticancer drugs. Platinum drugs, such as cisplatin, carboplatin and oxaliplatin, are the mainstay of the metal-based compounds in the treatment of cancer, but the delay in the therapeutic accomplishment of other metal-based compounds hampered the progress of research in this field...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28424537/awake-craniotomy-anesthetic-management-using-dexmedetomidine-propofol-and-remifentanil
#17
Andrea Prontera, Stefano Baroni, Andrea Marudi, Franco Valzania, Alberto Feletti, Francesca Benuzzi, Elisabetta Bertellini, Giacomo Pavesi
INTRODUCTION: Awake craniotomy allows continuous monitoring of patients' neurological functions during open surgery. Anesthesiologists have to sedate patients in a way so that they are compliant throughout the whole surgical procedure, nevertheless maintaining adequate analgesia and anxiolysis. Currently, the use of α2-receptor agonist dexmedetomidine as the primary hypnotic-sedative medication is increasing. METHODS: Nine patients undergoing awake craniotomy were treated with refined monitored anesthesia care (MAC) protocol consisting of a combination of local anesthesia without scalp block, low-dose infusion of dexmedetomidine, propofol, and remifentanil, without the need of airways management...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28424536/rifapentine-linezolid-loaded-plga-microspheres-for-interventional-therapy-of-cavitary-pulmonary-tuberculosis-preparation-and-in-vitro-characterization
#18
Jieyun Huang, Zhi Chen, Ying Li, Li Li, Guangyu Zhang
In this study, we aimed to design controlled-release microspheres for the treatment of cavitary pulmonary tuberculosis (TB) for solving the issues of poor drug delivery and short duration maintained at effective drug concentration during bronchoscopic interventional therapy. We fabricated rifapentine-linezolid-loaded poly(lactic acid-co-glycolic acid) microspheres (RLPMs) using the oil-in-water emulsion solvent evaporation method and assessed their in vitro release as well as the bronchial mucosal retention characteristics...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28424535/human-papillomavirus-hpv-systemic-treatment-with-gene-eden-vir-novirin-safely-and-effectively-clears-virus
#19
Hanan Polansky, Edan Itzkovitz, Adrian Javaherian
PURPOSE: This paper reports the results of a clinical study that tested the effect of systemic treatment with the botanical product Gene-Eden-VIR/Novirin on the clearance rate (also called time to clearance) of the human papillomavirus (HPV). The study compared the clearance rate in treated and untreated individuals suffering from a symptomatic HPV infection. The data on the untreated individuals were obtained by reverse engineering of the Kaplan-Meier figures in five published papers...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28408805/effect-of-berberine-on-the-renal-tubular-epithelial-to-mesenchymal-transition-by-inhibition-of-the-notch-snail-pathway-in-diabetic-nephropathy-model-kkay-mice
#20
Guannan Yang, Zongjiang Zhao, Xinxue Zhang, Amin Wu, Yawei Huang, Yonghui Miao, Meijuan Yang
Renal tubular epithelial-to-mesenchymal transition (EMT) and renal tubular interstitial fibrosis are the main pathological changes of diabetic nephropathy (DN), which is a common cause of end-stage renal disease. Previous studies have suggested that berberine (BBR) has antifibrotic effects in the kidney and can reduce apoptosis and inhibit the EMT of podocytes in DN. However, the effect of BBR on the renal tubular EMT in DN and its mechanisms of action are unknown. This study was performed to explore the effects of BBR on the renal tubular EMT and the molecular mechanisms of BBR in DN model KKAy mice and on the high glucose (HG)-induced EMT in mouse renal tubular epithelial cells...
2017: Drug Design, Development and Therapy
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